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They may be applied to the skin, or used nasally, vaginally, or rectally. 3 Symbol: IDEAL PROPERTIES OF SEMISOLID DOSAGE FORMS PHYSICAL PROPERTIES a) Smooth texture b) Elegant in appearance c) Non dehydrating d) Non gritty e) Non greasy and non staining f) Non hygroscopic PHYSIOLOGICAL PROPERTIES g) Non irritating h) Do not alter membrane / skin functioning i) Miscible with skin secretion j) Have low sensitization index APPLICATION PROPERTIES k) Easily applicable with efficient drug release. l) High aqueous washability. 4 med_0015_slide: ADVANTAGES Avoid of first pass metabolism. Site specific action of drug on affected area. Convenient for unconscious patient or patient having difficulty on oral administration. Suitable dosage form for bitter drugs. More stable than liquid dosage form. 5 1_med_0015_slide: DISADVANTAGES May cause staining. They are bulky to handle. Application with finger may cause contamination. Physico-chemically less stable than solid dosage form. May cause irritation. Allergic to some patients. 6 1_Default Design: CLASSIFICATION SEMISOLID creams poultice gels pastes ointments suppositories plasters non-sterile sterile 7 Business design slide: OINTMENTS Homogeneous, translucent, viscous, semi-solid preparation, most commonly a greasy, thick oil (oil 80% - water 20%) with a high viscosity, Applied to the skin or mucous membranes. Uses Emollients application of active ingredients to the skin Occlusive 8 INTRODUCTION TO SEMI-SOLID DOSAGE FORM: CREAMS Viscous semisolid emulsion system with opaque appearance as contrasted with translucent ointments. Consistency depends on weather the cream is w/o or o/w. W/O creams O\W creams Contains lipophilic emulsifying agent. Used as emollient and as cleansing agent. Contains O\ W emulsifying agent. O/W creams are elegant drug delivery system. CONTENTS: PASTES Contains high percentage of insoluble solid (usually 50 % or more) Pastes are usually prepared by incorporating solids directly into a congealed system by levigation with a portion of the base to form a paste like mass. They have good adhesion on skin and less greasy. 10 DEFINITION: GELS AND JELLIES Gels and jellies are semisolid system in which a liquid phase is constrained within a 3-D polymeric matrix having a high degree of physical or chemical cross-linking. Gels are aqueous colloidal suspensions of the hydrated forms of insoluble medicament. Jellies are transparent or translucent non-greasy semisolid and contains more water than gels. Used for medication, lubrication and carrier for spermicidal agents to be used intra vaginally with diaphragms. 11 IDEAL PROPERTIES OF SEMISOLID DOSAGE FORMS : POULTICES (CATAPLASMS) They are wet masses of solid matter applied to the skin in order to reduce inflammation and in some cases to act as a counter-irritant. Poultice must retain heat for a considerable time. After heating the preparation is spread on dressing and applied to the affected area. E.g. Kaolin poultice (B.P.C.) 12 ADVANTAGES: PLASTERS Plasters are solid or semisolid masses made by incorporating medicaments in resinous or waxy bases which are melted and spread on suitable backing material they are mainly used to, Afford protection and mechanical support. Furnish an occlusive and macerating action. Bring medication into close contact with the surface of the skin. 13 DISADVANTAGES: SUPPOSITORIES It is solid or stiffened semisolid dosage form intended for insertion into body orifices where they melt, soften, or dissolve and exert local or systemic effects. TYPES Rectal suppositories Pessaries Urethral bougies Nasal bougies Ear cones 14 CLASSIFICATION: FORMULATION OF SEMISOLID DOSAGE FORMS INGREDIENTS USED IN PREPARATION OF SEMISOLIDS Active pharmaceutical ingredient (API) Bases Preservative Humectants Antioxidants