Pharmaceutical Dosage Forms & Drug Delivery Systems PDF

09/08/2022 Module 5 Review on Pharmaceutical Dosage Forms & Drug Delivery Systems Competency Number Level of difficulty of question s Manufacturing 29 K 6 C 6 Ap An S 12 2 2 E 1 Asst. Prof. Margarita M. Gutierrez, RPh, MHPEd, PhD College of Pharmacy University of the Philippines- Manila...

09/08/2022 Module 5 Review on Pharmaceutical Dosage Forms & Drug Delivery Systems Competency Number Level of difficulty of question s Manufacturing 29 K 6 C 6 Ap An S 12 2 2 E 1 Asst. Prof. Margarita M. Gutierrez, RPh, MHPEd, PhD College of Pharmacy University of the Philippines- Manila Pharmaceutical dosage forms Physical pharmacy Jurisprudence and ethics 29 6 6 12 2 2 1 25 5 5 10 2 2 1 17 3 3 6 2 1 2 Outline of Pharmaceutics Part I: Introduction Part II: Solid dosage forms  Part III: Liquid dosage forms  Part IV: Dispersed systems and Semisolid dosage forms  PART I: INTRODUCTION  Drug product Dosage Form Drug delivery system Drugs  An active ingredient, Therapeutic moiety an agent intended for use in the ◦ diagnosis ◦ mitigation ◦ treatment ◦ cure ◦ prevention  Drugs      mydriatics miotics emetics diuretics analgesics - - - dilate pupils - constrict pupils - induce vomiting - increase flow of urine - alleviate pain - - of diseases in man or in animals 1 09/08/2022 Drug  Excipient  the component which produces the pharmacological activity   Drug Product  finished dosage form that contains the active ingredient, generally, but NOT necessarily, in association with one or more other ingredients Aka Additives, pharmaceutical adjuncts or necessities inactive ingredient present in a dosage form vehicle, suspending agents, lubricants, binders Dosage Form  formulation containing a specific quantity of active ingredient(s) in combination with one or more excipients Dosage Form Drug Delivery System  It provides mechanism for the safe and convenient delivery of the drugs  means of administering drugs as formulated preparations  Concealment of offensive taste   Protection from destructive influence of the environment formulations which provide a therapeutic amount of drug to the proper site in the body promptly and maintain the desired drug concentration 2 09/08/2022 Drug Delivery System  products that allow for the uniform release or targeting of drugs into the body  encompass the drug formulation, interaction among drugs, formulation matrix, the container and the patient PART II: SOLID DOSAGE FORMS Powders and granules Capsules Tablets A. Powders  POWDERS & GRANULES mixture of finely divided drugs or chemicals in dry form which can be used internally or externally powders Comminution Process I. Comminution  II. Blending  III. Particle size determination 1.  Trituration • mortar and pestle • Aka 1:10 dilution (10%) 3 09/08/2022 & Types of mortar and pestle  a.) Glass – solution, suspension, and ointments (smooth) highly staining b.) Wedgewood-crystalline solid Comminution Process 2. Pulverization by intervention • with the use of volatile solvent • for gummy like particles (like camphor) -    c.) Porcelain - soft aggregates/ crystals  Eg. Camphor + Alcohol, I2 crystals + ether Comminution Process Comminution Process 3. Levigation 4. Milling • with the use of non-volatile, non-solvent • Form a paste through the addition of anon solvent levigating agent • with the use of rotary cutter • hammer • roller mills Levigating agent- do not dissolve the active ingredient Eg. Mineral oil, glycerine Blending of Powders 1. Spatulation • use of spatula on a pill tile or sheet of paper • Not for potent powders Blending of Powders 3. Geometric dilution • used when a potent substance is to be mixed with a large amount of diluent • 1:1 Ratio 4.Trituration Mortar and pestle (grinding action) Aka 1:10 dilution (10%) 4 09/08/2022 Blending of Powders Types Of Powder 5.Tumbling • process of mixing powders in a large container rotated by a motor  I. Bulk Bulk powders Powder  II. Divided Powder Bulk Powders Large quantities (non potent powders)  Dentrifices  - mild abrasive for teeth  Oral powders  - intended for oral  Dusting powders  - locally applied  Insufflation  - body cavities through the use of an insufflators *  mouth wash-topical II. Divided powders Papers for Divided Doses  Aka “chartulae”  1.) glassine  2.) vegetable -thin, semi opaque and moisture resistant parchment absorb moisture  3.) waxed  potent substances  -individualized doses paper Tabs  4.) bond -glazed, transparent, moisture resistant 80IFX -used for hygroscopic and deliquescent powders Sapsormaitueee -no moisture resisting properties, for pharmaceutical elegance 5 09/08/2022 USP Standards for Powders of Chemicals o Classification Based on particle size Coarse Sieve Limit (% passed through) number No. 20 nmt o 60% through No. 40 Moderately No. 40 nmt o 60% through No. 60 coarse Fine No. 80 No limit Very fine No. 120 no limit - ↑ St #ofsquare - opening openings per uch length The " - USP Standards for Powders of Animal & Vegetable Drugs Sieve number Limit (% passed through) Very coarse Passed through no. 8 nmt 20% through No. 60 Coarse No. 20 nmt 40% through No. 60 Moderately coarse No. 40 nmt 20% through No. 80 Fine No. 60 nmt 20% through No. 100 Very fine All process thru No. 80 no limit B. Granules  are prepared agglomerates of smaller particles of powder  passed through no. 4-12 sieves  for flowability for tableting Granules  Method of Preparation 1.) Dry granulation ↑ -> formed tablets poorly granule 2.) wet granulation -> I ] smg-gramulator poder liquid + met mass xm5% moisture content -> <- # sine Even 60-80 6 09/08/2022 CAPSULES Capsules  Gelatin are solid dosage forms in which medicinal agents and/or inert substances are enclosed in a small gelatin shell  is obtained by the partial hydrolysis of collagen obtained from the skin, white connective tissues and bones of animals Type A – acid hydrolysis Type B – alkali hydrolysis Base Capsule  the larger the numerical size the smaller the size smallest for human consumption = 5 animals  largest = 000 Largest size for human consumption = 0  ->  Capsule Sizes Powder capacity (mg) No. 5 No. 000 60-130 650-2000 1 in. 0.5 in. 000 00 0 1 2 3 4 5 7 09/08/2022 Hard Gelatin Capsules Soft Gelatin Capsules  -dry extemporaneous compounding - 13-16% moisture  -gelatin + polyhydric alcohol (glycerol C3O3 H10, soribtol  made from a mixture of gelatin, colorants & opacifying agents  - to render the capsule elastic or plastic like)  - increased to 6-10% moisture capacity sulfur dioxide - preservative Ti0e-oparifying agent Soft Gelatin Capsules   used to contain liquids, suspensions, pastes, dry powders or pellets prepared by the plate process or rotary Tablets   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 Tablets Advantages: Disadvantages: 1. low manufacturing cost, easy to package and ship 2. precision and low content variability 3. easy to swallow 4. most stable of all oral dosage forms 1. some drugs are incompressible 2. some drugs are sensitive to humidity and air 8 09/08/2022 Compressed tablet  A. dry granulation Types of Tablets -slugging ( big tablets) then granulate , heat labile, not for water - ball of mass screen  B. wet granulation  C. direct - Powder inherent compression compressibility Types of Tablets · ·DI: Nmt s0mins in · First Pass distilled HzD Effect A.1 Multiple-Compressed tablets mixed a Active inquedient · traether Types of Tablets Hardness:2-3 K9 DI:None 2. Chewable tablets A. Compressed tablets Hardness:4-10kg o meant to be chewed and subsequently swallowed for children, elderly, and patients who cannot swallow 3. Buccal tablets ◦ designed to be absorbed DI:4 hours in the buccal cavity 4.. Sublingual tablets ◦ designed to be absorbed under the tongue Hardness:2-3 kg Xylitol- sweetening agent used in the manufacture of sugar-free chewable tablets DI: Diment ofchoice:Mannitol, * 3 mins index glyomic NOT SUITABLE FOR DIABET X Types of Tablets Effervescence 5. Effervescent tablets  ◦ release carbon dioxide when dissolved in water  sodium bicarbonate (naHCO3) citric acid and tartaric acid 6 rati:1:1 6 sticky crumble CO2 Hardness:8-10Kg -> +H2O liberate CO2 (effervescent) – to increase palatability of the preparation  Citric acid alone sticky tablet Tartaric acid alone- crumbling or drying  -others- bubbles  mask bitter taste 9 09/08/2022 Other types of tablet  a.) RDTs ( rapidly disintegrating tablets)  b.) immediate release  c.) delayed release  d. )Extended release  e) sustained release  f.) Vaginal tablets  w1  repeat-action.Two-layer tablets may be prepared with one layer of drug for immediate release with the second layer designed to release drug later as either a second dose or in an extended-release manner.  Targeted release describes drug release directed towards isolating or concentrating a drug in a body region, tissue, or site for absorption or for drug action. + W ⑰ ⑩ B. Types of Coated tablets Types of Coated Tablets 2. Sugarcoated tablets 2. Film coated less bulky, less time consuming and more durable  mask offensive taste  disadvantage: bulky 3. Enteric-coated tablets ◦ designed to dissolve in alkaline pH to release medication in the small intestine  SOLID DOSAGE FORMS Solid Dosage Forms 1.) lozengestroches or pastilles  4. Pills- are small round solid dosage forms containing medicinal agents and intended to be administered orally  5. Lollipops- a sugar based lozenges on stick  6. Bolus-large, long tablet intended for administration to animals - discoid shaped solids - used by doctor for extemporaneous 2.) Hypodermic for parenteral solutions tablets -issue: None sterile environment 3.) Pellets -formed by compression from medicated mass intended to be implanted subcutaneously to release the medication over a long period time. 10 09/08/2022 SOLID DOSAGE FORMS 7. cataplasm (poultices) -moist mass of meal, herb, etc -applied hot in cloth 8. Plasters -solid/semisolid adhesive masses -spread upon a backing material (local) 9. Transdermal-administers drug in prolong period of time patch (systemic) 10. Band aid -Protective 11. Dressing -external application resembling ointments used as covering or protection TDDS  Electroporation short, high-voltage electric pulses  Iontophoresis electric current  Phonophoresis low-frequency ultrasound  high velocity powder particles supersonic shock waves of helium gas Suppositories  from “supponere”- administration under the body  are solid (semi solid) dosage forms intended for insertion into body orifices where they melt, soften, or dissolve and exert local or systemic effects SUPPOSITORIES Suppositories Useful in infants  debilitated or comatose patients  patients who vomit  who have nausea or gastrointestinal disturbances  11 09/08/2022 Types of supository: rectal vaginal urethral Other names Weight none pessaries Bougies 2g 5g M= 4g (longer) F= 2g Size 32mm none M= 140mm F= 70mm Shape Bullet/torpedo Oviform/ globular Penal like Only for adults Only for adults female Both Infants= ½ of Age differences size and weight both Gender Suppository Bases A. Fatty / Oleaginous Bases Fatty / Oleaginous Bases 1.cocoa butter (Theobroma cacao) 2. Wecobee- coconut oil ◦ is a form of triglyceride exsist in different crystalline form ( polymorphism)  Alpha form – melting point (20c)  Beta form- more stable form (solid at 32c, melting point 34.5c) 3. Witepsol ◦ Saturated fatty acid C12-C18 ◦ Lauric(C12) Glycerol monopalmitate 4. Hydrogenated fatty acid of vegetable oils Suppository Bases Preparation 2.Water-Soluble and Water-Miscible Bases 1. Hand-rolling   Precaution: moisten the tip of supp. w/ H2O to enhance lubrication and axoid mucosal irritation Glycerinated gelatin, PEG 3. Miscellaneous Bases ◦ are mixtures of oleaginous and water-soluble or water-miscible materials ◦ molding of suppository with the fingers 2. Compression ◦ uses a mold 3. Fusion method ◦ commercial method of manufacture; uses heat 12 09/08/2022 Advantages PART III: LIQUID DOSAGE FORMS 1. Completely homogenous doses 2. Immediate availability for absorption and distribution 3. Flexible dosage form    Solutions are liquid preparations, that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents easy to swallow easy to adjust dose can be used by any route of administration Solubility Very soluble Freely soluble Soluble Sparingly soluble Slightly soluble Very slightly soluble <1 1-10 10-30 30-100 100-1000 1000-10,000 Practically incoluble >10,000 13 09/08/2022 1. Water A. AQUEOUS SOLUTION  most commonly used solvent for drug solutions  the USP recognizes six types of water for the use & preparation of dosage forms 1. Purified Water, USP  obtained by distillation, ion-exchange, reverse osmosis or other suitable process  pH 5-7  used in preparation of aqueous dosage forms except parenteral products 2. Water for Injection, USP 3. Sterile Water for Injection, USP  purified water that is FREE of pyrogens  WFI that is sterilized & packaged in single-dose containers ≤ 1L  obtained by distillation or reverse osmosis  used for already sterilized and packaged medications  used for the manufacture of parenteral products that are to be sterilized after preparation 14 09/08/2022 5. Sterile Water for Inhalation, USP 4. Bacteriostatic Water for Injection, USP  SWFI that contains 1 or more antimicrobial agents (0.9% Benzyl Alcohol)  packaged in single or multiple-dose containers ≤ 30ml WFI that is sterilized and suitably packaged  must be labeled with: “For Irrigation Only, Not for Injection” Aromatic Waters  uses: ◦ flavored vehicle for water soluble drugs ◦ aqueous phase in some emulsions or suspensions  storage: tight, light-resistant bottles water purified by distillation or reverse osmosis & rendered sterile for inhalational use  not used for the preparation of parenteral solutions 2. Aromatic Waters 6. Sterile Water for Irrigation, USP    aka: Medicated Waters  are clear, aqueous solutions saturated with volatile oils or other aromatic or volatile substances 3. Syrups  solutions containing high concentration of sucrose or other sugars  examples: ◦ ◦ ◦ ◦ cherry syrup cocoa syrup orange syrup raspberry syrup 15 09/08/2022 Syrup, NF Syrup, NF  aka: simple syrup  low solvent capacity for water soluble drugs  nearly saturated aqueous solution of sucrose (85% w/v)  inherently stable and resistant to the growth of microorganisms when properly prepared and maintained Syrups- Method of preparation 1.) solution with the aid of heat  2.) solution by agitation w/o heat  3.) percolation (USP method)  4.) reconstitution   - rapid, 80-85c - heat labile, slower B. NON AQUEOUS SOLUTION -use of percolator -inc stability of syrups 5.) addition of sucrose to an already prepared - dry syrups, minimize flavoured/ medicated microbial liquid contamination Elixirs    are clear, pleasantly flavoured, sweetened hydroalcoholic solutions intended for oral use Spirits  aka: Essences  alcohol content: 5-40%, but most of the time, varies widely are alcoholic or hydroalcoholic solutions of volatile substances  alcohol content: generally over 60% Aromatic Elixir, NF  uses: flavoring agents, vehicle  Storage: tight, light-resistant containers ◦ 22% alcohol 16 09/08/2022 Tinctures Sample preparations  are alcoholic or hydroalcoholic solutions prepared from vegetable materials or from chemical substances  alcohol content: 15-80%  Tinctures of potent vegetable drugs essentially represent the activity of 10 g of the drug in each 100 mL of tincture  simple solution-Aromatic Ammonia Spirit, USP  Solution Spirit with maceration - Peppermint  Chemical reaction - Ethyl nitrite spirit  Distillation - brandy and whisky 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  Process A is a method of percolation that can be modified for fluidextracts that must be assayed.  