Dosage Form

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• Dosage form are the means by which drug molecules/API are delivered are delivered to sites of action within

the body to produce optimum desired effects and minimum adverse effect.
• Dosage form = API + Excipents
• The means by which drug molecules are delivered to sites of action with in the body.
• A dosage form is a pharmaceutical preparation consisting of drug and excipients to
facilitate dosing, administration, and delivery of the content to the drug product
• API
• Chemical compound intended for use in diagnosis, prevention and treatment of disease
• It is the part of any drug that produces its effect.
• Excipents
• Donot increase or affect the therapeutic action of active ingredients
• Inactive ingredients may also be reffered to as inert ingredient or excipient and generally have no
pharmacological action
• Examples are binding material, dyes, preservative, flavouring agent, sweetening agent, coloring agent etc
• Importance of dosage form
• Dosage uniformity
• Stability
• Bioavailability
• Direct use of API is rare because of:
• API handling and accurate dosing can be difficult or impossible
• API administration can be impractical/unfeasible because of size,
shape, smell, taste and low activity.
• Some API are chemically unstable in light ,moisture,oxygen
• API can be degraded at the site of administration(low pH in stomach)
• API may cause local irritation or injury when they are present at high
concentration at site of administration
Need of dosage form

• Provide safe and convenient delivery of accurate dosage


• Eg tablet, capsule, syrup
• Protection of drug substance from atmospheric oxygen or moisture
• Eg coated capsule, sealed ampules
• Protection of drug substance from gastric acid after oral administration eg enteric coated tablet
• Conceal bitter taste or odour of drug substance
• Eg capsule,coated tablet, flavoured syrup
• Provide optimal drug action from topical administration sites
• Eg ointment, cream, ear and nasal preparation
• Provide for insertion of drug into one of the body orifices
• Eg rectal and vaginal suppository
• Provide extended drug action through controlled release mechanism
• Eg controlled release tablet, capsule, suspension
• Provide for the placement of drug within body tissue
• Eg implant
• Provide for optimal drug action through inhalation therapy
• Eg inhalant
Classification of dosage form
• Based on route of administration
• Oral
• Parenteral
• Topical
• Transdermal
• Respiratory
• Opthalmic
• Rectal
• Based on physical form
• Solid
• Semi solid
• Liquid
• gases
Based on physical form
• Solid dosage form
• Shaped tablet, Capsule, Implants, Transdermal patches
• Unshaped powder for external/internal use
• Semisolid dosage form
• Shaped suppositories(for rectal administration), pessaries(vaginal suppositories)
• Unshaped gel, cream, ointment, paste
• Liquid dosage form
• Monophasic solution(syrup, spirit, elixir, tincture)
• Biphasic emulsion, suspension
• External solution lotion,liniments,collodions
• Gaseous dosage form
• Medicinal gases Aerosol
• Aerodispersion antiasthmatic spray
• Tablet
• It is a unit dosage form containing one or more active pharmaceutical ingredients along
with excipients.
• Common excipients used in tablet are
• Diluents provide bulkiness of tablet
• Disintegrant ensure disintegration of tablet in GI tract
• Binder ensure binding of particles
• Glidant inhibit the friction between powder partcles
• Lubricant inhibit friction between powder particle and machine
• Sweetner /flavour mask the unpleasant taste
• Color to increase aesthetic
• Types of tablet are buccal and sublingual tablet, effervescent tablet, chewable tablet.
• Eg paracetamol, pantoprazole,folic acid,iron tablet
• Tablets are solid preparations each containing a single dose of one or more active
substances. They are obtained by
• compressing uniform volumes of particles or
• by another suitable manufacturing technique, such as
• extrusion,
• moulding or
• freeze-drying (lyophilisation).
• Tablets are intended for oral administration.
• Some are swallowed whole,
• some swallowed after being chewed,
• some are dissolved or dispersed in water before being administered
• some are retained in the mouth where the active substance is liberated.
• Categories of tablets for oral use:
• uncoated tablets;
• coated tablets;
• effervescent tablets;
• soluble tablets;
• dispersible tablets;
• orodispersible tablets;
• gastro-resistant tablets;
• modified-release tablets;
• tablets for use in the mouth;
• oral lyophilisates.
• Advantage
• Greatest dose precision with least content variability.
• Production aspects- Large scale production at lowest cost.
• Lighter and compact so easiest and cheapest form to package and ship.
• High chemical, mechanical & biological stability.
• Lend to give special release profile products e.g. enteric or delayed release tablets.
• Objectionable odor and bitter taste can be masked by coating technique.
• Product identification is easy and rapid requiring no additional steps when employing an embossed and/or
monogrammed punch face
• Disadvantage
• Difficult to swallow in case of children and unconscious patients.
• Some drugs resist compression into dense compacts, owing to amorphous nature, low density character.
• Drugs with poor wetting, slow dissolution properties, slow absorption in GIT may be difficult to formulate or
manufacture as a tablet that will still provide adequate or full drug bioavailability.
• Bitter testing drugs, drugs with an objectionable odor or drugs that are sensitive to oxygen may require encapsulation
or coating. In such cases, capsule may offer the best and lowest cost.
General properties of Tablet dosage forms

