PH-PHR 214 – MIDTERMS DIFFERENT TYPES OF OINTMENT BASES

Hydrocarbon bases  Emollient effect

SEMI-SOLID DOSAGE FORMS (oleaginous base)  Protect against escape of moisture
 Intended for topical application  Effective as occlusive dressing
 May be applied  Can remain on the skin for long periods without
 There is no API drying out
 Opthalic ointment  Non-polar
 Difficult to wash-off because it is immiscible with
TOPICAL DERMATOLOGICAL PRODUCT AND TRANSDERMAL PRODUCT water
Topical Dermatological Transdermal Product Examples: o Petrolatum USP – Purified mixture of
Product semi-solid hydrocarbons obtained from
 Only intention is for topical  Products that are placed on the skin petroleum (semi solid hydrocarbon)
absorption or for local (patches) o White Petrolatum – Decolorized version
effect  Meant for systemic absorption of Petrolatum USP
 Applied on the skin only  Example: o Yellow ointment (95%
o Nicotine patches (for smoking petrolatum+5%yellow wax)
cessation therapy) o Yellow wax – purified wax obtained from
 Contain dose of nicotine honeycomb of the bee
without smoking o White ointment, USP – plain petrolatum
 Tapping down nicotine and white wax
o Mineral oil – liquid hydrocarbon from
OINTMENT petrolatum
 Semi-solid preparations of one or more medicinal agents in any of the Absorption bases  May be used as emollients
various classes of bases and is intended for external uses  Not easily removed from the skin
 Medicated o Aquaphor – refined hydrophilic
 Non-medicated petrolatum, takes up 3 times of its weight
in water
Advantages Disadvantages o Lanolin, USP – Obtained from wool of
 Easy to apply  Greasy sheeps
 Multiple effect – more than one  May cause skin irritation
type of therapeutic agent Two types o Permit incorporation of aqueous solutions
 Soothing – property of o Water-in-oil emulsions that permit
ointment base incorporation of additional quantities of
 Healing – from API aqueous solutions
Water-removable  Oil-in-water emulsion resembling creams
QUALITIES OF AN IDEAL OINTMENT BASE bases  Water soluble because of its external phase
 Compatible with skin Water-soluble bases  Greaseless
 Soften greatly in addition of water
 Stable
 Smooth, permanent and pliable
SELECTION OF APPROPRIATE BASE
 Non-irritating, non-sensitizing
 Desired release rate
 Inert (should not destroy or should not have interactions with the drug)
 Desirability for enhancement of percutaneous absorptions
 Able to release incorporated medication
 Advisability of occlusion
 Short-term or long-term stability of the drug in ointment base
Occlusive  Physically traps moisture
 Influence of drug on consistency or other features of ointment base
Emollient  Fills the spaces in the skin causing a smooth
surface  Patient factor – dry or weeping (oozing) skin
Humectant  Attracts moisture towards the stratum corneum  Ability to be removed by water
 Hydrating skin surface  Characteristic of the surface to which it is applied

