SA

M
PL
E
PD
F
G
D
C
PR
IM
E
SA
M
PL
E
PD
F
G
D
C
PR
IM
E
 PHARMACEUTICAL TECHNOLOGY : PREFORMULATION Module-9

SCAN ME
CHAPTER

01 Preformulation
To Join FREE
Online Test

E
INTRODUCTION

IM
 It is defined as the phase of research and development in which preformulation studies
characterize physical and chemical properties of a drug molecule in order to develop safe,

PR
effective and stable dosage form.

Particle size and shape, Density,

Dielectric constant, Wetting
Study of physical property, Solubility, Dissolution,

C
properties of drugs Stability and Bioavailability
PREFORMULATION
Study of chemical
properties of drugs
D Hydrolysis, Oxidation, Reduction,
Racemisation, Polymerization,
G
Drug excipient and Compataibility

 Objective
F

 Develop the most safe, stable and efficacious dosage form with maximum bioavailability.
PD

 To determine its kinetics and stability.

 Produce necessary and useful data for development of analytical methods.
 Determine most stable polymorph and salts forms that give maximum bioavailability.
 Minimize the time and money required for formulations.
E

PHYSICAL CHARACTERISTICS
PL

PHYSICAL CHARACTERISTICS
M

BULK CHARACTERIZATION SOLUBILITY ANALYSIS STABILITY ANALYSIS

SA

Crystallinity and Intrinsic solubility Solution stability

Polymorphism Partition coef ficient (Ko/w) Solid state stability
Fine particle Ionization constant (pKa ) Excipients compatibility
characterization Common ion effect (Ksp)
Powder density and flow
property pH Solubility profile
Hygroscopicity Solubility enhancement
Compaction properties Dissolution
Thermal ef fects

Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
1
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 GPAT DISCUSSION CENTER
Module-9 Makes Study Easy

Packing properties • Molar volume and density

[GPAT-2020] • Refractive index
• Conductivity electrical and thermal
• Hygroscopicity
Kinetic properties • Dissolution rate
• Rates of solid state reactions
• Stability
Surface properties • Surface free energy
•

E
Interfacial tensions
• Habit (i.e. shape)

IM
Mechanical • Hardness
properties • Tensile strength
• Compactibility tableting

PR
• Handling flow and blending

DETERMINATION OF SURFACE AREA

C
SURFACE AREA MEASURED BY
CHARACTERISTICS
ADSORPTION METHOD AIR PERMEABILITY METHOD
Definition
D
Volume of nitrogen absorbed Rate at which gas or liquid
to form a monolayer permeates a bed of powder
G
Equations BET Equation Poiseuille’s Equation
πΔpr2t
P 1 (b -1)p V=
F

= + 8ηL
V(po - p) Vm b Vm bp o
PD

Kozeny – Carman Equation

A ΔP ε2
V= 2 + ×
ηS KL (1 - ε)2
Instrument Quantasorb Fisher subsieve sizer
E

Detector Thermal conductivity Water monometer

PL

WETTING AGENTS
 The wetting agent molecule has a portion with an affinity for the particle surface and a portion
M

with an affinity for water. CONTACT ANGLE (COS θ) DEGREE OF WETTING

 It facilitates intimate contact of the θ=0 Perfect wetting
SA

liquid with particle surfaces. 0<θ<90° High wettability

 Wetting agents for concentrates are 90° ≤ θ < 180° Low wettability
usually nonionic surfactants. θ = 180° Perfectly non-wetting

 = 0o  < 90o  = 90o  > 90o  = 180o

Complete wetting Partial wetting Non wetting


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
14
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : INTRODUCTION OF DIFFERENT DOSAGE FORM Module-9

SCAN ME
CHAPTER
Introduction of Different
02 Dosage Form
To Join FREE
Online Test

E
INTRODUCTION

IM
 Pharmaceutics is the branch of science which deals with the formulation of drug into dosages
form. It is the science of compounding and dispensing drugs.

