Introduction to different dosage forms SUDHA ASSISTANT PROFESSOR GNIT COLLEGE OF PHARMACY GREATER NOIDA
Contents Introduction Classification of dosage forms Solid dosage forms Liquid dosage forms Semi solid dosage forms New drug delivery system
Introduction Dosage form ( Medicines) API + Excipients The means (or the form) by which drug molecules are delivered to sites of action within the body . Drug (Active pharmaceutical ingredients ) Chemical compound intended for used in diagnosis, treatment prevention, of disease. OR The Active Pharmaceutical Ingredient (API) is the part of any drug that produces its effects. Excipients do not increase or affect the therapeutic action of the active ingredient,. Inactive ingredients may also be referred to as inert ingredients or excipients , and generally have no pharmacological effect. Examples of inactive ingredients include binding materials, dyes, preservatives, and flavoring agents,sweetening agents,coloring agents etc.
Direct clinical use of the active drug substances is rare: Why ?? API handling and Accurate dosing can be difficult or impossible (e.g., potent drugs: low mg and µg doses). API administration can be impractical/unfeasible because of size, shape, smell/ odour , taste and low activity. Some API are chemically unstable in light, moisture, O2 API can be degraded at the site of administration (e.g., low pH in stomach). API may cause local irritations or injury when they are present at high concentrations at the site of administration. Administration of active substance would mean to have no chance for modification (improvement) of its PK profile.
The need for dosage forms: Accurate dose. Protection e.g. coated tablets, sealed ampules . Protection from gastric juice. Masking taste and odour . Placement of drugs within body tissues. Sustained release medication. Controlled release medication. Optimal drug action. Insertion of drugs into body cavities (rectal, vaginal) Use of desired vehicle for insoluble drugs.
Solid dosage forms Solid dosage forms are available mostly in unit dosage forms. Some solids are packed and supplied in bulk. The bulk forms meant for internal use are supplied either as granules or fine powder. The bulk powder meant for external use are dusting powder, insufflations, snuffs and tooth powders.
Tablets They are unit solid dosage form consisting of active ingredients and suitable pharmaceutical excipients . they may very in size, shape, hardness, thickness, weight, disintegration,dissolution characterisitics and in other aspect.
Capsules Capsule are solid unit dosage forms in which one or more medicaments enclosed within a shell. Types – Hard gelatin capsule ( powder,granules,bead,tablet ) Soft gelatin capsule (liquids or semisolids)
Pills These are small, rounded solid dosage forms containing medicaments intended for oral use. The medicaments are mixed with excipients to forms a firms plastic mass. The mass is rolled to uniform pill pipe, which cut into numbers of uniform pills. The pills are spherical in shape & produced by rolling them under wooden pill rounder.
Lozenge It is a solid preparation consisting of sugar and gum & are intended to dissolve or disintegrate slowly in the mouth. It is used to medicate the mouth and throat for the slow administration of indigestion or cough remedies.
Pastilles They are solid medicated preparations designed to dissolve slowly in the mouth. They are softer than lozenges and their bases are either glycerol and gelatin , or acacia and sugar.
Powder Powders are solid dosage form of medicaments which are meant for internal or external use. They are available in amorphous and crystalline forms. TYPES OF POWDERS 1. Bulk Powders for internal use e.g. fine powders or granules 2. Bulk Powders for external use e.g. snuff, dusting powders, tooth powder 3. Simple and compound powder for internal use. 4.Powders in the form of compressed tablets and tablet triturates. 5.Powders enclosed in cachets and capsules
Dusting powders These are meant for external application to the skin and are generally in a very fine state of subdivision to avoid local irritation. These are mainly used for their antiseptic, astringent, absorbent, antiperspirant and antipruritic action.
Insufflations These are medicated dusting powders meant for introduction into body cavities (nose, throat, ear, vagina etc) with the help of an apparatus known as a insufflator . It sprays the powders (in a state of fine particles) on site of application.
Snuffs These are finely divided solid dosage forms of medicaments which are inhaled into nostrils. They are mainly used for their antiseptic, bronchodilator and decongestion action.
