Drug Formulations

&
Routes of Administration
Dr. Rodney Martinez

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Route of admnistration
Important
Info

The ROA is determined by the

physical characteristics of the
drug, the speed which the drug is
absorbed and/ or released, as well
as the need to bypass hepatic
metabolism and achieve high
conc. at particular sites
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No single method of drug
administration is ideal for all
drugs in all circumstances

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General Considerations
• Pharmaceutics – branch of
Pharmacy that deals with drug
formulations
• Pharmaceutical products need to be
presented in a form that can be
administered to an organism
• Formulation takes into consideration
easy delivery as well as guaranteed 4
desired action (drug reaches target,
achieves therapeutic action)
Drug Absorption

• Absorption is the process by which a

drug enters the bloodstream without
being chemically altered or
• The movement of a drug from its site
of application into the blood or
lymphatic system

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Drug Absorption
• Factors which influence the rate of absorption
• types of transport
• the physicochemical properties of the
drug
• protein binding
• routes of administration
• dosage forms
• circulation at the site of absorption
• concentration of the drug 6
Drug Absorption

• The rate at which a drug reaches it

site of action depends on:
• Absorption - involves the passage of
the drug from its site of administration
into the blood
• Distribution - involves the delivery of
the drug to the tissues

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Routes of Drug Administration

The route of administration (ROA)

that is chosen may have a profound
effect upon the speed and
efficiency with which the drug acts

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• The possible routes of drug entry
into the body may be divided into
two classes:

•Enteral
•Parenteral
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Enteral Routes
• Enteral - drug placed directly in the GI
tract:
• sublingual - placed under the
tongue
• oral - swallowing (p.o., per os)
• rectum - Absorption through the
rectum

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Parenteral Routes
• Intravascular (IV,
IA)- placing a drug
directly into the blood
stream
• Intramuscular (IM) -
drug injected into
skeletal muscle
• Subcutaneous -
Absorption of drugs
from the
subcutaneous tissues
• Inhalation -
Absorption through the
lungs 12
Parenteral administration
• Intravenous, Intramuscular, Subcutaneous,
• Ensures active drug absorption
• More rapid drug delivery than Oral
• Only route acceptable for unconscious
patients, uncooperative patients
• Systemic absorption depends on capillary
membrane surface area, drug solubility in
interstitial fluid
• Advantages:
• Rapid precise blood drug levels
• Irritant drugs more comfortably administered 13
• Drug is rapidly diluted
Routes of administration

Oral Topical
Enteral

Parenteral
Sublingual Subcutaneous
Rectal Inhalation
Intramuscular
Intravascular
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Intravascular
Absorption phase is bypassed
(100% bioavailability)
1.precise, accurate and almost immediate
onset of action,
2. large quantities can be given, fairly pain
free
3. greater risk of adverse effects
a. high concentration attained rapidly
b. risk of embolism
c. risk of mistake 15
Intravascular drug
administration

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Intramuscular
• 1. very rapid
absorption of drugs
in aqueous solution
• 2.repository and
slow release
preparations
•
• 3.pain at injection
sites for certain
drugs
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Subcutaneous
• 1. slow and constant
absorption
• 2. absorption is
limited by blood flow,
affected if
circulatory problems
exist
• 3. concurrent
administration of
vasoconstrictor will
slow absorption
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Inhalation
• 1.gaseous and volatile
agents and aerosols
• 2.rapid onset of action
due to rapid access to
circulation
• a.large surface
area
• b.thin membranes
separates alveoli
from
circulation
• c.high blood flow
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 Topical
• Mucosal membranes (eye
drops, antiseptic, sunscreen,
callous removal, nasal, etc.)
• Skin
• a. Dermal - rubbing in of oil
or ointment
(local action)
• b. Transdermal - absorption
of drug through
skin (systemic action)
• i. stable blood levels
• ii. no first pass metabolism
• iii. drug must be potent or
patch becomes to large
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 Route for administration
-Time until effect-

• intravenous 30-60 seconds

• intraosseous 30-60 seconds
• endotracheal 2-3 minutes
• inhalation 2-3 minutes
• sublingual 3-5 minutes
• intramuscular 10-20 minutes
• subcutaneous 15-30 minutes
• rectal 5-30 minutes
• ingestion 30-90 minutes
• transdermal (topical) variable (minutes to hours)
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Parenteral
Preparations

