甲苯磺酸舒他西林分散片人体生物利用度实验研究

建立了测定人血浆中氨苄西林和舒巴坦浓度的高效液相色谱 紫外检测法，采用此方法测定１０ 名健康男性志愿者单剂量交叉口服７５０ ｍｇ 甲苯磺酸舒他西林分散片（ 受试制剂） 和优立新片（ 参比制剂） 后血浆中氨苄西林和舒巴坦的浓度，发现受试者服用优立新后，血浆中氨苄西林和舒巴坦的Ｃｍａｘ 分别为（１０－３２ ±２－９４） 和（１０－１６ ±３－１３）μｇ／ｍＬ，摩尔比为０－６８∶１ ．同时考察氨苄西林和舒巴坦的药物动力学特性，进行生物等效性评价．结果为受试制剂中氨苄西林的相对生物利用度为（１１０－３ ±２０－６） ％ ；舒巴坦为（１０８－０ ±２０－１）％ ．对受试制剂和参比制剂的主要药物动力学参数进行统计学分析，结果表明２ 种制剂生物等效

A Study on Bioavailability of the Sultamicillin Dissoluble Tablets

A sensitive and reliable HPLC UV method was established and validated for determination of ampicillin and sulbactam in human plasma respectively.Plasma levels of both substances in 10 healthy volunteers were determined by the method after administration of 750 mg single dose of sultamicillin dissoluble tablets (test formulation) and Unasyn(reference formulation) in an open randomized cross over trial.It was found that C -{max} of ampicillin and sulbactam were (10^32±2^94) and (10^16±3^13)μg/mL respectively(molar ratio,0^68∶1).The pharmacokinetics and bioavailability of ampicillin and sulbactam were also studied.The relative bioavailability of ampicillin was (110^3±20^6)%,and that of sulbactam was (108^0±20^1)%.The statistical analysis results showed that there was no apparent difference between the test formulation and reference formulation.The two formulations were bioequivalent.