PR
 Dosages form: Drugs are rarely administered in their original pure state. They are converted into
suitable formulation called as dosages form.
 Based on physical state dosages form are-
 Liquid - Aromatic water, Mixtures, Syrups, Elixir, Linctuses, Liniment, Lotion, Douches, Eye

C
drops, Ear drops, Nasal drops, Gargles, Mouthwash, Throat paint.
 Semisolid - Cream, Jellies, Ointment, Pastes
D
 Solid - Tablet, Capsule, Suppositories, Cachets, Powder, Insufflations
G
 Gaseous - Aerosols
Based on physical state dosages form are-
F

DIFFERENT DOSAGE FORM

PD

SOLID DOSAGE FORM LIQUID DOSAGE FORM SEMI-SOLID DOSAGE FORM

E

SOLID DOSAGE FORM

PL

Unit Dosage Form Bulk Dosage Form

M

Tablets Powder Capsule Cachets Pills External Use

SA

Internal Use Ear Powder

Soft Hard Dry Wet
Gelatin Gelatin Seal Seal Snuff Powder
Fine Powder
Granules Ophthalmic
Lozenges Oral Sublingual Buccal Powder

Effervescent Dusting Powder

Chewable Hypodermic Effervescent Non- Effervescent Dental Powder


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
15
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICS : MONOPHASIC LIQUID DOSAGE FORM Module-9

SCAN ME
CHAPTER
Monophasic Liquid
03 Dosage Form To Join FREE
Online Test

E
INTRODUCTION

IM
 Monophasic liquid dosage form refers to liquid preparation in which there is only one phase. It is
represented by true solution.

PR
 The component of solution present in large amount is known as ‘solvent’ and the component
present in small amount is known as ‘solute’.

C
SOLUTION

D
 Solutions are clear liquid preparations containing one or more active ingredients dissolved in a
G
suitable vehicle.
 Solutions are dosage forms prepared by dissolving the active ingredients in an aqueous or
non-aqueous solvent.
F

 The rate of drug bioavailability is most rapid when the drug is formulated as a solution
PD

[GATE-2001]

CLASSIFICATION OF SOLUTION
E

 According to the Route of administration

PL
M
SA

 Monophasic liquid dosage form for internal use

Mixture • It is a liquid preparation meant for oral administration in which medicament

or medicaments are dissolved or suspended in a suitable vehicle.
Aromatic • Solution of aromatic or volatile material in water. They will deteriorate with
water time.
• e.g - Rose water, Peppermint water, Camphor water, Chloroform water
and Cinnamon water.


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
17
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : BIPHASIC LIQUID DOSAGE FORM Module-9

Topical • Suspension are applied topically, “shake lotion” is the oldest

suspension example for these suspension.
• It should contain high amount of dispersed phase often in excess
20% (w/v).
• e.g. - Calamine lotion
Parenteral • Solid content of parenteral suspension is usually between 0.5 and
suspension 0.5% (w/v), except for insoluble form of penicillin, where

E
concentration of antibiotic may exceed 30% (w/v).
• e.g. - Procaine penicillin G, Insulin Zinc Suspension

IM
Ophthalmic • These are prepared only in those cases, when the drug is insoluble
suspensions in the desired solvent or unstable in liquid form.

PR
• e.g. - Prednisolone acetate ophthalmic suspension, USP

BASED ON ELECTROKINETIC NATURE OF SOLID PARTICLES

C
FLOCCULATED SUSPENSION
[GPAT – 2015]
D DEFLOCCULATED SUSPENSION
G
Particles forms loose aggregates and Particles exist as separate entities.
form a network like structure called
floccules.
F

Rate of sedimentation is high. Rate of sedimentation is slow.

PD

Sediment is rapidly formed. Sediment is slowly formed.

Supernatant liquid is clear Supernatant liquid is cloudy
Sediment are loosely packed and hard Sediment are closely packed and hard
cake is not formed. cake is formed.
E

Sediment is easy to redisperse Sediment is difficult to redisperse

Unpleasant in appearance Pleasant in appearance.
PL

Exhibits plastics or pseudoplastics flow In low concentration it exhibits Newtonian

flow, where as in high concentration it
exhibits dilatant behaviour
M

Bioavailability is comparatively less due Bioavailability is higher due to large

to small specific surface area. specific surface area.
SA


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
27
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : BIPHASIC LIQUID DOSAGE FORM Module-9

FACTORS AFFECTING TYPES OF EMULSIONS

FACTORS DESCRIPTION
Particle size When size of dispersed globule is less – decrease
creaming
Critical value for phase- 74% for o/w emulsions and 40% for w/o ones
volume ratio

E
Phase volume ratio Type of flow
5% Newtonian

IM
50% Pseudoplastic
74% Plastic flow

PR
Type of HLB value of surfactant used decides the type of
surfactants/adsorbed emulsion.
chemical
Viscosity of both phases Diffusion of surfactant into surface is reduced under
high viscosity. The process of coalescence decreases

C
under high viscosity.

