GPAT conetent of Capsule, Microencapsulations and Aerosol

1. Dr. Sanjeev Kumar Gothwal
M.Pharm. PhD. (Pharmaceutics)
Associate Professor
Guru Gobind Singh College of Pharmacy
Yamunanagar

2. Capsules are the solid unit dosage form of
medicament in which the drug(s) is enclosed
in a practically tasteless, hard or soft
container made up of gelatin.
Hard capsules for filling the solid substances,
while soft capsules for the liquid or semisolid
substances.

3.  Capsules are tasteless, odorless & easily
administered.
They are economical.
They are easy to handle not carry.
They can be filled quickelyand conviently
therfore the physician can change the dose
and combination of drugs.
They can mask the unpleasant odour and
taste of the drugs.

4. RAW MATERIALS EXAMPLES FUNCTIONS
Gelatin Pharmagel A: Acid
Hydrolysis, pH:4.8-5.2
Pharmagel B: Basic
Hydrolysis, pH:6.5-9.5
The viscosity of the
gelatin solution is used to
control the thicknee of the
films.
Plasticizers Glycerin, Sorbitol,
Propylene Glycol, Sucrose,
Acacia.
Maintaining the shape of
the capsules
Colorants
Flavours (<2%)
Sweeting Agent (<5%)
Titanium dioxide, oxides of
Iron(Black, Red, Yellow)
Ethylvanillin or essential
oils
Sugar
Opacifying agent, For the
bicoloured soft gelatin
capsules Aluminium lakes
are used to prevent the
colour transfer between
rhe two layers of the
capsules.
Preservatives (0.2%) Methyl parabene (4 parts),
propyl parabene (1parts)
To prevent the shell from
microbial contamination

5. INGRADIENTS EXAMPLES FUNCTIONS
Diluents Diluent has to be added
to bring the medicament
up to the desired bulk.
Protective absorbents To prevent the
absorption of moisture
by hygroscopic substance
Glidants Talc, Magnesium
Stearates
Anti-dusting Compounds

6.  Some Machines can fill 15,000 to 20,000 capsules per
hour.
 ROTOSORT is a new filled sorting machine sold by
Eli Lily and Company. It can handle up to 150,000
capsules per hour.
 The Eweka KEA dedusting and polishing machine for
hard gelatin capsules moves the capsule between soft
tassels against a prforated plastic steeve, under
vacuum.

7. Difficulties Descriptions Solutions
Deliquscent or
Hygroscopic Powders
Hygroscopic drugs
absorbs the water from the
gelatin shell, which leads
to brittleness and cracking
of capsule
Using absorbent like
Magnesium Carbonate,
Heavy Magnesiumoxide,
Light Magnesium oxide
Eutectic Mixtures
Whem substances tend to
liquefy or form a pasty
mass on mixing togather,
the formed mixture has a
lowermelting point than
room temperature.
The absorbent used are
Magnesium oxide and
Kaolin is added.
Not preferable of Mgo
both light and heavy due
to forms a very hard
cement.
Addition of Inert
Powder
It is difficult to fill the
small quantity of drug in
capsules
Inert substance or diluents
is added so as toincrease
the bulk of the powder.

8. Difficulties Descriptions Solutions
Filling of Granular
Powders
Some powder which lack
adhesiveness and most
granular powers are
difficult to fill in the
capsules by punch method
because they are not
compressible.
The non-adhesive
powders should be
monitered with alcohol
and the granular powders
should be reduced to
powder before filling into
cspsules.
Use of two Capsules
To separate the
incompatible ingredients
of the formulation
By placing one of the
ingredients in smaller
capsule and then placing
this smaller capsule into
large capsule.
Liquids Oils and liquids which not
dissolve gelatin may be
filled into hard gelatin
capsules
Used liquids with an
absorbent, viscous liquids
and semisolids are mixed
with an absorbent.

