Dosage Form and Drug Delivery Systems PDF

MODULE 5 DOSAGE FORM AND DRUG DELIVERY SYSTEMS LECTURER: Mr. Jemar Wilian N. Labausa PACOP REVIEW - an agent intended for use in the diagnosis, treatment, mitigation , cure and prevention DRUGS of diseases in man or in animals the component which produces the pharmacological activity - inactive i...

MODULE 5 DOSAGE FORM AND DRUG DELIVERY SYSTEMS LECTURER: Mr. Jemar Wilian N. Labausa PACOP REVIEW - an agent intended for use in the diagnosis, treatment, mitigation , cure and prevention DRUGS of diseases in man or in animals the component which produces the pharmacological activity - inactive ingredient present in a dosage EXCIPIENT form vehicle, suspending agents, lubricants, binders finished dosage form that contains the DRUG active ingredient, generally, but NOT PRODUCT necessarily, in association with one or more other ingredients Dosage Form Drug Delivery System - formulation containing a specific quantity of active ingredient(s) in combination with one or more excipients - It provides mechanism for the safe and convenient delivery of the drugs - Concealment of offensive taste - Protection from destructive influence of the environment - means of administering drugs as formulated preparations - formulations which provide a therapeutic amount of drug to the proper site in the body promptly and maintain the desired drug concentration products that allow for the uniform release or targeting of drugs into the body New Chemical Entity Organic Synthesis Molecular Modification Isolation from Plants Pre-Clinical Studies Chemistry Physical Properties Biological Pre-formulation Investigational New Drug Clinical Trials Phase 1 Phase 2 Phase 3 Pre-Clinical Studies (continued) New Drug Applicatio n (NDA) Long term animal toxicity Product Formulation Manufacturing Control Package and Label design Postmarketing (Phase 4) New Molecular Entity (NME) - Defined by the FDA as an active ingredient that has never before been marketed in the US. LEAD COMPOUND • A prototype chemical compound that has a fundamental desired biologic or pharmacologic activity. GOAL DRUG Produces the specifically the desired effect Administered by the most desired route(Generally orally) Minimal dosage and dosage frequency Has optimal onset and duration of activity Easily produced at low cost PRODRUG A compound that requires metabolic biotransformation after administration to produce the desired pharmacologically active compound. Orphan disease is defined as a rare disease or condition that affects fewer than 200,000 people in the United States (chronic lymphocytic leukemia, Gaucher disease, cystic fibrosis, and conditions related to AIDS) Orphan drug- The FDA provides support grants to conduct clinical trials on safety and effectiveness. TREATMENT IND Permits the use of an investigational drug in the treatment of patients not enrolled in the clinical study but who have a serious or immediately life threatening disease for which there is no satisfactory alternative therapy PLACEBO Dosage form without containing any medication. DRUG PRODUCT RECALL Class I – cause serious adverse effects or death Class II – cause temporary or medically reversible adverse health consequences Class III – not likely to cause adverse health consequences 1.) In Vitro Test – Initial bioassay that takes place outside the organism, in an artificial environment such as a laboratory where drug activity is tested on isolated tissues, cells, or enzymes. 