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目的:比较愈创甘油醚双层缓释片与普通片在犬体內药动学特征。方法:Beagle犬单剂量给予600mg愈创甘油醚双层缓释片或愈创甘油醚普通片后,用RP-HPLC法测定犬血浆中愈创甘油醚的药物浓度,计算药动学参数和相对生物利用度。结果:Beagle犬单剂量口服给药后,受试制剂和参比制剂中愈创甘油醚的AUC_(0-12h)分别为(15.96±6.41)μg·h·ml~(-1)和(19.23±4.96)μg·h·ml~(-1);C_(max)分别为(7.31±2.86)μg·ml~(-1)和(14.24±5.34)μg·ml~(-1);t_(max)分别为(0.79±0.25)h和(1.08±0.38)h;t_(1/2)分别为(2.50±1.67)h和(0.42±0.05)h;MRT_(0-1)分别为(2.37±0.61)h和(1.42±0.30)h。结论:愈创甘油醚双层缓释片的C_(max)较普通片显著降低,MRT_(0-1)和t_(1/2)明显延长,差异有统计学意义(P<0.05),说明该受试制剂具备一定的缓释药动学特征。
Objective: To compare the pharmacokinetics of guaifenesin double-layered sustained-release tablets and common tablets in dogs. Methods: Beagle dogs single dose of 600mg guaifenesin double-coated tablets or guaifenesin ordinary tablets, RP-HPLC method for the determination of dog plasma guaifenesin drug concentration calculated pharmacokinetic parameters and relative bioavailability. Results: The AUC_ (0-12h) of guaifenesin in test and reference preparations were (15.96 ± 6.41) μg · h · ml -1 and (19.23 ± 4.96 μg · h · ml -1 and C max were (7.31 ± 2.86) μg · ml -1 and (14.24 ± 5.34) μg · ml -1, respectively; t_ ( max were (0.79 ± 0.25) h and (1.08 ± 0.38) h respectively; t 1/2 was (2.50 ± 1.67) h and (0.42 ± 0.05) h respectively; MRT 0-1 was (2.37 ± 0.61) h and (1.42 ± 0.30) h. CONCLUSION: The C max of guaifenesin double-coated sustained-release tablets were significantly lower than those of normal tablets, and MRT 0-1 and t 1/2 were significantly prolonged (P 0.05) The test preparation has certain sustained-release pharmacokinetic characteristics.