论文部分内容阅读
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。
In this paper, penicillin V potassium capsules and imported penicillin V potassium tablets for human pharmacokinetics and bioavailability studies. Twelve healthy male volunteers were selected and their own cross-over control test method was adopted. The single oral dose of penicillin V potassium was 500mg. The concentration of penicillin V potassium was determined by microbiological method and Bacillus subtilis (63501) was used as the test strain. Penicillin V potassium concentration-time data were automatically fitted using the 3p87 program and the pharmacokinetic parameters were calculated. Bioassay was performed using the NDST program for the AUC, T max and C max values. Results: The pharmacokinetic parameters of penicillin V potassium after oral administration of penicillin V potassium tablet and capsule were as follows: T (1/2) was 31.27 ± 11.12min, 27.57 ± 6.46min (P > 0.05); C max was 9.14 ± 3.07 mg L -1 and 9.69 ± 2.66 mg · L -1, respectively (P> 0.05). The relative bioavailability of penicillin V potassium was 97.99% ± 13.44%. CONCLUSION: The AUC, T max and C max of penicillin V potassium were tested by paired t-test and two-sided one-sided t-test. The ANOVA analysis showed that penicillin V potassium capsule was equivalent to imported penicillin V potassium tablet.