2.) In Vivo Test- Subsequent bioassay by biological experiment or technique carried out within a living organism Papyrus Ebers - Most famous surviving memorials of early drugs with more than 800 formulas or prescriptions Types of Dosage form Routes of Administration Oral Topical Rectal Parenteral Vaginal Inhaled Ophthalmic Otic Physical Form Solid Semi-solid Liquid Gas Solid Dosage Form: Powder and Granules A. Powders Mixture of finely divided drugs or chemicals in dry form which can be used internally or externally Comminution Process -- TPLM 1.Trituration - mortar and pestle (GRINDING) Types of mortar and pestle a.) Glass (SOS) b.) Wedgewood – For Crystalline solid c.) Porcelain– soft aggregates/crystals 2. Pulverization by intervention E.g. Camphor + _________, I2 crystals + _________ with the use of volatile solvent for gummy like particles (like camphor) 3. Levigation E.g. Mineral oil, glycerin - with the use of non-volatile solvent - Form a paste through the addition of non-solvent to a soluble material - Levigating agent- do not dissolve the active ingredient 4. Milling with the use of rotary cutter: hammer: roller mills Blending of Powders 1. Spatulation use of spatula on a pill tile or sheet of paper 2. Sifting powders are mixed by passing them in sifters resulting to a light, fluffy product 3. Geometric dilution 1:1 Ratio 4. Trituration Mortar and pestle (grinding action) Aka 1:10 dilution (10%) 5. Tumbling process of mixing powders in a large container rotated by a motor Types of Powder: Bulk powder • Large quantities • non potent powders) Divided Powder • Aka “chartulae” • Potent substances -individualized doses paper Tabs Dentifrices Oral powders Dusting powders Insufflation Triturations Aerosol Powders Douche Powders Papers for Divided Doses 1.) Glassine 2.) Waxed 3.) Vegetable parchment 4.) Bond Classification of powders based on particle size: USP Standards for Powders of Animal and Vegetable drugs FINENESS SIEVE SIZE All particles that pass thru SIZE UNIT % of particles passed. Very coarse #8 236mm nmt 20% thru #60 Coarse #20 850um nmt 40% thru #60 Moderately coarse #40 425um nmt 40% thru #80 Fine #60 250um nmt 40% thru #100 Very fine All passed #80 180um No limit to greater fineness USP Standards for Powders for Chemicals FINENESS Coarse Moderately coarse Fine Very fine SIEVE SIZE All particles that pass thru SIZE UNIT % of particles passed. #20 #40 850um 425um nmt 60% thru sieve#40 nmt 60% thru sieve #60 #80 #120 180um 125um no limit to fineness no limit to greater fineness B. Granules > are prepared agglomerates of smaller particles of powder Ø passed through no. 4-12 sieves For flowability for tableting Method of Preparation: 1.) Dry granulation 2.) Wet granulation REVIEW 1. A finished dosage form ready for marketing. 2. Mortar and pestle used for suspension, solution and ointment 3. Phase 4 Clinical Trial is aka _____. 4. A CHEMICAL powder that passes through sieve #80. 5. A tablet granulation resulting into poorly formed tablets. 6. A thin semi-opaque paper 7. Principle of tumbling 8. Large scale comminution process. 9. AKA 1;1 dilution. 10. Give atleast 1 example of levigating agent. 11. Anti-cavity powders. 12. AKA chartula 13. A drug with desired effect and desired route. 14. A mortar and pestle used for soft aggregates. 15. Phase 3 clinical trials is for __ and __. 16. Latest edition of USP/NF as of November 2018. 17. A substance that will absorb moisture then liquify. 18. This is blending of powders for fluffy products. 19. Comminution process for gummy-like particles. 20. AKA 1:10 dilution PACOP BREAK 1. Automatic device for selfinjecting Valium (diazepam) (tablet and injection solution) 2. Dose of magnesia magma as a laxative 3. What is the ACTIVE INGREDIENT in polymagma? 4. Selsun blue is used as ______. 5. Ideal container for dusting powder Effervescent Powders citric acid monohydrate and tartaric acid used in the ratio of 1:2 • Sodium bicarbonate reacts with both of the acids to produce CO2 • Citric acid alone – sticky Tartaric acid alone – friable and crumble Capsules • are solid dosage forms in which medicinal agents and/or inert substances are enclosed in a small gelatin shell • Gelatin is obtained by the partial hydrolysis of collagen obtained from the skin, white connective tissues and bones of animals Type A Type B Hard gelatin capsules (12-16 OR 13-15 % MC) Soft gelatin capsule (5-8% OR 6-10% MC) • - made from a mixture of gelatin, colorants & opacifying agents • - Storage: tightly closed glass containers, protected from dust, extremes of humidity and temperature • Prepared by pin method • made from gelatin shells with glycerin or sorbitol to render it elastic or plastic-like • used to contain liquids, suspensions, pastes, dry powders or pellets • prepared by the plate process or rotary die CAPSULE SIZES ESTIMATED (mL) EASIER VERSION (mL) 000 1.40 1.4 00 0.95 1.0 0 0.68 0.7 1 0.5 0.5 2 0.37 0.4 3 0.30 0.3 4 0.21 0.2 5 0.13 0.1 TABLETS • are solid dosage forms usually prepared with the aid of suitable pharmaceutical excipients • are primarily prepared by compression, with a limited number prepared by molding Advantages - Low manufacturing cost, easy to package and ship - Precision and low content variability - Easy to swallow - Most stable of all oral dosage forms Disadvantages - Some drugs are incompressible - Some drugs are sensitive to humidity and air DRY GRANULATION WET GRANULATION Methods of Tablet Manufacture FLUID BED PROCESSING DIRECT COMPRESSION - Classical COMPRESSED TABLETS - No special coating MULTIPLE - Layered tablets COMPRESSED - More than one compression - Meant to be chewed and subsequently swallowed CHEWABLE - For children, elderly, and TABLETS patients who cannot swallow BUCCAL - designed to be absorbed in the buccal cavity SUBLINGUAL EFFERVESCENT - designed to be absorbed under the tongue - UTILIZES SUPERDISINTEGRANTS(3MINS) - release carbon dioxide when dissolved in water - mask offensive taste SUGAR COATED - disadvantage: bulky FILM COATED ENTERIC COATED - less bulky, less time consuming and more durable - designed to dissolve in alkaline pH to release medication in the small intestine Rapidly Disintegrating Tablets (RDTs) Immediate Release Extended Release Repeat Action Sustained Release Delayed Release Vaginal Tablets Targeted Release 1.) lozenges(troches or pastilles) - disc shape, intended to dissolve or disintegrate slowly in the mouth 2.) Hypodermic tablets - used by physician to create parenteral products 3.) Pellets - small sterile df containing a concenctration of drug for subcutaneous implantation 4.) Cataplasm (poultices) - a soft moist mass of meals, herb, seed etc. usually applied hot in clothes. 5.) Plasters - solid/semisolid adhesive masses spread on a backing paper, fabric, moleskin or plastic to provide prolonged contact at the site 6. Transdermal patch - medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream. 9. Pills- are small round solid dosage forms containing medicinal agents and intended to be administered orally 10. Bolus- large, long tablet intended for administration to animals 7.) Dressing – used for cover or protection: resembling ointment 8. Lollipops- a sugar based lozenges on stick REVIEW 1. A soft moist mass of meals, herb, seed etc. usually applied hot in clothes. 2. mL in capacity of Capsule No.4 3. Moisture content of HGC. 4. AKA sodium starch glycollate 5. Preservative in HGC 6. A tablet prolonging the effect of the drug 7. Other name of fisherman’s tablet 8. Shellac, CAP and PAP are used for ______ coating tablets. 9. A type of TDDS with drug reservoir 10. Method of preparing HGC. Transdermal administration Electroporation is a TDDS enhanced by the application of short, high-voltage electric pulses to create aqueous pores in the lipid bilayer of skin and thereby facilitate drug diffusion. Iontophoresis is a TDDS enhanced by the use of applied electric current to facilitate drug diffusion through the skin. Phonophoresis is a TDDS enhanced by the application of low-frequency ultrasound to facilitate drug diffusion through the skin. High velocity powder particles A transdermal drug delivery system using supersonic shock waves of helium gas to enhance drug diffusion through the skin SUPPOSITORIES • Are solid dosage forms intended for insertion into body orifices where they melt, soften, or dissolve and exert local or systemic effects. • useful in infants, debilitated or