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Pharmaceutics I DOSAGE FORM

This document provides an introduction to different dosage forms. It discusses that drugs are rarely administered in their crude form and are instead formulated into suitable dosage forms using excipients. The key dosage forms are described as solid (tablets, capsules), semi-solid (ointments, creams), and liquid (syrups, drops). Tablets are specifically described as the most common oral solid dosage form and details are given on tablet coatings and types of tablets like effervescent and chewable tablets.

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0% found this document useful (0 votes)
230 views160 pages

Pharmaceutics I DOSAGE FORM

This document provides an introduction to different dosage forms. It discusses that drugs are rarely administered in their crude form and are instead formulated into suitable dosage forms using excipients. The key dosage forms are described as solid (tablets, capsules), semi-solid (ointments, creams), and liquid (syrups, drops). Tablets are specifically described as the most common oral solid dosage form and details are given on tablet coatings and types of tablets like effervescent and chewable tablets.

Uploaded by

Ali Elmehdawi
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPT, PDF, TXT or read online on Scribd
You are on page 1/ 160

INTRODUCTION TO DIFFERENT

DOSAGE FORMS

Powered By Ms. Shubhangi V. Shekade


M. Pharm (Pharmaceutics)
Drug
 Drug may be defined as an
agent or substance, intended
for use in the diagnosis,
mitigation, treatment, cure or
prevention of disease in human
beings or animals.
 Drugs are rarely administered
in their original or crude
forms. They are administered
in different dosage forms by
converting them into suitable
formulations.
Crude Drugs
DRUG / ACTIVE DRUG SUBSTANCES /
API
DRUG / ACTIVE DRUG SUBSTANCES / API

• Drug ?
• International nonproprietary names (INN, „generic“ names)

• Direct clinical use of the active drug substances is rare: Why??


• API handling and Accurate dosing can be difficult or impossible
(e.g., potent drugs: low mg and g doses)
• API administration can be impractical/unfeasible because of
size, shape, smell/odour, taste and low activity.
• Some API are chemically unstable in light, moisture, O2
• API can be degraded at the site of administration (e.g., low pH
in stomach).
• API may cause local irritations or injury when they are present
at high concentrations at the site of administration.
• Administration of active substance would mean to have no
chance for modification (improvement) of its PK
(Pharmacokinetic)profile
Drug:-(active pharmaceutical ingredient - API)
chemical compound intended for used in
diagnosis, treatment or prevention of diseases.

Excipients:-
(inactive pharmaceutical ingredients)
Technological, biopharmaceutical and/or
stability reasons.
Diluents/fillers, binders, lubricants,
disintegrants, coatings, preservants and
stabilizers, colorants and flavourings
dosage form:-
Drug+excipients
Dosage Forms
 Definition: Dosage forms are the means by
which drug molecules are delivered to sites of
action within the body.
 Every dosage forms is a combination of the
drug and different kinds of non – drug
components called as Excipients or additives.
 The additives are used to give a particular
shape to the formulation, to increase stability,
palatability & more elegance to preparations.
Dosage
from/

Medicine

API (Active
Pharmaceutical Excipients
Ingredients)

6
Excipients:(inactive pharmaceutical ingredients)
Technological, biopharmaceutical and/or stability
reasons .
 Coloring agents  Thickening agents
 Sweetening agents  Suspending agents
 Flavoring agents  Binding agents
 Solubilizing agents  Solvents
 Antioxidants  Lubricants
 Preservatives  Perfumes
7
Need of dosage forms: overcoming the difficulties
1. To provide for the safe and convenient delivery of accurate dosage
Examples: Tablets, Capsules, syrups
2. For the protection of a drug substance from the destructive influence of
atmospheric oxygen or moisture.
Examples: coated tablets, sealed ampules

3. For the protection of a drug substance from the destructive influence of


gastric acid after oral administration.
Example: enteric coated tablets
4. To conceal the bitter taste, salty obnoxious or odor of a drug substance.
Examples: Capsules, coated tablets, flavored syrups
Need of dosage forms: overcoming the difficulties
The majority of drug substances are administered in manufacturing amounts,
much too small to be weighed on anything but a sensitive analytical balance.
Example: How can a layman accurately obtain 325 mg or 5 gr of aspirin found
in common aspirin tablets from bulk supply of aspirin?
Examples Of Drugs with Low Usual doses

Ferrous sulfate 300 mg Hematinic


Cimetidine 300 mg Antiulcer
Amoxicillin 250 mg Antibacterial
Propoxyphene HCl 65 mg Analgesic
Phenobarbital 30 mg Sedative
Diphenhydramine HCl 25 mg Antihistamine
Morphine sulfate 10 mg Narcotic Analgesic

Cochicine 0.5 mg Gout suppressant


Nitroglycerin 0.4 mg Antianginal
Digoxin 0.25 mg Cardiotonic
Ethinyl Estradiol 0.05 mg Estrogen
Need of dosage forms: overcoming the difficulties

5. To provide liquid preparations of substances that are either


insoluble or unstable in the desired vehicle.
Example: suspension
6. To provide liquid dosage forms of substances soluble in desired
vehicle.
Example: solution
7. To provide extended drug action through controlled release
mechanisms
Examples: controlled release tablets, capsules, suspensions
8. To provide optional drug action from topical
administration sites
Examples: ointments, creams, ophthalmic, ear and nasal preparations
Need of dosage forms: overcoming the difficulties

9. To provide for insertion of a drug into one of the body’s


orifices
Examples: rectal and vaginal suppositories

10. To provide for the placement of


drugs within body tissues.
Examples: Implants

11. To provide for the optimal drug action through


inhalation therapy.
Examples: inhalants and inhalations

12. In addition, many dosage forms permit ease of drug


identification through distinctiveness of color, shape, or
identifying markings
TYPES OF DOSAGE FORMS

They are classified according to:

1.Route of administration 2.Physical form


Oral Solid
Topical Semisolid
Transdermal Liquid
Parenteral Gases
Inhalation
Buccal & sublingual
Ophthalmic
Otic
Rectal
Vaginal
Classification acc.to physical form

Solid dosage Liquid dosage Semi solid dosage Gaseous


forms forms forms dosage
form

Biphasic Monophasic Internal External


Inhaler
Unit dosage Bulk
forms aerosols
Emulsion
Suspension External
Internal Ointment
Tablets
Capsule Creams
Liniments pastes
Pills Syrups Lotions
External Gargles
Jellies
Internal Elixirs
Linctus Throat paints
Mouth washes
Dusting powders Drops
Fine powders & Sprays Suppositories
Insufflations
granules Eye lotions Pessaries
Dentifrice
Eye drops
Snuffs
Nasal drops
Ear powders
I) Oral dosage
forms:
1-Tablet:
A tablet is a hard, compressed medication in round, oval or square
shape.

The excipients include:


-Binders, glidants
(flow aids) and lubricants to ensure efficient

-Disintegrants to ensure that the tablet breaks up in the digestive tract.


-Sweeteners or flavours to mask the taste of
bad-tasting active ingredients.
-Pigments to make uncoated tablets visually attractive.

