Pharmaceutical Dosage Forms PDF

Pharmaceutic al Dosage Forms PDF Dr. Ahmed Rashed TYPES OF DOSAGE FORMS: Definition: Are the forms by which drug molecules are delivered to sites of action within the body. The need for dosage forms: 1-Accurate dose. 2-Protection e.g. coated tablets, sealed ampoules. 3-Protection fro...

Pharmaceutic al Dosage Forms PDF Dr. Ahmed Rashed TYPES OF DOSAGE FORMS: Definition: Are the forms by which drug molecules are delivered to sites of action within the body. The need for dosage forms: 1-Accurate dose. 2-Protection e.g. coated tablets, sealed ampoules. 3-Protection from gastric juice. 4-Masking taste and odor. 5-Placement of drugs within body tissues. TYPES OF DOSAGE FORMS: 6-Sustained release medication. 7-Controlled release medication. 8-Optimal drug action. 9-Insertion of drugs into body cavities (rectal, vaginal) 10-Use of desired vehicle for insoluble drugs. They are classified according to: A – Route of administration B – Physical form 1. Oral 1. Solid 2. Topical 2. Semisolid 3. Rectal 3. liquid 4. Parenteral 5. Vaginal 6. Inhaled 7. Ophthalmic 8. Otic Choice of dosage form depend on: 1.Type of patient 2.Type of drug 3.Type of disease ORAL DOSAGE FORMS: 1-Tablet: A tablet is a hard, compressed medication in round, oval or square shape. Solid dosage form containing unit dose of one or more medicament. ORAL DOSAGE FORMS: 1-Tablet: Molded Tablets Compressed tablets Multiple Compressed tablets Sugar-Coated Tablets Film Coated Tablets Gelatin Coated Tablets Enteric Coated Tablets Buccal or Sublingual Tablets Chewable Tablets Effervescent Tablets Tablet s Molded Tablets Compressed tablets Multiple Compressed tablets Tablets Sugar-Coated Tablets Film Coated Tablets Gelatin Coated Tablets Tablets Enteric Coated Tablets Sublingual Tablets Chewable Tablets Effervescent Tablets Modified-Release Dosage Forms The pattern of drug release from modified-release (MR) dosage forms is deliberately changed from that of a conventional (immediate-release) dosage formulation to achieve a desired therapeutic objective or better patient compliance. Types of MR drug products include delayed release (e.g., enteric coated) and extended release. Modified-Release Dosage Forms 1. Extended Release Sustained Release (SR) Controlled Release (CR) Long Acting (LA) 2. Delayed Release ORAL DOSAGE FORMS: 1-Tablet: Prepared by 1.mold method 2.compression method 2. Compressed tablet manufacturing The classification of manufacturing methods wet granulation: suitable for drugs that are stable to moisture and heat dry granulation: suitable for drugs that are sensitive to moisture and heat (direct compression) powder compression : suitable for drugs that are sensitive to moisture and heat, fill material possessing, good flowability and compressibility crystal compression ： suitable for drugs with proper crystal form and good flowability tablet compression machine ORAL DOSAGE FORMS: 1-Tablet: The excipients include: 1. DILUENTS 2. BINDERS 3. DISINTEGRANTS 4. LUBRICANTS ORAL DOSAGE FORMS: 1-Tablet: The excipients include: 1. DILUENTS Diluents increase the volume to a formulation to prepare tablets of the desired size. Widely used fillers are lactose, dextrin, microcrystalline cellulose starch, pregelatinized starch, powdered sucrose, and calcium phosphate. ORAL DOSAGE FORMS: 1-Tablet: The excipients include: 2. BINDERS Binders promote the adhesion of particles of the formulation. Such adhesion enables preparation of granules and maintains the integrity of the final tablet. Commonly used binding agents include: water, ethanol, starch, gelatin and sugars (sucrose, glucose, dextrose, and lactose). ORAL DOSAGE FORMS: 1-Tablet: The excipients include: 3. DISINTEGRANTS The breakup of the tablets to smaller particles is important for dissolution of the drug and subsequent bioavailability. Disintegrators promote such breakup. To rupture or breakup of tablets, disintegrating agents must swell or expand on exposure to aqueous solution. Thus, the most effective disintegrating agents in most tablet systems are those with the highest water uptake property. In general, the more hydrophilic, the better disintegrating agents are therefore highly hydrophilic. ORAL DOSAGE FORMS: 1-Tablet: The excipients include: 4. LUBRICANTS Lubricant is a substance capable of reducing or preventing friction, heat, and wear when introduced as a film between solid surfaces. It works by coating on the surface of particles, and thus preventing adhesion of the tablet material to the dies and punches.Commonly used lubricants include: talc, magnesium stearat, calcium stearate ,stearic acid, hydrogenated vegetable oils and PEG. 1-Tablet: A coating may be applied to: 1-hide the taste of the tablet's components. 