Final Post Lab Discussion - PDDS211 - PDF

OUR LADY OF FATIMA UNIVERSITY COLLEGE OF PHARMACY NUEVA ECIJA PDDS211 Charlene M. Sta Ana  Liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents  Syrups – aqueous solutions containing...

OUR LADY OF FATIMA UNIVERSITY COLLEGE OF PHARMACY NUEVA ECIJA PDDS211 Charlene M. Sta Ana  Liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents  Syrups – aqueous solutions containing a sugar Elixirs- sweetened hydroalcoholic solutions Spirits – alcoholic solutions of aromatic materials Aromatic waters- aqueous solutions of aromatic materials Injections – solutions prepared to be sterile and pyrogen free and intended for parenteral administration  Drug available immediately for absorption Flexible dosing May be designed for any route of administration No need to shake container Facilitates swallowing in difficult cases  Drug stability often reduced in solution Difficult to mask unpleasant tastes Bulky, difficult to transport and prone to container breakages Technical accuracy needed to measure dose on administration Some drugs poorly soluble Measuring device needed for administration 1. ALCOHOL Next to water, alcohol is the most useful solvent in pharmacy. It is used as the primary solvents for most organic compounds. Can be used as preservative 2. DILUTED ALCOHOL, NF Prepared by mixing equal volumes of Alcohol and Purified water. Useful hydroalcoholic solvent in various pharmaceutical preparations. 3. GLYCERIN, USP Clear syrupy liquid with a sweet taste It is miscible with both water and alcohol. Has preservative qualities. 4. PROPYLENE GLYCOL, USP Viscous liquid that is miscible with water and alcohol Used frequently as a substitute for glycerin 5. PURIFIED WATER, USP Obtained by distillation, ion exchange treatment, reverse osmosis and other suitable process. Intended for use in the aqueous dosage forms except those intended for parenteral administration  Colorless to slightly yellow clear effervescent having a sweet, acidulous taste, and a lemon flavor. Citrate of Magnesia Saline cathartic  Prepared by chemical reaction (Magnesium carbonate with citric acid) Lemon oil (flavorant), Syrup (Sweetening agent), Potassium bicarbonate (Carbonating agent) The solution provides an excellent medium for the growth of molds, and any mold spores present during the manufacture of the solution must be killed if the preparation is to remain stable. Concentrated,aqueous preparations, intended for oral use, containing: 1. Sugar or Sugar substitutes 2. Flavoring agent 3. Medicinal agent A. Medicated Syrups B. Non-Medicated Syrups or Flavored vehicles 1. Cherry and Orange Syrups – good vehicle for drugs requiring acid medium 2. Cocoa Syrup – effectively masks bitter tasting drugs 3. Ora-Sweet and Ora-Sweet SF – alcohol free vehicle for extemporaneous compounding of syrup  – 4. Raspberry Syrup – used to disguise salty or sour taste of drugs 5. Syrup, NF or Syrup, USP - with 85% w/v concentration II. NON - MEDICINAL CLASSIFICATION A. SUGAR-BASED SYRUP Contains Sucrose / Cane Sugar Imparts a characteristic “body” to the preparation Glycogenetic Sorbitol or Glycerin may be added to prevent crystallization of sucrose  A concentrated or nearly saturated aqueous solution of sugar (85% w/v, 65% w/w) Specific gravity = 1.313 (each 100ml syrup weighs 1.313g) Have low solvent capacity for water- soluble drugs  Self-preserving, however diluted syrups are prone to microbial contamination thus require additional preservative (i.e. parabens) Concentrated sugar solutions are quite resistant to microbial growth because of the unavailability of the water required for the growth of microorganisms. Saturated solutions tend to undergo crystallization (Syrup, USP – minimal tendency to undergo crystallization)  Syrupus Aurantii Clear yellowish syrup with agreeable flavor and odor The volatile oil of the fresh, sweet orange peel, together with coloring matter, is dissolved by the alcohol. It is an excellent flavoring substance for mixtures. II. NON - MEDICINAL CLASSIFICATION B. NON SUGAR-BASED SYRUPS (NON NUTRITIVE SYRUPS) Formulated with; 1. artificial sweeteners 2. viscosity builders Non glycogenetic 1. Sugars, or sugar substitutes 2. Antimicrobial preservatives 3. Flavorants 4. Colorants 5. Special solvents, stabilizers, solubilizing agents and thickeners I. SOLUTION WITH THE AID OF HEAT - Excessive heating tends to cause inversion / caramelization of sucrose II. SOLUTION BY AGITATION WITHOUT THE AID OF HEAT III. ADDITION OF SUCROSE TO A MEDICATED LIQUID OR TO A FLAVORED LIQUID - Used in the preparation of Senna Syrup, NF IV. PERCOLATION - An extraction method utilizing a glass percolator. May be used to prepare: Simple Syrup Ipecac syrup (Cephaelis ipecacuanha)  Are clear, sweetened, hydroalcoholic solutions intended for oral use, and are usually flavored for palatability. Its Alcohol Content may vary from as low as 5% to as high as 40%.  