PREPARATION OF OINTMENTS
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Incorporation  Components are mixed until a uniform preparation
is attained
For solids
o Done on small-scale
o Mortar and pestle is being used
o Spatula
o To rub ingredients on an ointment slab or
non-absorbent paper
For liquids
 Ointment base capacity to accept the volume
required
o Small amounts for oleaginous bases
o Alcoholic solutions may be added
 Ointment or roller mills can be used to force
coarsely formed ointments to produce more uniform
and smooth ointments
Fusion  All or some components melted together and
cooled with constant stirring until congealed
 Large scale production
- Components not melted are added as the
ointment is being and stirred
Equipments used:  Porcelain dish or beaker (small-scale)
 Steam jacketed kettels (large-scale)
 Easy to control temperature
PRESERVATION OF OINTMENTS
 Determine and control microbial content
o Pseudomonas aeruginosa and staphylococcus aureus are the
common bacterium that can cause infections
 Employ sterile techniques
 Add antimicrobial preservatives: p-hydroxybenzoates, phenols, benzoic acid,
sorbic acid, quaternary ammonium salts (benzalkonium chloride), organic
mercury compounds formaldehyde
PACKAGING, STORAGE AND LABELING
 Large-mouth jars or metal or plastic tubes
 Well-closed container to protect against contamination
 Store in cool place to protect against separation in hear
 Light resistant containers
 Type of base used for certain required by USP in product labels
CREAMS AND GELS
Creams  Semi-solid preparations containing one more
medicinal agents dissolved or dispersed in a water-
in-oil emulsion or o/w emulsion or in another type of
water
 Easier to spread and easier to remove than
ointments
 Used as emollients or as medicated application to
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the skin
Gels  Semi solid systems consisting of dispersions of
small or large molecules in an aqueous liquid
vehicle
Gelling Agents  Synthehic macromolecules
 Cellulose (carboxymethylcellulose)
 Natural gums (acacia, tragacanth)
SUPPOSITORIES
 Solid dosage forms intended for insertion into body orifices
 Fusible dosage forms of various weights and shapes
 “supponere” to place under
TYPES OF SUPPOSITORIES
Vaginal  Synonym: Pessary
 Globular, conical or oviform in shape
 5g
Urethral  Synonym: Bougie
 Meant to be inserted into the urethra
 Slender, pencil-shaped
Rectal  Tapered at one or both ends
 Shaped like a bullet
o Adults = 2g
o Infancts = 1g
ADVANTAGES AND LIMITATIONS OF SUPPOSITORIES
ADVANTAGES LIMITATIONS/DISADVANTAGES
 Safe and painless administration  Unacceptability and poor
 For drugs which are degraded compliance
when orally administered  Leaking
 For large dose drugs  Problematic insertion
 Duration of action can be controlled
– it melts when it contact with body
temperature
 For uncooperative patients
 For nauseous or vomiting patients
Qualities of an Ideal Suppository Base
 Non-toxic and non-irritating
 Compatible with a variety of drugs
 Melts or dissolves in body fluids
 Stable on storage
 Does not interfere with the release of the drug
SUPPOSITORY BASES
Fatty or Oleaginous  Theobroma oil (cocoa butter)
Base  At obtained from roasted seed of Theobroma
Cocoa
  Melts between 30 and 36 degree Celsius aluminum, brass and plastic
Polymorphic Forms of Melting Points o Capacity: 6, 12 & 50g
Cocoa Butter
Form I – Beta’2 16-18 Steps in Molding: 1) Lubricate
Form II – Alpha 21-22 2) Calibrate (will dictate the weight of the
Form III – Mixed 25.5 suppository)
3) Melt the base
Form IV – Beta1 27-29
4) Incorporate required medicaments
Form V – Beta2 34-35
5) Pour melt into molds
Form VI – Beta’1 36 6) Allow melt
Form IV and VI – Usual na ginagamit kasi 7) Remove suppositories from the mold
mas stable Compression Molding  Forcing the suppository mixture into special
molds using suppository making machines
Cocoa Butter  Melts just below body temperature but maintains  For drugs that are thermobile and for drugs that
(Theobroma Oil) solidity at room temperature
insoluble in the base
 Exhibits polymorphism
Hand Rolling and  Traditional method
 When quickly chilled, turns into a form that has a
Shaping  Uses grated cocoa butter
melting point lower than normal
 Has tendency to leak
1) Triturate cocoa butter with the other ingredients
 A solid fat expressed from the roasted seeds of
2) Roll into a ball using cooled hands
Theobroma cacao.
3) Shape into a cylinder using a spatula
 A pale yellow solid, becoming white on keeping,