2-make the tablet smoother and easier to swallow. 3-make it more resistant to the environment. 4-extending its shelf life. 2-BUCCAL AND SUBLINGUAL TABLET: Sublingual and buccal medications are administered by placing them in the mouth, either under the tongue (sublingual) or between the gum and the cheek(buccal). The medications dissolve rapidly and are absorbed through the mucous membranes of the mouth, where they enter in to the blood stream. 2-BUCCAL AND SUBLINGUAL TABLET: Avoid the acid and enzymatic environment of the stomach and the drug metabolizing enzymes of the liver. Examples of drugs administered by this route: e.g. vasodilators, steroidal hormones. 3. Oral thin film (OTF) Oral thin films are loaded with active substances. The Thin films are taken orally and dissolve immediately in the mouth or are applied to the mucosa. For transmucosal films, the active substance enters the bloodstream directly via the oral mucosa, without having to first pass through the gastrointestinal tract. 3. Oral thin film (OTF) The advantages of OTFs  For patients: 1. easy application, safe, reliable, precise and pain-free application 2. can be taken without extra water 3. easier to treat children, as well as older patients and patients requiring complex care 4. ideal for patients who have difficulty swallowing  For pharmaceutical companies: 1. avoidance of the first-pass effect 2. improved bioavailability 3. potentially requires lower amounts of active substances than tablets or solutions 4. controlled application of the required dose 5. improved compliance on the part of patients 4-EFFERVESCENT TABLET: Effervescent tablets are un coated tablets that generally contain acid substances (citric and tartaric acids) and carbonates or bicarbonates and which react rapidly in the presence of water by releasing carbon dioxide. 4-EFFERVESCENT TABLET: They are intended to be dissolved or dispersed in water before use providing: A- Very rapid tablet dispersion and dissolution. B- pleasant tasting carbonated drink. 5-CHEWABLE TABLET: They are tablets that chewed prior to swallowing. They are designed for administration to children e.g. vitamin products. 6-CAPSULE: A capsule is a medication in a gelatin container. Advantages : mask the unpleasant taste of its contents. 6-CAPSULE: The two main types of capsules are: 1-Hard- gelatin capsules, which are normally used for dry, powdered ingredients. 2-Soft- gelatin capsules, primarily used for oils and for active ingredients that are dissolved or suspended in oil.  7-LOZENGE: It is a solid preparation consisting of sugar and gum, the latter giving strength and cohesiveness to the lozenge and facilitating slow release of the medicament. It is used to medicate the mouth and throat for the slow administration of indigestion or cough remedies. 8-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. 9-DENTAL CONES: A tablet form intended to be placed in the empty socket following a tooth extraction, for preventing the local multiplication of pathogenic bacteria associated with tooth extractions. The cones may contain an antibiotic or antiseptic. 10-GRANULES: They are consisting of solid, dry aggregates of powder particles often supplied in single dose sachets. They are irregular shape particle which are made to improve flow property of powder. 10-GRANULES: Some granules are placed on the tongue and swallowed with water, others are intended to be dissolved in water before taking. Effervescent granules evolve carbon dioxide when added to water. 11-POWDERS: Solid dosage forms, intimate mixtures of dry finely divided drug or chemicals intended for internal or external use. The mixed powders may be stored in dry form and mixture prepared by the pharmacist when required for dispensing, by suspending the powders in the appropriate vehicle. 11-POWDERS: Bulk Powders are multi dose preparations consisting of solid, loose, dry particles of varying degrees of fineness. Contain one or more active ingredients, with or without excipients and, if necessary, coloring matter and flavoring substances. Usually contain non-potent medicaments such as antacids since the patient measures a dose by volume using a 5 ml medicine spoon. The powder is then usually dispersed in water or , in the case of effervescent powders, dissolved before taking. 