Emulsifier Gelling agent Permeation enhancer Buffers 15 PowerPoint Presentation: 1. BASES It is one of the most important ingredient used in formulation of semisolid dosage form. Ointment and suppository bases do not merely act as the carriers of the medicaments, but they also control the extent of absorption of medicaments incorporated in them. 16 PowerPoint Presentation: IDEAL PROPERTIES OF A BASE They should be, Inert, non-irritating and non-sensitizing. Compatible with skin pH and the drug. Good solvent and/or emulsifying agent. Emollient, protective, non-greasy and easily removable. Release medicament readily at the site of application. Pharmaceutically elegant and possess good stability. 17 PowerPoint Presentation: TYPES OF BASES Oleaginous bases. Absorption bases. Emulsion bases. Water soluble bases. 18 PowerPoint Presentation: A) Oleaginous (hydrocarbon) bases. They consist of a combination of more than one oleaginous material such as water-insoluble hydrophobic oils and fats. They are highly compatible; occlusive; good emollients. They are anhydrous, do not absorb water, readily (hydrophobic) insoluble in water, not washable. Examples: Vaseline, hard paraffin, liquid paraffin, white ointment. Uses: protectants, emollient, and vehicle for solid drugs. 19 PowerPoint Presentation: B) Absorption (Emulsifiable) Bases Have capacity to absorb considerable quantities of water or aqueous solution and turn to w/o without marked changes in consistency. They are anhydrous, water insoluble and water unwashable. They have good emollient but poor occlusive property. Uses: protectants, emollient, and vehicle for aqueous solutions and solid drug. 20 PowerPoint Presentation: C) Emulsion Bases According to the type of emulsion, these bases are classified as either W/O or O/W. Uses: Cleansing creams, emollients and vehicle for solid and liquid drugs. 21 Emulsion Ointment Base (W/O): Hydrous Will absorb water Insoluble in water Not washable Water-Oil-Emulsion Emulsion Ointment Base (O/W): Hydrous Will absorb water Insoluble in water Washable Oil-in-Water Emulsion Hydrophilic Ointment PowerPoint Presentation: D) Water Soluble Bases These include both anhydrous and hydrous dermatological non-emulsion bases which are water soluble and contain no oil phase. Water soluble, water washable, greaseless. Because they soften with the addition of water, large amounts of aqueous solutions are not effectively incorporated into these bases. Examples . Carbowax compounds such as the polyethylene glycol bases containing pectin, cellulose, Bentonite, and gelatin. 22 FORMULATION OF SEMISOLID DOSAGE FORMS : 23 BASES USED IN SEMI-SOLID DOSAGE FORM 1. BASES: 2. PRESERVATIVE Some base, although, resist microbial attack but because of their high water content, it require an antimicrobial preservative. Commonly used preservatives include Methyl hydroxybenzoate Propyl hydroxybenzoate Chlorocresol Benzoic acid Phenyl mercuric nitrate 24 IDEAL PROPERTIES OF A BASE: 3. ANTIOXIDANTS Oxygen is a highly reactive atom that is capable of becoming part of potentially damaging molecules commonly called “free radicals.” Free radicals are capable of attacking the healthy cells of the body, causing them to lose their structure and function. To prevent this an antioxidants are added. E.g. Butylated hydroxy anisole, Butylated hydroxy toluene. 