Pharmaceutical Solutions: Lecture Notes PDF

Purified water Water Widely used Alcohol ethyl alcohol Dissolve polar and semi-polar substances Ethanol C2H5OH Miscible with water, used internally Antimicrobial activity External use Isopropyl alcohol (7...

Purified water Water Widely used Alcohol ethyl alcohol Dissolve polar and semi-polar substances Ethanol C2H5OH Miscible with water, used internally Antimicrobial activity External use Isopropyl alcohol (70%) Vehicle for topical preparations Glycerin Clear, viscous liquid with sweet taste CH2OH CHOHCH2OH miscible with water and alcohol Propylene Glycol Viscous liquid, miscible, substitute glycerin CH3CH(OH)CH2OH in pharmaceutical preparations Corn oil ,Cotton seed oil Organic solvents for oleaginous injection Peanut oil and Sesame oil  pH required (7.4 for injectable solutions, eye, nose)  (5.5 for dermal application)( vaginal 4-5)  Buffering capacity  Compatible with other excipients  Low toxicity  Carbonates, citrates, gluconates, lactates phosphates and tartrates are widely used.  Borates are used for external application but not to abraded skin or internally Taste of product Suitable masking flavor Salty Apricot, butterscotch, liquorice, peach vanilla Bitter Anise, chocolate, mint, passion fruit, wild cherry Sweet Vanilla, fruits, berries Sour Citrus fruits, liquorice, raspberry Additives: Flavors and perfumes Product use Flavor preferred Relief of indigestion Mint Antiseptic activity Terpineol Oral mucosa anesthetic Clove oil (eugenol) Children Fruity taste and smell Adult Flowery odours, acid taste  The colour of the product is associated with the flavor Flavor Colour Mint Green Chocolate Brown Cherry , strawberry Pink – red  Product identification  Safe, acceptable  Drinking water must be clear, colorless, odorless, and neutral or only slightly acid or alkaline  Not accepted for manufacture of aqueous pharmaceutical preparations because of chemical compatibility of the dissolved solids with the medicinal agents (ppt.,discoloration, effervescence)  Used for washing, in extraction of the crude vegetable drugs  Prepared from tap water complying with the Environmental Protection Agency for drinking water.  Purified Water has fewer solids impurities than ordinary drinking water, when evaporated to dryness it must not yield more than 1mg solids per 100ml water  Intended for use in preparation of aqueous dosage forms except those intended for parenteral administration.  Used in preparation of all medications containing water except injectable preparation and other specialized products  Purification of water is done by 1) Distillation 2) De-ionization (Ion exchange) 3) Reverse osmosis  Distilled water is water that has many of its impurities removed through distillation. Distillation involves boiling the water and then condensing the steam into a clean container Typical laboratory Definition distillation unit  On a large or small scale, ion exchange for the preparation of purified water offers a number of advantages over distillation. 1. The requirement of heat is eliminated and with it, 2. The costly and troublesome maintenance frequently encountered in the operation of the more complex distillation apparatus. 3. Because of the simpler equipment and the nature of the method, ion exchange permits ease of operation, minimal maintenance, and a more mobile facility. Water purified in this manner, referred to as demineralized or deionized water, may be used in any pharmaceutical preparation or prescription calling for distilled water Is an water insoluble, synthetic, polymeric resin of high molecular weight containing phenolic, carboxylic, amino, or sulfonated groups. The beads are typically porous, providing a high surface area. definition Ion exchange beads  1-Acid or cationic exchanger  which permit the exchange of the cations in solution with hydrogen ion from the resin;  H- resin + M+ + X- + H2O → M-resin + H+ + X- + H2O (pure)  2- Base or anionic exchanger  which permit the removal of anions  Resin-NH2 + H+ + X- + H2O → Resin-NH2 ♦ HX + H2O (pure)  Ion exchange is a method widely used in water filters to produce soft water. The trapping of ions occurs with concomitant releasing of other ions; thus the process is called ion-exchange.  Water purification is accomplished by exchanging calcium Ca2+ and magnesium Mg2+ cations against Na or H cations + +  The most commercial resins are made of polystyrene sulfonate these polymers have a higher affinity to divalent cations than monovalent cations. Principle Water softener illustration  Reverse osmosis is one of the processes referred to in the industry as cross-flow membrane filtration.  In osmosis the flow through a semipermeable membrane is from a less concentrated solution to a more concentrated solution,  Reverse osmosis: the flow in this cross-flow system is from a more concentrated to a less concentrated solution; thus the term reverse osmosis.  Osmosis is the passage or diffusion of water or other solvents through a semipermeable membrane that blocks the passage of dissolved solutes Principle Osmosis Principle  In RO, an applied pressure is used to overcome osmotic pressure, a colligative property, that is driven by chemical potential, a thermodynamic parameter.  The result is that the solute is retained on the pressurized side of the membrane and the pure solvent is allowed to pass to the other side.  