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目的:观察研究制备的双嘧达莫胃漂浮型缓释微丸在Beagle犬体内的药动学参数并对其体内外相关性做出评价。方法:对6条Beagle犬进行双周期双交叉实验,采用高效液相色谱法测定不同时间Beagle犬血浆中的药物浓度并利用DAS2.0统计软件计算有关药动学参数。采用Wanger-Nelson法计算体内吸收百分数。结果:双嘧达莫胃漂浮型缓释微丸与普通片主要药动学参数分别为tmax(8.333±0.516)和(1.833±0.258)h;Cmax(4.085±0.819)和(5.473±0.735)μg.mL-1;t1/2(3.378±0.967)和(3.159±1.128)h;AUC0～t(40.375±9.459)和(15.365±3.527)μg.h.mL-1,且体内外相关性较好。结论:双嘧达莫胃漂浮型缓释微丸的血药浓度平稳,与普通片相比,其可较长时间保持有效的血药浓度。
OBJECTIVE: To observe the pharmacokinetic parameters of dipyridamole floating sustained-release pellets prepared in Beagle dogs and to evaluate their in vitro and in vivo correlation. Methods: Six Beagle dogs were subjected to double-cycle double-crossover test. The plasma concentrations of Beagle dogs were determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters were calculated by DAS2.0 statistical software. In vivo absorption percentage was calculated using the Wanger-Nelson method. RESULTS: The main pharmacokinetic parameters of dipyridamole gastric floating sustained-release pellets and ordinary tablets were tmax (8.333 ± 0.516) and (1.833 ± 0.258) h respectively; Cmax (4.085 ± 0.819) and (5.473 ± 0.735) μg mL-1, t1 / 2 (3.378 ± 0.967) and (3.159 ± 1.128) h, AUC0 ~ t (40.375 ± 9.459) and (15.365 ± 3.527) μg.h.mL- . Conclusion: The dipyridamole gastric floating sustained-release pellets have a steady plasma concentration, which can maintain the effective plasma concentration for a long time compared with ordinary tablets.