25 TYPES OF BASES: CLASSIFICATION OF ANTIOXIDANTS ANTIOXIGENS REDUCING AGENT ANTIOXIDANT SYNERGISTS Acts by reacting with free radical. e.g. Butylated hydroxyanisole (BHA) Butylated hydroxytoluene (BHT) Tocopherlos (used for oil system) Have lower redox potential than drug, hence gets oxidised first. e.g. Ascorbic acid Potassium and sodium metabisulfite Thiosulfite (used for aqueous system) Chelating or sequestering agent,enhacne the effects of antioxidants. e.g. Citric acid Tartaric acid lecithin 26 A) Oleaginous (hydrocarbon) bases. : 4. GELLING AGENTS Gelling agents, forms a gel, dissolving in the liquid phase as a colloid mixture that forms a weakly cohesive internal structure. These are organic hydrocolloids or hydrophilic inorganic substances. E.g. Tragacanth, Sodium Alginate, Pectin, Starch, Gelatin, Cellulose Derivatives, Carbomer, and Poly Vinyl Alcohol Clays. Material % Brookfield viscosity ‘CP 0’ Carbomer 941resin NF Carbomer 941resin NF Guar gum Methyl cellulose Sodium alginate 0.15 0.25 1.50 2.00 2.50 2900 6300 8040 5200 10400 27 B) Absorption (Emulsifiable) Bases : 5. PERMEATION ENHANCERS Skin can act as a barrier. With the introduction of various penetration enhancers, penetration of the drug through the skin can be improved. Sr. no Permeation enhancer Drugs used 1. Menthol, carvacrol, linalool Propranolol hydrochloride 2. Limonene Indomethacin, ketoprofen 3. Geraniol, nerolidol Diclofenac sodium 4. Oleic acid Piroxicam 28 C) Emulsion Bases : 6. EMULSIFIER An emulsifier (emulgent) is a substance that stabilizes an emulsion by increasing its kinetic stability. One class of emulsifiers is known as surface active substances, or surfactants. Ideal properties of emulsifier includes, a) Must reduce surface tension for proper emulsification. b) Prevents coalescence and should quickly absorb around the dispersed phase. c) Ability to increase the viscosity at low concentration. d) Effective at low concentration 29 D) Water Soluble Bases : Anionic Cationic Nonionic Alkyl sulfates Soaps Dodecyl benzene sulfonate Lactylates Sulfosuccinates Monoglyceride sulfonates Phosphate ester Silicones Taurates Quaternary ammonium compounds Alkoxyalkylamines Polyoxyethylene alkyl-aryl ethers Polyoxyethylene sorbitan esters Sorbitan fatty acid esters Glyceryl fatty acid esters Emulsifiers 30 PowerPoint Presentation: 7. HUMECTANT A humectant is a hygroscopic substance. It is often a molecule with several hydrophilic groups, most often hydroxyl groups. Since hygroscopic substances absorb water from the air, they are frequently used in desiccation or for humidity buffering. Humectants are used to : increase the solubility of the active ingredient. to elevate its skin penetration. elevate the hydration of the skin. 31 2. PRESERVATIVE: 8. BUFFERS Buffers are added for various purpose such as : Compatibility with skin. Drug solubility. Drug stability. Influence ionization of drug. Skin, due to its weak acidic nature, tolerates weak acidic preparations. E.g. sodium acetate, sodium citrate, potassium metaphosphate. 32 3. ANTIOXIDANTS : 9. VEHICLE Purified water Water for injection Water for injection may be used in ophthalmic semi solid preparations like eye ointment, gels etc. 33 CLASSIFICATION OF ANTIOXIDANTS: METHODS OF PREPARATION A. TRITURATION This method is also known as levigation, incorporation or mechanical mixing. When base contain soft fats and oils or medicament is solid and insoluble or liquid, then this method is use. 34 4. GELLING AGENTS : COMPOUNDING OF OINTMENT BY TRITURATAION METHOD 35 5. PERMEATION ENHANCERS : B. FUSION This method is used :- When soft fats or waxes are to be incorporated with hard fats or waxes then of this to be melted to get homogenous mixture with stirring. Solid drugs that are readily soluble in melted base. 36 6. EMULSIFIER : COMPOUNDING OF OINTMENT BY FUSION METHOD 37 PowerPoint Presentation: C. CHEMICAL REACTIONS In chemical method a new product is formed by chemical reaction, which involves both fusion and mechanical mixing. Best example of such method is Iodine ointment. E.g. Ointment containing free iodine Iodine is only slightly soluble in most fats and oils. Iodine is readily soluble in concentrated solution of potassium iodide due to the formation of molecular complexes KI.I 2 , KI.2I 2 , KI.3I 2 etc. These solutions may be incorporated in absorption-type ointment bases. 