comatose patients, patients who vomit, who have nausea or gastrointestinal disturbances TYPES OF SUPPOSITORIES RECTAL VAGINAL URETHRAL Criteria for Satisfactory Suppository Base: 1. Should be inert, nonirritating and nonsensitizing 2. Should be firm and should not melt at room temperature 3. Should dissolve rapidly in the cavity fluid (have narrow or sharp melting range) Suppository Bases: 1. Fatty / Oleaginous Bases 2. Water-Soluble and WaterMiscible Bases 3. Miscellaneous Bases •Fattibase, Wecobee bases, Witepsol base, Cocoa butter •Cocoa butter •good base for rectal suppository •melting just below body temperature and yet maintaining its solidity at usual room temperatures • glycerinated gelatin, PEG • are mixtures of oleaginous and water-soluble or water-miscible materials Methods of Preparing Suppository Bases: 1. Hand-rolling – Molding of suppository with the fingers 2. Compression – uses a mold 3. Fusion method – Commercial method of manufacture; uses heat PACOP BREAK 1. Bullet shaped capsules. 2. Ideal container for ointment. 3. Ointments that demonstrate some systemic effect 4. Type of extract used for ointment/ paste 5. Process of obtaining aromatic water by redistillation one or more times from the fresh delicate drugs. LIQUID DOSAGE FORM: SOLUTION - are liquid preparations, that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents Advantages: 1. Completely homogenous doses 2. Immediate availability for absorption and distribution 3. Provides a flexible dosage form -easy to swallow -can be used by any route of administration -easy to adjust dose 1. know the solubility characteristics of the drug or chemical General Rules in Preparing Solutions: 2. choose the proper solvent the salt form of the drug is used 3. when adding salt to syrup, dissolve salt in a few ml of water then add syrup to volume 4. If an alcoholic solution of a purely water-soluble drug is used, add the aq. solution to the alcoholic solution 1. Purified Water obtained by distillation, ion-exchange or reverse osmosis pH 5-7 used in prescription and manufactured finished products except parenteral and other sterile solutions 2. Water for Injection purified water that is FREE of pyrogens obtained by distillation or reverse osmosis - used for the preparation of parenteral solutions 3. Sterile Water for Injection -WFI that is sterilized & packaged in single-dose containers < 1L 4. Bacteriostatic Water for Injection SWI that contains 1 or more antimicrobial agents packaged in single or multiple-dose containers <30ml 5. Sterile Water for Inhalation Water purified by distillation or reverse osmosis & rendered sterile Not used for the preparation of parenteral solutions or other sterile dosage forms 6. Sterile Water for Irrigation WFI that is sterilized and suitably packaged Magnesium Citrate Oral Solution: - Colorless to slightly yellow, clear effervescent with sweet acidulous taste and lemon flavor. - Magnesium carbonate reacts with excess citric acid. - required to contain amount of Magnesium Citrate equivalent to between 1.55 and 1.99 of MgO in each 100mL NON- STERILE SOLUTIONS 1. SYRUPS - solutions containing high concentration of sucrose or other sugars examples: cherry syrup (47% cherry juice), cocoa syrup, orange syrup, raspberry syrup Syrup, NF (simple syrup) - nearly saturated aqueous solution of sucrose(85% w/v) - inherently stable and resistant to the growth of microorganisms when properly prepared and maintained solution with the aid of heat solution by agitation without the aid of heat percolation Methods of Preparation addition of sucrose to medicated or flavoured liquid reconstitution 2. ELIXIRS - are clear, pleasantly flavoured, sweetened hydroalcoholic solutions intended for oral use alcohol content: 5-40%, but most of the time, varies widely - Aromatic Elixir, NF 22% alc. Methods of Preparation SOLUTION WITH AGITATION ADMIXTURE OF 2 OR MORE LIQUID INGREDIENT Methods of Preparation CHEM RXN AMYL NITRITE SPIRIT