8 .
1-Tablet (Cont.)
A coating may be applied to:
1- hide the taste of the tablet's components.
2- make the tablet smoother and easier to
swallow .
3- make it more resistant to the environment.
4- extending its shelf life.

9
2-Buccal and
sublingual tablet:
- Sublingual and buccal medications are administered by placing
them in the mouth, either under the tongue (sublingual) or
between the gum and the cheek (buccal).

- The medications dissolve rapidly and are absorbed through the


mucous membranes of the mouth, where they enter into the
bloodstream.

- Avoid the acid and enzymatic environment of the stomach and


the drug metabolizing enzymes of the liver.

- Examples of drugs administered by this route: e.g. vasodilators,


steroidal hormones.
3-Effervescent
tablet:

Effervescent tablets are uncoated tablets that generally


contain acid substances (citric and tartaric acids)
and carbonates or bicarbonates and which react
rapidly in the presence of water by releasing carbon
dioxide.
-They are intended to be dissolved or dispersed in
water before use providing:
A- Very rapid tablet dispersion and dissolution.
B- pleasant tasting carbonated drink.
4- Chewable
tablet:
- They are tablets that chewed prior to swallowing.
- They are designed for administration to children e.g.
vitamin products.
Dosage forms (Tablet) for oral
administration

 Generations of
dosage forms
– 1st gen.
conventional
(unmodified)
release of API

– 2nd gen. controlled


release of API
(CR)
vinay gupta
Conventional vs. controlled release
forms

 I. Gen. – disintegration of the dosage form and


dissolution of API is spontaneous process;
– drug absorption and distribution is based only
on physico-chemical properties of API
 II.Gen. The release of API is under control of the drug
delivery system (temporal control)
– Advantages:
 Avoids fluctuations of plasma drug concentration  better
safety and efficacy
 Decreased frequency of drug administration (often once daily
admin)  better compliance
Sustained
– release (SR) – release of the initial API dose
& further prolonged release
Controlled
– release (CR) – properly controlled (Zero
order) release of API

15
16
Hard gelatin capsule
Soft gelatin capsule

Spansules
5- Capsule:
A capsule is a medication in a gelatin container.

-Advantage: mask the unpleasant taste of its contents.

-The two main types of capsules are:


1.hard-shelled capsules, which are
normally used for dry, powdered ingredients,

2.soft-shelled capsules, primarily used for oils and for


active ingredients that are dissolved or suspended in
17 oil.
6- Lozenge:

-It is a solid preparation consisting of sugar and gum,


the latter giving strength and cohesiveness to the
lozenge and facilitating slow release of the
medicament.
- It is used to medicate the mouth and throat for the
slow administration of indigestion or cough
remedies.
7-Pastilles:

They are solid medicated preparations designed to


dissolve slowly in the mouth. They are softer than
lozenges and their bases are either glycerol and
gelatin, or acacia and sugar.
8- Dental Cones:
- A tablet form intended to be
placed in the empty socket following a
tooth local, for multiplication of
pathogenic bacteria associated tooth
with
- extractions.
The may contain antibiotic
cones an or
antiseptic.
9-Pills:

- Pills are oral dosage forms which consist of spherical


masses prepared from one or more medicaments
incorporated with inert
- excipients.
Pills are now rarely used.
10- Granules:
- They are consisting of solid, dry aggregates
powder particles often of suppliedin single-
sachets. dose

- Some granules are placed on the tongue and


swallowed with water, others are intended to be
dissolved in water before taking.

- Effervescent granules evolve carbon dioxide


when added to water.
11- Powder
(Oral):
There are two kinds of powder intended for internal use.

1-Bulk Powders are multidose preparations consisting of solid,


loose, dry particles of varying degrees of fineness. They contain
one or more active ingredients, with or without excipients and, if
necessary, coloring matter and flavoring substances.

- usually contain non-potent medicaments such as antacids since


the patient measures a dose by volume using a 5ml medicine
spoon. The powder is then usually dispersed in water or, in the
case of effervescent powders, dissolved before taking.

2-Divided Powders are single-dose presentations of powder ( for


example, a small sachet) that are intended to be issued to the
patient as such, to be taken in or with water.
12- Powders for mixtures:

- The mixed powders may be stored in dry form and


mixture prepared by the pharmacist when required
for dispensing , by suspending the powders in the
appropriate vehicle.
13-Liquid preparations:
a. Oral solution:
Oral solutions are clear Liquid preparations for oral use containing
one or more active ingredients dissolved in a suitable vehicle.
b. Oral emulsion:
Oral emulsions are stabilized oil-in-water
dispersions, either or both phases of which may contain
dissolved solids.

c. Oral suspension:
- Oral suspensions are Liquid preparations for oral use
containing one or more active ingredients suspended in a
suitable vehicle.
- Oral suspensions may show a sediment which is readily
dispersed on shaking to give a uniform suspension which
remains sufficiently stable to enable the correct dose to be
delivered.
13-Liquid preparations
(Cont.):

d- Syrup:
- It is a concentrated aqueous solution of a sugar, usually
sucrose.
- Flavored syrups are a convenient form of masking
disagreeable tastes.
e- Elixir:
-It is pleasantly flavored clear liquid oral preparation of potent or
nauseous drugs.
- The vehicle may contain a high proportion of ethanol or sucrose
together with antimicrobial preservatives which confers the
stability of the preparation.
13-Liquid preparations
(Cont.):
f- Linctuses:
-Linctuses are viscous, liquid oral preparations that are usually prescribed for
the relief of cough.
-They usually contain a high proportion of syrup and glycerol which have a
demulcent effect on the membranes of the throat.
-The dose volume is small (5ml) and, to prolong the demulcent action, they
should be taken undiluted.

g- Oral drops:
Oral drops are Liquid preparations for oral use that are intended to be
administered in small volumes with the aid of a suitable measuring device.
They may be solutions, suspensions or emulsions.
13-Liquid preparations:
h- Gargles:

- They are aqueous solutions used in the


prevention or treatment of throat infections.
Usually they are prepared in a concentrated
solution with directions for the patient to
- dilute with warm water before use.

i- Mouthwashes:
These are similar to gargles but are used for
oral hygiene and to treat infections of the
mouth.
II) Topical dosage forms:
1- Ointments:
-Ointments are semi-solid, greasy
preparations for application to the skin, rectum or nasal
mucosa.

-The base is usually anhydrous and immiscible with skin


secretions.

-Ointments may be used as emollients or to apply


suspended or dissolved medicaments to the skin.
Topical dosage forms (Cont.):

2- Creams:
- Creams are semi-solid emulsions, that is mixtures of oil and water.
- They are divided into two types:
A- oil-in-water (O/W) creams: which are composed of small droplets of
oil dispersed in a continuous aqueous phase.
Oil-in-water creams are more comfortable and cosmetically acceptable as
they are less greasy and more easily washed off using water.
B- water-in-oil (W/O) creams: which are composed of small droplets of
water dispersed in a continuous oily phase.
Water-in-oil creams are more difficult to handle but many drugs which are
incorporated into creams are hydrophobic and will be released more
readily from a water-in-oil cream than an oil-in-water cream.
Water-in-oil creams are also more moisturising as they provide an oily
barrier which reduces water loss from the stratum corneum, the
outermost layer of the skin.
30
Topical dosage forms (Cont.):
3- Gels (Jellies):
-Gels are semisolid system in which a liquid phase is constrained within a 3-D
polymeric matrix (consisting of natural or synthetic gum) having a high degree
of physical or chemical cross-linking.
-They are used for medication, lubrication and some miscellaneous
applications like carrier for spermicidal agents to be used intra vaginally .