12-LIQUID PREPARATIONS: a- Oral solution: Oral solutions are clear Liquid preparations for oral use containing one or more active ingredients dissolved in a suitable vehicle. 12-LIQUID PREPARATIONS: b- Oral emulsion: Oral emulsions are stabilized oil-in-water dispersions, either or both phases of which may contain dissolved solids either oil is dispersed in finely divided form in water or vice versa 12-LIQUID PREPARATIONS: c- Oral suspension: Liquid preparations for oral use containing one or more active ingredients suspended in a suitable vehicle. may show a sediment which is readily dispersed on shaking to give a uniform suspension which remains sufficiently stable to enable the correct dose to be delivered 12-LIQUID PREPARATIONS: d-Syrup: It is a concentrated aqueous solution of a sugar, usually sucrose to which medicaments are added. Flavored syrups are a convenient form of masking disagreeable tastes. 12-LIQUID PREPARATIONS: e- Elixir: It is pleasantly flavored clear liquid oral preparation of potent drugs. The vehicle may contain a high proportion of ethanol or sucrose together with antimicrobial preservatives which confers the stability of the preparation. 12-LIQUID PREPARATIONS: f- Oral Drops: Oral drops are Liquid preparations for oral use that are intended to be administered in small volumes with the aid of a suitable measuring device. They may be solutions, suspensions or emulsions 12-LIQUID PREPARATIONS g-Gargles: They are aqueous solutions used in the prevention or treatment of throat infections. Usually they are prepared in a concentrated solution with directions for the patient to dilute with warm water before use. 12-LIQUID PREPARATIONS (CONT.): h-Mouthwashes: These are similar to gargles but are used for oral hygiene and to treat infections of the mouth. TOPICAL DOSAGE FORMS: 1-Ointments: Ointments are semi- solid, greasy preparations for application to the skin, rectum or nasal mucosa. The base is usually anhydrous and immiscible with skin secretions. Ointments may be used as emollients or to apply suspended or dissolved medicaments to the skin. TOPICAL DOSAGE FORMS (CONT.): 2-Creams: Creams are semi-solid emulsions, that is mixtures of oil and water. TOPICAL DOSAGE FORMS (CONT.): 2-Creams: They are divided into two types: A-oil-in- water (O/W) creams: which are composed of small droplets of oil dispersed in a continuous aqueous phase. Oil-in- water creams are more comfortable and cosmetically acceptable as they are less greasy and more easily washed off using water. TOPICAL DOSAGE FORMS (CONT.): 2-Creams: B-water-in- oil (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 but many drugs which are incorporated into creams are hydrophobic and will be released more readily from a water in-oil cream than an oil-in-water cream. TOPICAL DOSAGE FORMS (CONT.): 3- Gels (Jellies): Gels are semi –solid system in which a liquid phase is consisting of natural or synthetic gum having a high degree of physical or chemical cross- linking. They are used for medication and lubrication. TOPICAL DOSAGE FORMS 4-Dusting powders: These are free flowing very fine powders for external use. Not for use on open wounds unless the powders are sterilized. TOPICAL DOSAGE FORMS (CONT.): 5-Lotions: These are fluid preparations(aqueous)for external application without friction either dabbed on the skin or applied on a suitable dressing and covered with a waterproof dressing to reduce evaporation. TOPICAL DOSAGE FORMS (CONT.): 6-Pressurized dispensers (aerosol sprays): Several different types of pharmaceutical product may be packaged in pressurized dispensers, known as aerosols. Surface sprays produce droplets of 100 µm diameter or greater. May be used as surface disinfectants, wound or burn dressing, relieve irritation of bites. Spray-on dusting powders are also available from pressurized containers. RECTAL DOSAGE FORMS: 1-Suppository: It is a small semi-solid medicated mass, usually cone-shaped, that is inserted either into the rectum(rectal suppository),vagina(vaginal suppository or pessaries)where it melts at body temperature. RECTAL DOSAGE FORMS (CONT.): 2-Enema: An enema is the procedure of introducing liquids into the rectum and colon via