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Dispensing of Pharmaceutical Solutions

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Information about Dispensing of Pharmaceutical Solutions
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Published on March 4, 2014

Author: pcteidf

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PowerPoint Presentation: Dispensing of Pharmaceutical Solutions Vikrant Saluja Faculty of Pharmaceutical Sciences PCTE Group of Institutes, Ludhiana Punjab, India PowerPoint Presentation: Pharmaceutical Solutions Aqueous Douches Enemas Gargles Mouthwashes Nasal washes Sprays Otic solutions Inhalations Sweet &/or Viscid Syrups Honeys Nonaqueous Elixirs Spirits Collodions Glycerins Liniments PowerPoint Presentation: Definition : A solution is a homogenous one-phase system consisting of two or more components . Or A solution is a thermodynamically stable, one-phase system composed of 2 or more components, one of which is completely dissolved in the other. PowerPoint Presentation: The solvent is that phase in which the dispersion occurs and the solute is that component which is dispersed as small molecules or ions in the solvent. In general, the solvent is present in the greater amount but there are several exceptions . For example, syrup BP contains 66.7% w/w of sucrose as the solute in 33.3 % w/w of water as the solvent . A  saturated solution  is one that contains the maximum amount of solute that the solvent will accommodate at room temperature and pressure. A   supersaturated solution  is one that contains a larger amount of solute than the solvent can normally accommodate at that temperature and pressure. It is usually obtained by preparing a saturated solution at a higher temperature. Saturated and supersaturated solutions are physically unstable and tend to precipitate the excess solute under less than perfect conditions (e.g. when refrigerated or upon the addition of other additives ). PowerPoint Presentation: Advantages of solutions as an oral dosage form : 1- Easier to swallow than solid dosage forms and are therefore particularly acceptable for pediatric and geriatric use . 2- A drug in solution is immediately available for absorption. Thus, the therapeutic response is faster than that from a solid dosage form which will require a dissolution step before drug absorption takes place . 3- A solution is a homogenous system with a uniform distribution of the drug throughout the preparation. In suspension or emulsion formulations uneven dosage can occur due to phase separation on storage and shaking is needed before use . 4- Immediately diluted by the gastric contents which reduce irritation to the gastric mucosa caused by high local concentration of some drugs (aspirin, KCl ) if administered as a solid dosage form. PowerPoint Presentation: Disadvantages of solutions as oral dosage form : 1- Liquids are bulky and are therefore inconvenient to transport and store. 2- Poor stability of the ingredients in aqueous environment of solutions compared to that formulated as a tablet or capsule, which is particularly important for drugs susceptible to hydrolysis . 3- Solutions often provide suitable media for the growth of microorganisms and may therefore require the incorporation of a preservative . 4- Inaccurate dosing may lead to loss of the therapeutic efficiency . 5- The unpleasant taste of drugs is more pronounced in solutions than when in a solid form . Sweetening agents & flavors can be used to make solutions more palatable. PowerPoint Presentation: Preservatives o Microbes will grow in an aqueous solution. Therefore, it is necessary that formulator should add a preservative to the product to decrease the probability of product contamination. o The major criteria that should be considered in selecting a preservative are as follows : 1- Effective against a wide spectrum of microorganisms. 2- Stable for the shelf life of the formulation. 3- Nontoxic. 4- Nonsensitizing . 