Pharmaceutical dosage forms

DOSAGE FORM

HARISHANKAR SAHUB.pharmacy 4th year

Shri Rawatpura Sarkar institute of pharmacy,Durg

Drug:-(active pharmaceutical ingredient - API) chemical compound intended for used in diagnosis, treatment or prevention of diseases.

Terms:-

Excipients:- (inactive pharmaceutical ingredients)

Technological, biopharmaceutical and/or stability reasons.

Diluents/fillers, binders, lubricants, desintegrants, coatings, preservants and stabilizers, colorants and flavourings

dosage form:-Drug+excipients

CLASSIFICATION

SOLID SEMI-SOLID LIQUID GAS

1.Unit solid:-_tablets_capsules2.Bulk dosage form:-_powder_Dusting powder

1.Monophasic liquid:-_syrup_solution2.Biphasic liquid:-_emulsion_suspension

_Inhaler_aerosols

CreamPasteGelsuppositories

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• Tablets:-– They are unit solid dosage

forms consisting of active ingredient and suitable pharmaceutical excipients.

– They may vary in size, shape, weight, hardness, thickness, disintegration and dissolution characteristics, and in other aspects.

Capsules:- • They are unit solid dosage forms

consisting gelatin shell that breaks open after the capsule has been swallowed and releasing the drug.

• Types- hard-shell gelatin capsule

soft-shell gelatin capsule

1. soft gelatin shell manufactured in one piece with drug usually in liquid form inside the shell, e.g. fat-soluble vitamins A and E, Procardia (nifidepine), etc.

2. hard shell manufactured in two pieces that fit together and hold the drug, either in powdered or granular form.

lozenges :-

tablets formed from hardened base or sugar and water containing drug and other flavors.

They are designed to dissolve slowly in the mouth and release the drug topically to the tissues of mouth and throat; they are not to be swallowed.

Powder:- • They are bulk solid dosage forms

consisting two or more medicament meant for internal use.

• The size of particle range from 10,000 microns to 0.1microns.

• Size of the powder determine the effectiveness of physiological properties.

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• Semisolids contain both liquids and solids semi-solid.• dosage forms that are too soft in structure to qualify for

solids but too thick to be considered liquid.• They are meant for topical application.

Creams: -

Creams are semi-solid emulsions, that is mixtures of oil and water. They are divided into two types-

1.O/W TYPE2.W/O TYPE

A.O/W creams:-• which are composed of small droplets

of oil dispersed in a continuous aqueous phase.

• cosmetically acceptable as they are less greasy and more easily washed off using water.

B.W/O creams:• which are composed of small droplets

of water dispersed in a continuous oily phase.

• Water-in-oil creams are more difficult to handle.

• Water-in-oil creams are also more moisturising as they provide an oily barrier which reduces water loss from the stratum corneum,the outermost layer of the skin.

Ointment/Pastes• Pastes are semisolid dosage forms

that contain one or more drug substances intended for topical application.

• Generally, pastes contain a higher proportion of solid materials than ointments.

• They are more stiff, less greasy, and more absorptive of serous secretions when used on the skin.

• Medicated dental pastes are also prepared for adhesion to the mucous membranes for local effect.

Elixirs:- solutions that contain an alcohol and water base, added sugar and

flavorings, e.g. Tylenol; commonly used for pediatric and elderly patients who have difficulty swallowing tablets or capsules.

Syrups:- do not contain alcohol and are concentrated solutions of sugar,

water, and flavorings. They are sweeter and more viscous than elixirs. Most OTC cough medications are syrup based and don’t only carry the drug but also act to soothe the inflamed mucous membranes of the throat.

Solutions:- one homogenous phase, prepared by dissolving one or more

solutes in a solvent.Emulsions:-

-a dispersion system consisting of two immiscible liquids-o/w or w/o-cloudy appearance.

Suspensions:-A dispersion system where solid particles are dispersed in liquid

phase• Solid particles called dispersed phaes and liquid called

continuous phaes.

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Liniments • Liniments are alcoholic or

oleaginous solutions, suspensions, or emulsions of medicinal agents intended for external application to the skin, generally by rubbing.

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Inhalations • Inhalations are finely

powdered drug substances, solutions, or suspensions of drug sub stances administered by the nasal or oral respiratory route for local or systemic effects.

• Special devices are used to facilitate administration.

Thanks to a new insulin inhaler, researchers say, the daily injections many diabetics take may become relics of the past.

aerosol sprays- Several different types

of pharmaceutical product may be packaged in pressurized dispensers, known as aerosols.

- used as surface disinfectants, wound or burn dressing, relieve irritation of bites.