4- Poultice:
It is soft, viscous, pasty preparation for external use. They are applied to skin
while they are hot. Poultice must retain heat for a considerable time because
they are intended to supply warmth to inflamed parts of body.
E.g. Kaolin poultice (B.P.C.)
Topical dosage forms (Cont.):
5- Pastes :
- Pastes are basically ointments into which a high percentage of insoluble solid
has been added
-The extraordinary amount of particulate matter stiffens the system.
-Pastes are less penetrating and less macerating
and less heating than ointment.
-Pastes make particularly good protective barrier when placed on the skin, the
solid they contain can absorb and thereby neutralize certain noxious chemicals
before they ever reach the skin.
- Like ointments, paste forms an unbroken relatively water – impermeable film
unlike ointments the film is opaque and therefore can be used as an effective
sun block accordingly.
-Pastes are less greasy because of the absorption of the fluid hydrocarbon
fraction to the particulates.
Topical dosage forms
(Cont.):
There are two types of paste:
a)Fatty pastes (e.g: leaser's paste) .
b)Non greasy pastes (e g: - bassorin paste).

6- Dusting powders:
- These are free flowing very fine powders for external
use.
- Not for use on open wounds unless the powders
are sterilized.
Topical dosage forms
(Cont.):
7- Transdermal patch:
-A transdermal patch or skin patch is a medicated adhesive
patch that is placed on the skin to deliver a specific dose of
medication through the skin and into the bloodstream.

-An advantage of a transdermal drug delivery route over other types


such as oral, topical, etc is that it provides a controlled release of
the medicament into the patient.

- The first commercially available patch was scopolamine for motion


sickness.
40
Topical dosage forms (Cont.):

8-Plasters:
- Plasters are solid or semisolid masses adhere to the
skin when spread upon cotton felt line or muslin as a
backing material and they are mainly used to,
A- Afford protection and mechanical support.
B- Furnish an occlusive and macerating action.
C- Bring medication into close contact with the surface
of the skin.

41
Topical dosage forms (Cont.):

9- Liniments:
-Liniments are fluid, semi-fluid or, occasionally, semi-
solid preparations intended for application to the skin.
-They may be alcoholic or oily solutions or emulsions.
-Most are massaged into the skin (e.g. counter-
irritant).
-Liniments should not be applied to broken skin.

42
Topical dosage forms (Cont.):
 10-Lotions:
 Theseare fluid preparations(aqueous) for
external application without friction.
 They are either dabbed on the skin or applied on a

suitable dressing and covered with a waterproof


dressing to reduce evaporation.

43
Topical dosage forms (Cont.):

11- Collodion:
Collodion is a solution of nitrocellulose in or acetone,
sometimes with the addition of alcohols. ether

-Its generic name is pyroxylin solution.

-It is highly flammable.

- As the solvent evaporates, it dries to a celluloid-like film.


- Compound Wart Remover consists of acetic acid and salicylic acid
in an acetone collodion base used in Treatment of warts by
38 keratolysis.
Topical dosage forms (Cont.):

12- Paints:
- Paints are application to the skin or
liquids for mucous
membranes.
- Skin paints contain volatile solvent that
evaporates quickly to leave a dry resinous film of
medicament.
- Throat paints are more viscous due to a high content
of glycerol, designed to prolong contact of the
medicament with the affected site.
39
Topical dosage forms (Cont.):

13- Pressurized dispensers (aerosol sprays):


- Several different types of pharmaceutical product may be
packaged in pressurized dispensers, known as
aerosols.
- Surface sprays produce droplets of 100 um diameter or
greater.

- May be used as surface disinfectants, wound or burn


dressing, relieve irritation of bites.

- Spray-on dusting powders are also available from


pressurized containers.
III) Rectal dosage forms:
1- Suppository:
It is a small solid medicated mass, usually
cone-shaped ,that is inserted either into the
rectum (rectal suppository), vagina (vaginal
suppository or pessaries) where it melts at
body temperature .

47
Rectal dosage forms:

2- Enema:
An enema is the procedure of introducing liquids into the rectum
and colon via the anus.
Types of enema:
1- Evacuant enema: used as a bowel stimulant to treat
constipation. E.g. soft soap enema & Mgso4 enema
-The volume of evacuant enemas may reach up
- to 2 liters. should be warmed to body
They before
temperature administration.
Rectal dosage forms
(Cont.):
2- Retention enema:
- Their volume does not exceed 100 ml.
- No warming needed.
- May exert:
A- Local effect: e.g. a barium enema is used
as a contrast substance in the radiological imaging of the bowel.
B- Systemic effect:
e.g. the administration of substances into the bloodstream. This
may be done in situations where it is impossible to deliver a
medication by mouth, such as antiemetics.
e.g. nutrient enema which contains carbohydrates,
vitamins & minerals.
IV) Vaginal dosage
forms:
1- Pessary:
- Pessaries are solid medicated preparations designed for
insertion into the vagina where they melt or dissolve.
- There are three types:

A- Moulded pessaries: they are cone shaped and prepared in a


similar way to moulded suppositories.
B- Compressed pessaries: made in a variety of shapes and are
prepared by compression in a similar manner to oral tablets.
C- Vaginal capsules: are similar to soft gelatin oral Capsules
differing only in size and shape.
Vaginal dosage
forms:
2- Vaginal ring:
Vaginal rings are 'doughnut-shaped' polymeric
drug delivery devices
designed to provide controlled release of drugs to the vagina over
extended periods of time.
Several vaginal ring products are currently available, including:

Femring :
a low-dose estradiol-acetate releasing ring, manufactured from
silicone elastomer, for the relief of hot flashes and vaginal atrophy
associated with menopause.
NuvaRing:
a low-dose contraceptive vaginal ring, releasing progesterone and
45 estrogen.
Vaginal dosage forms (Cont.):
3- Douche:

A douche is a device used to introduce a stream


of water into the body cavity for medical or
hygienic reasons.

52
Vaginal dosage forms
(Cont.):
4- Intrauterine device:
-It is a birth control device placed in the uterus, also known as an IUD or a
coil.

-The IUD is the world's most widely used method of reversible birth control.

-The device has to be fitted inside or removed from the uterus by a doctor .

-It remains in place the entire time pregnancy is not desired. Depending on
the type, a single IUD is approved for 5 to 10 years use.