TESTS FOR IDENTIFICATION OF EMULSION TYPE D

G
Dilution test  Dilute the emulsion with water or oil
F

 O/W Emulsion: Diluted with water → emulsion is stable/

Diluted with oil → cracking occurs
PD
E

 W/O Emulsion: Diluted with oil → emulsion is stable/

Diluted with water → cracking occurs
PL
M

Dye solubility  An oil-soluble or water-soluble dye is added to the emulsion and

SA

test observed under a microscope.

 Water soluble dye - Amaranth and Methylene blue → O/W
emulsion
 Oil soluble dye – Sudan III and Scarlet red → W/O emulsion


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
35
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 GPAT DISCUSSION CENTER
Module-9 Makes Study Easy

Conductivity  Test is based on the ability of water to conduct electricity.

test  If water is the continuous phase, then the emulsion conducts
electricity
 If the oil is the continuous phase, the emulsion fails to conduct.

E
IM
Creaming test  Position of oil indicates types of creaming
 Water in oil emulsion – cream downward

PR
 Oil in water emulsion – cream upward

C
CoCl2/Filter
paper D
Filter paper impregnated with CoCl2 and dried changes to pink
when o/w emulsion is added
G
[GATE – 2007]
F

Fluorescence Since oils fluoresce under UV light, o/w emulsions exhibit dot
PD

test pattern, w/o emulsions fluoresce throughout

FORMULATION OF EMULSIONS
E

EMULSION
PL

Oil phase Aqueous Emulgent Other Co -Surfactant

phase additives
M

Preservatives Antioxidants Hydrophilic

colloids
SA

 Oil phase
 Oils, fats and waxes require emulsifying agents of required HLB (RHLB), which have been
calculated depending on the type of emulsion required.


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
36
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 GPAT DISCUSSION CENTER
Module-9 Makes Study Easy

 Petrolatum is a complex mixture of semisolid

Petrolatum
(Soft paraffin)
hydrocarbons, containing aliphatic, cyclic, saturated,
unsaturated, branched and unbranched substances in
varying properties.
 Yellow soft paraffin
 White soft paraffin
Hard paraffin  It is obtained from petroleum
 Melting points ranging from 35 to 75°C.

E
 Ozokerite is a mined wax with a melting point range of
Oleaginous

IM
65 to 75°C and consists of a mixture of saturated
bases
hydrocarbons ranging in carbon content from C 35 to C55
 Another wax that is often used is ceresin, which is a

PR
mixture of ozokerite and paraffin wax.
Liquid paraffin  It is obtained from petroleum
 The lower viscosity oils are preferred for semisolids,
since they are less tacky and greasy.

C
 Soft petrolatum base is a mixture of 90% white
petrolatum with 10% mineral oil.
Fixed oils
D
Almond oil, Castor oil and Cotton seed oil
 Anhydrous lanolin (Wool fat), beeswax, hydrophilic petrolatum and
G
organosilicones are examples of anhydrous vehicles that absorb water to
form water in oil emulsions
 Commercially available absorption bases include AQUAPHOR and
F

POLYSORB
Absorption
PD

Anhydrous or Non  Wool fat :- derived from sheep’s wool.

bases
– emulsified bases  Lanolin alcohols :- it is the crude mixture of sterols
[GPAT-2021,
and triterpene alcohol and also contains at least 30%
2023 ]
cholesterol and 10-13% isocholesterol.
E

 Beeswax esters of aliphatic alcohols (C24 – C36) and

linear aliphatic fatty acids.
PL

Hydrous or w/o They have more capacity to absorb water, as compared to

emulsifying bases anhydrous bases, e.g lanolin (Hydrous wool fat ); it is the
product of wool fat formed by addition of 25-30% water.
M

Anionic  These emulsifiers are more acid stable and permit

emulsifying wax adjustment of the pH level of emulsions to the
SA

desirable range of 4.5 to 6.5.