4) Cylinder is cut into appropriate lengths
with a slight odour of cocoa and a bland taste.
 It is sometimes deodorised.
PACKAGING, STORAGE AND LABELLING OF SUPPOSITORIES
 M.P. 31C to 34C (below body temperature).
 Well-closed, screw-capped glass container
 Slightly soluble in alcohol; soluble in benzene,
 Cocoa butter-based suppositories are wrapped individually into partitioned
chloroform, ether, light petroleum. and boiling
boxed to prevent contact and adhesion
dehydrated alcohol.
 Light-sensitive containers
Water-soluble and  Glycerinated gelatin, polyethylene glycols, glycol-
 Strip-packaging of individual suppositories separated by tear-along
Water-miscible Bases surfactant combinations
perforations
o Polybase
 Cool place but not frozen
 Does not need refrigeration
o Cocoa butter suppositories – below 30°C; preferably in
 Does not leak out of the body orifice
refrigerator
 Does not melt at room temperature or water
o Glycerinated gelatin suppositories – below 35°C
weather
o Polyethylene glycol suppositories – room temperatures
Glycerinated Gelatin  Dissolves not melt
 Slower to soften and mix with body fluids
PASTES, GELLIES, PLASTERS AND GLYCEROGELATIN
 Provides prolonged release
Pastes  Semi solid prep intended for application to the
 Hygroscopic effect can cause irritation due to
skin
dehydration of rectal mucosa
 Contain a larger percentage of solid material
 Better suited for urethral suppositories
than ointments
Miscellaneous Base  Mixtures of oleaginous and water-soluble or water
 Will not soften and flow after application
miscible materials
 Remain in place after application and effective
 Polyoxyl 40 stearate – mixture of monostearate
employed to absorb serous secretions
and distearate esters of mixed polyoxyethylene
Gellies  Gels which contain high proportion of liquid,
diols and free glycols
usually water
Plasters  Adhesive masses spread on a backing of paper,
METHODS OF PREPARING SUPPOSITORIES
fabric
Fusion/Melt Molding  Most common method
Glycerogelatins  Plastic masses containing gelatin (15%),
 Employs the use of the mold
glycerin (40%), water (35%) and an added
o Mold is made from stainless steel,
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 medicinal substance (10%) such as zinc oxide POWDERS
 Applied to the skin for the long term, melted  Dry mixtures of finely divided medicinal and non-medicinal agents intended
before application, cooled to slightly above body for internal or external uses science of small particles; the study of a number
temperature, applied to affected area with a fine of characteristics, including particle size, and size distribution, shape, angle
brush of repose, porosity true volume, bulk volume apparent density, and
bulkiness.
Example:  Zinc gelatin used in the treatment of varicose  Particles – any unit of matter having defined physical dimensions
ulcers
PARTICLE SIZE ANALYSIS
Compendial Requirements Purpose:
 Should meet acceptable microbial limits  To obtain quantitative data on the size, distribution, and shapes of drug and other
 Ophthalmic prep required to be sterile components to be used in pharmaceutical formulations
 Preparations susceptible to microbial growth may contain antimicrobial
preservatives like methylparaben, propylparaben, phenols, benzoic acid, FACTORS INFLUENCED BY PARTICLE SIZE
sorbic acid, and quaternary ammonium salts  Dissolution of particles intended to dissolve
 Preparations that contain water tend to support microbial growth  Suspendability of particles intended to remain undissolved but uniformly
dispersed in a liquid vehicle
Minimum Fill  Uniform distribution of a drug substance in a powder mixture or solid dosage
 Net weight or volume of the contents of filled containers to ensure proper form to ensure dose-to-dose content uniformity
contents as against label claim  Penetrability of particles intended to be inhaled for deposition deep in the
 Done for semi solid dosage forms respiratory tract
 Lack of grittiness of solid particles in dermal ointments, creams and
ADDITIONAL STANDARDS ophthalmic preparations
 Manufacturer’s test for viscosity and in-vitro drug release
o Diffusion cell studies METHODS OF DETERMINING PARTICLE SIZE
 Franzel diffusion – set-up; the drug is being diffused on  Sieving
the skin or membrane  Microscopy
 Sedimentation Rate
SOLID DOSAGE FORMS  Light Energy Diffraction or Light Scattering
 Powders  Laser Halography
 Granules  Cascade Impaction
 Pellets
 Capsules COMMINUTION
 Tablets  Mechanical process of reducing the size of particles or aggregates

