【摘要】 本文用青霉素Ｖ钾胶囊剂与进口青霉素Ｖ钾片剂进行人体药代动力学和生物利用度研究。选择１２名健康男性志愿者，采用自身交叉对照试验方法，分别单剂量一次口服青霉素Ｖ钾５００ｍｇ，青霉素Ｖ钾血药浓度用微生物法测定，以枯草芽孢杆菌（６３５０１）作为检定菌。青霉素Ｖ钾血药浓度－时间数据用３ｐ８７程序进行自动拟合并求算药代动力学参数，用ＮＤＳＴ程序对ＡＵＣ、Ｔ_ｍａｘ和Ｃ_ｍａｘ的实测值作生物等效性检验。结果：口服青霉素Ｖ钾片剂和胶囊剂两种制剂后青霉素Ｖ钾药代动力学参数分别为： Ｔ（１／２）为３１．２７ ± １１．１２ｍｉｎ，２７．５７ ± ６．４６ｍｉｎ（Ｐ＞０．０５）；Ｃ_ｍａｘ为９．１４± ３．０７ｍｇ Ｌ^－１，９．６９ ± ２．６６ｍｇ· Ｌ^－１（Ｐ＞０．０５）。青霉素Ｖ钾的相对生物利用度为９７．９９％±１３．４４％。结论：青霉素Ｖ钾的ＡＵＣ、Ｔ_ｍａｘ和Ｃ_ｍａｘ经配对ｔ检验、双单侧ｔ检验、方差分析表明国产青霉素Ｖ钾胶囊剂与进口青霉素Ｖ钾片剂为等效制剂。更多还原

【Abstract】 The pharmacokinetics and bioavailability of penicillin V were conducted in 12 Chinese healthy volunteers after a single oral dose（500mg）of home made penicillin V capsule compared with penicillin V tablet imported.In this paper,microbiological assay was used,plasma penicillin V concentration was determined by using Bacillus subtilis（CMCC 63501 ）as test strain.The concentration time curves of penicillin V were fitted to one compartment model estimated by 3p87 program. Statistical software’s NDST were used for the calculation of results.The mean terminal half-life(T_1/2) of the two preparations, tablet and capsule, were 31 .27 ± 11. 12 and 27.57 ± 6.46 min respectively （P >0.05）,and the averages of the peak plasma levels(C_max) were 9.14 ± 3.07 and 9.69 ± 2.66 μ g· ml^-1respectively （P >0.05）.The relative bioavailability of penicillin V capsule compared with tablet was 97.99 1 13.M%.The results showed that the two preparations were bioequivalent.更多还原