-There are two broad categories of intrauterine contraceptive devices: A-


53 inert and copper-based devices.
V) Parenteral dosage
forms:
An injection is an infusion method of putting liquid into
the body, usually with a hollow needle and a syringe
which is pierced through the skin to a sufficient depth
for the material to be forced into the body.
There are several methods of injection, including: 1-An
intravenous injection:
It is a liquid administered directly into the bloodstream
via a vein.
It is advantageous when a rapid onset of action is
needed.

54
Parenteral dosage
forms :
2- Intramuscular injection:

-It is the injection of a substance directly into a muscle.

-Many vaccines are administered intramuscularly.

-Depending on the chemical properties of the drug, the


medication may either be absorbed fairly quickly or more
gradually.

-Intramuscular injections are often given in the deltoid, vastus


lateralis, ventrogluteal and dorsogluteal muscles.
55
Parenteral dosage
forms:
3- Subcutaneous injection:

Subcutaneous injections are given by injecting a


fluid into the sub cutis, the layer of skin directly
below the dermis and epidermis.
Subcutaneous injections are highly effective in
administering vaccines and such medications as
insulin.
56
57
VI) Inhaled dosage :
forms
1- Inhaler :
- Inhalers are solutions, suspensions or emulsion of drugs in
a mixture of inert propellants held under pressure in an
aerosol dispenser.
- Release of a dose of the medicament in the form of
droplets of 50 um diameter or less from the container
through a spring-loaded valve incorporating a metering
device. The patient then inhales the released drug through
a mouthpiece.
- In some types, the valve is actuated by finger pressure, in
other types the valve is actuated by the patient breathing in
through the mouthpiece.
- It is commonly used to treat asthma and other respiratory
52 problems.
Inhaled dosage forms
(Cont.):
2 Nebulizer or (atomizer):
A nebulizer is a device used to administer medication to people in forms of
a liquid mist to the airways.
-It is commonly used in treating asthma, and other respiratory diseases.
-It pumps air or oxygen through a liquid medicine to turn it into a vapor,
which is then inhaled by the patient.
-As a general rule, doctors generally prefer to prescribe inhalers for their
patients, because:
1-These are cheaper 2- more portable
3- carry less risk of side effects.
Nebulizers, for that reason, are usually reserved only for serious cases of
respiratory disease, or severe attacks.

59
VII) Ophthalmic dosage
forms:
1- Eye drops:
Eye drops are saline-containing drops used as a
vehicle to administer medication in the eye.
Depending on the condition being treated, they may contain
antihistamines or topical anesthetics. steroids,
Eye drops sometimes do not
have medications lubricating and in them and
tear-replacing solutions. are only
2- Ophthalmic ointment & gel:
These are sterile semi-solid
Preparations intended for application
To the conjunctiva or eyelid margin.

60
VIII) Otic dosage
forms:
 - Ear drops are solutions, suspensions or emulsions of
1- Ear drops:
drugs that are instilled into the ear with a dropper.
 It is used to treat or prevent ear infections,
-
especially infections of the outer ear and ear canal.

61
IX) Nasal dosage
forms:
1- Nasal Drops and Sprays:
Drugs in solution may be instilled into the nose from a
dropper or from a plastic squeeze bottle.

The drug may have a local effect, e.g. antihistamine,


decongestant.

Alternatively the drug may be absorbed through the


nasal mucosa to exert a systemic effect.

The use of oily nasal drops should be avoided because


of possible damage to the cilia of the nasal mucosa.
56
Solid dosage forms
Solid dosage forms

Tablets Pills

Dusting Powders

Capsules
Granules
 Solid dosage forms one of the oldest dosage forms and most of the
solid dosage forms are available in Unit dose.
 Unit dose may be defined as a exact quantity of the drug
administered at once. e.g. Tablets, Capsule, pills, cachets, powders
etc.
 When drugs are to be administered orally in dry state, then tablets,
capsules are most convenient dosage forms.
 Some solids are supplied in bulk (Means quantity available in
large). Bulk powders can be supplied as Internal (Granules, Fine
powders) as well as External (Dusting Powders, Insufflations etc)
Dusting Powders
 Dusting powders are applied externally to skin, so they
should be applied in very fine state to avoid local irritation.
Hence dusting powders should be passed through sieve no 80
to obtained fined powders.
 Dusting powders are prepared by mixing of more than one
ingredients in which either starch, kaolin, or talc are used in
their formulation. Generally talc or kaolin are used because
they are inert in nature.
 Dusting powders are used for antiseptic, astringent,
absorbent, antiperspirant etc.
 Dusting powders are of two sub type they are as
I) Medical dusting powder
II) Surgical Dusting powders
Medical Dusting
Powders
 Medical Dusting powders are used to increase
superficial condition of skin.
 These are not applied on wounds, burns etc
 Medical dusting powders must be free from
dangerous pathogenic micro- organism.
Surgical Dusting Powders
 Surgical dusting powders are used in body cavities
and also on major wounds like as burns etc.
 They should be sterilized before use.
 They are mainly used for their antiseptic, absorbent
action.
Insufflations
 These are medicated dusting powders meant for
introduction into body cavities (nose, throat, ear, vagina
etc) with the help of an apparatus known as a insufflator.
 It sprays the powders (in a state of fine particles) on site
of application.
 Now a days insufflations are also available in pressure
aerosols. This pressure aerosols are used for
administration of potent drug.
 They are used in the treatment of ear, nose, throat
infections with antibiotics to produce local effect of drugs.
Snuffs
 These are finely divided solid dosage forms of
medicaments which are inhaled into nostrils.
 They are mainly used for their antiseptic,
bronchodilator and decongestion action.
Granules
 Granulation is the process in which primary
powder particles are made to adhere to form larger
multiparticle or large particles entities called
granules.
 The bitter, nauseous, unpleasant powders can not
be given tablets, capsule due to bulk quantity are
required to be taken, as well as they are not given
in liquid dosage forms due to their stability such
powders are given in the granules forms.
 These powders are mixed with suitable exicipent
along with granulating agent, prepare a coherent
mass then dried & passed through the sieve to
obtained desired size of granules.
 E.g. Effervescent granules
Effervescent Granules
 Effervescent granules are meant for internal use.
 They contained medicaments mixed with citric acid, tartaric
acid & sodium bi carbonates, sometime saccharin or sucrose
may be added for sweetening taste.
 Before, administration desired quantity of granules are
dissolved in water, the acid & bicarbonate reacts with each
other to produce effervescence.
 Effervescent granules are prepared by two methods, namely
as, I) Heat method, II) Wet method
Heat method

 A large porcelain or stainless steel evaporating dish is placed over the


boiling water bath.
 The dish must be sufficiently hot (generally heating takes place for 1 – 5
min.) before transferring the powders into it, to ensure rapid liberation of
water of crystallization from citric acid.
 If heating of the dish is delayed then the powder which is added to it, will
heat up slowly & liberated water of crystallization will also be liberated
simultaneously.
 As a result, sufficient water will not be available to make a coherent mass.
 This coherent mass will pass through the sieve to obtained suitable size of
granules, dry it in oven at 600c then packed in air tight container.
Wet method

 In this methods all the ingredients are mixed thoroughly


 This powders mixture make moistened with non – aqueous
vehicle (e.g. alcohol), to prepare a coherent mass which is
then passed through sieve no 8 to obtained suitable granules.
 Then dried in oven at 600c. The dried granules are again
passed through the sieve to break the lumps which may be
formed during drying.
 The dried granules are packed in air tight container.
Tablets
 These are solid dosage forms of medicaments which are
prepared by moulding or by compression with or without
Excipients.
 The tablets can be prepared by two methods namely as a
I) Dry granulation, II) Wet Granulation
Capsule
 Capsules are solid unit dosage forms in which one or more
medicaments enclosed within a shell.
 Capsules mainly divided in to two parts namely as –
I) Body (Longest part of capsule shell), II) Cap (Smallest part of
capsule shell)
 The capsule are generally prepared by gelatin.
 Depending on their formulation, two types of gelatin are used
namely as – I) Hard gelatin, II) Soft gelatin.

