Effect of the Extent of Pharmaceutical Formulation on Bioavailability of Sulfamethoxazol in Human

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Abstract
In order to examine the effect of the amount of starch as a binder in the preparation of tablets on the bioavailability of drugs in humans, sulfamethoxazole tablets were prepared with the amount of starch varied from 5, 10 and 15%, and a mixed powder and fine granules prepared with the same composition as the tablets with 5% starch, and these 5 preparations were submitted to the dissolution test and measurement of sulfamethoxazole in serum after a single administration in healthy females. The dissolution rate tended to prolong with increasing amount of starch, but little difference was found in the area under blood concentration curve (AUC) of sulfamethoxazole by increase in the amount of starch. This difference in the in vitro and in vivo results was considered to be due to the rapid transition of the tablet into the intestines when administered on any empty stomach, and because the tablets are rapidly disintegrated and dissolved in the intestines by the use of a digestible starch, and because sulfamethoxazole dissolves easily at pH above 6.5. In the case of a mixed powder, maximum serum level of sulfamethoxazole was the lowest among all preparations, and the time to reach the maximum was also delayed. The reason for this was considered to be because moistening of the sulfa powder with water is rather poor in the mixed powder, the sulfa attaches on the stomach wall, becomes mixed with food and its transition into the intestine is delayed. Such delay in reaching the maximum serum level was not observed in fine granules.

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