• A tablet should have elegant product identity while free of defects like chips, cracks, discoloration, and
contamination.
• Should have sufficient strength to withstand mechanical shock during its production packaging, shipping and
dispensing.
• Should have the chemical and physical stability to maintain its physical attributes over time
• The tablet must be able to release the medicinal agents in a predictable and reproducible manner.
• Must have a chemical stability over time so as not to follow alteration of the medicinal agents.
Types of tablets

• A. Tablets ingested orally:


• 1. Compressed tablet,
• e.g. Paracetamol tablet
• 2. Multiple compressed tablet
• 3. Modified release tablet
• a. Delayed release tablet, e.g. Enteric coated Bisacodyl tablet
• b.Targeted tablet
• i. gastro-retentive/floating tablet
• ii. Colon targeting tablet

4. Sugar coated tablet, e.g. Multivitamin tablet
• 5. Film coated tablet, e.g. Metronidazole tablet
• 6. Chewable tablet, e.g. Antacid tablet
• 7. Dispersible tablets e.g antibiotics
• B. Tablets used in oral cavity:
• 1. Buccal tablet, e.g. Vitamin-c tablet
• 2. Sublingual tablet, e.g. GTN
• 3. Troches or lozenges
• 4. Dental cone
• 5. Mouth dissolve tablet

C. Tablets administered by other route:
• 1. Implantation tablet
• 2. Vaginal tablet, e.g. Clotrimazole tablet

D. Tablets used to prepare solution:
• 1. Effervescent tablet, e.g. Dispirin tablet (Aspirin)
• 2. Dispensing tablet, e.g. Enzyme tablet
• 3. Hypodermic tablet
• 4. Soluble tablets
• 5. Tablet triturates e.g. Enzyme tablet
• Capsules:
• Solid dosage forms in which drug is enclosed within either hard or soft
soluble shell (gelatin).
• Advantages:
• Elegant, easy to use and portable
• Tasteless/Odourless dosage form
• Ease in swallowing (smooth & hydrates in mouth)
• Aesthetically pleasing (in many colours)
• Can be economically produced in large quantities.
• Ready availability of contained drug.
• Limitations: Cannot be used in case of
• Extremely water soluble drugs
• KCl, KBr, Al2CL4, GI irritation
• Highly efflorescent drugs
• Soft capsules
• Deliquescent drugs
• Dry capsules
• Two types:
• Soft gelatin capsules (Softgels)
• Hard gelatin capsules
• Non-gelatin made from PVA, Starch and HPMC
• Interest in non-gelatin capsules due to religious, cultural and vegetarian needs.
Powder