Cap

Body
Pills
 These are small, rounded solid dosage forms containing
medicaments intended for oral use.
 The medicaments are mixed with excipients to forms a firms
plastic mass.
 The mass is rolled to uniform pill pipe, which cut into
numbers of uniform pills. The pills are spherical in shape &
produced by rolling them under wooden pill rounder.
 Sometimes pills are coated with varnish, gold leaf, etc to
improve finish, unpleasant taste & stability.
 Now a days pills are outdated preparations because of number
of disadvantages such as -
 Disintegration time of pill is uncertain means freshly prepared
pills are disintegrates readily rather than old dried pills.
 It is difficult to prepare pills of uniform size & weight.
Liquid dosage forms
Liquid dosage forms
 It may be defined as “A solution is a liquid-preparation that
contains one or more soluble chemical substances dissolved in
a specified solvent”
 Liquid dosage forms are intended for External, Internal or
parenteral use.
 The component of the solution which is present in a large
quantity is known as “SOLVENT” where as the component
present in small quantity is termed as “SOLUTE”
 They mainly classified in to two category namely as –

I) Monophasic Liquid dosage forms.


II) Biphasic liquid dosage forms.
Advantage
 Immediately available for absorption.
 Administration convenient, particularly for infants, psychotic
patients.
 Easy to color, flavor & sweeten.
 Liquids are easier to swallow than solids and are therefore
particularly acceptable for pediatric patient.
 A solution is an homogeneous system and therefore the drug
will be uniformly distributed throughout the preparation.
 Some drugs like aspirin, KCl can irritate gastric mucosa if
used orally as a solid dosage forms. But this effect can be
reduce by solution system.
Disadvantage

 Less stable in aqueous system. Incompatibility is faster in


solution than solid dosage form.
 Patients have no accurate measuring device.
 Accident breakage of container results in complete loss.
 Solution often provide suitable media for the growth of micro
organisms.
 The taste of a drug, which is often unpleasant, is always more
pronounced when in solution than in a solid form.
 Bulky than tablets or capsule, so difficult to carry transport.
Monophasic liquid dosage forms
 Monophasic liquid dosage forms are represent by true or colloidal
solution.
 The component of the solution which is present in a large quantity is
known as “SOLVENT” where as the component present in small
quantity is termed as “SOLUTE”.
 A solution is homogenous because the solute is an ionic or molecular
forms of subdivision.
 In case of colloidal solutions, the solutes are present as aggregates
although they cannot be seen by necked eye or ordinary microscope.
 It is sub classified as –
I) Internal Use, II) External use
Monophasic Liquid Dosage
forms

Internal Use External Use

 Liniments
 Syrup  Lotions
 Elixirs  Gargles
 Linctuses  Mouth Wash
 Drops  Throat paints
 sprays
 Inhalations
 Nasal drops
 Eye drops
 Eye lotions
 Ear drops
Monophasic liquid dosage forms
for Internal Use
Syrup

 It is a concentrated or saturated solutions of sucrose in purified


water.
 The concentration of sucrose is 66.7% w/w & due to that it is a
viscous preparations.
 The syrup which contains medical substance called as a
medicated syrup & those containing aromatic or flavored
substance known as a flavored syrup.
Importance of syrup
 It retards oxidation because its partly hydrolyzed into
reducing sugar.
 It prevents decomposition of many vegetable substance
because its have high osmotic pressure which prevent the
growth of bacteria.
 They are palatable due sweet taste.
Elixirs
 It is clear, sweetened, aromatic,
hydroalcholic preparations meant for
oral use.
 The medicated elixirs are generally
contained potent drug like as
antibiotics, antihistamine or sedative ,
where as non – medicated elixirs
contained flavoured.
 The composition of elixirs contained
mainly as ethyl alcohol (active
ingredients),water, glycerin or
propylene glycol, colouring agent,
flavouring agent & preservative.
Linctuses
 These are viscous liquid preparations that’s
are used for the treatment of cough.
 They contain medicaments which have
demulcent, sedative, expectorant action.
 They are taken in small doses without
diluting with water to have prolonged
effect of medicines.
 Simple syrup is used as a vehicle for most
of the linctuses.
 Tolu syrup is preferred in certain cases
because of its aromatic odour & flavour.
Moreover it have a mild expectorant action
Drop
s
 These are liquid preparations meant for oral administration.
 The oil soluble vitamins, such as vitamin A & D concentrates
in fish – liver oil are presented as drops for administration.
 Since these preparations contain potent medicaments, the dose
must be measured accurately
 The following two methods are commonly used for this
purpose.
 Use of a dropper which is accurately graduated in fractions of
a milliliters.
 Use of a pre – calibrated dropper.
Monophasic liquid dosage forms
for External use
Liniments
 Liniments are liquid or semi- liquid preparations
meant for external application to the skin.
 They are usually applied to the skin with friction
& rubbing of the skin.
 Are usually alcoholic and oily liquid preparations
(monophasic) or emulsion (biphasic).
 Alcoholic liniments are used generally for their
rubefacient and counterirritant effects. Such
liniments penetrate the skin more readily than do
those with an oil base.
 The oily liniments are milder in their action and
may function solely as protective coatings
 Liniments should not be applied to skin that are
bruised or broken.
Lotions
 Are usually aqueous, alcoholic or oily
liquid preparations.
 They are intended for external
application without friction or rubbing
to the affected area
 Usually applied with the help of some
absorbent material such as cotton wool
or gauze.
 It is generally used to provide cooling,
soothing and protective & antiseptic
action.
Gargles
 Gargles are aqueous solutions used for treating throat infection
(pharynx and nasopharynx part)
 Supplied in concentrated forms with directions of dilution with warm
water before use
 They are used into intimate contact with the mucous membrane of
throat for few seconds, before they are thrown out of the mouth.
 They are used to relieve soreness in mild throat infection.
 They are also used for their antiseptics, antibiotics and/or anesthetics
Mouth wash
 These are aqueous solutions with
pleasant or acceptable taste & odour
 These are used to make clean &
deodorise the buccal cavity or used for
oral hygiene and to treat infections of
the mouth.
 They mainly contain antibacterial
agent, alcohol, glycerin, sweetening
agent, flavoring agent & colouring
agent.
Throat paints
 Throat paints are viscous liquid
preparations used for mouth and
throat infections
 Glycerin is commonly used as a
base because being viscous it
adheres to mucous membrane for
long period and it possess a sweet
taste.
Sprays
 These are the preparations of drugs in media
which may be aqueous, alcoholic, or glycerin.
 They are applied to the mucous membrane of
throat or nose with an atomizer.
 The throat sprays must be sprayed from a
special type of atomizer known as a nebulizer,
which removes the large droplets by baffling
system. Only precaution should be taken that
the fine droplet will used to easily reach the
lungs.

