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目的:制备一种新型乌贝速释片,并研究该剂型与乌贝散在Beagle犬体内的药代动力学和生物等效性。方法:采取粉末直接压片法制备乌贝速释片,将6只Beagle犬随机分为2组,分别口服给予乌贝速释片和乌贝散,采用LC-MS/MS测定给药后不同时刻血浆中贝母素甲的浓度,采用DAS 2.0软件按非房室模型处理得药动学参数,评价速释片剂与散剂的生物等效性。结果:乌贝速释片中贝母素甲的主要药动学参数为Cmax(7.4±2.3)μg·L-1,AUC0-t(59.13±15.25)μg·L-1·h-1,Tmax(1.5±0.0)h,乌贝散中贝母素甲的主要药动学参数为Cmax(8.0±1.7)μg·L-1,AUC0-t(68.78±16.27)μg·L-1·h-1,Tmax(1.5±0.0)h,乌贝速释片中贝母素甲的lnAUC0-t和lnCmax的90%置信区间分别为乌贝散相应参数的95.4%～104.6%,90.9%～109.1%。结论:自制的乌贝速释片与乌贝散具有生物等效性,且生产工艺简单,服用方便。
OBJECTIVE: To prepare a new type of Ubbeli fast-release tablets and study its pharmacokinetics and bioequivalence in Beagle dogs. Methods: Ube sustained release tablets were prepared by powder direct compression method. Six Beagle dogs were randomly divided into two groups. Obese instantaneous release tablets and Ube powder were orally administered. LC-MS / MS was used to determine the difference Time plasma concentrations of peimine A, using DAS 2.0 software non-compartmental model treated pharmacokinetic parameters, evaluation of immediate-release tablets and powder bioequivalence. Results: The main pharmacokinetic parameters of clarithromycin A in Uubel immediate-release tablets were Cmax (7.4 ± 2.3) μg · L-1, AUC0-t (59.13 ± 15.25) μg · L-1 · h-1, (1.5 ± 0.0) h, and the main pharmacokinetic parameters of Peucedanum pearl A were Cmax (8.0 ± 1.7) μg · L-1, AUC0-t (68.78 ± 16.27 μg · L-1 · h- 1, Tmax (1.5 ± 0.0) h. The 90% confidence intervals of lnAUC0-t and lnCmax of peperetinin in Wuube fast-release tablets were 95.4% -104.6% and 90.9% -109.1% . Conclusion: The self-made Ubbeli fast release tablets and the Ube powder have bioequivalence, and the production process is simple, easy to take.