• Pharmaceutical powder are solid dosage form of medicament in which one or more drug are
dispensed in finely divided state with or without excipient
• They are available in crystalline or amorphous form
• Advantage
• It is both used internally or externally
• It is more stable then liquid dosage form
• Onset of action is faster as compared to tablet, capsule
• Easy to carry
• Easy to administration to the patient orally by dissolving in suitable liquid
• Disadvantage
• Drug have bitter taste, nausea and unpleasant taste cannot be administered in powder form
• Deliquescent and hygroscopic drug cannot be dispensed in powder form
• Drug which get affected by atmospheric condition are not suitable for dispense
• Classification of powder
• Bulk powder for internal use
• Bulk powder for external use
• Simple and compound powder for internal use
• Powder enclosed in cachets and capsule
• Compressed powder(tablet)
• Eg Rhubarb powder, dentifrices, medical dusting powder, surgical
dusting powder
granules
• Granules are prepared agglomerates of smaller particle of powder
• Reason for granulation
• To prevent segregation of the constituent of powder mix
• To improve flow property of powder mix
• To improve compaction characteristics of powder mix
• Eg Biaxin granules for oral suspension
• Omnicef for oral suspension
• Effervescent granule
Suppository
• Drug delivery system where drug is incorporated in inert vehicle
• Suppositories are solid, single-dose preparations
• The shape, volume and consistency of suppositories are suitable for rectal administration
• Excipients such as diluents, adsorbents, surface-active agents, lubricants, antimicrobial preservatives and colouring
matter, authorised by the competent authority, may be added if necessary
• Suppositories may contain medicaments, dissolved or dispersed in the base, which are intended to exert a systemic effect
• The bases used either melt when warmed to body temperature or dissolve or disperse when in contact with mucous
secretions.
• Alternatively the medicaments or the base itself may be intended to exert a local action
• Suppositories are prepared extemporaneously by incorporating the medicaments into the base and the molten mass is
then poured at a suitable temperature into moulds and allowed to cool until set
• Eg metronidazole suppository, paracetamol suppository
Lozenges
• It is a solid dosage form containing a drug along with flavouring and
sweetening agent
• These are solid preparation that are intended to dissolve or
disintegrate slowly in mouth
• Most often used for localized effect in oral cavity
• They are available in flat, circular, octagonal, biconvex and cylindrical
form
• Eg Medicated lozenges: Strepsil, Clotrimazole, Nystatin
• Non medicated lozenges: candies lollipop
Solution
• Stable homogenous mixture of two or more components
• One or more solute is dissolved in one or more solvents
• Solvent is often aqueous but can also be oily or alcoholic
• Formulations: --- oral dosage forms, mouthwashes, gargles, nasal drops, ear drops or available for external
applications
• Eg cough syrup, PCM, potassium chloride, Theophylline oral solution, dicyclomine HCL syrup
(anticholinergic), chlorpomazine HCL syrup (antiemetic),sodium valproate syrup, cyproheptadine HCl syrup
(antihistamine), lactulose syrup (cathartic), metoclopramide syrup (GI stimulant)
Syrup

• Solution of sucrose in water


• Used as a vehicle for different pharmaceutical preparation like solution
• Highly concentrated, aqueous solutions of sugar or a sugar substitute that traditionally contain a flavouring agent, e.g. cherry
syrup, cocoa syrup, orange syrup, raspberry syrup
• The major components of syrups are as follows:
• Purified water
• Sugar (sucrose) or sugar substitutes (artificial sweeteners)
• Can promote dental decay
• Unsuitable for diabetic patients
• Due to the inherent sweetness and moderately high viscosity of these systems addition of other sweetening agents and
viscosity-modifying agents is not required
• Other non-sucrose bases may replace traditional syrup E.g Sorbitol
• Sorbital Solution USP which contains 64% w/w sorbitol (a polyhydric alcohol)
• More recently, many products have been formulated as medicated sugar-free syrups due to the glycogenetic and cariogenic
(causing tooth decay) properties of sucrose.
• All medicinal products designed for administration to children and to diabetic patients must be sugar-free.
• syrup substitutes must therefore provide an equivalent sweetness, viscosity and preservation to the original syrups
• E.g cyproheptadine syrup, cetrizine syrup
Syrup
• They are concentrated aqueous preparation of sugar or sugar
substitute with or without flavouring agent and medicinal substane
• Type of syrup : simple syrup, medicated syrup, nonmedicated syrup
• Simple syrup contain only sucrose and purified water
• Syrup containing agent but not medicinal substance are called non
medicated or flavoured syrup.
• Syrup containing therapeutic agent are called medicated syrup
• Eg Mepridine HCl, Diclomine HCl, Amantadine HCl, Sodium valproate
• Elixirs –
• Elixir are clear, sweetened, hydroalcoholic preparation intended for oral use and usually flavoured for
palatability
• Alcoholic content vary from 10-40%
• An elixir must always contain alcohol whereas a syrup may or maynot use alcohol
• Elixir are meant to be clear liquid whereas syrup amy contain natural or artificial dye
• In general elixir are less viscous then syrup due to their higher alcohol content and their minimal use of sugar
and other viscosity improving agent
• Some drug are insoluble in water so in this case we cannit use syrup and suspension
• Type of elixir : Medicated and non medicated elixir
• Medicated elixir : antihistamine elixir, phenobarbital elixir, theophylline elixir
Emulsion
• An emulsion may be defined as a biphasic system consisting of two immiscible liquids, one of which (the
dispersed phase) is finely and uniformly dispersed as globules throughout the second phase (the continuous
phase)
• The particle size of the dispersed phase commonly ranges from 0.1 to 100 μm
• Since emulsions are a thermodynamically unstable system a emulsifier is added to stabilize the system
• Emulsifier stabilizes the system by forming a thin film around the globules of dispersed phase
• Emulsions include:
• Oral preparations
• External applications --- Lotions, liniments or creams
• Some parenteral products may also be formulated as emulsion
• E.G cod liver oil emulsion, liquid paraffin oral emulsion, propofol emulsion
• Emulsion Types
• Oil in Water Emulsions (O/W) --- Oil is dispersed in continuous phase of water
• Water in Oil Emulsion (W/O) --- Water is dispersed in continuous phase of Oil
Suspension
• Disperse system in which one substance (Disperse Phase) is distributed in particulate form throughout
another phase (Continuous phase)

• Contains one or more insoluble medicaments in a vehicle with other additives such as preservatives,
flavours, colours, buffers and stabilizers.