5- Relatively free of taste and odour. PowerPoint Presentation: Acidic Neutral Mercurial Quaternary Ammonium Compounds Phenol (0.2-0.5%) Cholorobutanol (0.5%) Thiomersal (0.001-0.1%) Bezalkonium chloride(0.004-0.02%) Cholorocresol (.05-0.1%) Benzyl alcohol(1.0%) Phenylmercuric acetate and nitrate (0.002-0.005%) Cetylpyridinium chloride (0.01-0.02%) O-phenyl phenol (.005-0.01%) Β-phenylethyl alcohol(0.2-1.0%) Nitromersal (0.001-0.1%) Alkyl esters of parahydroxybezoic acid (0.001-0.2%) Benzoic acid and its salts (0.1-0.3%) Boric acid and its salt (0.5-1.0%) Sorbic acid and its salts(0.05-0.2%) PowerPoint Presentation: Solvents/Co-Solvents Water is the solvent most widely used as a vehicle. Water-miscible co-solvents : Propylene glycol Glycerin Ethanol PEGs (low molecular weight) Non-aqueous solvents: Glycerol dimethyl ketal Glycerol formal Glycofurol Dimethyl acetamide Ethyl acetate Ethyl Carbonate 1 , 3 butylene glycol PowerPoint Presentation:  Sweetening Agents Natural sweeteners – Sucrose; soluble in water (vehicle), colourless, stable (pH 4-8). – Sorbitol lower sweetness intensity than sucrose . Artificial sweeteners – Regulatory review required – often restricted territories – Much more intense sweeteners compared with sucrose – As a consequence the levels are much lower (<0.2%) – Can impart a bitter or metallic after-taste (hence used in combination with natural sweeteners) – Examples: • Saccharin and it’s salts • Aspartame • Acesulfame –K • Sucralose – excellent sweetness, non-cariogenic, low calorie, wide & growing regulatory acceptability but relatively expensive PowerPoint Presentation:  Anti-Oxidants Used to control oxidation of: API Preservative Vehicle, e.g. oils or fats susceptible to β- oxidation ( rancidification ) Colourants (ageing discolouration) They are sacrificial (more oxidisable than API, preservative, etc ). Light exposure and metal ion impurities can accelerate oxidative degradation and hence depletion of anti-oxidant PowerPoint Presentation: Sodiun sulfite Ascorbic acid Sodium metabisulpfite Thioglycerol Sodium bisulfite Thioglycolic acid Sodium thiosulfate Cysteine hydrochloride Sodium formaldehyde sulfoxylate Acetylcysteine Sulphur dioxide Antioxidants for aqueous system Antioxidants for oil system Ascorbyl palmitate Hydroquinone Tocopherol Propyl gallate Lecithin Butylated hydroxy toulene Butylated hydroxy anisole PowerPoint Presentation: SYRUPS Syrups are concentrated solutions of sucrose or other sugars to which medicaments or flavourings are often added. Simple syrup : when water is used alone for making syrup. Medicated syrup : when the aqueous preparation contains some added medicinal substance Flavored syrup : which contains aromatic or pleasantly flavored substances and is intended to used as a vehicle or flavor for prescription . Syrup USP is a 85% w/v or an approximately 65% w/w sucrose solution with a specific gravity of 1.313. It is used as sweetening agent and a vehicle for other syrups. Syrup BP contains 66.7% w/w of sucrose as the solute in 33.3% w/w of water as the solvent . PowerPoint Presentation:  Syrups containing 65% by weight or more of sugars, are capable of resisting bacterial growth by virtue of their osmotic effect . Syrups often contain additional preservatives due to possibility of surface dilution of a syrup in a closed container . Additives: Polyols , such as glycerin or sorbitol, may be added to retard crystallization of sucrose or to increase the solubility of added ingredients. Alcohol often is included as a preservative and also as a solvent for flavors . Further resistance to microbial attack can be enhanced by incorporating antimicrobial agents. PowerPoint Presentation: If syrups are prepared by excessive heat, inversion of a slight portion of the sucrose may take place. This reaction is termed inversion because invert sugar (dextrose plus levulose ) is formed . C12H22O11 + H2O C6H12O6 + C6H12O6 Sucrose Dextrose Levulose ( Glucose) (Fructose) The speed of inversion is increased greatly by the presence of acids. The levulose formed during inversion is sweeter than sucrose, and thus the resulting syrup is sweeter than the original syrup. The levulose formed during the hydrolysis also is responsible for the darkening of syrup . Overheating of syrup leads to degradation of levulose formed by inversion, the sweet taste is destroyed and a dark brown liquid is formed. This process is known as caramelization . PowerPoint Presentation: Methods of preparation Solution With The Aid Of Heat Excessive heating tends to cause inversion / caramelization of sucrose 2. Solution By Agitation Without The Aid Of Heat 3 . Percolation In this procedure, purified water, or an aqueous solution, is permitted to pass slowly through a bed of crystalline sucrose in a cylindrical percolator, thus dissolving it and forming a syrup . PowerPoint Presentation: Addition of a medicating liquid to syrup This method is used in those cases in which fluidextracts, tinctures, or other liquids are added to syrup to medicate it . Syrups made in this way usually develop precipitates because alcohol is often an ingredient of the liquids used, and the resinous and oil substances dissolved by the alcohol precipitate when mixed with the syrup, producing unsightly preparations. A modification of this process, frequently