ADVANTAGES AND LIMITATIONS OF SOLID DOSAGE FORMS REASONS FOR REDUCING PARTICLE SIZE
ADVANTAGES LIMITATIONS  To aid processing of solid particles by facilitating powder
 Increased stability  Inconvenient to carry  Mixing
 Convenience when dispensing  Problems in masking unpleasant  To improve pharmacological performance of the drug
drugs with a large dose tastes  To improve transportation efficiency by reducing bulk volume
 Faster dissolution rate  Not for drugs with a low dose
 Greater flexibility in compounding  Not for drugs inactivated in the MORTAL AND PESTLE
solids stomach  For small scale comminution
 Time-consuming to prepare
 Not for drugs that are hygroscopic TYPES OF MORTAR AND PESTLE
or deliquescent Wedgewood  For crystalline solids or hard lumps
 Modern prescription practice
 Relatively porous and stains easily
 Interior is roughened
 Aids in comminution
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  Requires meticulous cleaning Sifting  Method of passing powders through sifters
• Remove trapped particles that may contaminate resulting in a light fluffy product
subsequent preparation  Not for potent drugs
 Pestle may have rubber or wooden handles Tumbling  Method of mixing powders in a closed rotating
Porcelain  For soft aggregates or crystals container
 For blending powders of the approximately uniform sizes  Results in thorough but time-consuming mixing
 Less porous than Wedgewood
 Exterior is glazed Extemporaneous Techniques for Preparing Powders
 Pestle may have a rubber or wooden handle  For incorporating small amounts of potent drugs, use geometric dilution
Glass  For preparing solutions, suspensions, and ointments  Reduce particle size of all ingredients to the same range to prevent
 Reduction of soft aggregates of powders or for the stratification of large and small particles
incorporation of relatively large amounts of liquid  Sieve when necessary to achieve mixing or reduce agglomerates
 Not for hard solids  To reduce bulkiness of a powder, use heavy trituration
 Nonporous  Protect the powder from humidity, air oxidation and loss of
 Does not stain easily  Volatile ingredients
 Preferred when flavoring oils or highly colored substances
are used Size Classification of Powders
Very coarse No. 8
METHODS OF COMMINUTION Coarse No. 20
Trituration Process of grinding a drug in a mortar using a pestle to Moderately coarse No. 40
reduce particle size
Fine No. 60
Levigation Process of triturating a drug with a small amount of
Very Fine No. 80
solvent liquid (levigating agent) in which the powder is
insoluble
MEDICATED POWDERS
Pulverization by Process of reducing the size of a drug with the aid of an
Internal  Inhaled for local or systemic effects
intervention additional material that can be removed easily after the
 For constitution with a liquid solvent or vehicle for
pulverization has been completed
administration
o Orally
BLENDING POWDERS
o As injection
Spatulation  Method by which small amounts of powders may o As vaginal douche
be blended by the movement of a spatula through External  Dusted on affected area from a sifter-type
the powders on a sheet of paper or an ointment
container
tile
 Powder aerosol
 Suitable for powders that liquefy (eutectic mixture)
when in prolonged contact with another
EXAMPLES OF MEDICATED POWDERS
substance
Aerosol Powders  Administered by inhalation with the aid of dry-
Not suitable for:  Large amounts of powders
powder inhalers, which deliver micronized particles
 Powders containing potent substances
of medication in metered quantities
Trituration  Method used both to comminute and to mix
o For treatment of asthma and other
powders usually with the use of a mortar and
bronchial disorders that require distribution
pestle
of mediation deep in the lungs
 For potent substances in small amounts,
o Use micronized particles
geometric dilution technique is used
o Contain propellants and pharmaceutical
Geometric Dilution  Adding the drug to an equal amount of diluent and
diluents
Technique mixing them thoroughly by trituration
Bulk Powders  Powders that are used in bulk and measured by the
 A second portion of the diluent equal in volume to
spoonful to
the mixture is added and the trituration is
 Use as is or to make a solution
repeated process is continued by adding equal
volumes of the diluent and the mixture and
For non-potent  Oral powders
repeating until all of the diluent is incorporated
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substances:  Dentrifices o Organic solvents
 Douche powders  Wet granulation equipment
 Dusting powders  Shear granulator
 Insufflations  High speed mixer/granulator
 Triturations  Fluidized bed granulator
Divided Powders  Blended powders divided into dosing units and  Spray dryer
dispensed in  Spheronizer/pelletizer
 Small pieces of paper called chartula or chartulae
folded to WET GRANULATION PROCESS
 Enclose the medication Pre-mixing  Diluent
 API
Dispensed in the form  Folded papers  Disintegrant
of individual doses:  Unit of dose envelopes  Colourant
 Metal foil Wet mixing  Add granulating fluid
 Small heat-sealed plastic bags Wet granulation  Sieve #4
 Other containers may also be used Drying  Eliminate granulating fluid
Dry granulation  Sieve #20
PACKAGING AND STORING OF POWDERS Final mixing  Lubricant
 For Divided Powders, specially manufactured papers and boxes are  Flavorant
available
 Powder Papers 2. DRY GRANULATION
o Vegetable parchment  Particles are aggregated using high pressure
o White Bond  For drugs which do not compress well after wet granulation and are sensitive
o Glassine to moisture
o Waxed  Two processes:
o Prescription label may be pasted on top of the lid or inside the lid  Slugging
o Hinged-shoulder
 Roller compaction
 Prevents the switching of lids
DRY GRANULATION PROCESS
GRANULES
 These are aggregates of powders that adhere or bond to each other to form
Mixing  Diluent
larger unit particles  API
 Disintegrant
Granulation  Colourant
 Process by which powder particles are made to adhere to form larger Slugging/compacting
particles Dry granulation
Final mixing
Reasons for Granulation Filling
 To prevent segregation of the constituents in the powder mix Packaging
 To improve the flow properties of the powder mix because particles are
larger and more isodiametric PELLETS
 To improve the compression characteristics of the mix  Spherical granules
 Pelletization – Process of compressing or molding a material into the shape
METHODS OF GRANULATION of a pellet

