新诺明片生物利用度的研究 1.新诺明片体外释放、兔体和人体内生物利用度

<正> 新诺明——磺胺甲基异噁唑及其制剂是常用的磺胺类药物,各国药典多有收载,由于其理化性质:如溶解度低(几乎不溶于水)、在不同pH值条件下吸收度不同、并存在多晶观象、以及产品质量波动等原因。所以对此药物及其制剂生物利用度的研究已经引起人们的注意。 1972年Mattok在稀盐酸溶液中用转篮法测定了磺胺甲基异噁唑片等磺胺类药物的溶出

STUDIES ON THE BIOAVAJLABJUTY OF SULFAMETHOXAZOLE TABLETS 1. Jnvetigation of Release in Vitro and Availability in Vivo (in Rabbits and in Human) of Sulfamethoxazole Tablets

Sulfamethoxazole tablet samples from ten different factories in the country were used in this study. Their release in vitro (using the rotating basket method 37°±0.5, rpm=100, didutc hydrochloric acid(7 in 100)as the dissolution medium) and availability in vivo (in rabbits and in human) were investigated. The results obtained from the variance analysis of the experimental parameters (Ymax the peak drug concentration in blood, Tmax the time of occurrence of peak drug concentration in the blood, and A the area under the blood drug concentration versus time curve) showed that the release in vitro and absorption in rabbits and in human were different from tablets to tablets produced by different factories. Therefore, it is necessary to make a criterian for the quality control of sulfamethoxazole tablets. A series of regression equations were formulated from the parameters. If one of the parameters is available, other parameters in vitro and/or in vivo could be made known using these equations. Based on the experimental results, the authors suggest that the parameter T(?) or T(?) in the rotating basket method be adopted as criterian in the standardization of quality control of sulfamethoxazole tablets in the Pharmacopoeia.