DISTILLATION WHISKY- FROM CEREAL GRAINS 3. SPIRITS OR ESSENCES - are alcoholic or hydroalcoholic solutions of volatile substances - alcohol content: generally over 60% - uses: flavoring agents, vehicle -Storage: tight, light-resistant containers BRANDY – FROM GRAPES SIMPLE SOLN WITH AGITATION AROMATIC SPIRIT OF NH3, CMPD. ORANGE SPIRIT, CAMPHOR SPIRIT, CMPD. CARDAMON SPIRIT SOLN WITH MACERATION PEPPERMINT SPIRIT 4. TINCTURES - are alcoholic or hydroalcoholic solutions prepared from vegetable materials or from chemical substances - alcohol content: 15-80% -Preparation 1.Maceration– PROCESS M 2.Percolation- PROCESS P examples: Iodine Tincture; Opium Tincture 5. FLUIDEXTRACTS -are liquid preparations of vegetable drugs containing alcohol as solvent, preservative or both and so made that unless otherwise specified in an individual monograph, - each mL contains 1 g of the standard drug PREPN: PROCESS A, B/D, E 6. AROMATIC WATERS - are clear, aqueous solutions saturated with volatile oils or other aromatic or volatile substances also known as medicated waters uses: -flavored vehicle for water soluble drugs -aqueous phase in some emulsions or suspensions storage: tight, light-resistant bottles Methods of Preparation SOLN OF THE AROMATIC SUBS WITH OR WITHOUT USE OF DISPERSING AGENT DISTILLATION 7. GARGLES 8. MOUTHWASHES - are aqueous solutions used for treating the pharynx and nasopharynx by forcing air from the lungs through the gargle which is held in the throat - are aqueous solutions used for its deodorant, refreshing or antiseptic effect or for control of plaque 9. TOPICAL SOLUTIONS Intended for topical application to the skin or mucous membranes SPRAYS are aqueous or oleaginous solutions in the form of coarse droplets or finely divided solids to be applied topically, most usually to the nasopharyngeal tract or to the skin locally applied solutions that constrict pores and precipitate proteins ASTRINGENT Aluminium acetate, aluminium subacetate, and calcium hydroxide topical solutions - kill microorganisms when TOPICAL ANTI-INFECTIVE skin or mucus membranes applied to the Povidone-iodine, thimerosal, and hydrogen peroxide topical solutions PACOP BREAK 1. 2. 3. 4. 5. Dental preparation employed as a temporary covering for exposed pulp Approves the name of non-proprietary drugs. Arsenic + Mercuric I Medicinal substance + saccharin-like jelliew or pupl of fruits. USP statement of required purity. 10. Enemas - rectal solutions employed to evacuate the bowel (evacuation enemas), influence the general system by absorption (retention enemas) or to affect locally the site of disease - Sodium phosphates enema, hydrocortisone enema, aminophylline enema 11. Douches - are aqueous solutions directed against a part or into a cavity of the body - functions as a cleansing or antiseptic agent -are frequently dispensed in the form of a powder with the directions for dissolving in a specified quantity of warm water 12. Liniments aka: embrocations - are nonaqueous alcoholic or oleaginous solutions (or emulsions) of various medicinal substances intended to be rubbed on the skin - rubefacient, counterirritant or penetrating action - pyroxylin - AKA soluble gun cotton - produced though the action of nitric acid and sulfuric acid (3:1)on purified cotton 13.COLLODIONS - are liquid preparations composed of pyroxylin dissolved in a nonaqueous solvent mixture usually composed of alcohol and ether, with or without added medicinal substances flexible collodion - prepared by the addition of castor oil (3%) (for flexibility) and camphor (for water-proofing) (2%) to collodion Sterile Solution Nasal Solution -are aqueous solutions designed to be administered to the nasal passages in drops or sprays -vehicle used is usually water, but a co-solvent system may be used -may contain preservatives, buffer, antioxidant, surfactant -are intended for installation into the ear -vehicle: water or glycerin, or co-solvent Otic -may contain