9.  Soft gelatin capsules are prepared by using sorbitol or
propylene glycol as plasticizer, gelatin and water
which makes it soft and elastic in nature.
 They usually contain a preservatives to prevent the
growth of bacteria and fungi.
 Shapes: Spherical, Ovoid, cylindrical and tubes.
 Spherical capsules are also known as pearls.
 Content of soft capsules may very 0.1-30ml.
 Soft capsules are formed and filled in one continuous
operation on semi-automatic or automatic machine

10.  Vitamins preparations e.g. Halibut liver oil, Vitamin A
and D and multivitamins are conveniently dispensed
in soft capsules.
 Used for containing eye, ear, nose and throat
preparations.
 Ophthalmic ointments are frequently packed in unit
dose capsules
 Now days soft capsules are also used for packing
cosmetics, flavours and food concentrates.

11. Ingredients Examples Functions
Opacifiers Titanium dioxide (0-
0.5%)
Opacifying agent
Colours Synthetic, vegetable,
insoluble inorganic and
organic pigments and
lackes.
Colors can be
incorporated into soft
gelatin shells
Water Demineralized water is
used
0.7 and 1.3 parts of water
to each part of dry gelatin,
with a 1:1 ratio being
typical.

12. Ingredients Examples Functions
Gelatin Low aqueous gelatin
solution, a thin, low
strength shell is produced.
To produce shell with
greater flxibilitiesthan
hardgelatin capsules
Plasticizers Glycerol, Propylene
Glycol and Sorbitol is
used in combination with
Glycerol
Greater the plasticizer
contents the greater the
flexibility of the shell.
Preservatives Potassium Sorbitate and
Mehyl, ethyl and Propyl
hydroxy benzoate
The free content of water
in shell is too low to
support the growth of
microorganism.
Enteric Treatment Cellulose Acetate
phthalate (4%)
Enteric properties can be
imparted tosoft gelatin
shells.

13. Ingredients Examples Functions
Gelatin Low aqueous gelatin
solution, a thin, low
strength shell is produced.
To produce shell with
greater flxibilitiesthan
hardgelatin capsules
Plasticizers Glycerol, Propylene
Glycol and Sorbitol is
used in combination with
Glycerol
Greater the plasticizer
contents the greater the
flexibility of the shell.
Preservatives Potassium Sorbitate and
Mehyl, ethyl and Propyl
hydroxy benzoate
The free content of water
in shell is too low to
support the growth of
microorganism.
Enteric Treatment Cellulose Acetate
phthalate (4%)
Enteric properties can be
imparted tosoft gelatin
shells.

14. Microencapsulation is a process of applying
relatively thin coating of small particles of
solids or droplets of liquids and dispersion of
size upto 5000 microns.

15. For masking the unplesant taste.
Stabilization to Oxidation.
Reduction of Volatility.
Conversion of liquid to solid.
Reduce gastric irritation
To formulate sustatined release formulations

16. Sr.
No.
Process of
Microencapsulation
Applicable core
material
Approximate
particle size
(µm)
1. Air Suspension Solids 35-5000
2. Coacervation- Phase
Separation
Solids & Liquids 2-5000
3. Multiorifice centrifugal Solids & Liquids 1-5000
4. Pan coating Solids 600-5000
5. Solvent Evaporation Solids & Liquids 5-5000
6. Spray drying & Congealing Solids & Liquids 600

17. Sr.
No.
Water Soluble Materials Sr.
No.
Water Insoluble Materials
1. Gelatin, Gum Arabic 1. Ethyl Cellulose
2. Starch, Arbinogalactan 2. Polyethylene
3. Poly Vinyl Pyrrolidone 3. Polymethacrylate
4. Hydroxethyl Cellulose 4. Polyamide Cellulose Nitrate
( Nylon)
5. Polyvinyl Alcohol 5. Pply (ethylne-vinyl-acetate)
6. Polyacrylic Acid 6. Poly (lactic-co-glycolide)

18. Sr.
No.
Waxes and Lipids Sr.
No.
Enteric Coating Materials
1. Paraffin wax 1. Shellac
2. Carnauba wax 2. Cellulose Acetate Phthalate
3. Spermaceti 3. Zein
4. Beeswax
5. Stearic Acid,
6. Stearyl Alcohol
7. Glyceryl Stearate

19. THE PROCESS CONSIST OF 3 STEPS
1. Formation of three immiscible chemical
phase:- a. liquid manufacturing vehicle
b. core material phase
c. coating material phase
2. Deposition of coating an core material
3. Rigidization of coating

20. 1. Coating material+volatile solvent which is
immiscible with the (LMVP)
2. Core material dispersed in coating polymer
solution with agitation
3. Corecoating materila mixture is dispersed in
LMVP to obtain desired size miroencapsules

21.  Dispersing the core material in a liquified
coating substance and spraying the core-coating
mixture into some environmental condition.
 Coating solidification is accomplished by rapid
evaporation in which coating material is
dissolved

22.  Dispersing the core material in a liquified
coating substance.
Coating solidification is effected by thermally
congealing a molten coating (spraying hot
mixture into cool air stream).

