Simultaneous in vitro and in vivo evaluation of both trimethoprim and sulfamethoxazole from certain dosage forms.
The dissolution rates of trimethoprim (T), and sulphamethoxazole (S), from different brands of tablets and suspensions were studied at pH = 1.1 and 7.2. The bioavailabilities of both drugs in humans were studied by the urine excretion method. The dissolution rates were dependent on the pH of the dissolution medium, the solubilities of the drugs at the pH involved, the dosage form and the brand studied. While the dissolution rates of T from all brands studied were consistent with their pH-dependent solubility, those of S were not. The dissolution rates of S from suspensions were found to be equal at pH = 7.2, but different at pH = 1.1. A correlation existed between the dissolution rate of T at pH = 1.1 from tablets and the excretion rate in humans. With S, however, no such correlation was observed at either pH.
D000042:Absorption; D000328:Adult; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004338:Drug Combinations / Q000032:analysis / Q000378:metabolism; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D012995:Solubility; D013420:Sulfamethoxazole / Q000032:analysis* / Q000378:metabolism; D013535:Suspensions; D013607:Tablets; D014295:Trimethoprim / Q000032:analysis* / Q000378:metabolism; D015662:Trimethoprim, Sulfamethoxazole Drug Combination
D004338:Drug Combinations; D013535:Suspensions; D013607:Tablets; D015662:Trimethoprim, Sulfamethoxazole Drug Combination; D014295:Trimethoprim; D013420:Sulfamethoxazole