preservatives, buffer, Solution antioxidants, viscosity agents and surfactants -are sterile, pyrogen-free and particle-free Ophthalmic solutions, suitably compounded and packaged for Solution instillation into the eye -contains water, preservatives, buffer, antioxidants, tonicity adjustors, viscosity enhancers -pH = 7.4 or pH = 6.5 to 8.5 Irrigating Solution -sterile solutions used to wash or bathe surgical incisions, wounds or body tissues -should be labeled “Not for Injection” and “For Irrigation Only” -pH and isotonicity must be considered Parenteral Solutions -solutions injected through the skin or directly into the blood vessel, muscle, organ, or other tissues -must conform to strict requirements for microbiological impurity, particulate matter, and pyrogenicity -special manufacturing equipment and facilities are needed -pH and isotonicity must be given special consideration 1. Alternative when patient in unable to take medication by mouth Uses of Parenteral Administration 2. for drugs that are inactivated by gastric acid or first-pass effect 3. When drug action is required immediately 4. When drugs are to be delivered to an organ, lesion, a muscle, or a nerve Intravenous Intraarterial Subcutaneous Routes of Administration Intracardiac Intrathecal Intramuscular Intraarticular Intraspinal Intradermal Epidural REVIEW 1. It is produced though the action of nitric acid and sulfuric acid (3:1)on purified cotton 2. Aqueous solutions used for treating the pharynx 3. Dosage form wherein each mL contains 1 g of the standard drug. 4. mL capacity for IM. 5. WFI that is sterilized & packaged in singledose containers < 1L 6. AKA poultice 7. It contains mainly lauric acid. 8. AKA embrocations. 9. AKA pessaries. 10. Peppermint spirit is prepared through what method? 11. Scientific name of grapes. 12. Methods of preparing syrup. 13. Self preserving elixir contains how many percent of alcohol? 14. AKA medicated water 15. Alcohol content of Spirit 16. It is used for water proof ability of collodion 17. Specific gravity of simple syrup 18. Ipecac syrup is prepare by what method? 19. Methods of preaparing fluidextract 20. Subcutaneous is administer at what degree? PACOP BREAK 1. An agreement which prohibits the use of CFC 2. Content in mg of capsule no. 5? Capsule no. 000? 3. Percentage content of water for lanolin, 4. Wholly or nearly decolorized petrolatum 5. Characteristic ingredient in poultice. 6. AKA WAFERS 7. Components of whitfield ointment 8. Castellani’s paint contains _____ soln. 9. Clyster is what type of dosage form? 10. Magnesium Sulfate Injection is used for the treatment of _______. Suspension - liquid dosage forms containing finely divided drug particles distributed somewhat uniformly throughout a vehicle in which the drug exhibits a minimum degree of solubility - particles have diameters for the most part greater than 0.1 mcm - purposes for formulating a suspension: 1. Sustaining effect 2. Stability 3. Taste Properties of a good suspension: particle size of the suspensoid should remain fairly constant throughout long periods of undisturbed standing dispersed particles of the suspension should settle slowly and should be readily redispersed upon gentle shaking of the container the suspension should pour readily and evenly from its container 1. Comminution of the drug General Steps in Preparing Suspension 2. Wetting of powder – accomplished by levigation to displace air in the crevices of the particle to make the drug more penetrable by the dispersion medium 3. The suspending agent dispersed in the vehicle is added to the wetted powdered by geometric dilution. 