Studies on dissolution tests of solid dosage forms. IV. Relation of absorption sites of sulfonamides administered orally in solid dosage form to their solubilities and dissolution rates.

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The relation of absorption sites of sulfonamides administered orally in uncoated tablets to their solubilities and dissolution rates was studied. Eight sulfonamides, sulfisomidine, sulfamethoxypyridazine, sulfamethizole, sulfamethoxazole, sulfisoxazole, sulfamonomethoxine, sulfaphenazole and sulfadimethoxine, were tested to determine their solubilities, dissolution rates and absorption rates following oral administration to humans. As a marker of gastric emptying time, the lag time of the urinary excretion of total salicylate was determined after the concurrent administration of enteric tablets of aspirin. A new parameter, RAAS (Relative Amount Absorbed in the Stomach) is proposed in order to represent the relative amount absorbed in the stomach region. RAAS values showed good correlations with the solubilities and dissolution rates of sulfonamides determined by means of the Sartorius solubility simulator with continuous pH change under non-sink conditions. It was concluded that : 1) The critical value of the solubility which distinguishes drugs according to their absorption sites, stomach or intestine, is about 3 mg/ml in 0.1 N HCl at 37° when 1 g of the drug is administered to humans orally with 200 ml of water after overnight fasting. 2) A drug having a solubility larger than the critical value can reasonably be tested for dissolution rate in an acidic medium, and a drug having a solubility less than the critical value should be tested under neutral conditions after pretreatment in acidic conditions.

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