Water  e.g. – Sodium lauryl sulphate and soaps such as
removable of Triethanolamine stearate.
Emulsifying Cationic This is also referred to as Cetrimide emulsifying wax
base emulsifying wax
Non-ionic  It is also referred to as Cetomacrogol emulsifying wax
emulsifying wax  They show excellent pH and electrolyte compatibility
in emulsions because they do not ionize in solution.


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
48
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : TABLET Module-9

SCAN ME
CHAPTER

07 Tablet
To Join FREE
Online Test

E
Tablet is a unit dosage form containing drug substance with or without suitable

IM
diluents prepared by either compression or molding methods.

TYPES AND CLASSES OF TABLETS

PR
TYPES OF TABLETS

C
Oral Tablet Tablet used Tablet administered Tablet used to
f or Ingestion in oral cavity by other route prepare solution

Compressed Tablets Buccal tablet D

G
Implantation or Effervescent Tablet
Multiple compressed Sublingual tablet depot tablet Dispensing Tablet
tablet Troches and Vaginal tablet Hypodermic Tablet
Enteric coated tablet
F

Lozenges Tablet Triturate

Chewable tablet Dental cone
PD

Film coated tablet

Sugar coated tablet
Controlled release
tablet
E

 Oral tablets for ingestion

1. Compressed tablets (CT) or standard compressed tablets
PL

 Formed by compression and contain no special coating.

 To provide rapid disintegration and drug release.
M

e.g. - Aspirin (Disprin), Paracetamol tablets (Crocin).

2. Multiple compressed tablets (MCT)
SA

 Prepared by more than one compression cycle.

 This type is prepared to:
 To separate physically or chemically incompatible ingredients
 To produce repeat action or prolonged action products
 Two classes:
(i) Layered Tablets: Two layered or three-layered tablet.
(ii) Compression Coated Tablets: Tablet within a tablet or tablet within a tablet within a tablet.


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
59
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : TABLET Module-9

DILUENTS DETAILS
Lactose Most widely used diluent
[GATE–1998] Good compressibility
Two grades:
(i) 60 to 80 mesh – coarse grade
(ii) 80 to 100 mesh – regular grade
 Types
i. α -Lactose(Hydrous) - Undergo the Maillard reaction

E
ii. β- Lactose (Anhydrous) - Does not undergo the Maillard reaction
→ lead to browning and discoloration with certain drugs.

IM
iii.Spray dried Lactose
• Prone to darkening in the presence of excess moisture, amines

PR
and other compounds, owing to the presence of a furaldehyde.
• Also has good flow characteristics
• A neutral or acid lubricant should be used.
 Maillard Reaction:
• Not used with isoniazid because of Millard reaction [GATE–1991,

C
GPAT-2010,2021]

D
G
F
PD

Dextrose
• Trade Name- Cerelose
• Two forms - Hydrous and Anhydrous form.
• Used in chewable tablets due to negative heat of solution, cooling
Mannitol effect.
E

• Non hygroscopic and used in vitamin formulation.

• Optical isomer of Mannitol
PL

Sorbitol • Sorbitol is hygroscopic at humidities above 65%. [GPAT-2014]

• Low caloric and non-carcinogenic.
• Also serves as binder or as a bulking agent and sweetener in
M

chewable tablets [GATE – 1989]

• Used in direct compression, Hygroscopic
SA

• Sucrose is called an invert sugar

• Some sucrose-based diluents are
Sucrose or sugar Sugartab - 90-93% Sucrose + 7-10% Invert sugar
DiPac - 97% sucrose + 3% modified dextrins
Nu Tab - 95% Sucrose + 4% Invert Sugar + small amount of corn starch +
magnesium stearate

• Sucralose is suitable for diabetic patient [GPAT -2014]

• Example of invert sugar - Sucralose

Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
63
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : TABLET Module-9

 Range of size: 0.2 mm to 4 mm. (0.2 mm to 0.5 mm)

 Formation of granules
Simple powder may not have desired flow property
After granulation

Powder material are improved by forming sphere shape

aggregate called granules

E
Having good flow property and prevent segregation

IM
 Shape factor of granule should be 6. Just like sphere for good flow.
 Measurement of Surface Area

PR
o Gas adsorption method
o Air permeability method
 Determination of Granule Density
o Mercury displacement method

C
o Pycnometer
As granule density increase – Bulk density increase

As particle become spherical – bulk density increase
D
G
 Strength- Determined by placing granules anvils (Tumbler test)
 Flow property measured by
1. Angle of repose
F