Maintain both Less effective in water-soluble and masking the taste of alcohol-soluble drugs because elixirs components in are less sweet and less solution viscous Stable Not recommended for Easy to prepare (by children due to their simple solution alcohol content method) 1. HIGH ALCOHOLIC ELIXIR (HAE) – 75% to 78% alcohol 2. LOW ALCOHOLIC ELIXIR (LAE) – 8% to 10 % alcohol NOTE: Elixirs containing at least 10% to 12% alcohol are already “self-preserving”  Alcohol and Water – primary solvents Glycerin and Propylene Glycol- adjuncts (viscosity builders and stabilizers) Sweeteners Flavorants and Colorants Medicinal substances I. NON-MEDICATED ELIXIRS Employed as vehicles Examples: Aromatic Elixir, NF Isoalcoholic Elixir Compound Benzaldehyde Elixir II. MEDICATED ELIXIRS Examples: Diphenhydramine Elixir Phenobarbital Elixir Digoxin Elixir  By simple solution method By admixture of two or more liquids  Stored in a tightly closed, light-resistant containers Protected from excessive heat (do not store above 400C)  Alcoholic or hydroalcoholic solutions of volatile substances. Usual alcohol content is 60%. When mixed with water, the volatile material separates and forms a milky solution. A. MEDICINAL SPIRITS AROMATIC SPIRIT OF AMMONIA – reflex / respiratory stimulant ( by inhalation) B. FLAVORING SPIRITS - Compound Orange Spirit - Compound Cardamom Spirit  Taken orally Brandy and Whisky Mixed with a portion of water to reduce pungency of the spirit Applied externally Used by inhalation Aromatic spirit of ammonia 1. Distillation Brandy (48 % – 54 % alcohol) Distilled from red grapes Whisky (47 % – 53% alcohol) Distilled from hops, barley and other grains 2. Solution with Maceration – Peppermint Spirit (maceration of peppermint leaves) 3. Solution by Chemical Reaction – Ethyl Nitrite Spirit 4. Simple Solution – Aromatic Spirit of Ammonia (Spirit of Sal Volatile)  Smelling salts Prepared by simple solution (Ammonium carbonate and strong Ammonia solution) Used to prevent of treat fainting Respiratory stimulant By inhalation  Medicated water are clear, saturated aqueous solution of volatile oils or other aromatic or volatile substances. They are used principally as flavored or perfumed vehicles if intended to be taken internally.  Volatile oils solutions represent an incompatibility problem of salting out. This occurs after the incorporation of a very soluble salt in their solution. Salting out is effect in which the solubility of a substance in a certain solvent is reduced by the presence of a second solute dissolved in the solvent.  Aromatic water will deteriorate with time, therefore: - should be made in small quantities - protected from intense light and excessive heat by storing in air tight, light resistant containers If they become cloudy or otherwise deteriorate; they should be discarded. Deterioration may be due to volatilization, decomposition or mould growth.  SIMPLE AROMATIC WATERS They contain purified water as a solvent but do not contain alcohol and are mainly used as vehicles. CONCENTRATED AROMATIC WATERS They contain alcohol as solvent for the volatile constituents. These products are alcoholic, non aqueous preparations containing 2% of volatile oils. They are 40 times stronger than the ordinary aromatic waters. 1. DISTILLATION METHOD Adv: most satisfactory method Disadv: slow and expensive The drug should be coarsely ground and mixed with sufficient quantity of purified water in the distillation unit. After distillation any excess oil in the distillate is removed by filtration. 1. DISTILLATION METHOD EXAMPLE: Stronger Rose Water NF Orange Flower NF In orange flower or rose water where the flavor or odor are in a small amount and delicate: the distillate is return in the several times to the still with fresh portions of flowers, consequently the water produced are commercially known as distilled according to the number of redistillation. This process is known as the cohobation. 2. SOLUTION METHOD This method is simpler, quicker and more economical as compared to distillation. In this method, aromatic water is prepared by intermittently shaking 2 ml (if liquid) or 2 g (if solid) of the volatile substance with 1000 ml of purified water in suitable container for a period of 15 minutes method. 2. SOLUTION METHOD  After the period of agitation the mixture is set aside for 12 hours or longer to permit the excess oil and the solid substance to settle.  Talc (inert) may be used to increase the surface of the volatile substance, insure more rapid saturation of the water and act as a filter aid.  Example: Peppermint water 3. ALTERNATIVE SOLUTION METHOD  The volatile oil or suitably comminuted aromatic solid is thoroughly incorporated with 15 g of distributing agent to this mixture is added 1000 ml of purified water. The resulting slurry is thoroughly agitated several times for the period of 30 minutes and then filtered.  