adopted, consist of mixing the fluidextract or tincture with the water, allowing the mixture to stand to permit the separation of insoluble constituents, filtering and then dissolving the sucrose in the filtrate. It is obvious that this procedure is not permissible when the precipitated ingredients are the valuable medicinal agents. PowerPoint Presentation: ELIXIRS Are clear, pleasantly flavored, sweetened hydroalcoholic liquids intended for oral use. The percentage of alcohol varies from 4-40 %. (Elixirs containing over 10-12% of alcohol are usually self- preservative) The main ingredients in elixirs are ethanol and water but glycerin, sorbitol, propylene glycol, flavoring agents, preservatives, and syrups are often used in the preparation of the final product . They are used as Non-Medicated Elixers : Used to flavors and vehicles for drug substances (e.g. aromatic elixir USP). Medicated elixirs: Dexamethasone elixir USP, Phenobarbital elixir USP PowerPoint Presentation: Methods of preparation An elixir may contain both water- and alcohol-soluble ingredients. If such is the case, the following procedure is indicated: Dissolve the water-soluble ingredients in part of the water . Add and solubilize the sucrose in the aqueous solution. Prepare alcoholic solution containing the other ingredients. Add the aqueous phase to the alcoholic solution, filter, and make to volume with water . Note: Sucrose increases viscosity and decreases the solubilizing properties of water and so must be added after primary solution has been affected. A high alcoholic content is maintained during preparation by adding the aqueous phase to the alcoholic solution . PowerPoint Presentation:  SYRUP ELIXIR Syrup is concentrated, viscous, aqueous solution of sugar or a sugar substitute with or without flavor and medical substance. Elixirs are clear, pleasantly flavored, sweetened hydro alcoholic liquids intended for oral use. Primary solvents is sugar and water. Primary solvents are alcohol and water. Syrups are more viscous than elixirs. Elixirs are less viscous than syrups. Syrup may or may not use an alcohol for solubility purpose. An elixirs must use alcohol for solubility purpose. Difference between syrups and elixirs PowerPoint Presentation: Linctuses A linctus is a viscous preparation, usually prescribed or the relief of cough. It normally consists of a simple solution of the active agent in a high concentration of sucrose, often with other sweetening agents i.e simple syrups act as vehicle Glycerin is added very often to provide sweet taste as well as demulcent effect on the mucous membrane of throat The usual dose is 5 ml. Linctuses should be taken in small doses, sipped and swallowed slowly without diluting it with water in order to have the maximum and prolonged effect of medicaments. Example Codiene Phosphate linctus PowerPoint Presentation: SOLUTIONS MEANT FOR EXTERNAL USE PowerPoint Presentation: LINIMENTS Are usually alcoholic and oily liquid preparations (monophasic) or emulsion (biphasic ). They are intended for external application with rubbing to the affected area Alcoholic liniments are used generally for their rubefaciant and counterirritant effects. Such liniments penetrate the skin more readily than do those with an oil base. The oily liniments are milder in their action and may function solely as protective coatings. Liniments should not be applied to skin that are bruised or broken. Soap is included in liniment which helps in easy application on skin Most liniments contains camphor for its local analgesic effect. Container: coloured fluted bottle . Labelling : “For external use only” and “Shake well before use ” Example: Turpentine liniment Methyl salicylate syrup PowerPoint Presentation: Lotions Are usually aqueous, alcoholic preparations (monophasic) or suspension and emulsion (biphasic ). They are intended for external application without rubbing to the affected area Usually applied with the help of some absorbent material such as cotton wool or gauze. Used generally to provide cooling, soothing and protective action . Container: Coloured flutted bottle Labelling : “For external use only” and “Shake well before use” Example: Calamine lotion Salicylic acid lotion PowerPoint Presentation: COLLODIONS Are liquid preparations containing pyroxylin (a nitrocellulose) in a mixture of ethyl ether and ethanol. They are applied to the skin by means of a soft brush or other suitable applicator and, when the ether and ethanol have evaporated, leave a film of pyroxylin on the surface. The official medicated collodion , Salicylic Acid Collodion USP, contains 10 % w/v of Salicylic Acid in Flexible