4. The product is brought to final volume using the vehicle Suspending Agents - Increase viscosity - Inhibit agglomeration - Decrease the rate at which particles settle Methods of Preparing Suspension: Discipitation Method Precipitation Method EMULSIONS - are dispersed systems in which the dispersed phase is composed of small globules of a liquid distributed throughout a vehicle in which it is immiscible - Particle size 0.1 to 100 microns - Phases: - dispersed phase / internal phase /discontinuous phase - dispersion medium / external phase / continuous phase THEORIES IN EMULSION ORIENTED WEDGE THEORY - asssumes monomolecular layers of emulsifying agent curved around a droplet of internal phase of emulsion INTERFACIAL FILM/ PLASTIC FILM THEORY - places ea at the interface of oil and water surrounding the droplets of the internal phase as the thin layer of film adsorbed on the surface of the drops. - Purposes of Emulsions 1. 2. 3. 4. Increased drug stability Prolonged drug action Improved taste Improved appearance TYPES OF EMULSION 1. Oil-in-Water (o/w) - Oil is dispersed as droplets in an aqueous medium - Oral products and external, washable products 2. Water-in-Oil (w/o) -Water is dispersed as droplets in an oil or oleaginous medium -Used for external preparations when emollient, lubricating, or protective properties are desired 3. Multiple Emulsions (o/w/o or w/o/w) 4. Microemulsions - appear translucent or transparent and have droplet diameter in the nanometer size range 1. Emulsifier Factors that determine Emulsion Type: 2. Phase ratio 3. Order of mixing NATURAL gelatin, egg yolk, casein, acacia, tragacanth, pectin, cellulose derivatives, lecithin, alginates, chrondus, wool-fat, cholesterol Emulsifying agents FINELY DIVIDED SOLIDS bentonite, magnesium hydroxide, aluminum hydroxide, magnesium trisilicate, veegum SYNTHETIC anionic, cationic, non-ionic HLB Value Surfactant Application Range 0-3 Antifoaming agents 4-6 W/O emulsifying agents 7-9 Wetting agents 8-18 O/W emulsifying agents 13-15 10-18 Detergents Solubilizing agents • 4:2:1(OWE) • MIXING:EWO • 4:2:1 (OWE) • MIXING: EOW Wet gum (English) method Dry gum (Continental) method Methods of Preparation Bottle (Forbes Bottle Method) • 2:2:1 or 3:2:1 • (OWE) • Low viscosity and volatile substances Nascent Soap (In Situ Soap Method) • - during chemical reaction EA is produced • Calamine Liniment DILUTION TEST • O/W– CAN BE DILUTED IN WATER • W/O- CAN BE DILUTED WITH OIL CONDUCTIVITY TEST •O/W EMULSION CONDUCTS ELECTRICITY DYESOLUBILITY TEST •WATER SOLUBLE & LIPID SOLUBLE DYE INSTABILITY EMULSION SUSPENSION SEMISOLIDS Coalescence Creaming Cracking Phase Inversion Aggregation Syneresis Sedimentation Swelling Caking Imbibition Bleeding REVIEW 1. The only surfactant with anti-bacterial activity. 2. HLB Value range of detergents. 3. -4. Methods of preparing Suspension. 5. The only emulsion which is homegenous. 6. Spans can produce what type of emulsion. 7. When there is a decrease in the Viscosity, sedimentation rate will ________. 8. It is also known as dry gum method 9. Ratio of oil, water and emulsifying agent in Continental Method. 10. Emulsifying agent in Calamine Liniment. SEMISOLID DOSAGE FORM: OINTMENTS (AKA UNGUENTS, CHRISMA, OCCULENTUM) - are semisolid preparations intended for external application to the skin or mucous membranes Uses 1. Emollients – make the skin more pliable 2. Protective barriers 3. Vehicles – in which to incorporate medication Oleaginous bases Watersoluble bases Absorption bases Waterremovable bases 1. OLEAGINOUS - hydrocarbon bases - not water-washable, incorporation of water with some degree of difficulty PETROLATUM WHITE PETROLATUM YELLOW OINTMENT WHITE OINTMENT (USP) MINERAL OIL 2. ABSORPTION are not easily removed from the skin B. Hydrous type A. Anhydrous type those that permit the incorporation of aqueous solutions resulting in the formation of w/o emulsions HYDROPHILIC ANHYDROUS AQUAPHOR AQUABASE POLYSORB those that are w/o emulsions that permit the incorporation of additional quantities of aqueous solutions PETROLATUM USP LANOLIN COLD CREAM HYDROCREAM LANOLIN EUCERIN NIVEA CREAM 3. WATER-REMOVABLE BASES - are o/w emulsions resembling creams - easily washed from the skin, hence called “water-washable” DERMOVAN HYDROPHILIC OINTMENT USP, UNIBASE VANISHING CREAM 