1. WET GRANULATION Effervescent Granules

 Massing of the powder mix using a solvent (alone or with an adhesive or  Granules containing sodium bicarbonate and either citric acid, tartaric acid,
binding agent) or sodium biphosphate in addition to the active ingredient and, which, on
 Solvents used: solution in water, carbon dioxide is released because of the acid-base
o Water reaction.
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  The release of the water of crystallization makes the powder coherent and  These capsules contain 13% to 16% water varying with
helps form the granules storage conditions. When humidity is low, the capsules
 The effervescence from the release of carbon dioxide masks the taste of become brittle.
salty or bitter medications  When humidity is high the capsules become flaccid and
shapeless
Methods of Producing Effervescent Granules  Storage at high temperatures also affects the quality of hard
 Fusion Method gelatin capsules
 Wet Method
Made in 8 sizes with 0-4 as the sizes normally acceptable to patients:
CAPSULES 000 1.36g
 Solid dosage form in which one or more medicinal and/or inert substances 00 0.76g
are enclosed within a small edible shell or container generally prepared from 0 0.54g
a suitable form of gelatin to produce a unit dose, mainly for oral use 1 0.4g
2 0.3g
ADVANTAGES AND LIMITATIONS OF CAPSULES 3 0.24g
ADVANTAGES LIMITATIONS 4 0.19g
 Better absorbed than tablets  Limited number of suppliers of 5 0.1g
 Easier to formulate capsule shells  Size OE is an elongated size 0
 Suitable for clinical trials  Slow filling operation
 Veterinary use; sizes 10 (30g), 11 (15g), 12 (7.5g)
 Easy to carry  Not for highly soluble salts  COMPUTATION:
 Readily identified (size, color,  May become lodged in the
 Capsule fill weight = tapped bulk density x capsule volume
shape, prints) esophagus
o If fill weight of formulation = 450 mg and tapped density of
 Easily taken (orally)
formulation = 0.80 g/mL
 Ease of manufacture and
o Then capsule volume = 0.56 mL
distribution
o Capsule size 0 has a fill volume of 0.54 and can accommodate
 More stable and longer shelf-life
this amount.
 Capsule volume = capsule fill weight/tapped bulk density
TYPES OF CAPSULES
o If fill weight of formulation = 500mg
o Tapped density of formulation = 1.25g/mL
1. HARD SHELL CAPSULE
o Capsule size 0 and has a fill volume of 0.4
 Capsule shells are cast by dipping cold metallic molds or pins into
 PARTS OF HARD SHELL CAPSULE
gelatin solutions that are maintained at a uniform temperature and exact
o Cap
degree of fluidity
o Body
 Variation in the viscosity of the gelatin solution increases or decreases
 Tapered Rim
the thickness of the gelatin wall.
 Groove
 After the pins are withdrawn from the gelatin solution, they are rotated
 Indentation
while being dried in kilns. A strong blast of filtered air with controlled
 CAPSULE SEALING
humidity is forced through the kilns. Each capsule is then mechanically
 Optional
stripped trimmed and joined.
 Traditional shape is symmetrical bullet shape o Colored band of gelatin (Kapseals,
 Self-locking capsules to prevent separation of filled capsules Parke-Davis)
o Posilok o Heat welding through double wall
o Loxit thickness at cap-body juncture
o Coni-Snap o Liquid wetting agent that lowers melting point in contact areas of cap
 Filled with powders, granules, pellets, semisolid matrices, tablets, and body
capsules, thermo-softening mixtures, thixotropic mixtures, pastes
 STORAGE: COMPONENTS OF HARD SHELL CAPSULE
 Hard capsules should be stored in tightly closed glass Active Ingredients
containers and protected from dust and extremes of humidity Diluents  If the drug dose is inadequate to fill the
and temperature capsule, a diluent (such as lactose) is added.
 Lactose, Microcrystalline Cellulose, Starch
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 Glidants  Facilitates the free-flow of powder to allow PREPARATION OF SOFT SHELL CAPSULE
steady passage from the hopper through the Plate Process  Medicated solution is placed on a warm sheet of
capsule shell gelatin placed on bottom plate and topped with
 Magnesium Stearate, Calcium Stearate, second sheet where pressure is applied to form,
Stearic Acid, Talc, Fumed Silicon Dioxide fill and seal the capsules simultaneously
Disintegrants  Assist the breakup and distribution of capsule Reciprocating Die  Capsules are formed from two continuous ribbons
contents in the stomach Process (sheets of gelatin) through rotary or vertical dies
 Pregelatinized Starch, Croscarmellose, where metered fill material is injected and form
Sodium Starch Glycollate pockets of gelatin ribbons/sheets. Filled pockets
Surfactants  Wetting agents (e.g. sodium lauryl sulfate) are sealed by pressure and heat
added to capsule formulations to facilitate in
drug dissolution Compendial Requirements for Capsules
 Sodium Lauryl Sulfate  Added Substances
 Container’s permeability and sealing
Filling Hard Capsule Shell  Disintegration – as in tablets
 Dissolution – as in tablets
 Hand filling or punch method
 Stability
 Small scale compounding
 Moisture
 Large scale production  Weight variation – as in tablets
 Content uniformity – as in tablets
Hard Shell Capsules
 Hard gelatin capsule, starch capsule, vegetel, hpmc Added Substances
 Hard gelatin capsules  Enhance stability, elegance, usefulness or facilitate manufacture
 Composition: mixture of gelatin, sugar, and water with 0.15%  Harmless in the quantities used
 Sulfur dioxide; colorants and opacifying agents may be added  Do not exceed minimum amounts required to provide intended effects
 Shells are manufactured in a separate operation from the filling process  Do not impair product bioavailability therapeutic efficacy or safety
 Do not interfere with compendial assays and tests
Additional Treatment for Hard Shell Capsule
• Dusting and Polishing TABLETS
• Banding - Solid dosage form which may or may not contain medicinal substances with
• Printing or without diluents and prepared either by compression or by molding
• Enteric Coating - Compressed using a tablet press
- Can be made in various sizes, shapes, and surface markings (scores or
2. SOFT SHELL CAPSULE
grooved) depending o the design of punches and dies
 Filled with pumpable solutions or suspensions of drugs in liquids - Caplets are capsule-shaped tablets that allow the product to be smaller than
which will not solubilize the shell; also pasty materials and dry a capsule filled with an equivalent amount of powder
powders - Boluses are large tablets intended for veterinary use
 Only prepared commercially since highly specialized and large-
scale equipment is required
ADVANTAGES LIMITATIONS
 May be shaped as oblong, spherical, tube, suppository-type; pearl
 Precision of dosage  Reduced bioavailability due to
 STORAGE:
 Durability of physical characteristics reduced surface area
o Stored at 21-25°C and 35-50% relative humidity
 Stability of chemical and physical  Some patients have difficulty in
o Bottles
activity swallowing solid dosage forms
 Glass or plastic
 Convenience of administration
 Coil
 Desiccant packet
TYPES OF TABLET
o Strip or blister packs
 CONTAINER’S PERMEABILITY AND SEALING: Compressed  Tablets made by compression process
o May be tight, well closed, and light resistant depending on Tablet o Uncoated or plain tablets
the characteristics of the drug  Plain tablets
 Multiple Compressed Tablets

