国产舒他西林胶囊的相对生物利用度

Relative bioavailability of domestic sultamicillin capsule

目的：了解国产舒他西林胶囊的相对生物利用度，评价其生物等效性。方法：１０名健康志愿者随机交叉ｐｏ单剂量７５０ｍｇ国产舒他西林胶囊和进口片剂后，采用ＨＰＬＣ测定血浆中的血药浓度。结果：口服国产舒他西林胶囊和进口片剂后，利用ＨＰＬＣ测得血浆中药物浓度舒巴坦分别在（３８．６６±１０．３９）ｍｉｎ和（３６．６８±１１．３７）ｍｉｎ达到峰值（３．４５±２．６３）ｍｇ·Ｌ－１和（４．２１±３．６７）ｍｇ·Ｌ－１；氨苄西林分别在（２６．１３±５．９８）ｍｉｎ和（２８．００±７．５４）ｍｉｎ达到峰值（７．１１±２．１９）ｍｇ·Ｌ－１和（７．４６±２．７９）ｍｇ·Ｌ－１。血药浓度曲线下面积舒巴坦分别为（６２９．９８±１７７．３４）ｍｇ·ｍｉｎ·Ｌ－１和（６８７．７８±２２５．４４）ｍｇ·ｍｉｎ·Ｌ－１；氨苄西林分别为（６９３．８７±１９２．１５）ｍｇ·ｍｉｎ·Ｌ－１和（７０８．８７±２０２．４８）ｍｇ·ｍｉｎ·Ｌ－１。经药代动力学程序计算拟合后，发现氨苄西林和舒巴坦在体内的过程符合一级吸收和消除的二室模型。国产舒他西林胶囊的相对生物利用度舒巴坦为９５％（８１％～１１８％），氨苄西林为９９％（８１％～１１５％）两药的主要药代动?

OBJECTIVE:To observe the relative bioavailability of domestic sultamicillin and evaluate the bioequivalence between the domestic capsule and the imported tablet.METHODS:The pharmacokinetics of sultamicillin capsule was determined following a single oral dose of 750mg give to 10 volunteers in an open randomized crossover study.Drug concentration in plasma was assayed by HPLC method.RESULTS:The sulbactam peak levels in plasma averaged(3.45±2.63) and (4.21±3.67)mg·L -1 at (38.66±10.39)and(36.68±11.37)min,respectively.The ampicillin peak levels in plasma averaged(7.11±2.19)and(7.46±2.79)mg·L -1 at(26.13±5.98)and(28.00±7.54)min,respectively.The AUC were (629.98±177.34) and (687.78±225.44)mg·min·L -1 for (693.87±192.15) and (708.87±202.48)mg·min·L -1 for domestic capsule and improrted tablet respectively.The concentration time courses after medication conformed to a 2 compartment open model with a first order obsorption.The sulbactam bioavailability of domestic capsule was 95%(81%～118%),the ampicillin bioavailability of it was 99%(81%～115%) compared with the standard preparation.The pharmacokinetic parameters between two products had no significant difference ( P >0.05).CONCLUSION:The two formulations were of bioequivalence.