Pharmaceutical Technology Solutions PDF

3rd year pharmacy Pharmaceutical technology Ansel’s pharmaceutical dosage forms and drug delivery systems Molecular Colloidal Coarse True Suspension solutions Intermediate Larger than Molecules 10−9 to1µ 1µ Ions  Physicochemical terms  One...

3rd year pharmacy Pharmaceutical technology Ansel’s pharmaceutical dosage forms and drug delivery systems Molecular Colloidal Coarse True Suspension solutions Intermediate Larger than Molecules 10−9 to1µ 1µ Ions  Physicochemical terms  One phase system  2 or more substances mixed together  Physically homogeneous system  Single phase system  Prepared from any combination of  solid liquid and gas  Liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents. Most common pharmaceutical solutions are Aqueous solutions (also the biological systems are mostly aqueous) Medicated solutions contain drugs that are usually soluble in water and their absorption is higher than from suspension or solid dosage forms because any drug must be molecular dispersed ( in- solution), before they can be absorbed across the biological membrane and be effective  Oral Otic , nasal Vaginal , Ophthalmic rectal solutions Topical Injectable Oral topical (mouthwash) Irrigation  Sweet thick oral solution Syrups Contains sucrose Hydro-alcoholic oral solutions Elixirs Sweetened Spirits, Spirits are alcoholic or hydro-alcoholic solution of aromatic material aromatic water Aromatic water the solvent is water Aqueous or hydroalcoholic or alcoholic extract Fluidextracts Plant or chemical origin Tinctures Differ in concentration of the extract Must be sterile, isotonic and buffered Injections Aqueous or non aqueous 1-Solutions prepared Gention violet solution1%in( 10%alcohol) by simple solution solution topical anti-infective Hydrogen peroxide solution 3% hydrolysis 2-Solution prepared of persulfuric acid used as topical anti by chemical reaction infective 3-Solutions prepared Atropine sulphate ophthalmic solution, by simple solution also 0.9%w/v NaCl I.V. fluid with sterilization 4- Solutions prepared Ipecac, tolu by extraction Advantages Disadvantage Easy to swallow , flow, Bulky, taste masking apply , spray Stability Good absorption M.O. growth Homogeneous Patient measurement  The solubility of an agent in a particular solvent indicates the maximum concentration to which a solution may be prepared with that agent and that solvent.  i.e, Amount of a solute dissolved in a solvent at a certain temperature(degree of solubility)  Saturated solubility  Excess amount of solid shaken at certain temperature, with a certain volume of liquid for a period of time  Super saturated solution  Heat the solution containing excess solid then filter and cool. No ppt of the excess solid Sodium thiosulfate Potassium acetate  Calcium Hydroxide Topical solution USP 140mg per 100ml of solution at 25°C  Potassium iodide solution 100g per 100ml of solution  The no. of ml. of a solvent required to dissolve 1 g of the solute (or 1 ml. of liquid)  1g of KI dissolves in 0.7 ml of water  0.5 ml boiling water  Expressed using physical units w/w w/v, v/v  Or chemical units milliequivalent  Used to express concentration of electrolytes depending on their ionic charge and valence activity Term Parts of solvent required for 1 part of solute Very soluble 10000  Temperature Agitation Particle size   Depend on the Exo- thermic  Nature of the solvent  Like dissolves like Temperature  Chemical nature of the solute (molecular Endo- structure and thermic functional groups) Temperature Chemical Constitution  Dipole moment polarity Electonegative difference Hydrogen Certain functional groups present bonds Low molecular wt  Drugs with low aqueous solubility present problems in relation to the formulation and bioavailability  Consider non- aqueous solutions for drugs of low solubility 1) Adjust the pH for drugs that are weak acids or bases. Weak acids and weak base solubility is effected by the pH of the solution. At a given pH the degree of ionization depends on the pKa. 2) Co-solvent change the polarity of water 3) Surfactant Micell formation 4) Complexation (chemical reaction), (Lugol’s solution) Iodine is slightly soluble in water(1g in 3000ml water) but freely soluble in solution of sodium iodide forming tri-iodide ion  Salting -In..addition of an electrolyte to a non electrolyte cause an increase in solubility  Salting- out..decrease in solubility  Addition of soluble salt to slightly soluble salt having a common ion will cause ppt. of the slightly soluble salt (according to the law of mass action) Like dissolves like The more solvents and solutes are structurally alike the more rapid solution takes place. Polar solvents dissolve electo-valent substances readily But are poor solvents for non polar substances add the opposite is true. Polar liquids are usually miscible with other polar liquids Non polar liquids are slightly miscible with polar liquids Complex organic substances which have polar and non polar groups may dissolve in polar liquids depending on the proportion of the polar groups to the non polar Semi polar liquids (ethyl alcohol) posses the character of both polar and non polar solvents Drug (1g) Water (ml) Alcohol (ml) Atropine 455 2 Atropine sulfate 0.5 5 Codeine 120 2 Codeine sulfate 30 1,280 Codeine phosphate 2.5 325 Morphine 5,000 210 Morphine sulfate 16 565 Phenobarbital 1,000 8 Phenobarbital sodium 1 10 Procaine 200 Slightly soluble Procaine HCl 1 15 Sulfadiazine 13,000 Sparingly soluble Sodium sulfadiazine 2 Soluble compound Formula MILLILITERS OF WATER REQUIRED TO DISSOLVE 1 G OF COMPOUND Benzene C6H6 1430 Benzoic acid C6H5COOH 275 Benzyl alcohol C6H5CH2OH 25 Phenol C6H5OH 15 Pyrocatechol C6H4(OH)2 2.3 Pyrogallol C6H3(OH)3 1.7  Salts of alkali metals( Na, K, Li,) are usually water soluble except Li2CO3  Ammonium and quaternary ammonium salts  Nitrates ,nitrites, acetates, chlorates lactates except silver and mercurous acetate  Sulfates ,sulfites and thiosulfates ,except calcium and barium salts  Chlorides, bromides and iodides except salts of silver and mercurous ions  Hydroxides and oxides of compounds other than alkali metals cations and the ammonium ion  Sulfides are water insoluble except for their alkali metal salts  Phosphates ,carbonates ,silicates borates and hypochlorite are water insoluble except for their alkali metal salts and ammonium salt  Molecules of 5 carbon chain length and one polar group are usually soluble  Branched chains are more soluble than the corresponding straight chain  Increasing molecular weight will usually decrease solubility  Increased structure similarity between solute and solvent is accompanied by increase solubility  Polar function groups include OH, CHO, COH, CHOH, CH2OH, COOH, NO2, CO, NH2 and SO3H. Solution formulation  The formulation additives used are according to  the type of solution and  the site of administration. Thank You