4. WATER-SOLUBLE BASES - do not contain oleaginous components - are completely water-washable, hence called “greaseless” PEG OINTMENT POLYBASE PG PEG Incorporation • MORTAR AND PESTLE, OINTMENT ROLLER MILLS • 1. Spatulation-- sulfur O 2. Pulverization by Intervention- camphor Fusion Method • PORCELAIN DISH, GLASS BEAKER, LARGE STEAM JACKETTED KETTLES • Ex: White Ointment CREAMS - are semisolid preparations containing one or more medicinal agents dissolved or dispersed in either a w/o emulsion or an o/w emulsion or in another type of waterwashable base ex. vanishing creams GELS are semisolid systems consisting of dispersions of small or large molecules in an aqueous liquid vehicle rendered jelly-like by the addition of a gelling-agent MILK is sometimes used for suspension in aqueous vehicles intended for oral MAGMA, which is often used to describe suspensions of inorganic acids such as clay in water. LOTION- are generally suspensions of solid materials in an aqueous vehicle. PASTES are semisolid preparations intended for application to the skin, and generally contain a larger proportion of solid material than ointments and therefore are stiffer Example: Zinc oxide paste/ Lassar’s Plain Zinc Paste GLYCEROGELATINS are plastic masses containing gelatin (15%), glycerin (40%), water (35%) and an added medicinal substance (10%) such as zinc oxide Ex. Zinc Gelatin boot Maceration is the process in which the solid ingredients are placed in a stoppered container with the whole of the solvent and allowed to stand for a period of at least three days, with frequent agitation. The mixture is strained and the marc pressed, and the combined liquids are clarified by filtration or by decantation after standing Percolation is where the active ingredients are extracted from a macerated drug mass in a narrow cone-shaped vessel open at both ends (percolator) through the passage of an extracting liquid called menstrum Digestion This is a form of maceration in which gentle heat is used during the process of extraction. Infusion is a dilute solution of the readily soluble constituents of crude drugs for a short period of time which either cold or boiling water is added Decoction extracts water-soluble and heat stable constituents from crude drugs by boiling in water for 15 minutes, cooling, straining and passing sufficient cold water through the drug to produce the required volume Drug Regulation and Control Federal Food, Drug and Cosmetics Act 1938 ◦ Additional standards were set DUE TO SULFANILAMIDE INCIDENT ◦ Requires filing of a NDA ◦ Assures products are safe for human use Durham-Humphrey Amendment 1952 ◦ Drug products were categorized into Rx and OTC ◦ Rx drugs may only be refilled upon consent of the prescriber ü “Rx Only” ü “Caution: Federal Law Prohibits Dispensing Without Prescription” ◦ Initiated by the 1960 tragedy ◦ Thalidomide as OTC (sedative and tranquilizer) ◦ Enacted to ensure greater degree of safety for approved drugs ◦ Requires filing for IND ◦ Drugs safety and effectiveness Kefauver – Harris Amendment Comprehensive Drug Abuse Prevention and Control Act of 1970 ◦ Control on drugs of abuse ◦ Led by DEA in DOJ ◦ Classified the controlled substances CLASSIFICATION OF DANGEROUS DRUGS I no accepted medical use, high potential for abuse All illegal under law Flunitrazepam Narcotics: Heroin Hallucinogens: LSD, Mescaline PCP, Psilocybin II accepted medical use, high potential for abuse – may lead to psycho or physical abuse No telephone prescription No refills Opiods: Morphine, Codeine Stimulants: Amphetamine BB (Amo, Pento, Seco) III medical use, less potential for abuse Prescription must be rewritten after 6 months or five refills Ketamine, Dronabinol, Anabolic steroids IV accepted medical use, low potential for abuse Prescription must be rewritten after 6 months or five refills Pentazocine BZD Phenobarbital V accepted medical use, low potential for abuse Diphenoxylate Dihydrocodeine Nonopioid prescription drugs