Liquid dosage form It may be defined as “A solution is a liquid-preparation that contains one or more soluble chemical substances dissolved in a specified solvent” Liquid dosage forms are intended for External, Internal or parenteral use. They mainly classified into two category namely as – I) Internal Liquid Preparations. Monophasic liquid preparations Biphasic liquid preparations II) External Liquid Preparations Applied on the skin Instilled into body cavities Used in mouth
Advantage Immediately available for absorption. Administration convenient, particularly for infants, psychotic patients. Easy to color, flavor & sweeten. Liquids are easier to swallow than solids and are therefore particularly acceptable for pediatric patient. A solution is an homogeneous system and therefore the drug will be uniformly distributed throughout the preparation. Some drugs like aspirin, KCl can irritate gastric mucosa if used orally as a solid dosage forms. But this effect can be reduce by solution system.
Disadvantage Less stable in aqueous system. Incompatibility is faster in solution than solid dosage form. Patients have no accurate measuring device. Accident breakage of container results in complete loss. Solution often provide suitable media for the growth of micro organisms. The taste of a drug, which is often unpleasant, is always more pronounced when in solution than in a solid form. Bulky than tablets or capsule, so difficult to carry transport.
Monophasic liquid dosage forms It contain only one phase. It is represented by true solution. A true solution is a clear homogenous mixture that is prepared by dissolving solute in a suitable solvent. Monophasic liquid dosage forms are – a)Syrup b)Elixirs c)Solutions d) Linctuses
Syrup It is a concentrated or saturated solutions of sucrose in purified water. The concentration of sucrose is 66.7% w/w & due to that it is a viscous preparations. The syrup which contains medical substance called as a medicated syrup & those containing aromatic or flavored substance known as a flavored syrup.
Elixirs It is clear, sweetened, aromatic, hydroalcholic preparations meant for oral use. The medicated elixirs are generally contained potent drug like as antibiotics, antihistamine or sedative , where as non–medicated elixirs contained flavored. The composition of elixirs contained mainly as ethyl alcohol (active ingredients),water, glycerin or propylene glycol, coloring agent, flavoring agent & preservative.
Linctuses These are viscous liquid preparations that’s are used for the treatment of cough. They contain one or more medicaments which have demulcent, sedative, expectorant action on the mucus membrane of throat. They are taken in small doses without diluting with water to have prolonged effect of medicines. Simple syrup is used as a vehicle for most of the linctuses.
The liquid which consist of two phases are known as a biphasic liquid dosage forms. They are sub categorized into two different forms namely as – I) Emulsion II) Suspension In emulsion both phases are available in liquid where as in suspension, finely divided solid particles are suspended in liquid medium. Biphasic liquid dosage forms
Emulsion Emulsion is a biphasic liquid preparations containing two immiscible liquid (Continuous Phase & dispersed phase) made miscible. The liquid which is converted into minute globules is called as dispersed phase & the liquid in which the globules are dispersed is called the continuous phase. dispersed phase continuous phase Two Immiscible Liquids Dispersed Phase (Internal phase) Continuous Phase ( External phase)
Types of emulsions Simple type Water in oil (w/o) Oil in water (o/w) Depending on globule size Micro emulsion Fine emulsion Special type Multiple emulsion (w/o/w, o/w/o)
Suspension Suspensions are the biphasic liquid dosage forms of medicament in which finely divided solid particles ranging from 0.5 to 5 micron are dispersed in a liquid or semisolid vehicle, with aid of single or combination of suspending agent. In which solid particles acts as disperse phase where as liquid vehicle acts as continuous phase The external phase (suspending medium) is generally aqueous in some instance, may be an organic or oily liquid for non oral use. The particle size for non oral suspension is so important to avoid grittiness to skin.
External liquid preparations Applied on the skin LOTIONS Are usually aqueous, alcoholic or oily liquid preparations. They are intended for external application without friction or rubbing to the affected area Usually applied with the help of some absorbent material such as cotton wool or gauze. It is generally used to provide cooling, soothing and protective & antiseptic action.
LINIMENTS Liniments are liquid or semi- liquid preparations meant for external application to the skin. They are usually applied to the skin with friction & rubbing of the skin. Are usually alcoholic and oily liquid preparations ( monophasic ) or emulsion (biphasic). Alcoholic liniments are used generally for their rubefacient and counterirritant effects. Such liniments penetrate the skin more readily than do those with an oil base. The oily liniments are milder in their action and may function solely as protective coatings Liniments should not be applied to skin that are bruised or broken.
B) Instilled into body cavities Ear drops Nasal drops Nasal Sprays Inhalations Douches Enemas
Ear drops These are the solutions of drugs that are instilled into ear cavity with the help of dropper. These are generally used for cleaning the ear, softening the wax & for treating the mild infections. The solutions is generally prepared in water, glycerin, propylene glycol & dilute alcohol.