Process D is used for preparing fluidextracts with boiling water as the menstruum, alcohol being added as preservative to the concentrated percolate  Sprays Astringents Local anti-infective solutions Topical Solutions  C. TOPICAL SOLUTIONS intended for topical application to the skin or mucous membranes   17 09/08/2022 Douches  are aqueous solutions directed against a part or into a cavity of the body Enemas     function as cleansing or antiseptic agents Mouthwashes  are aqueous solutions used for deodorant, refreshing or antiseptic effect or for control of plaque Astringents - rectal injection -employed to evacuate the bowel (evacuation enemas) -influence the general system by absorption or affect a local disease (retention enema) Gargles  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 Local Anti-Infective Solutions  locally applied solutions that constrict pores and precipitate proteins  kill microorganisms when applied to the skin or mucus membranes  aluminum acetate aluminum subacetate calcium hydroxide topical solution  povidone-iodine thimerosal hydrogen peroxide topical solution     18 09/08/2022 Hydrogen peroxide  The dilute solution which contains about 3% hydrogen peroxide liberates 10 times its volume of oxygen.  Alcohol Liniments  aka: embrocations  oleaginous solutions (or emulsions) of various medicinal substances intended to be rubbed on the skin  For massage 70%, it is a good anstiseptic for the skin and also for instruments.  50% ethanol is also used to prevent sweating in astringent and anhidrotic lotions.  25%, ethanol is employed for bathing the skin for the purpose of cooling and reducing fevers.  A 20-volume preparation of HPTS, on the other hand, contains 6% hydrogen peroxide. Pyroxilin  aka: soluble gun cotton  produced though the action of nitric acid and sulfuric acid on purified cotton  1 Nitric Acid: 3 Sulfuric Acid Alcoholic iniments  rubefacient, counterirritant or penetrating action Collodions  are liquid preparations composed of pyroxylin dissolved in a nonaqueous solvent mixture usually composed of 1 alcohol and 3 ether, with or without added medicinal substances 19 09/08/2022 Flexible Collodion prepared by the addition of  castor oil (for flexibility)  and camphor (for water-proofing) to collodion  Parts of the sprayer  actuator is the button the user presses to activate the valve assembly for emission of the product. The  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 Parts of the sprayer housing links the dip tube and the stem and actuator   dip tube formulation from the container to the valve  The spring holds the gasket in place and is the mechanism by which the actuator retracts MDI DPI   a dosage form that is packaged under pressure E. STERILE SOLUTIONS active ingredient is released upon activation of an appropriate valve system 20 09/08/2022 Nasal Solutions  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   are intended for instillation into the ear  vehicle: water or glycerin, or co-solvent  may contain preservatives, buffer, antioxidants, viscosity agents and surfactants may contain preservatives, buffer, antioxidant, surfactant Ophthalmic Solutions  are sterile, pyrogen-free and particle-free solutions, suitably compounded and packaged for instillation into the eye  contains water, preservatives, buffer, antioxidants, tonicity adjustors, viscosity enhancers  pH = 7.4 or pH = 6.5 to 8.5 Parenteral Solutions  Otic Solutions solutions injected through the skin or directly into the blood