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目的:比较美乐托宁缓释片与普通片在Beagle犬体内的药动学参数。方法:6条Beagle犬三交叉单剂量口服美乐托宁缓释片、普通片和国外缓释片6 mg后,采用LC-MS-MS法测定血浆药物浓度,计算各制剂的药动学参数。结果:上述3种制剂在Beagle犬血浆中的Cmax分别为(8.929±5.220),(29.653±14.503)和(8.196±4.723)ng.mL-1,Tmax分别为(1.140±0.608),(0.250±0.051)和(1.083±0.492)h,t1/2分别为(1.723±1.080),(0.946±0.548)和(1.105±0.308)h,MRT分别为(1.834±0.651),(0.784±0.637)和(1.617±0.296)h,AUC0-12分别为(13.832±6.967),(12.272±5.623)和(14.190±7.003)ng.mL-1.h,AUC0～∞分别为(13.873±6.941),(12.308±5.556)和(14.216±7.004)ng.mL-1.h。结论:与普通片比较,缓释片吸收较慢,药物达峰时间更长,峰浓度更低,维持时间更长。3种制剂具有生物等效性。
OBJECTIVE: To compare the pharmacokinetic parameters of Meleotronine sustained release tablets and common tablets in Beagle dogs. Methods: Six Beagle dogs were treated with triple crossover single dose of Melatonu sustained release tablets, common tablets and 6 mg sustained-release tablets from foreign countries. The plasma drug concentrations were determined by LC-MS-MS. The pharmacokinetic parameters . Results: The Cmax of Beagle dogs were (8.929 ± 5.220), (29.653 ± 14.503) and (8.196 ± 4.723) ng.mL-1, respectively, and the Tmax were (1.140 ± 0.608) and (0.250 ± (1.723 ± 1.080), (0.946 ± 0.548) and (1.105 ± 0.308) h, respectively, and the MRT were (1.834 ± 0.651), (0.784 ± 0.637) and 1.617 ± 0.296) h and AUC0-12 were (13.832 ± 6.967), (12.272 ± 5.623) and (14.190 ± 7.003) ng.mL-1.h respectively, AUC0 ~ ∞ were (13.873 ± 6.941) and (12.308 ± 5.556) and (14.216 ± 7.004) ng.mL-1.h. Conclusion: Compared with ordinary tablets, sustained-release tablets absorb slower, the drug peak longer, peak concentration lower, longer maintenance. Three formulations were bioequivalent.