38 7. HUMECTANT: EVALUATION OF SEMI SOLID DOSAGE FORM (1) Physical methods Test of rate of absorption Test of non-irritancy Test of rate of penetration Test of rate of drug release Test of rheological properties Test of content uniformity (2) Microbiological methods Test of microbial content Test of preservative efficacy 39 8. BUFFERS: PHYSICAL METHODS TEST OF RATE OF ABSORPTION The ointment should be applied over a definite area of the skin by rubbing. At regular intervals of time, serum and urine samples should be analyzed for the quantity of drug absorbed. 40 9. VEHICLE: 2. TEST OF NON-IRRITANCY Non-irritancy of the preparation is evaluated by patch test. In this test 24 human volunteers are selected. Definite quantity of ointment is applied under occlusion daily on the back or volar forearm for 21 days. Daily the type of pharmacological action observed is noted. No visible reaction or erythema or intense erythema with edema and vesicular erosion should occur. A good ointment base shows no visible reaction. 41 METHODS OF PREPARATION : 3. TEST OF RATE OF PENETRATION Flow-through diffusion cell or microdialysis method is used. Animal or human skin of definite area should be collected and tied to the holder present in a diffusion cell. The diffusion cell is placed in a fluid bath. Measured quantity of the preparation is applied over the skin and the amount of drug passed into the fluid is measured at regular intervals by analyzing the aliquots of fluid using a spectrophotometer. 42 PowerPoint Presentation: 4. TEST OF RATE OF DRUG RELEASE A clean test tube is taken and the internal surface is coated with the preparation as a thin layer. Saline or serum is poured into the test tube. After a certain period of time, the saline is analyzed for the quantity of the drug. The amount of drug when divided by the time period gives the rate of drug release. 43 PowerPoint Presentation: 5. TEST OF RHEOLOGICAL PROPERTIES The viscosity of the preparation should be such that the product can be easily removed from the container and easily applied to the skin. Using cone and plate viscometer the viscosity of the preparation is determined. 44 PowerPoint Presentation: MICROBIOLOGICAL METHODS 1. TEST OF MICROBIAL CONTENT Solutions of different samples of the preparation are made. Each sample is inoculated into separate volumes of 0.5 ml of rabbit's plasma under aseptic conditions and incubated at 37 0 C for 1-4 hours. No formation of the clot in the incubated mass indicates the absence of the micro-organisms. 45 PowerPoint Presentation: 2. TEST OF PRESERVATIVE EFFICACY Using pour plate technique the number of micro-organisms initially present in the preparation are determined. Solutions of different samples of the preparation are made and mixed with Tryptone Azolectin (TAT) broth separately. All cultures of the micro-organisms are added into each mixture, under aseptic conditions. All mixtures are incubated. The number of micro-organisms in each sample are counted on 7th, 14th, 21st and 28th days of inoculation. 46 EVALUATION OF SEMI SOLID DOSAGE FORM: REFERENCES Cooper and Gunn’s ; Dispensing for Pharmaceutical Students; 12 th edition; CBS publishers and distributors Pvt. Ltd; 192-229. Atamaram Pawar and R.S. Gaud; Modern Dispensing Pharmacy; 1 st edition; Career Publications; 199-232. Leon Lachman, Herbert A. Lieberman, Joseph H. kanig; The Theory and Practice of Industrial Pharmacy; 3 rd edition; Varghese publication; 534-563. Dr. A.K. Seth; Pharmaceutics-II (Dispensing and Formulation); S. Vikas and Co. Publishing house; 262-319. http://www.pharmainfo.net/free-books/novel-semisolid-dosage-forms http://www.pharmainfo.net/evaluation-ointments 47 PHYSICAL METHODS: 48 You do not have the permission to view this presentation. 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