Collodion USP and is used as a keratolytic agent in the treatment of corns and warts. Collodion is made flexible by the addition of castor oil and camphor. Examples: Pyroxylin collodion Flexible collodion PowerPoint Presentation: SOLUTIONS TO BE USED IN MOUTH PowerPoint Presentation: GARGLES Gargles are aqueous solutions frequently containing antiseptics, antibiotics, and/or anesthetics used for treating the pharynx and nasopharynx by forcing air from the lungs through the gargle that is held in the throat; subsequently, the gargle is expectorated. Many gargles must be diluted with warm water prior to use. Phenol or thymol are usually present for antiseptic action Potassium chlorate is also included for weak astringent action. Although mouthwashes are considered as a separate class of pharmaceuticals, many are used as gargles, either as it is, or diluted with water . Examples: Potassium chlorate gargles PowerPoint Presentation: MOUTH WASHES Mouthwashes are aqueous solution often in concentrated form containing one or more active ingredients and excipients. Mouthwashes can be used for two purposes, therapeutic and cosmetic: Therapeutic rinses or washes can be formulated to reduce plaque, gingivitis, dental caries and stomatitis. Cosmetic mouthwashes may be formulated to reduce bad breath through the use of antimicrobial and/or flavoring agents. Examples: Compound sodium chloride mouth wash Zinc sulphate and zinc chloride mouth wash PowerPoint Presentation: Throat paints They are viscous liquid preparation used for mouth and throat infections. Glycerin is the most commonly used vehicle because it is very viscous and it adheres well to the mucous membrane of mouth and throat. It also gives a sweet taste and warm sensation to the inflamed area. Examples : Compound iodine paint ( Mandl’s paint), boric acid glycerin , phenol glycerin , tannic acid glycerin PowerPoint Presentation: SOLUTIONS TO BE INSTILLED INTO BODY CAVITIES PowerPoint Presentation: DOUCHES o A douche is an aqueous solution directed against a part or into a cavity of the body that function as a cleansing or antiseptic agent . o Douches are usually directed to appropriate body part by using bulb syringes . Douches are most frequently dispensed in the form of a powder or tablet with directions for dissolving in a specified quantity of water (usually warm ). Example: Potassium permagnate douche solution PowerPoint Presentation: Types of douches : 1) Eye douches: • Used to remove foreign particles and discharges from the eyes. • Method of application: directed gently at an oblique angle and allowed to run from the inner to the outer corner of the eye . 2) Pharyngeal douches : • Used to prepare the interior of the throat for an operation and cleanse it. 3 ) Nasal douches : • Used for cleansing of the nasal cavity 4) Vaginal douches: • The most common type of douches. • Used for cleansing the vagina and for hygienic purposes. • Supplied as a liquid concentrates or powders, which may be prepared in bulk or as single-use packages, that require to be diluted or dissolved in the appropriate amount of warm water prior to use. PowerPoint Presentation: Enema Enema preparations are rectal injections employed to: Evacuate the bowel (evacuation enemas ). Influence the general system by absorption, or to affect a local disease (retention enemas ). They may possess anthelmintic, nutritive, sedative, or stimulating properties, or they may contain radiopaque substances for roentgenographic examination of the lower bowel.. Evacuation enemas act by Stimulating Prestalsis Lubricative action Evacuation enemas usually are given at body temperature in quantities of 1 to 2 pt injected slowly with a syringe (pint; pt = 473 ml ). Retention enemas are to be retained in the intestine and should not be used in larger quantities than 100 ml for an adult . Example: Soft soap enema, paraldehyde enema, prednisolone enema PowerPoint Presentation: Ear drops Ear drops are medicated solutions to be instilled in to the ear with the help of a dropper. They are generally used for cleaning the cerumen (ear wax) and for treating infections The main classes of drugs used for topical administration to the ear include local anesthetics, e.g.: benzocaine; antibiotics e.g.; neomycin; and anti-inflammatory agents, e.g.; cortisone. These preparations include the main types of solvents used, namely glycerin or water. The viscous glycerin vehicle permits the drug to remain in the ear for a long time. Anhydrous glycerin, being hygroscopic, tends to remove moisture from surrounding tissues, thus reducing swelling.

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