 Measuring resistance to particle movement is a quantity called the angle of repose of a

PD

powder.
 Flow property of powder is measured by - fixed cone method.
h 2h
θ = tan -1 or θ = tan -1
E

r D
Where,
PL

= Angle of repose

h = Height of the powder bed
r = Radius of the powder bed
M

D = Diameter of powder bed

 Other method
SA

(a) Fixed height (b) Fixed base cone (c) Tilting table (d) Rotating
cone method method method cylinder method


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
69
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 GPAT DISCUSSION CENTER
Module-9 Makes Study Easy

 Equipments of Wet granulation

Littleford Littleford Diosna Sigma blade

Gral mixer Nauta mixer
Lodige mixer MGT mixer mixer mixer

E
EQUIPMENTS DESCRIPTION
Littleford • High-shear powder blenders

IM
Lodige mixer • Capable of mixing and blending wet mass
Littleford MGT Capable of producing agglomerated granular particles → ready for

PR
mixer fluid bed or other drying methods
• High-speed powder mixer and processor
Diosna mixer • Contains bowl in vertical position
• Also work as vacuum drying, with a wide range of batch sizes
• Modification of planetary mixer.

C
Gral mixer
• A high shear granulator → cylinder/conical mixing bowl, three-
bladed impeller, a chopper, an auxiliary chopper→ a motor to drive
the blades →a discharge pot.
• Mechanism of mixing is shearing. D
G
Sigma blade
mixer
• Inter meshing of sigma shaped blades → high shear and kneading
actions.
[GATE-1992]
• Mass mixer
F

Nauta mixer Conical screw mixer → segregative, free-flowing powders and pastes.
PD

2. DRY GRANULATION METHOD

Weighing Mixing of Drug &

E

of Drug & Excipients (Diluent, Slugging(Tablet press

Excipients Disintegrant) or Roller Compactor)
PL

Screening of Sieving Slugs (Large size

Granules (#20-25) but loose tablets)
M
SA

Mixing of dried granules with

disintegrants lubricants and glidants Compression Tablets

Steps invovled in the Dry Granulation method of tablet

 Slug: Poorly formed tablets or compacted mass of powdered material.
Purpose: To impart cohesiveness to the ingredients ! to form tablets of desired properties.
Method: It is done either by
(i) High-capacity heavy duty tablet press
(ii) Chilsonator roller compactor [GATE-1989]

Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
72
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : TABLET Module-9

 Noyes - Whitney equation –

 Used to determine dissolution to tablet [GATE–1999, GPAT-2021]
 An increase of dissolution rate if the particle size is reduced by micronization because of an
increase in area [GPAT-2023]
 Noyes - Whitney equation calculated by-
dC DA
= =  Cs - C 
dt hV
Where,

E
D = Diffusion coefficient

IM
h = Thickness of the diffusion layer
A = Surface area of drug exposed to the dissolution media
V = Volume of media

PR
Cs = Concentration of a saturated solution
C = Concentration of drug in solution at time ‘t’
dC/dt = dissolution rate

C
 Types of USP dissolution apparatus & their application [GPAT-2016, 2017, 2023]

TRICK TO REMEMBER DISSOLUTION APPARATUS

D
G
F
PD
E
PL

USP ROTATING
DESCRIPTION DOSAGE FORM
APPRATUS SPEED
50-120 Conventional tablet, chewable
Type I Basket Apparatus
rpm tablet, controlled release
M

Orally disintegrating tablet,

Type II Paddle Apparatus 25-50 rpm chewable tablet, controlled release,
SA

suspension
Reciprocating
Type III 6-35 rpm Controlled release, chewable tablet
Cylinder
ER, poorly soluble API, Powder,
Type IV Flow Through Cell N/A
granules, microparticles, implants
Type V Paddle Over Disk 25-50 rpm Transdermal
Type VI Cylinder NA Transdermal
Reciprocating
Type VII 30 rpm Controlled Release Dosage Forms
Holder

Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
79
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 GPAT DISCUSSION CENTER
Module-9 Makes Study Easy

Blistering It is local • Too rapid Uses the mild drying

detachment of evaporation of the condition.
film from the solvent from the core
substrate and the effect of high
6. forming blister. temperature on the
film
[GATE-1990, • Overheating during

E
2006] spraying.