Nebulizer
Inhalations
 These are liquid preparations containing volatile substance & are used to
relieve decongestion & inflammations of respiratory tract.
 The volatile substance in inhalations would be volatile at room
temperature so that they should be placed on some adsorbent pad or
handkerchief.
 In some cases inhalations will added to hot water (650c) then vapors will
inhaled.
Nasal drops
 Drugs in solution may be instilled into the nose from a dropper or from a
plastic squeeze bottle.
 The drug may have a local effect, e.g. antihistamine, decongestant.
 Alternatively the drug may be absorbed through the nasal mucosa to exert a
systemic effect.
 The use of oily nasal drops should be avoided because of possible damage
to the cilia of the nasal mucosa & if it is used for long period may reach the
lungs & cause lipoid pneumonia.
 To avoid that Nasal drops are prepared so that they are similar in many
respects to nasal secretions, so that normal ciliary action is maintained thus
aqueous nasal solutions usually are isotonic and slightly buffered to
maintain a pH of 5.5 to 6.5.
Eye drops
 Sterile, aqueous/oily solutions or suspensions intended for instillation in
eye sac.
 Eye drops may contain buffers, stabilizing agents, dispersing agents,
solubilising agents, anti-oxidants & agents required for tonicity/ viscosity
adjustment
 Single dose container should not contain anti-microbial preservative.
 In case of multi dose container a dropper should be supplied with it for
administration. Maximum size of such containers is 10 ml.
Eye lotions
 These are the aqueous solutions used for washing the eyes.
 These are supplied in concentrated forms & are required to diluted with
warm water immediately before use.
 They should be free from foreign particles to avoids irritation to the eye.
 They are required to prepared fresh & should not be stored for more than
two days to avoid microbial contaminations.
Ear drops
 These are the solutions of drugs that are instilled into ear cavity with the
help of dropper.
 These are generally used for cleaning the ear, softening the wax & for
treating the mild infections.
 The solutions is generally prepared in water, glycerin, propylene glycol &
dilute alcohol.
Biphasic liquid dosage
forms
Biphasic liquid dosage forms
 The liquid which consist of two phases are known as a biphasic liquid
dosage forms.
 They are sub categorized into two different forms namely as –
I) Emulsion
II) Suspension

 In emulsion both phases are available in liquid where as in suspension,


finely divided solid particles are suspended in liquid medium.
Emulsion
 Emulsion is a biphasic liquid preparations containing two immiscible
liquid (Continuous Phase & dispersed phase) made missicible.
 The liquid which is converted into minute globules is called as dispersed
phase & the liquid in which the globules are dispersed is called the
continuous phase
Two Immiscible Liquids
dispersed phase
Dispersed Phase
(Internal phase)
continuous phase
Continuous Phase
(External phase)

 An emulsion is a thermodynamically unstable system consisting of at least


two immiscible liquid phases one of which is dispersed as globules in the
other liquid phase stabilized by a third substance called emulsifying agent.
The globule size in emulsion varies from 0.25 to 25 µm.
 Examples for emulsions:- milk, rubber latex, crude oil etc.

A.: Two immiscible liquids not emulsified


B. An emulsion of phase B dispersed in Phase A
C. Unstable emulsion slowly separates.
D. The emulsifying agent ( black film) places it self on the interface between
phase A and phase B and stabilizes the emulsion.
Types of emulsions
Simple type
 Water in oil (w/o)

 Oil in water (o/w)

Depending on globule size


 Micro emulsion

 Fine emulsion

Special type
 Multiple emulsion (w/o/w, o/w/o)
Water in oil (w/o)
 In this types of emulsion water is dispersed phase & oil is continuous
phase
 w/o types of emulsion generally meant for External use.
 Examples are butter, lotions, creams etc.
 In rare case they are used internally.

Water is dispersed phase


Oil is continuous phase
Oil in water (o/w)
 In this types of emulsion oil is dispersed phase & water is continuous
phase
 o/w types of emulsion meant for both Internal use & External use.
 Examples for internal use are Vitamin A in corn oil, liquid paraffin in
water etc.
 Examples for External use are Benzyl benzonate emulsion.

Oil is dispersed phase


water is continuous phase
Micro Emulsion
 These are clear dispersions of o/w or w/o in which the globules have small
size like as a 10nm or 0.01 µm..
 Being cleared products micro emulsion are more popular now a days.
 Micro emulsions are thermodynamically stable optically transparent ,
mixtures of a biphasic oil –water system stabilized with surfactants.
Fine emulsion
 Normally these have a milky appearance.
 The globule size ranges from 0.25 to 25 µm.
Multiple emulsion
 These are emulsion with in emulsion & designated as w/o/w or o/w/o.
 The drugs that is incorporated in the innermost phase must cross two
phase boundaries before getting absorbed.
 It is generally used in oral sustained release or intramuscular therapy.
Identification tests
 Dilution test
 Conductivity test
 Dye test
 Fluorescence test
 Cobalt chloride test
 Filter paper test
Dilution test
 The emulsion is diluted with water, after dilution emulsion remain stable
then it is said to be o/w type of emulsion because water is in continuous
phase. If emulsion is break after dilution with water then it is said to be
w/o type of emulsion.

Add drops of water Add drops of water

Water distribute
Uniformly

O/W Emulsion W/O Emulsion


Conductivity test
 Conductivity test can be performed by dipping a pair of electrode
connecting with low voltage bulb & pass the current.
 If bulb glows then it is said to be o/w type of emulsion because water is in
continuous phase & it is good conductor of electricity.
 If bulb doesn't glow then it is said to be w/o type of emulsion because oil
is bad conductor f electricity.

Emulsion
Emulsion

Bulb glows with O/W Bulb doesn’t glow with W/O


Dye test
 Oil soluble Scarlet red dye is mixed with emulsion.
 Place a drop of emulsion on microscopic slide cover it with cover slip &
examine under microscope.
 If disperse globules appears red & ground is colourless then it said to be
o/w type of emulsion because water is present in continuous phase.