23.  The coating is applied as solution,or asan
atomized spray to the desired solid core material
in a coating pan.
To remove the coating solvent warm air is passed
over coated materials.
Most widely used for controlled relesase beads.

24.  This involves the formation of protective
microcapsule coating in-situ.
A interface is existing between the core material
and continuous phase in which the core material
is dispersed.
Continuous phase is usually a liquid or gas.
Polymerization reaction occur at following
interfaces
Liquid-Liquid
Liquid-Gas
Solid-Liquid
Solid-Gas

25. Mechanical process for producing microcapsule
that utilizes centrifugal forces to hurl a core
material particle through an enveloping
microencapsulation membrane.

26.  Pressurized dosage forms.
Contaning one or more active ingredients.
Actuation emit a fine dispersion of liquid and
or solid materials in gaseous medium.
Use of gaseous propellants which forces the
contents of the package out through opening of
the valve.

27. Components Examples Functions
Chlorofluoro
Hydrocrbons
(CFC)
Propellant
Trichlormonofluoromethane(011),
Dichlorodifluoromethane(012),
Dichlorotetrafluoromethane (114)
To produce pressure to
expell the medicament.
*Responsible for the
depletion of ozone layer
of atomsphere
Hydrocarbon
Propellant
n-butane, isobutane and pantane Ability to dissolve
medicament, stable,lack
odour, low cost,
immiscible with water
Compressed
Gas Propellant
Nitrous Oxide , Carbon dioxide,
Nitrogen
Tomaintain the pressure
of the propellant after
actuation

28.  Liquified gas system.
Two phase system or solution system
Three phase system: aqueous solution of active ingredient, liquid
propellant, vaporised propellant.
 Continuous spray valve has following components:
Ferrule or mounting cap to attach valve to container.
Valve housing having opening between 0.033-0.20 cm at a point
of attachment to dip tube.
Gasket to provide a seal between valve and container.
Spring helps to return the valve to the closed position after
actuation.
Dip tube made upto of polyethylene or polypropylene having
diameter between 3-3.2 mm. Its bring formulation from
container upto valve.
Stem is pressed the product is emitted from the container.
Actuator alloweasy opening and closing of the valve. To produce
spray aerosol mechanical break up actuatorare used.
Semisolids are delivered usingactuator with large orifice.

29. Sr.
No.
Cold Filling Pressure Filling
1. Low temperature range -34ºC
to -40ºC
The product concentrate is
added to container at room
temperature
2. The product concentrate is
chilled and added to open
container
3. A valve is then crimped into
places.
A valve is then crimped into
places.
4. Container passed through a
heated test bath forleakage and
container strength
Propellant is added under
pressure through the valve
stem
5. Not Suitable for aqueous
products or adversely affected
by low temperatures.
Can be used for all types of
aerosols

30. Sr.
No.
Material Functions
1. Tin-plated steel It is light inexpensive and durable
2. Stainless Steel Resistant to corrosionand no coating is
required, expensive, with stand high
pressure
3. Aluminium More resistant to corrosion, made by
extrusion process
4. Glass Often coated with plastic, transparent,
virtually inert.
5. Plastic Not widely used for containing
polyethylenetetraphthalate PET

31. Sr.
No.
Evaluation Tests Functions
1. Particle Size
Determination
Particle Size Microscopy,Cascade
Impaction (0.2-20µm), Light Scattering
Experiment (0.1-20µm) monitored by
Photodetector
2. Physicochemical
Properties
Vapour Pressure by container puncturing
device.
Density of aerosol by hydrometer and
pycnometer
Moisture content by Karl Fischer method
3. Aerosol Performance
Test
•Measuring Content of container usually by
weighing before and after filling
•Check the leakage in container
•Rate of discharge through the valve
•Pattern of spray