May be used for


• Oral administration
• Inhalation – Budesonide inhalation suspension via nebulizer
• Topical application – Sodium sulfacetamide suspension used in acne
• Ophthalmic application -- PREDNISOLONE ACETATE
• Parenteral administration– Methylprednisolone acetate injectable suspension USP, Procaine Penicillin G,
Insulin zinc suspension (Ultrlente)
• Aerosols –
• Ipratopium inhalation aerosol suspension --- via Metered dose inhaler, nebulizer
Liniments
• Liniments are solution or mixture of various substance in oil, alcoholic solution of soap or emulsion and may
contain suitable antimicrobial agent.
• These preparation that may be liquid or semi liquid are intended for external application and should be so
labeled
• They are rubbed onto the affected area because of this they were once called embrocation. They are
applied with friction and rubbing of skin , the oil or soap base providing for ease of application and massage
• Only suitable for external use
• Different form are
• Antipruritic used to relieve itching
• Astringent cause biological tissue to contract
• Emollient product that soften skin
• Rubefacient substance that cause redness
• Compound calamine liniment(used to treat discomfort of dermatitis and eczemz), efficascent
liniment(temporary relief of minor ache), white liniment
Tincture
• These are liquid extract which are alcoholic or hydroalcoholic solution
of non volatile drug of vegetable and chemical origin
• In herbal medicine alcoholic tincture are made with various ethanol
concentration
• Eg tincture of calendula, opium tincture, benzoin tincture
Ointment
• Any greasy or oily semisolid preparation usually medicated that can
be applied externally to skin in order to heal, soothe or protect it
• It is viscous semisolid preparation used topically on a variety of body
surface
• Drug ingredient can be dissolved, emulsified or suspended in
ointment base
• Types of medicated ointment are dermatologic, ophthalmic, rectal,
vaginal and nasal ointment
• Eg nitroglycerine ointment, sulfacetamide sodium ointment,
benzocaine ointment , ipratropium bromide ointment
Cream
• Cream are defined as semisolid dosage form containing one or more
drug substance dissolved or dispersed in suitable base.
• Cream are semisolid emulsion of oil and water either O/W or W/O
type.
• They are of softer consistency and lighter body then true ointment
• Eg cetrimide cream, hydrocortisone cream, zinc oxide cream
Paste
• They are homogeneous semisolid dosage form containing high
concentration of insoluble powder substance (not less then 20%)
dispersed in suitable base
• The paste are usually less greasy, more absorptive and stiffer then
ointment
• They have good adhesion on skin and they donot melt at ordinary
temperature.
• Eg magnesium sulfate paste, zinc and coal tar paste, resorcinol and
sulfur paste
Gels
• Gel are semisolid dosage form in which there is dispersion of small or
large molecules in aqueous liquid vehicle.
• They produce jelly like consistency
• Types of gel are single phase gel, two phase gel
• Eg clindamycin gel, metronidazole gel, cyanocobalmine gel
Arerosol
• Pharmaceutical aerosols is a solutions, supensions or emulsions of drugs mixed with
inert propellants.
• Mixture are contained under pressure in metal canisters fitted with a valve
• On depression of valve --- canister is fired and medicament is expelled
• Pharmaceutical aerosols are used to deliver drugs to produce both local and systemic
effects
• Eg Salbutamol, terbutaline
Inhalants
• These are the drug or chemicals which are in the vapour form inhaled
in the body
• Inhalation of gases changes the physiological function and bring
pharmacological action
• Administered by nasal respiratory route for local or systemic effect
• Eg nitrogen, oxygen(to support respiration in critical situation), carbon
dioxide(relieve persistent hiccup), nitrous oxide(anesthetic) are
commonly used inhalant
Injection
• Injection are sterile solution, suspension or emulsion
• They are prepared by dissolving, emulsifying or suspending an API and
any other excipient in water for injection
• Injecting is act of giving medication by use of syring and needle to
obtain desired therapeutic effect
• Eg Insulin, paracetamol injection,

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