Peppermint oil is extracted from Mentha piperita. Peppermint oil is non-toxic and non-irritant in low dilutions, but sensitization may be a problem due to the menthol content. Used as an antispasmodic and carminative in flatulence of the gastrointestinal tract, cramping and bloating, flatulent colic to relieve nausea and vomiting, and as a gentle aromatic stimulant  rectal injection preparations administered to evacuate the bowel, influence the general system by absorption or to affect a local disease  Retention enema – to provide systemic or local effect Evacuation enema – to provide mechanical effect  Sodium Phosphate enema - bowel stimulant Sulfasalazine rectal enema – ulcerative colitis Starch and opium enema – sedative Mesalamine enema – inflammatory bowel disease Dextrose and saline enema – nutritive Barium sulfate enema - radiopaque contrast media  Aqueous suspensions of insoluble, inorganic drugs Particles are bigger than the particles of gel Magmas are already viscous and because of this, there is no need to add a suspending agent. 1. HYDRATION METHOD Similar to chemical reaction but utilizes the use of water as one of the reactants Advantage: This method is used industrially because this method does not require washing. Disadvantages: Produces highly viscous preparation The pH of the preparation produced is approximately 10. (Remedy: add 0.1% citric acid) 2. HYDRATION and PRECIPITATION A solution of NaOH is triturated with MgO to form a smooth cream. It is diluted with water. The cream is mixed with a MgSO4 solution while stirring. After some time, the magnesium hydroxide will settle. The supernatant liquid is decanted and the precipitation is washed with purified water. The precipitate will be mixed with chloroform water to give the final product.  Bentonite - Colloidal hydrated aluminum silicate Use: Suspending agent to other preparations Cream to gray brown, odorless dispersion Boston round, wide mouth, amber, tight container Shake well before use, do not freeze Thixotropic preparation  A two phase system in which one immiscible liquid is intimately dispersed in another liquid (as droplets).  DISPERSED PHASE The undissolved or immiscible drug (suspensoid) distributed throughout the liquid vehicle. Also called the “internal phase”  DISPERSION MEDIUM The liquid vehicle, to which the insoluble drug is distributed. Also called “external phase”  DISPERSING /SUSPENDING/ EMULSIFYING AGENT Stabilizes the suspension, maintains the homogeneity of the internal and external phases, after agitation of the contents.  Colloidal dispersions – 1 nm to 0.5 nm Coarse dispersions (suspensions and emulsions) – 10 um to 50 um Fine dispersions ( magmas and gels) – 0.5 um to 10 um  W/O emulsion - water is the internal phase - oil is external phase O/W emulsion - oil is the internal phase - water is external phase  Any compound that lowers the interfacial tension and forms a film at the interface TYPES: 1. Natural emulsifying agents – acacia, tragacanth, agar, pectin, gelatin, methylcellulose 2. Synthetic emulsifying agents – anionic, cationic, or nonionic 1. ANIONIC AGENTS – include sulfuric acid esters, sulfonic acid derivatives, and soaps Alkali soaps – form O/W emulsion Metallic soaps – form W/O emulsion Monovalent and Polyvalent soaps – form W/O emulsion  Used as surfactant in 1% concentration Example: Benzalkonium chloride 3. NONIONIC EMULSIFIERS Resistant to the addition of acids and electrolytes Examples: Sorbitan esters – SPANS, hydrophobic, low HLB values, form W/O emulsions Polysorbates – TWEENS, hydrophilic, high HLB values, form O/W emulsions  HYDROPHILE – LIPOPHILE BALANCE Used to classify non-ionic surfactants All NON –IONIC surfactants have an HLB value. The higher the HLB number, the more hydrophilic. The lower the HLB number, the more lipophilic.  HYDROPHILIC SURFACTANTS High HLB values (>10) Form O/W emulsion LIPOPHILIC SURFACTANTS Low HLB values (1-10) Form W/O emulsion 1. WET GUM METHOD English method 4:2:1 of oil : water : gum Formation of Primary Mucilage as the nucleus of the emulsion. 2. DRY GUM METHOD Continental method 4:2:1 ratio of oil: water: gum Formation of Primary Gum as the nucleus of the emulsion 3. BOTTLE METHOD Forbes Bottle method or 2:2:1 method 2:2: 1 ratio of oil : water : gum Applicable to emulsions containing Volatile Oils. 4. NASCENT SOAP METHOD The soap is formed first by mixing equal volumes of oil and alkali. The soap acts as emulsifying agent. A 50:50 ratio of oil to water ensures sufficient emulsion. DYE SOLUBILITY TEST Uses methylene blue or brilliant blue If the dye is dissolve and uniformly diffuse – O/W If the particle of the dye lie in clumps on the surface – W/O DILUTION TEST If freely mixes with water – O/W If not diluted with water – W/O ELECTRIC CONDUCTIVITY TEST O/W conducts electric current W/O do not conduct electric current  Mineral Oil Emulsion Use: Laxative Cream or light yellow viscous liquid Boston round, wide mouth, amber, tight container Shake well before use, do not freeze