To be "selective," this membrane should not allow large molecules or ions through the pores (holes), but should allow smaller components of the solution (such as the solvent) to pass freely.  Depending on their pore size, cross-flow filter membranes can remove particles defined in the range of  microfiltration (0.1 to 2 µm, e.g., bacteria);  ultrafiltration (0.01 to 0.1 µm, e.g., virus);  nanofiltration (0.001 to 0.01 µm, e.g., organic compounds  in the molecular weight range of 300 to 1,000); and reverse osmosis (particles less than 0.001 µm).  Reverse osmosis removes virtually all viruses, bacteria, pyrogen, and organic molecules and 90% to 99% of ions  Pyrogen free water (polysaccharide byproduct of bacterial origin)  Purified by distillation and used within 24 hr. after collection.  Intended to be used as a solvent for parental products preparation to be sterilized after preparation  Sterilization is achieved by autoclave (steam under pressure)  Water for injection sterilized and packed in suitable single dose container preferably Type I glass and not larger than 1000ml size.  This water is intended to be used as a solvent, vehicle, or diluent for already sterilized and packaged injectable medications.  They are used to reconstitute of antibiotics  Sterile water for injection that contains bacteriostatic agent (benzyl alcohol)  May be packed in single dose container (not larger than 5ml)or multiple dose containers (not larger than 30ml)  Not used for neonates.  Sodium chloride injection USP  Bacteriostatic sodium chloride injection USP  Ringer injection USP  Lactated Ringer injection USP  Dextrose 5% solution  Sterile by autoclave or filtration Isotonic Preserved (multi-dose )by phenyl ethyl-alcohol, chorobutanol, benzalkonium chloride, phenyl mercuric nitrate Optimum pH low buffer capacity Final Drug solution Sweetening agent Flavoring agent Preservative Colors Buffers Density modifiers Viscosity enhancers Reducing agents Oral solutions Dry for reconstitution  Mostly used for small 1. Unstable in aqueous and old aged patients media  Cold remedies and 2. Uniform dose bronchodilators  vitamins  ORS (Oral rehydration sol.  Laxative solutions  Orodispersible tablet  Mist Diuretic (Halazone) or powder Voltafast ®  Effervescent tablets or powder ORS  Used for diarrhea to replenish electrolytes  This equates to  45 mEq sodium,  35 mEq chlorine, and  20 mEq potassium  30mEq citrate  25g dextrose per liter of fluid.  These formulation are available in liquid or powder packet form for reconstitution  Used before bowel procedures (colonscopy)  Balanced solutions of electrolytes with PEG- 3350  Lactulose is a colonic acidifier that works by increasing stool water content and softening the stool. It is a man-made sugar solution laxative used to treat constipation.  Mouthwashes/gargles are designed for the treatment of infection and inflammation of the oral cavity. Formulations designed for this purpose employ water as the vehicle, although a co-solvent, e.g. alcohol, may be employed to solubilize the active agent.  The use of alcohol as a co-solvent may act to enhance the antimicrobial properties of the therapeutic agent.  Other formulation components are frequently required to enhance the palatability and acceptability of the preparation. These include preservatives, colors, flavoring agents and non- cariogenic sweetening agents.   Used for irrigation, Powders for solution cleansing of the vagina for hygienic effect Liquid solutions or concentrates  Astringents  Antimicrobials Vaginal preparations properties 1. Maintain optimal pH  Adjusting pH 2. Ease of application 3. May be used externally OR internally Retention enemas Evacuation enemas 1. Local effect (hydrocortisone)  Used to cleanse as enemas for ulcerative the bowel colitis available in 2. Systemic absorption disposable plastic (aminophylline) rectal administration minimizes the squeeze bottles undesirable GIT reaction, containing a effective blood levels within 30 premeasured min after rectal instillation amount of enema Viscosity-enhancing agents, solution e.g. glycerol, may be included to aid retention of the formulation within the rectum and to reduce the incidence of seepage.  Enemas are pharmaceutical solutions that are administered rectally and are employed to ensure clearance of the bowel, 1. Oil-based solutions and, in some formulations, the vehicle is the agent that promotes bowel evacuation, e.g. Arachis oil enema. Softening the feces 2. Aqueous formulations usually contain salts (e.g. phosphates) to alter the osmolality within the rectum, thereby increasing the movement of fluid to the rectal contents. Increasing the amount of water in the large bowel (osmotic laxatives).  conc Vehicle Hydrogen peroxide 3% Aqueous Chlorhexidine gluconate 4% Aqueous Iodine tincture 2% Alcohol, water Povidone Iodine 7.5%, 10% Aqueous Clindamycin phosphate 1% Isopropyl alcohol Water Erythromycin 2% PEG/acetone/alcohol Clotrimazole 1% PEG400 Ketoconazole 1% Water Tolnaftate 1% PEG Drug Conc Vehicle Use Fluorouracil 2.5% PG antineoplastic Minoxidil 2 ,5% Alcohol, water, PG Baldness Hydroquinone Water Alcohol ,PG Podophyllum Benzoin tincture Warts Fluocinolone PG Adrenocortical acetonide steroid Betamethasone Mometasone Thank You