the anus. VAGINAL DOSAGE FORMS: Pessary: Pessaries are solid/semi-solid medicated preparations designed for insertion into the vagina where they melt or dissolve. There are three types: A- Moulded pessaries : they are cone shaped and prepared in a similar way to moulded suppositories. VAGINAL DOSAGE FORMS: Pessary: B- Compressed pessaries : made in a variety of shapes and are prepared by compression in a similar manner to oral tablets. C-Vaginal capsules: are similar to soft gelatin oral differing only in size and shape. PARENTERAL DOSAGE FORMS: An injection is an infusion method of putting liquid into the body, usually with a hollow needle and a syringe which is pierced through the skin to a sufficient depth for the material to be forced into the body. PARENTERAL DOSAGE FORMS: There are several methods of injection, including: 1-An intravenous injection ( IV ): It is a liquid administered directly into the blood stream via a vein. It is advantageous when a rapid onset of action is needed. PARENTERAL DOSAGE FORMS (CONT.): 2-Intramuscular injection (IM): It is the injection of a substance directly into a muscle. Many vaccines are administered intramuscularly. Depending on the chemical properties of the drug, the medication may either be absorbed fairly quickly or more gradually. Injection fibrosis is a complication that may occur if the injections are delivered with great frequency or with improper technique.  PARENTERAL DOSAGE FORMS (CONT.): 3-Subcutaneous injection (SC): Subcutaneous injections are given by injecting a fluid into the sub-cutis, the layer of skin directly below the dermis and epidermis. Subcutaneous injections are highly effective in administering vaccines and such medications as insulin. PARENTERAL DOSAGE FORMS (CONT.): 4- Intradermal injection (ID): The most common sites used are the inner surface of the forearm and the upper back, under the scapula. An injection site must be free from lesions, rashes, moles, hair or scars The ID injection route has the longest absorption time of all parenteral routes. These types of injections are used for sensitivity tests  INHALED DOSAGE FORMS: 1-Inhaler : Inhalers are solutions, suspensions or emulsion of drugs in a mixture of inert propellants held under pressure in an aerosol dispenser. Release of a dose of the medicament in the form of droplets of 50 µm diameter or less from the container through a spring-loaded valve incorporating a metering device. The patient then inhales the released drug through a mouth piece. INHALED DOSAGE FORMS: 1-Inhaler : In some types, the valve is actuated by finger pressure, in other types the valve is actuated by the patient breathing in through the mouth piece. It is commonly used to treat asthma and other respiratory problems. INHALED DOSAGE FORMS (CONT.): 2-Nebulizer or (atomizer): A nebulizer is a device used to administer medication to people in forms of a liquid mist to the air ways. It is commonly used in treating asthma, and other respiratory diseases. It pumps air or oxygen through a liquid medicine to turn it into a vapor, which is then inhaled by the patient. INHALED DOSAGE FORMS (CONT.): 2-Nebulizer or (atomizer): As a general rule, doctors generally prefer to prescribe inhalers for their patients, because: 1-These are cheaper 2-more portable 3-carry less risk of side effects. OPHTHALMIC DOSAGE FORMS: 1-Eye drops: Eye drops are saline- containing drops used as a vehicle to administer medication in the eye. Depending on the condition being treated, they may contain steroids, antihistamines or topical anesthetics. Eye drops sometimes do not have medications in them and are only lubricating and tear- replacing solutions. OPHTHALMIC DOSAGE FORMS: 2-Ophthalmic ointment & gel: These are sterile semi-solid Preparations intended for application To the conjunctiva or eyelid margin. OTIC DOSAGE FORMS: Ear drops: Ear drops are solutions, suspensions or emulsions of drugs that are instilled into the ear with a dropper. It is used to treat or prevent ear infections, especially infections of the outer ear and ear canal. NASAL DOSAGE FORMS: Nasal Drops and Sprays: 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. NASAL DOSAGE FORMS: Nasal Drops and Sprays: Alternatively the drug may be absorbed through the nasal mucosa to exert a systemic effect. The use of oily nasal drops should be avoided because of possible damage to the cilia of the nasal mucosa. 84