TABLET

Tablets

• Tablets are oral solid unit dosage form of medicaments with or without suitable diluents and prepared either by molding or compression. They are solid, flat or biconvex disc in shape. •They vary greatly in shape, size and weight which depend upon amount of medicament used and mode of administration. •They also vary in hardness, thickness, disintegration and dissolution characteristics and in other aspects depending upon their intended use and method of manufacture

•They are used for local & systemic effect.

• Usually used for oral administration

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Advantages

– Large scale production at lowest cost

– Easiest and cheapest to package and ship

– High stability– Easy to handling– Easy to administration– Lightest and most compact– Tablets are formulated as a

special release of products such as enteric or delayed release products.

Disadvantages

• It’s not suitable for poorly water-soluble or poorly absorbable drugs, less bioavailability.

• Drugs that are sensitive to oxygen or may also require special coating.

• Enhances local irritant effect of some drugs or cause harm to the gastrointestinal mucosa

Types of tablets

• 1)compressed tablets • 2)sugar coated tablets• 3)film coated tablets• 4)enteric coated tablets• 5)effervescent tablets• 6)chewable tablets• 7)dispersible tablets• 8)sustained release tablets• 9)multilayer tablets• 10)sublingual tablets• 11)buccal tablets• 12)vaginal tablets

Tablet Ingredients (excipients)

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They use to make required bulk of the tablet . to provide better tablet properties such as to improve cohesion, to permit use of direct compression manufacturing to improve flowEx:-1. Lactose, sucrose, mannitol; frequently used, water soluble, improves tablet disintegration.2.Dicalcium phosphate dihydrate, insoluble in water, disintegrating agent is a must.3. Mannitol, dextrose, sucrose, 4. Lactose-anhydrous and spray dried lactose5.Directly compressed starch-Sta Rx 15006. Hydrolyzed starch-Emdex and Celutab 7. Microcrystalline cellulose-Avicel (PH 101, 102)

Filler or diluent

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Role: to ensure that the tablet, when in contact with a liquid, breaks up into small fragments, which promotes rapid drug dissolution.

Mode of action:  1. Facilitate water uptake into the pores of tablet,e.g. surface active agents 2.facilitate rupture of tablet by swelling during water sorption,e.g. Sodium –starch glycolate, Crosscarmelose- cross linked cellulose; modified cellulose, Ac-Di-Sol

3. Release of gases to disrupt the tablet structure, normally carbon dioxide, in contact with water. e.g. effervescent tablets. 

Disintegrant

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Role: Ensure that granules and tablets can be formed with the required mechanical strength.( glue that holds powders together to form granules )Examples:

starch paste 5-25% gelatin solution 10-20%, gum acacia, tragacanth, 10-25%Liquid glucose 50%,Cellulose derivativePolyvinylpyrrolidone 2% (PVP), PEG

Binder and adhesive

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Role: Lubricants prevent adherence of granule/powder to die wall and promote smooth ejection from the die after compaction, reduce inter particle friction and improve the rate of flow of the tablet granulation.

Lubricant

Glidant

Role: Improve flowability of the powder They are added during direct compaction and to granulation before tabletting ( they reduce interparticulate friction).Ex.-1. Talc (at concentration 1-2 %).2. Colloidal silica (0.2 %).3. Corn Starch 5-10%

Manufacturing

Stages of pharmaceutical manufacturing

API

Excipients

PrimaryPackaging

SecondaryPackaging

API FinishedProduct

Starting Materials(Chemicals)

Processing routes

Fill die

Coating, Packaging etc..

Compress Tablet

Direct Compression

DrugDiluentGlidantDisintegrant

Lubricant Mixing

Mixing

Dry Granulation

Disintegrant GlidantLubricant

DrugDiluentLubricant

Mixing

Compression

Comminution

Screening

Mixing

Mixing

Wetting

Granulation

Drying

Screening

Mixing

DrugDiluent

BinderSolvent

Disintegrant GlidantLubricant

Wet Granulation

Other Routes

Fluidized bed granulationExtrusion / rotary granulation

Tablet Compression

Tablet compression machines

• Hopper for holding and feeding granulation to be compressed

• Dies that define the size and shape of the tablet• Punches for compressing the granulation within

the dies• Cam tracks for guiding the movement of the

punches• Feeding mechanisms for moving granulation

from the hopper into the dies

Single punch machine

Multiple punch machine

Upper andLower Collar

Collar locker

Single Punch Machine (Tablets)

Multi-station rotary presses

• The head of the tablet machine that holds the upper punches, dies and lower punches in place rotates

• As the head rotates, the punches are guided up and down by fixed cam tracks, which control the sequence of filling, compression and ejection.

• The portions of the head that hold the upper and lower punches are called the upper an lower turrets

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