Nasal drops Nasal drops are aqueous or liquid paraffin solutions meant for instillation into nostrils. Drugs in solution may be instilled into the nose from a dropper or from a plastic squeeze bottle. The drug may have a local effect, e.g. antihistamine, decongestant . Alternatively the drug may be absorbed through the nasal mucosa to exert a systemic effect.
douche A douche is a device used to introduce a stream of water into the body for medical or hygienic reasons, or the stream of water itself. Douche usually refers to vaginal irrigation, the rinsing of the vagina , but it can also refer to the rinsing of any body cavity. A douche bag is a piece of equipment for douching—a bag for holding the fluid used in douching.
C) Used in mouth Gargles Gargles are aqueous solutions used for treating throat infection by forcing air from lungs through the gargle that is held in the throat. dispensed in concentrated forms with directions of dilution with water before use They are used into intimate contact with the mucous membrane of throat for few seconds, before they are thrown out of the mouth. They are also used for their antiseptics, antibiotics anesthetics, astringent,alkalinizing antifungal action.
Mouth wash These are aqueous solutions with pleasant or acceptable taste & odour These are used to make clean & deodorise the buccal cavity or used for oral hygiene and to treat infections of the mouth. They mainly contain antibacterial agent, alcohol, glycerin, sweetening agent, flavoring agent & colouring agent.
Semisolid dosage forms Semisolid dosage forms meant for external application They contain one or more active ingredients dissolved or uniformly dispersed in a suitable base and any suitable excipients such as emulsifiers, viscosity-increasing agents, antimicrobial agents, antioxidants, or stabilizing agents Semisolid dosage forms subcategorized are as- I) ointment II) creams III) paste IV) Jellies V) Suppositories
Ointment Ointments are homogeneous semisolid preparation meant for application to skin or mucous membrane. The ointments are mainly used for their protective or emollient properties
Creams Creams are homogeneous, semi-solid preparations consisting of opaque emulsion systems Cream is divided in to two types namely as I) Aqueous creams II) Oily creams In case of aqueous creams the emulsions are o/w type & it is relatively non greasy. In case of oily creams w/o type & it is relatively greasy The cream should be store in collapsible tube & supplied in well closed container to prevent evaporation & contamination.
Pastes Pastes are homogeneous, semi-solid preparations containing high concentrations of insoluble powdered substances (usually not less than 20%) dispersed in a suitable base. They are mainly used as a antiseptic, protective, soothing dressings. Pastes should be stored & supplied in containers made of materials which do not allow absorption or diffusion of content.
Gel Gels are usually transparent or translucent,non -greasy semi-solid preparations. Gels are applied to the skin or certain mucous membranes for protective, therapeutic, or prophylactic purposes. These are also used for lubricating catheters, surgical gloves & rectal thermometer.
New drug delivery system With the advancement of pharmaceutical sciences, a new concept have evolved various modern dosage forms & methods of their administration. Some of the modern dosage forms are Implants Films & strips Liposome drug carriers Controlled drug delivery modules Erythrocytes Nanoparticles prodrugs
Implants These are hypodermic tablets are placed under the skin by a minor surgery in order to release drugs over prolonged periods of time. Now the magnetically controlled implants have been developed. These implants are useful in hormone therapy.
Films & strips These are meant for topical application for slow release of drug over predetermined period of time. Films & strips are more popular these days. They are sub categorized in to following types namely as Zero order release films Buccal strips Spray bandages
Liposome drug carriers Liposomes are defined as the nanosized vesicular structures consisting of an aqueous core surrounded with phospholipid layers These can transport both hydrophilic & hydrophobic drugs.
Controlled drug delivery modules These are the device which are formed by embedding the drug within a polymeric matrix so that it gets released slowly to the body over a long period of time. It will formed drug – polymer complex & may be formulated in to tablet, capsule or any other suitable formulation. The drugs is released from these modules by diffusion, osmosis or chemical reactions. These are applied to skin, implanted subcutaneously or inserted into various body cavities.
Erythrocytes Erythrocytes are tried in order to achieve controlled release of drugs. It can allow a drug to circulate in the body for long period of time which help slow release of the drugs in to serum. Released erythrocytes are prepared by putting them in to a hypotonic medium. So that they can easily swollen. The aqueous solutions of the drug is added to the medium so that drugs gets in to erythrocytes through open pores. When isotonicity is adjusted the erythrocytes shrink, thus encapsulating the drug with in them. These erythrocytes may be suspended in normal saline solutions for preparing injections.