Water is Oil is dispersed phase


continuous phase

 If reserve condition occurs (If disperse globules appears colourless &


ground is red colour then it said to be w/o type of emulsion because oil is
present in continuous phase.)
Water is disperse phase

Oil is continuous
phase
Fluorescence test

 Certain fixed oil posses the physical properties of fluorescing in the


presence of ultraviolet radiations.
 If examine under microscope ground is fluorescence then it said to be w/o
type of emulsion because oil is present in continuous phase.
 If examine under microscope droplet is fluorescence then it said to be o/w
type of emulsion because oil is present in disperse phase.
Creaming test

 The direction of creaming identifies the emulsion type, if the densities


of aqueous and oil phases are known.
 Water-in-oil emulsions normally cream downward as oil is usually less
dense than water.
 Oil-in-water emulsions normally cream upwards.
Cobalt chloride test

 Pour the emulsion on filter paper then it is soaked in cobalt chloride


solutions & allowed to dry turns from blue to pink.
 Then this emulsion is said to be o/w type of emulsion.
 This test may fail if emulsion unstable or breaks in presence of
electrolyte.
Filter paper test

 This test is based on the fact that an o/w emulsion will spread out
rapidly when dropped onto filter paper.
 In contrast, a w/o emulsion will migrate only slowly. This method
should not be used for highly viscous creams.
Suspension
 Suspensions are the biphasic liquid dosage forms
of medicament in which finely divided solid
particles ranging from 0.5 to 5 micron are
dispersed in a liquid or semisolid vehicle, with aid
of single or combination of suspending agent.
 In which solid particles acts as disperse phase
where as liquid vehicle acts as continuous phase
 The external phase (suspending medium) is
generally aqueous in some instance, may be an
organic or oily liquid for non oral use.
 The particle size for non oral suspension is so
important to avoid grittiness to skin.
Advantage of suspension
 Suspension can improve chemical stability of certain drug. E.g. Procaine
penicillin
 Drug in suspension exhibits higher rate of bioavailability than other
dosage forms.
Solution > Suspension > Capsule > Compressed Tablet > Coated
tablet
 Duration and onset of action can be controlled. E.g. Protamine Zinc-
Insulin suspension.
 Suspension can mask the unpleasant/ bitter taste of drug. E.g.
Chloramphenicol
Disadvantage of suspension

 Physical stability , sedimentation and compaction can causes problems.


 It is difficult to formulate.
 Uniform and accurate dose can not be achieved unless suspension are
packed in unit dosage form.
 All suspensions are required to be shaken before measuring of dose.
 The storage of suspension may lead to changes in disperse system
especially, when there is fluctuations in temperatures.
Ideal qualities of good suspension

 It should settle slowly & easily re – dispersed on shaking


 It should readily & evenly pour from container.
 It should be chemically inert.
 It should not forms hard cake.
 It should prevent degradation of drug or to improve stability of drug.
 It should mask the taste of bitter of unpleasant drug.
Flocculated suspension
 In this type, solid particles are loosely aggregates themselves, means individual
particles are come in contact with each other to forms network like structure
called as a floccules.
 These flocs are light, fluffy in nature, which are held together by weak van der
waals force of attraction.
 Aggregation is achieved by adding flocculating agent.
 This suspension will readily sediments.
 This suspension posses better physical stability but less bioavailability as
compared to deflocculated suspension due to dissolution of floccules.
Deflocculated suspension
 In this type of suspension, individual particle exits as a separate entity, means
particles carry a finite charges on their surface . Hence particles approaches each
other, they experience repulsive forces. This force create a high potential barrier,
which prevents a aggregation of particles.
 During storage, these suspension shows a sedimentation at slow rate, due to that
particles forms a close packing arrangement.
 So that it is difficult to re dispersed on agitation & forms a cake or claying which is
hard in nature.
 This type of suspension have shorter shelf life but high bioavailability as compared
to flocculated suspension.
Difference between flocculated & deflocculated suspension

Flocculated Suspension Deflocculated suspension


Particles form loose aggregates & forms Particle exist as separate entities.
network like structure.
Particles experience attractive forces. Particles experience repulsive forces.
Supernatant liquid is clear. Supernatant liquid is cloudy.
The rate of sediment is high. The rate of sediment is slow.
Sediment is rapidly formed. Sediment is slowly formed.
sediment are loosely packed, hence hard Sediments are closely packed, hence
cake is not formed. hard cake is formed.
The sediment is easy to redisperse on Sediment is difficult to redisperse on
shaking. shaking. (due to formation of hard cake)
Bioavailability is comparatively less. Bioavailability is relatively high.
The suspension is not pleasing in The suspension is pleasing in
appearance. appearance.
Semisolid dosage forms
Semisolid dosage forms
 Semisolid dosage forms meant for external application
 Semisolid dosage forms subcategorized are as-
I) ointment
II) creams
III) paste
IV) Jellies
V) Suppositories

 The suppositories are also included in this category but it is a unit dosage
forms.
Ointment
 Ointment are semisolid preparation meant for application to skin or
mucous membrane.
 The ointments are mainly used for their protective or emollient properties
 It may be defined as a medicament or medicaments dissolved, suspended
or emulsified in ointment base.
 There is no single ointment base which possesses all the qualities of ideal
ointment base, so it become necessary to use more than one ointment base
in the preparation of ointment.
Qualities of ideal ointment base
 It should be inert, odourless & colourless & smooth.
 It should be physically & chemically stable.
 It should be compatible with the skin & with incorporated medicaments.
 It should be of such consistency that it spread & soften when applied to
skin with stress.
 It should not retard healing of wound.
 It should produce irritation or sensitization of the skin.
Classification of ointment base

 Oleaginous bases
 Absorption bases
 Emulsion bases
 Water soluble bases
Oleaginous base
 These bases consist of water soluble hydrocarbons, vegetable oils, animal
fats & wax.
 The constituents of hydrocarbon bases are soft paraffin, hard paraffin &
liquid paraffin.
 The vegetable oils are mainly used in ointment to lower the melting point
or to soften the bases.
 These bases serve to keep the medicaments in prolonged contact with the
skin & also act as occlusive dressings. They have a low capacity to absorb
water & are used chiefly for their emollient effect.
 These bases losing their importance now a days for the many reason.
Disadvantages of oleaginous bases

 They are greasy.


 They are sticky & are difficult to remove both from skin & clothing.
 They retain body heat which may produce an uncomfortable feeling of
warmth.
 They do not help in the absorption of medicaments.
Absorption bases
 These bases are generally anhydrous substance which have the property of
absorbing considerable quantities of water but still retaining their ointment
like consistency.
 The absorption bases are of two type namely as
I) Non emulsified bases
II) Water in oil emulsion
 Non emulsified bases absorb water & aqueous solutions producing w/o
emulsion. E.g. Wool fat, wool alcohol, beeswax & cholesterol.
 Water in oil emulsions are capable of absorbing more water & have the
properties of non- emulsified bases. E.g. hydrous wool fat ( lanoline)
Emulsion bases


These bases are semisolid or have cream like consistency.
 Both o/w or w/o emulsions are used as a ointment base.
 The o/w emulsion base is more popular now days because ease of
application will easily achieved.
 The w/o type of emulsion bases are greasy & sticky.
 The emulsifying ointment is prepared from emulsifying wax, white soft
paraffin & liquid paraffin.
Water soluble bases

 These are commonly known as greaseless ointment bases.