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Parenteral Administration
injecting drugs
Parenteral – mode of drug administration that avoids the
GIT. Drug injections. Use of ASEPTIC TECHNIQUE
very very important!!
• Intravenous (IV) injections – fast action due to
avoidance of GI absorption
• Intradermal – injected into the dermis; very slow
absorption; only small quantities of the drug can be
given this way.
• Subcutaneous – just beneath the skin; very slow route;
poor blood supply
• Intramuscular – into the fleshy part of the muscle:
gluteus, deltoid, anterior thigh; 23
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Specialized Modes of
Administration
• Intrathecal – drug is introduced into the CSF-
filled space surrounding the spinal cord; for
giving of drugs directly into the CNS,
avoiding the blood-brain barrier e.g.
Baclofen, Morphine
• Epidural – drug is introduced into the space
above the dura; useful in administering local
anesthetics for surgical procedures in the
pelvic area & below
• Intra-articular – injection directly into joint
spaces 26
DRUG FORMULATIONS 27
 Oral Preparations
• Pill – round or ovoid solid body; may be
coated with sugar or other substance
• Tablet – granulated powder containing one or
more medications, compressed into a disc;
must disintegrate in the GIT, so starch is often
incorporated; + sugar-/film- coating;
• Dragees – chewable tablets
• Enteric-coated tablets – coated with a
substance that is stable at acidic pH (will not
disintegrate in the stomach) but breaks down
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rapidly at higher pH (small intestines)
 Oral Preparations
• Capsule – an outer “shell” holds the drug
inside
• Hard gelatin capsule – contains solid drug
in powder form; may be opened
• Soft gelatin capsule – contains the drug in
liquid or semi-liquid form; cannot be
opened; useful for drugs that are insoluble
in water
• Sustained/Slow-release preparations – drug
is formulated in such a way that it releases
very slowly in the GIT; a single dose suffices
for delivery of the drug over a period of hours,
ensuring sustained action. 29
Oral drugs

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 Oral Preparations
Liquid preparations – for children & for adults
who have difficulty swallowing pills; usually
flavored to make them palatable;
• Elixirs – drugs insoluble in water are
dissolved in Alcohol
• Syrups – sugared liquid preparations
• Suspension – drug in solid form, not
dissolved in Alcohol
• Emulsion – drug in liquid form, not dissolved
in Alcohol 31
Liquid drugs

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Oral Drug Formulations
Solid
• Pill
Liquid
• Tablet
• Dragee
•Elixirs
• Enteric Coated Tablets •Syrups
• Capsule
• Sustained/Slow •Suspension
release preparations
•Emulsion 33
 Topical
Preparations
Topical – application of a drug to the skin/ mucosa
overlying the area to be treated
• Drops – isotonic solutions – ophthalmic, nasal, otic
(eardrops – formulated as oily solutions for
adherence to the aural cavity)
• Creams – water-based, poorly absorbed; drug is left
on skin surface as water evaporates
• Ointments – lipid-based, greasy appearance & feel;
drug penetrates deeply into tissues, especially if with
“occlusive” dressing
• Pastes – have a very high powder content; water-
repellent.
• Gels & Lotions – used on hairy parts of the body.
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PROBLEMS 36
Case 1
• Linda is a 16 year old girl that is having an acute asthma
attack, she is taken to the ER and the doctor over there
finds her with wheezing in both pulmonary fields,
cyanosis a breathing rate of 45 bpm, a pulse of 140 bpm,
an axilar temperature of 38º C, and 110/90 mmHg of
blood pressure.
• The doctor requests a CBC and a chest x-ray and while
completing the work he knows that he has to admnister:
• Salbutamol, a beta adrenergic drug
• Hydrocortisone, a corticosteroid
• Dipirone, a pyrolitic
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Questions
1) What route of admnistration are you going to use for
the
• Salbutamol
• Hydrocortisone
• Dipirone
2) What advantages and disadvantages this decisions may
present?
3) What considerations must be taken before
administerring the drugs?
4) What considerations should we have after we
administered the drugs? 38
Case 2
• Leonard is a 22 year old student of accounting that is affected
wirth epilepsy and now is under oral valproic acid as
treatment.
• One day studing for his finals he forgets to take the
medication and has a seizure over the university and is taken
to the ER.
• The Doctor in the ER, finds him with loss of counsiosness,
pallor, a pulse of 120 bpm, a breatihng rate of 40 per minute,
reactive tu pupilary response, deep osteotendinous reflexes
present.
• He knows that the treatment for the acute episode of seizure
includes midazolam in the ER, Phenobarbital if admitted and 39
ieventually the reposition of the therapy for the seizure
Questions
1. What of the drugs would you administered? Why?
1. Midazolam
2. Phenobarbital
3. Valproic Acid
2. If you have a patient with seizure in the ER what route of
administration would you choose? Why?
3. If you have a children what type of formulation is more
appropiate for the valproic acid of enteral routes
4. In this patient what can be occuring with the valproic acid?
How can you be sure eventually?

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Case 3
• Mary takes her 3 months old baby to the pediatritian because
is been having a lot of fever, cough and runny nose for the
past 3 days.
• She’s been giving the baby flu medicine by herself and as the
baby does not seem to improve decides to take him to the
doctor.
• The doctor after examing the baby makes a diagnosis of
tonsillopharingitis and decides to initiate amoxicilin in syrup
and continuing with the pyrolitics.
• After 30 minutes of administering the first dose of the syrup
the baby starts to have a skin rush, vomits and difficulty to
breath
• Because of this Mary takes her to the ER, and they make the
diagnosis of Adverse effect anaphylactic reaction to the 41
amoxicilin
Questions
1) Why do the adverse effects start to appear after 30 minutes
of administering the drug?
2) What type of route of admnistration will present adverse
effect more rapidly? And which one will present adverse
effects the latest?
3) In the ER with a patient like this you got to administer
clorfeniramine, and antihistamiinic drug, and hydrocortisone
a corticosteroid. What routes are you going to choose?
Why?
4) If you have a patient in which you prescribed a cream what
particularities the adverse effects may have?
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