vessel, muscle, organ, or other tissues Irrigating Solutions  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  must conform to strict requirements for microbiological impurity, particulate matter, and pyrogenicity 21 09/08/2022 Parenteral Solutions  special manufacturing equipment and facilities are needed  pH and isotonicity must be given special consideration Parenteral Solutions - Uses 1. alternative when patient in unable to take medication by mouth 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 II. Routes of Drug Adminsitration            Parenteral intravenous Intraarterial intracardiac intramuscular subcutaneous intraarticular intradermal/intracutanenous Intrathecal intraspinal epidural http://www.leer-leren.com/wpcontent/uploads/2012/07/Like-a-boss.jpg 22 09/08/2022 http://www.leer-leren.com/wpcontent/uploads/2012/07/Like-a-boss.jpg http://www.leer-leren.com/wpcontent/uploads/2012/07/Like-a-boss.jpg 23 09/08/2022 F. DISPERSE SYSTEM 1. Suspensions  Types of suspension 1. Suspended Solution 2. Gel  3. Magma or milk  liquid dosage forms containing finely divided drug particles distributed somewhat uniformly throughout a vehicle in which the drug exhibits a minimum degree of solubility  Gels Properties of particles flocullated definition Deffloculated Loose aggregates of particles (granule like) Sedimentation rate faster Particles are separate entities (powder like) slower Sediment formation hard cake Appearance slower faster (-) Absent (+) present (unsightly) Cloudy appearance Supernatant liquid + sediments  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 24 09/08/2022  taking up of a certain amount of liquid of gel  Imbibition- No increase in the size of a gel  Syneresis - No increase in volume  Swelling- With Increase in volume. a. Glycerogelatins are plastic masses containing gelatin (15%),  glycerin (40%),  water (35%)  and an added medicinal substance (10%) such as zinc oxide   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 micrometers xerogel is formed when the liquid is removed from a gel and only the framework remains  Thixotropy is the ability of the gel to become fluid on agitation, only to resume their solid or semisolid state after remaining undisturbed for a period of time. Magma / Milk  a two-phase system gel consisting of floccules of small distinct particles  ex. Milk of Magnesia / Magnesia Magma  2. Emulsions  Cod Liver Oil Emulsion 25 09/08/2022 Phases of an emulsion   Types of Emulsion 1. Oil-in-Water (o/w) dispersed phase / internal phase /discontinuous phase dispersion medium / external phase / continuous phase Types of Emulsion ◦ oil is dispersed as droplets in an aqueous medium ◦ oral products and external, washable products Types of Emulsion 2. Water-in-Oil (w/o) 3. Multiple Emulsions ◦ water is dispersed as droplets in an oil or oleaginous medium ◦ used for external preparations when emollient, lubricating, or protective properties are desired Types of Emulsion ◦ (o/w/o or w/o/w) Factors that determine emulsion type 4. Microemulsions ◦ ◦ Emulsifier 1. ◦ appear translucent or transparent have droplet diameter in the nanometer size range some emulsifiers form either w/o or o/w emulsions, others form only one type Phase ratio (relative amounts of oil and water) 2. ◦ phase present in greater concentration tends to be the external phase Order of mixing 3. ◦ the phase that is being added by portions tends to be the internal phase 26 09/08/2022 Emulsifying Agents Emulsifying Agents 1. Natural 2. Finely Divided Solids ◦ derived from animal or plant sources Animal: gelatin, egg yolk, casein, Plant: acacia, tragacanth, pectin, cellulose derivatives Emulsifying Agents 3. Synthetic Aka Clays Veegum -Magnesium aluminum silicate Bentonite -Aluminum Silicate Griffin Hydrophilic-Lipophilic Balance (HLB) System HLB Value Range Surfactant Application • • Anionic – sodium lauryl sulfate, soaps Cationic – benzalkonium chloride 0-3 Antifoaming agents 4-6 W/O emulsifying agents • Non-ionic – sorbitan esters (Spans); polysorbates (Tweens) 7-9 Wetting agents 8-18 O/W emulsifying agents 13-15 Detergents 10-18 Solubilizing agents A formula for an water in Oil emulsion calls for a 150 g of an emulsifier blend consisting of Tween 20 and Span 40, how many grams of each emulsifier should be used in emulsifying the cream? (HLB of Tween 20 is 16 and Span 40 is 6) A formula for a dermatologic cream calls for a 15 g of an emulsifier blend consisting of Tween 20 and Span 40. If the required HLB is 11.70, how many grams of each emulsifier should be used in emulsifying the cream? (HLB of Tween 20 is 16.7 and Span 40 is 6.7) a. 5 g Tween 20 and 10 g Span 40 b. 7.5 g Tween 20 and 7.5 g Span 40 c. 2.5 g Tween 20 and 12.5 g of Span 40 d. none of the above 27 09/08/2022 Methods of Preparation 1.  Wet Gum Method (English Method) 2. Dry Gum Method (Continental Method) -(water + emulsifier) + oil  - (oil + emulsifier) + water oil: add slowly ( 1-5 mL)  4 parts oil: 2 parts water: 1 part gum.  -water is added rapidly   Methods of Preparation Methods of Preparation Methods of Preparation 3. Bottle Method 4. Nascent Soap Method  extemporaneous compounding of emulsion from volatile oil or oils of low viscosity   -alkali + FA (50:50)  Soap formed act as emulsifier O:W: E (3:2:1) (2:1: 1) Problems in emulsion 1.) creaming- upward 2.) sedimentation- downward 4.) aggregation- globules come together but do not fuse 5. )coalescence- globules come together and fuse 3.) cracking- complete separation 6. inversion o/w w/o vie versa PART IV: SEMI SOLID DOSAGE FORMS 28 09/08/2022 1. Ointments  Ointment Bases are semisolid preparations intended for external application to the skin or mucous membranes 1. Oleaginous Bases ◦ hydrocarbon bases ◦ not water-washable, incorporation of water with some degree of difficulty ◦ ex. petrolatum, white petrolatum, yellow ointment, white ointment Ointment Bases   Lanolin, USP, obtained from the wool of sheep, is a purified wax-like substance that has been cleaned, deodorized, and decolorized. Anhydrous lanolin contains not more than 0.25% water Absorption Bases  anhydrous type ◦ ◦ ◦ ◦ ◦ hydrophilic petrolatum lanolin (0.25% water) Aquaphor® Aquabase® Polysorb® 2. Absorption Bases ◦ are not easily removed from the skin ◦ two types:  Anhydrous lanolin  w/o emulsion  Cold cream Ointment Bases  w/o emulsion ◦ hydrous lanolin (25 – 30% water) ◦ cold cream ◦ Eucerin® ◦ Hydrocream® 3. Water-Removable Bases ◦ are o/w emulsions resembling creams ◦ easily washed from the skin, hence called “water-washable” ◦ ex. hydrophilic ointment, vanishing cream, Unibase® 29 09/08/2022 Ointment Bases Preparation: 4. Water-Soluble Bases  Incorporation  Fusion Method ◦ do not contain oleaginous components ◦ are completely water-washable, hence called “greaseless” ◦ ex. polyethylene glycol (PEG) ointment 2. 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 4. 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 3. Lotion  a fluid suspension or emulsion applied to the surface of the skin In summary  Part I: Introduction ◦ Drug + excipient ◦ Drug productDosage formDrug delivery system  Part II: Solid dosage forms ◦ Powdergranule capsuletablet 30 09/08/2022 In summary  Part III: Liquid dosage forms ◦ Solution      THANK YOU!!! Disperse system Aqueous Non aqueous Sterile Topical suspension emulsion Part IV: Semisolid dosage forms ◦ Suppositories ◦ Topical system  Powders containing hygroscopic or deliquescent materials should be wrapped in what type of paper? A. B. C. D.  