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  Layered Tablets o Opaquant and colorant
 Tablet within a tablet o Sweeteners, flavors, aromas
 Chewable tablet o Glossant
 Molded tablet
 Tablet triturates
 Hypodermic tablets Aqueous film coating  Film former – cellulose ether polymers like
 Dispensing tablets solution hydroxypropyl methylcellulose and methylcellulose
 Lozenges  Plasticizer – glycerin, propylene glycol, diethyl
 Lollipops phthalate
 Pills  Colorant (titanium dioxide, FD&Cor D&C dyes)
Coated Tablet  Sugar coated tablets  Vehicle - water
 Film coated tablets Enteric Coating  For tablets intended to pass though the stomach
o Gelatin-coated tablets intact to disintegrate and release drug content for
absorption in the intestines
Function:  To protect the drug from the environment  Based on factors of pH
 To provide a barrier for the unpleasant taste and odor of some  Hydroxypropyl methylcellulose phthalate, polyvinyl
drugs acetate phthalate, diethyl phthalate, cellulose
 To provide aesthetics or distinction to the product acetate phthalate
Uncoated or  Tablets made by compression of powders or granules without Fluid Bed o
Plain Tablets any additional coating Compression Coating  Similar to multiple coated compressed tablets
Multiple  Tablets prepared by more than one compression cycle having an inner core of and an outer shell of drug
Compressed resulting to a multi-layered tablet or tablet-within-a-tablet material
Tablets  Used for incompatible substances  Core tablets may be sugar coated by compression
 Anhydrous operation and may be safely employed
TYPE OF COATING PROCESSES in the coating of tablets containing drugs labile to
Sugar Coating  Coated with a sugar layer that is colored or moisture
uncolored
 Water soluble coating OTHER TYPES OF TABLETS
 Coating is water soluble and quickly dissolves after Buccal Tablets  Tablets inserted in the buccal pouch
swallowing Sublingual Tablet  Tablets inserted beneath the tongue
Chewable Tablet  Pleasant-tasting tablets formulated to disintegrate
Steps in Sugar Coating 1. Seal Coating smoothly in the mouth with or without chewing
2. Subcoating  For pediatric formulations, antacids, selected
3. Grossing (Smoothing) antibiotics
4. Heavy Syruping Effervescent Tablets  Compressed effervescent powders
5. Regular Syruping  Produced by compressing granular effervescent
6. Finishing salts that release gas when in contact with water
7. Polishing  Usually dissolved in a glass of water before
Film Coated Tablets  Coated with a thin layer of polymer administration
Molded Tablets  Or Tablet Triturates
Gelatin Coated Tablets  Gelcaps - caplet  Made by pressing alcohol-dampened masses of
 Coated with a gelatin layer that allows the coated powders into molds
product to be about one-third smaller than capsule  Solidification depends upon crystal bridges built up
filled with same amount of powder during the subsequent drying process and not upon
the compaction force
Film Coating  Non-aqueous (organic) film coating solution Tablet Triturates  Small, usually cylindrical, molded or compressed
 Film former tablets containing small amounts of usually potent
 Alloying substance drugs
 Plasticizer Dispensing Tablets  Tablets containing large amounts of potent drug
o Surfactant substances used by pharmacists to obtain
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 premeasured amounts for compounding multiple  Carminic acid
dosage units. Used by pharmacists to compound  Riboflavin
prescriptions and not for dispensing to patients.  Saffron
 No longer in use as this had the dangerous Flavors  Added to improve the aesthetic value of the
potential of being inadvertently dispensed to preparation
patients  Available as oils and as spray dried beadlets
Rectal Tablets  Tablets for administration through the rectum Sweeteners  Added to improve the taste value of the preparation
Vaginal Tablets and  Uncoated bullet-shaped or ovoid tablets inserted
Vaginal Inserts into the vagina for local effects Sugars:  Lactose
 Packaged with a plastic device for convenient  Sucrose
placement of the tablet in the vagina  Mannitol
Lozenges  Made using high degree of compression to produce  Dextrose
harder than ordinary tablets so that they dissolve or  Saccharin
disintegrate slowly in the mouth  Aspartame
Lollipops  Sugar-based lozenge on a stick Adsorbents  Substance capable of holding quantities of fluids in
Pills  Small, round solid dosage forms containing a an apparently dry state
medicinal agent intended to be administered orally
Examples of adsorbents:  Silicon Dioxide
COMPONENTS OF A TABLET  Magnesium Carbonate
TABLET EXCIPIENTS  Magnesium Oxide
Diluent  Substance that adds the necessary bulk to a  Bentonite,
formulation to prepare tablets of the desired size  Kaolin
Binder  Substance that “glue” powders together and cause  Magnesium Aluminum Silicate
them to form granules  Tricalcium Phosphate
Lubricant  Flow Activator/ Antifrictional Agent/Glidant/Anti-
adherent METHODS OF MANUFACTURE OF COMPRESSED TABLETS
 Enhance flow of materials during tablet WET GRANULATION  Spraying of liquid binder solution
compression or prevent the wear and tear of
punches and dies, prevent sticking to punches and Fluid Bed Process  The entire process of wet granulation is done in a
dies, produce tablet with a sheen continuous process using a single piece of