IM
Hazing and dull It is defect where • Too high processing • Decrease the
film (blooming or the coating temperature for plasticizer and
blushing) becomes dull formulation. Coating increase the

PR
immediately or tablet are exposed to molecular weight
after prolonged high humidity
7.
storage at higher condition and partial
temperature. solvation of film.

C
[GATE-2006]
• High concentration
and low molecular
D
weight of plasticizer.
It is the defect in Occurs of the internal •
G
Cracking Internal stresses in
which the film stress in the film the film can be
either cracks exceed the tensile minimized by
F

across the crown strength of the film adjusting the

PD

8. of the tablet and tensile strength of plasticizer type and

(cracking) or film increased by concentration
[GATE- 1990, splits around the using high molecular • Uses the low
2006] edge of the tablet polymer molecular polymers
E

(splitting)
Twinning Twinning is form Increase the Causing of • Balance the pan speed
PL

of Over wetting Over wetting and spray rate,

9.
whereby two or • Reduce the spray rate
more of tablet or increase the pan
M

core are stuck speed.

together
SA


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
88
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 GPAT DISCUSSION CENTER
Module-9 Makes Study Easy

MACHINE NAME USE SPEED(CAPSULE)

Hofliger and Karg Bulk Powder 300-2500/min.
Osaka Based on vibration principle 70000-165000/hrs
Perry Bulk powder 60000/ hours
Eli Lilly/ Parke-Davis For palletized or granular material 1200/min
Zanasi Powder, pellet, granules & tablet 30000-150000/hrs
Farmatic Bulk powder 16000/hrs
Macofar Bulk powder 3500-5000 /hrs

E
mG2 Continuous motion filling of powder 150-1000/min

IM
OTHER EQUIPMENTS USED IN CAPSULE FORMATION

PR
C
EQUIPMENT
Rotofill
USE
For filling of pellets. [GATE–1995] D
G
Rotosort New filled capsule sorting machine. [GATE-1990, 1994, 1997]
Vericap – 1200 Sorting of capsule on the basis of weight.
Quali-seal Filling of liquids.
F

Erweka KEA Dusting and polishing machine.

Seidenader PM 60 Cleaning and polishing of capsule.
PD

Rotoweigh Automatic capsule weighing machine

Measures weight by reflected energy of low of X- ray beam.
Reflected energy weight of filled capsule.
E

DEFECTS OF HARD GELATIN CAPSULES

PL

DEFECT APPROX. WT. IN MG APPEARANCE

Colour
Relative bad stability of selected dyes and pigments
M

deviation

Short body / Insufficient entry of the body/cap into the collet

SA

Cap prior to cutting operation

Long body / Caused by a missing knife/broken knife during
Cap cutting operation
Small fragments of shell walls generated during the
Dots/ Specks
trimming process getting into the dipping area.
Loose cap fits over the body of another capsule after
Double cap one of the caps is loose due to insufficient pre-lock
position in joining block

Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
96
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : PARENTERAL PREPARATION Module-9

RU B B ER
 Teflon lining of rubber closure provide effective barrier against sorption and leaching.
 Additives in Rubber
ADDITIVES PURPOSE EXAMPLES
Natural rubber, Butyl rubber,
Elastomer Basic component of rubber
Neoprene, Polypropen
Cross Linking of elastomer in

E
Vulcanizing Sulfur peroxide
3D network
Guanithidine and sulfide

IM
Accelerator Increase rate of vulcanisation
2 -mercaptobenzothiazole
Activator Increase rate of cross linking Zinc oxide, Stearic acid

PR
Filler Increases the bulk Carbon black, Clay
Prevent oxidative degradation
Antioxidant BHA, BHT
of rubber
Pigments To provide the colour Zinc Chromate, Inorganic oxides

C
Prevent oxidative degradation
Plasticizers Dibutyl phthalate, Stearic acid
of rubber

QUALITY CONTROL TESTING D

G
F

QUALITY CONTROL TESTING

PD

Raw material In-Process Finished

& components testing quality testing Packaging & Labelling Product
control testing

Enviornmental & Testing of Glass,

E

microbial control Plastic and Rubber

Leaker Clarity Pyrogen Sterlity
PL

test test test test

i. Methylene
M

blue test LAL test

ii. Spark test Rabbit test
SA

iii.Hammer test

QUALITY CONTROL TESTING OF PARENTERAL PRODUCTS (FINISHED PRODUCT TESTING)

1. LEAKER TEST (PACKAGING INTEGRITY TEST)

i. Methylene Blue Test (For ampoules)
 1% Methylene blue dye and vacuum used.
 Test can be carried during autoclaving.