A. hydrocarbon bases B. oleaginous bases C. absorption bases D. water-soluble bases E. water-removable bases Which of the following statement/s is/are NOT true for liniments? A. A. They are not applied to broken skin because excessive irritation might result B. B. Oleaginous liniments are employed primarily when rubefacient, counterirritant, or penetrating action is desired C. C. Oleaginous liniments are less irritating to the skin than alcoholic liniments D. D. both B and C A.white bond paper B. vegetable parchment C. waxed paper D. glassine These ointment bases are water-in-oil emulsions that permit the incorporation of additional quantities of aqueous solutions A. B. C. D. E.   10 volumes of Hydrogen Peroxide Topical Solution is equivalent to ___ H2O2. A. B. C. D. A. 3% B. 4% C. 5% D. 6% 31 09/08/2022  These are concentrated preparations of vegetable or animal drugs obtained by the removal of the active constituents with suitable menstrua A. B. C. D.   A. Spirits B. Tinctures C. Extracts D. Fluidextracts Cocoa butter A. B. C. D.  A. A. is a water-soluble base B. B. exhibits marked polymorphism C. C.has a tendency to have a higher melting point when combined with phenol and chloral hydrate D. D. both B and C E. E. all of the above  It is the taking up of a certain amount of liquid without a measurable increase in the size of a gel A. B. C. D. A. syneresis B. swelling C. imbibition D. thixotropy Which of the following excipients is NOT used alone in the formulation of effervescent granules since it will cause the resulting granules to readily lose their firmness and crumble? Collodions are prepared by dissolving pyroxylin in ____ solvent mixture A. B. C. D.  A. tartaric acid B. succinic acid C. citric acid D. fumaric acid A. 1 alcohol: 3 ether B. 3 alcohol: 1 ether C. 1 nitric acid: 3 sulfuric acid D. 3 nitric acid: 1 sulfuric acid A tablet which contains 2 single doses of medication, one for immediate release and another for delayed release A. B. C. D. A. extended-release B. repeat-action C. targeted release D. both A and B 32 09/08/2022  The sweetening agent used in the manufacture of sugar-free chewable tablets A. B. C. D.   A. dextrose B. xylitol C. Mannitol D. fructose Solubility descriptive term wherein 60 parts of the solvent is required to dissolve 1 part of the solute A. B. C. D. Concentration of Alcohol in a Tincture? These are flat oval tablets intended to be dissolved beneath the tongue for absorption in the oral mucosa A. B. C. D.  A. sublingual tablets B. buccal tablets C. hypodermic tablets D. both A and C HLB value needed for oil-in-water emulsions A. B. C. D. A. freely soluble B. soluble C. slightly soluble D. sparingly soluble A. 40%  B. 80%  C. 60%  D. 10%   A. 1 - 3 B. 3 - 6 C. 8 - 18 D. 13 - 15 Another term for vaginal suppositories is:  A) Bougies  B) Pessaries  C) Enema  D) Vaginitis  33 09/08/2022  A semisolid preparation that is stiffer and less greasy than ointments is:  A) Pastes  B) Dressing  C) Cerates  D) Creams   The dry-gum method of preparing emulsions is also called:  A) English method  B) Continental method  C) 4:2:1 method  D) B and C  A very soluble solute is an expression of one gram dissolved in:  A) Less than one part of solvent./ B) From 1 to 10 parts of solvent  C) From 10 to 30 parts of solvent D) 30 to 100 parts of solvent.   Oleovitamins generally consist of:  A) Vitamins A & D  B) Vitamin B  C) Vitamin A & B  D) Vitamin A Table triturates for use by the physicians in his extemporaneous preparation of parenteral solutions are:  A) Pastilles  B) Hypodermic Tablets  C) Sublingual  D) Pellets Tablet dosage form not requiring disintegration:  A) Film-coated  B) Enteric coated  C) Sustained release  D) Chewable 34 09/08/2022 This is an oil-in-water emulsion:  A) Cold cream  B) Butter  C) Dairy cream  D) Vanishing cream  Fusing together of droplets into larger globules:  A) Coalescence  B) Aggregation  C) Creaming  D) Sedimentation  Glycerogelatine contain high percentage of glycerin which is about:  A) 60%  B) 40%  C) 85%  D) 65%  35