Colorants  Subbstances added improve the aesthetic value of equipment (fluid bed granulator)
the preparation
Dyes  Soluble Process performed:  Preblending
 FD and C  Wet granulation
 D and C  Drying to desired moisture content
 C DIRECT COMPRESSION  Process of tablet manufacture using materials that
Synthetic Colorants  Erythrosine posses free-flowing and cohesive characteristics
 Allura red that enable them to be compressed directly without
 Tartrazine the need of granulation
 Sunset yellow  Materials are pre-processed to render them
 Brilliant blue compressible with the addition of suitable
 Fast green excipients
 Indigotine
Natural Colorants  Bixin Usual Compression  Capping/Splitting/Laminating
 Anthocyanin Problems:  Soft Tablets
 Betacyanin  Variable Weight
 Betacarotene  Mottling
 Titanium dioxide DRY GRANULATION 
 Iron oxides
 Turmeric
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TABLETTING
 Tabletting
 Single punch tablet press
 Rotary tablet machines (high speed)
 Induced die feeder
o Dedusting – removes traces of powder adhering to tablets after
compression
COMPENDIAL REQUIREMENTS FOR TABLETS
Weight and Weight  Quantity of fill in the die of a tablet press
Variation  USP Weight Variation test
Content Uniformity  USP method - 10 tablets assayed individually (85% -
115%)
Thickness  Determined amount of fill that enters the die,
compaction characteristics of fill materials and
compression pressure
Hardness  High pressure, high hardness
 Hardness testers used to measure degree of force
(Kgs, lbs, or arbitrary units)
Friability  Ability of tablets to crumble under determined stress
factors (rolling in a drum for specified time)
 Measured as resistance to loss of weight
 Maximum weight loss of 1% generally considered
acceptable
Disintegration  Ability of tablets to disintegrate into smaller particles
with increased surface area for dissolution in body
fluids
 Measured in vitro using a Tablet Disintegratio
Testing Apparatus
Dissolution  In vitro testing that provides reasonable prediction of
or correlation with the product’s in vivo bioavailability
 Reasons for conducting dissolution tests
o Guides formulation and product
development toward product optimization
toward in vivo bioavailability
o Component of overall quality assurance
program in monitoring manufacturing
operations
o Requirement for regulatory approval of
products for marketing
FACTORS AFFECTING QUALITY AND PERFORMANCE OF SOLID DOSAGE
FORMS
Changes in  Use of starting raw materials – use materials of the
Formulation same specifications as standards set for components
 Use of different pharmaceutical excipients –
magnesium vs calcium stearate
 Use of different quantities for same excipients in
formulation – more concentrated binder
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 Addition of new excipients in formula – use different
coating formula
Change in Method of  Use of manufacturing equipment with different
Manufacture design
 Change in steps or order in manufacturing process
 Different in-process controls – quality tests or assay
methods
 Different batch sizes
 Different product reprocessing procedures
 Different manufacturing site
CHANGES IN MANUFACTURING
o Document
o Validate
o Register with regulatory body
PACKAGING AND STORING TABLETS
o Store in tight containers in places of low humidity and protected from
extremes in temperature
o If prone to decomposition due to the presence of moisture, co-package with
a desiccant packet
o If adversely affected by light, store in light-resistant containers
o A coil or plug, usually cotton wool, may be added in the container to prevent
abrasion of tablets
IMPORTANT CONSIDERATIONS IN PACKAGING
o Storage conditions
o Expiration date
o Dispense in similar type containers
Instantly Disintegrating or Dissolving Tablets
 Characterized by disintegrating or dissolving in the mouth within one minute
 Designed for children and elderly or any patient who has difficulty swallowing
tablets
DRUG RELEASE PATTERNS OF SOLID DOSAGE FORMS
Immediate Release  Designed to release the drug without any rate-
controlling features such as special coatings and
other formulation techniques
Modified Release  Designed to release the drug in a predetermined
manner
 Drug release features are based on time, course,
and/or location that are designed to accomplish
therapeutic or convenience objectives
Delayed Release
 Usually designed to pass through the stomach unaltered, later to release the
medication in the intestinal tract
 To protect a substance from destruction by gastric fluids or reduce stomach
distress caused by irritating drugs
  To facilitate gastrointestinal transit for drugs that are better absorbed from ethylcellulose, polyvinyl chloride and other synthetic
the intestines. polymers
 Designed to release the drug at a time other than promptly after
administration USP Requirements
 Delay may be time based or based on the influence of environmental  Drug release
conditions like gastrointestinal pH o Based on drug dissolution from the dosage unit against elapsed
time
Targeted Release  Drug release is directed towards isolating or  Uniformity of Dosage Units
concentrating a drug in a body region, tissue or site  In Vivo-In Vitro Correlations
for absorption or for drug action  Labeling
Enteric Coated  Specifically coated to remain intact in the stomach
and to yield their ingredients in the intestines
Repeat Action

