家犬口服盐酸利福喷丁胶囊的药物动力学研究

Study on pharmacokinetics of rifapentine hydrochloride capsule in dogs

目的研究健康家犬口服盐酸利福喷丁胶囊的药物动力学。方法采用高效液相色谱法测定家犬交叉口服盐酸利福喷丁胶囊和参比制剂利福喷丁胶囊后的血药浓度，应用3P97程序计算主要药代动力学参数，估算其相对生物利用度，并进行等效性检验。结果盐酸利福喷丁胶囊的T1／2、Cmax、Tmax、AVC0～60分另0为（13．72±4．21）h、（22．09±7．13）mg／L、（5．17±0．41）h、（307．37±114．48）mg／（L·h），利福喷丁胶囊的上述参数分别为（14．62±3．47）h、（21．01±7．43）mg／L、（5．67±0．52）h、（291．13±104．06）mg／（L·h）。其血药浓度时间曲线均符合一级吸收的一房室模型，且两制剂药代动力学参数接近。两制剂间的lnAUC0-60，lnAUC0-∞及lnCmax经方差分析和双单侧t检验发现，两制剂之间具有生物等效性。Tmax经Wilcoxon检验发现，两制剂间也具有等效性。盐酸利福喷丁胶囊的相对生物刊用度为94．7％。结论盐酸利福喷丁胶囊和参比制剂利福喷丁胶囊生物等效。

Objective To study the pharmacokinetics of rifapentine hydrochloride capsule in dogs. Methods The plasma concentrations of rifapentine hydrochloride capsule and reference preparation rifapentine capsule were determined with HPLC in 6 dogs. The pharmacokinetic parameters and relative bioavailability and bioequivalent evaluation of two drugs were calculated by 3P97 software. Results The pharmacokinetic parameters of rifapentine hydrochloride capsule and reference preparation rifapentine capsule were as follows： T1/2 were（ 13.72 ± 4. 21 ）h and （14. 62 ± 3. 47 ） h , Cm= were （ 22. 09 ± 7.13 ） mg/L and （ 21. 01 ±7.43） mg/LTm=were （5.17±0.41）h and （5.67 ±0. 52）h,AUC0-60 were（307.37 ± 114.48）μg/（h · ml） and（291.13 ± 104. 06） μg/（h · ml）. The concentration - time curves of the two drugs confirmed to one compartment model with a first order absorption and no statistical significant difference was found in the pharmacokinetic parameters between the two drugs. The lnAUC0-60, lnAUC0-∞ and lnCmax of the two drugs were bioequivalent analyzed with analysis of variance and double single t-test,the relative bioavailability＇ of rifapentine hydrochloride capsule was 94. 7%. Conclusion Rifapentine hydrochloride capsule was bioequivalent to reference preparation rifapentine capsule.