 The water soluble bases consist of water soluble ingredients such as
carbowaxes ( polyethylene glycol polymer)
 The carbowaxes are water soluble, non – volatile & inert substance.
 Selection of appropriate carbowaxes is depend on their molecular weight.
creams
 These are viscous semisolid emulsions which are meant for external use.
 Cream is divided in to two types namely as
I) Aqueous creams
II) Oily creams
 In case of aqueous creams the emulsions are o/w type & it is relatively non
greasy. The emulsifying waxes are anionic, cationic & non –ionic used.
Generally polysorbate, triethanolamine soap are used as emulsifying agent.
 In case of oily creams w/o type & it is relatively greasy. The emulsifying
agent such as wool fat, wool alcohols, beeswax & calcium soap is used.
 The cream should be store in collapsible tube & supplied in well closed
container to prevent evaporation & contamination.
pastes
 Pastes are semisolid preparations intended for
external application to skin.
 The pastes are generally very thick & stiff.
 They do not melt at ordinary temperature & thus
forms a protective coating over the area where
they are applied.
 Pastes are differ from ointment as they contain a
high proportion of finely powdered medicaments.
 They are mainly used as a antiseptic, protective,
soothing dressings.
 Pastes should be stored & supplied in containers
made of materials which do not allow absorption
or diffusion of content.
jellies
 Jellies are transparent or translucent, non greasy, semi solid preparations
mainly used for external application to skin.
 These are also used for lubricating catheters, surgical gloves & rectal
thermometer.
 The substance like gelatin, starch, tragacanth, sodium alginate & cellulose
derivatives are used for the formulation of jellies.
 Jellies are of three types namely as
 Medicated jellies
 Lubricating jellies
 Miscellaneous jellies
New drug delivery system
Introduction
With the advancement of pharmaceutical sciences, a new concept have
evolved various modern dosage forms & methods of their administration.
Some of the modern dosage forms are
 Implants
 Films & strips
 Liposome drug carriers
 Controlled drug delivery modules
 Erythrocytes
 Nanoparticles
 prodrugs
Implants
 These are hypodermic tablets are placed under the skin by a minor surgery in order to
release drugs over prolonged periods of time.
 Now the magnetically controlled implants have been developed which can be opened or
closed at will in order to release or stop the drug.
 These implants are placed at upper thigh at a depth of 5mm.
 These implants are useful in hormone therapy.
Films & strips
These are meant for topical application for slow release of drug over
predetermined period of time. Films & strips are more popular these days.
They are sub categorized in to following types namely as
 Zero order release films
 Buccal strips
 Spray bandages
Zero order release films
 These are called as laminates & meant for topical application. E.g.
 Nitroglycerine laminates are prepared by mixing propylene glycol with
about 1% carbopol resin. The mixture is neutralized with NaoH solution &
then 0.1% of nitroglycerin is added. It is then placed in polythene sheet
5*5 cm & its edges are sealed by heat. It is then placed on pressure
sensitive adhesive sheet of 5.5 * 5.5 cm so that it can be properly
adhesive to skin. Such laminates release the drug slowly into circulation
for about 12 hours.
Buccal strips
 The buccal & sublingual tablets are now replaced with buccal strips.
 These strips consist of a thin absorbent base of fabrics, filter paper &
cotton etc.
 The buccal strips are prepared by immersing a long piece of fabric made
from polyamide fibers into a molten mixture of carbowaxes & dissolved
or dispersed the drug.
 The fabric is then cooled & cut into small pieces.
 It should be contact with buccal mucosa for about 15 min. & then
removed & discarded.
Spray bandage

 These bandage are prepared by spraying the solution of drug in polylactide


(polymer of lactic acid anhydride)
 A solution of purified lactide polymer is made in chloroform.
 It is then packed in aerosol container having suitable propellant.
 When these solution sprayed then it will be a comfortable bandage which
can simply washed of with warm water.
Liposome drug carriers
 These are several carriers in our body which transport both to an other like
as enzymes, proteins etc.
 These are phospholipids which can transport both hydrophilic &
hydrophobic drugs.
 The large multilamellar vesicles (LMV), small unilamellar vesicles (SUV),
large unilamellar vesicles (LUV) are some of the liposome's known today.
Applications
 Used in diseases caused by intracellular parasites. E.g. malaria,
tuberculosis & amoebiasis.
 It entrapped insulin is active orally & can be replaced by IM
administration of insulin.
 It can be used to transport functional DNA/RNA molecules into cell.
 It can be used to transport radio pharmaceuticals & immunological
products.
 Liposomal daunomycin has longer duration of action than free
daunomycin which is used in the treatment of neoplasia.
Controlled drug delivery modules
 These are the device which are formed by embedding the drug within a
polymeric matrix so that it gets released slowly to the body over a long
period of time.
 It will formed drug – polymer complex & may be formulated in to tablet,
capsule or any other suitable formulation.
 These modules are punctured before administration with leaser beam to
make a small orifice for release of the drugs.
 The drugs is released from these modules by diffusion, osmosis or
chemical reactions.
 These are applied to skin, implanted subcutaneously or inserted into
various body cavities.
Erythrocytes
 Erythrocytes are tried in order to achieve controlled release of drugs.
 The life span of erythrocytes are 120 days.
 It can allow a drug to circulate in the body for long period of time which
help slow release of the drugs in to serum.
 Released erythrocytes are prepared by putting them in to a hypotonic
medium. So that they can easily swollen.
 The aqueous solutions of the drug is added to the medium so that drugs
gets in to erythrocytes through open pores.
 When isotonicity is adjusted the erythrocytes shrink, thus encapsulating
the drug with in them. These erythrocytes may be suspended in normal
saline solutions for preparing injections.
Applications
 Released erythrocytes of urease have been used in kidney failure to
degrade serum urea.
 Released erythrocytes of asparaginase have shown good result in
asparaginase dependent leukemia.
 Released erythrocytes of methotrexate & adrianycin have been tried in
cancer therapy.
 Released erythrocytes of prednisolone have shown good result to prolong
the anti-inflammatory action.
Nanoparticles

 It is based on colloidal drug delivery system.


 The particles size of this system is in nanometer range (200 – 500 mm)
 The system consist of a drug & carriers to deposit the drug at target site.
 The carriers used are naturally occurring macromolecules like human
serum albumin, bovine serum albumin, & other substances like gelatin,
casein & ethylcellulose.
Applications

 Flourescein isothinocyanate (FITC) nanoparticles have been used to


incorporate cytotoxic agent into tumor cell in cancer chemotherapy.
 Nanoparticles along with biological maker like immunoglobulin can be
used to target the drugs to very specific site.
Prodrugs

 The compound which undergo biotransformation before showing desired


pharmacological activity are called prodrugs or proagents.
 Prodrugs are generally the ester or amides of parent drugs.
 These are useful to improving the stability, solubility, bioavailability of
drugs, masking the unpleasant taste & odour of the parent drug & reducing
the toxicity
Applications

 Choramphenicol palmitate, the prodrug of chloramphenicol is used in the


preparation of pediatrics suspension because it has no bitter taste.
 Procaine penicillin G & benzathine penicillin G are prodrugs of penicillin
G which shows resistance to hydrolysis as compared to the parent drug.
 Cindamycin 2- phosphate the prodrug of cindamycin has no bitter taste of
parent drug.
Thank you

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