Extended Release Product

 Designed to release the medication in a controlled manner at a
predetermined rate, duration, and location to achieve and maintain optimum
therapeutic blood levels of drug
 Allows a reduction in dosing frequency from that necessitated by a
conventional dosage form

Advantages of Extended Release Product

 Less fluctuations in drug levels
 Frequency reduction in dosing
 Enhanced convenience and compliance
 Reduction in adverse side effects
 Reduction in overall healthcare costs
 Complex Formation

Rate of drug release modified by technologies based on:

 Modifying drug dissolution by controlling access of biologic fluids to the drug
through the use of barrier coatings
 Controlling drug diffusion rates from dosage forms
 Chemical reaction or interaction between the drug substance or its
 pharmaceutical barrier and site specific biologic fluids

EXTENDED RELEASE TECHNOLOGY

Coated Beads, o Solution of drug substance is placed on small inert
Granules, and nonpareil seeds or beads made of sugar and starch
Microspheres or on microcrystalline cellulose spheres
Multitablet System o Small spheroid tablets of varying sizes having
varying drug release characteristics are placed in
gelatin capsule shells to provide desired pattern of
drug release
o Some uncoated for immediate release, others coated
for extended drug release
Microencapsulated o Drug in solid, liquid or even gaseous form is
Drug enclosed in microscopic particles by formation of thin
coatings of wall material around the substance
o Wall material – gelatin, polyvinyl alcohol,

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