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
123
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : OPHTHALMIC PREPARATION Module-9

SCAN ME
CHAPTER

12 Ophthalmic Preparation
To Join FREE
Online Test

E
INTRODUCTION

IM
 Ophthalmic preparations are sterile, liquid, semisolid or solid preparations, designed to be instilled
on to the external surface of the eye, administered inside or adjacent to the eye.

PR
TYPES OF OPHTHALMIC PREPARATIONS

Eye drops Eye drops are sterile aqueous or oily solutions or suspensions of
drugs that are instilled into the eye with a dropper.

C
Eye lotions
D
The eye lotions are supplied in concentrated form and are
required to be diluted with warm water immediately before
G
use.

Eye ointments  These are prepared under aseptic conditions and packed in
F

sterile collapsible tubes which keep the preparation sterile

PD

until whole of it is consumed.

 Ocular tension measured by Tonometer
Eye suspensions They are prepared only in those cases, when the drug is
insoluble in the desired vehicle or unstable in liquid form.
E

(>10 microns )
PL

Ophthalmic insert  Containing solids or semisolids

 Whose size and shapes are especially designed to increase
ocular residence, possibility of releasing drug at a slow
M

constant rate. e.g. - Ocusert

SA

REQUIREMENT FOR OPHTHALMIC PREPARATIONS

Clarity By filtration
Stability Solution pH must be selected for optimum drug stability, tear
fluid pH – 7.4
Buffer system Within stable range
Viscosity Usually 15 to 25 cps is used
Sterility Autoclaving
Particle size Less than 10µm to avoid irritation

Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
127
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 GPAT DISCUSSION CENTER
Module-9 Makes Study Easy

Skin sprays  Generally used for local effects.

e.g.- Coolants, anaesthetics, analgesics etc.

Dental sprays  Generally used for local analgesic or anaesthetic action.

COMPONENTS OF AEROSOL PACKAGE

E
1. PRODUCT CONCENTRATE

IM
2. PROPELLANT
3. VALVE AND ACTUATOR

PR
4. CONTAINER

C
D
G
F

1. PRODUCT CONCENTRATE
PD

 Contain ingredients or mixture of active ingredients with other additives like solvents, antioxidants
and surfactants.
2. PROPELLANT
 Function of propellant is to produce pressure to expel the medicaments.
E

 A propellant has pressure greater than atmospheric pressure at 40 oC.

PL

 Aerosols are gases at room temperature and pressure, but they are readily liquefied by
decreasing temperature or increasing pressure.
 Propellants (like chlorofluorocarbons) used in preparation of aerosols causes
M

environmental harm such as ozone layer depletion.

SA

TYPES OF PROPELLANTS

Liquid gases Dimethyl ether Compressed gases

Chlorof luoro carbons Hydrocarbon Non-soluble

Soluble compressed
e.g.- (CFC)134a e.g.-Propane compressed
[GATE-1997,1999] gases e.g.- CO2
gases e.g.- N2


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
132
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : PHARMACEUTICAL PACKAGING Module-9

SCAN ME
CHAPTER
Pharmaceutical
14 Packaging
To Join FREE
Online Test

E
DRUG PACKAGING

IM
Drug packaging involves the packages and packaging processes for pharmaceutical drugs, from
production through distribution to the end consumer.

PR
C
D
G
F

 Packaging systems classified according to the dosage capacity of the container:

PD

Single-unit container: Contains an only a unit quantity of medication which can be

used one time.
Single-dose container: Designed for Unit-dose container: Single-unit
E

parenteral administration only container intended for solid oral dosage

forms.
PL

Multiple-unit container: Permits multiple withdrawals of oral dosage forms,

designed for parenteral administration only.
 Different types of containers that may be specified based on the stability and usage:
M

 Tamper-Resistant Packaging: Single-use packaging product that is designed to provide evidence

when it has been opened or interfered with.
SA

 Types of Tamper-Resistant Packaging

Film wrappers End-folded wrapper: Cellophane and polypropylene.
Fin seal wrapper: Polyethylene or Surlyn.
Shrink wrapper: Polypropylene, polyethylene, and PVC.
Blister package Used for the thermoformable blister are PVC,
PVC/polyethylene combinations, polystyrene, and
polypropylene.

Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
139
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 PHARMACEUTICAL TECHNOLOGY : NOVEL DRUG DELIVERY SYSTEMS Module-9

SCAN ME
CHAPTER

15
Novel Drug Delivery
Systems
To Join FREE
Online Test

E
DEFINITION

IM
 A Novel Drug Delivery System (NDDS) can be defined as a new
approach that combines innovative development, formulations,

PR
new technologies, novel methodologies for delivering
pharmaceutical compounds in the body as needed to safely achieve
its desired pharmacological effects.

C
VARIOUS DRUG DELIVERY CARRIERS

LIPOSOMES [GATE-1998, 2003, 2009] D

G
 A liposome is a spherical-shaped vesicle that is composed
of one or more phospholipid bilayers, which closely
F

resembles the structure of cell membranes.

PD

 The ability of liposomes to encapsulate hydrophilic or

lipophilic drugs have allowed these vesicles to become
useful drug delivery systems.
 Advantages of liposome:
E

 Increased efficacy and therapeutic index of drug.

PL

 Increased stability via encapsulation.

 Non-toxic, flexible, biocompatible, completely biodegradable, and non-immunogenic for systemic
and non-systemic administrations.
M

 Reduce the toxicity of the encapsulated agent.

 Help reduce the exposure of sensitive tissues to toxic drugs.
SA

 Liposome classification based on pharmaceutical and therapeutic aspects:

Based on structural parameters
MLV: Multilamellar large vesicles, >0.5 μm MUV: Medium-sized unilamellar vesicles
OLV: Oligolamellar vesicles, 0.1-1 μm LUV: Large unilamellar vesicles, > 100 nm
UV: Unilamellar vesicles, (all size range) GUV: Giant unilamellar vesicles, > 1 μm
SUV: Small unilamellar vesicles, 20-100 nm MV: Multi vesicular vesicles, >1 μm


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
147
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)
 GPAT DISCUSSION CENTER
Module-9 Makes Study Easy

Delivery orifice Release of drug through

delivery orifice
Semi-permeable membrane

Osmotic core with drug

 Osmotic systems release: Drug at a predetermined, typically zero-order rate, based on the
principle of osmosis.

E
 Swelling controlled release: Systems are initially dry and when placed in the body absorbs water
or other body fluids and swells. Swelling increases the aqueous solvent content within the

IM
formulation as well as the polymer mesh size, enabling the drug to diffuse through the swollen
network into the external environment.

PR
5. Hydrogels: Made from water-soluble/insoluble polymers with
cross-linked networking. The drug is dispersed in a glassy polymer
which upon contact with water, swells and releases the drug.
6. Ion exchange resin: Reversible process in which ions of like sign are

C
exchanged between liquid and solid when in contact with a highly
insoluble body. The drug is released from resinate by exchanging with ions in the gastrointestinal

D
fluid, followed by drug-diffusion. e.g. - ER Diclofenac Na, Diltiazem HCl etc.
G
7. Chemically Controlled Drug Delivery Systems: Change their chemical structure when exposed to
the biological milieu. These are made of biodegradable polymers which degrade in the body as a
result of natural biological processes, eliminating the need to remove the delivery system after
F

exhausting an active agent from the system. e.g. - Nifedipine Tablets, Zolpidem Tartrate Tablet etc.
PD

NITRO-DUR: A TRANSDERMAL DRUG DELIVERY SYSTEM

 Designed for application onto intact skin to provide a continuous transdermal infusion of
nitroglycerin, at a daily dose of 0.5 mg/cm2, for the prevention of angina pectoris.
E

Absorbent pad Impermeable backing

Occlusive base plate
PL
M

Adhesive rim Drug reservoir

 Franz diffusion cell system
SA

 Consists of a receiver chamber and a donor

chamber. [GPAT-2014]
 The dissolution medium is contained in receiver
chamber whereas drug product is introduced into
donor chamber.
 The skin or membrane is placed between the two
chambers.


Gpat Discussion Center Pvt. Ltd. |  www.gdconlinetest.in, www.gdc4gpat.com |  [email protected] | 8602227444, 9770765680
154
Download “GDC CLASSES” App (Type GDC CLASSES in Playstore to Download the app)