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目的:建立高效液相色谱法(HPLC)测定BeagIe犬血清中愈创木酚甘油醚的浓度,研究愈创木酚甘油醚缓释片在Beagle犬体内的药动学与相对生物利用度。方法:采用HPLC测定6只Beagle犬口服供试品愈创木酚甘油醚缓释片及参比制剂愈创木酚甘油醚普通片后的经时血药浓度,计算主要药动学参数及相对生物利用度,并进行等效性检验。结果:供试品与参比制剂的主要药动学参数分别是:t_(max)为(1.83±0.26)h和(0.92±0.13)h,C_(max)为(4.7±11.6),(7.4±0.7)mg·L~(-1);AUG_(0-T)为(18.4±2.0),(17.3±2.5)mg·h~(-1)·L~(-1),AUG_(0-∞)为(19.8±2.4),(18.4±2.8)mg·h~(-1)·L~(-1)。两制剂间的lnAUG(0-T)及ln AUG_(0-∞)经方差分析和双单侧t检验,表明两制剂具有生物等效性。愈创木酚甘油醚缓释片的相对生物利用度F_(0-T)为(107.1±8.0)%,F_(0-∞)为(108.3±9.0)%。结论:愈创木酚甘油醚缓释片在Beagle犬体内具有缓释效果,与参比制剂愈创木酚甘油醚普通片生物等效。
Objective: To establish a high performance liquid chromatography (HPLC) method for the determination of guaifenesin in beagle dog serum and to study the pharmacokinetics and relative bioavailability of guaifenesin sustained-release tablets in Beagle dogs. Methods: The pharmacokinetic parameters and their relative pharmacokinetic parameters were determined by HPLC after oral administration of guaifenesin sustained-release tablets and reference preparations of guaifenesin-normal tablets to six Beagle dogs. Bioavailability, and the equivalence test. Results: The main pharmacokinetic parameters of test and reference preparations were as follows: t max was 1.83 ± 0.26 h and 0.92 ± 0.13 h, C max was 4.7 ± 11.6, ± 0.7) mg · L -1; AUG 0-T was (18.4 ± 2.0), (17.3 ± 2.5) mg · h -1 · L -1, AUG 0- ∞) were (19.8 ± 2.4) and (18.4 ± 2.8) mg · h -1 · L -1, respectively. The differences in lnAUG (0-T) and ln AUG_ (0-∞) between the two formulations were analyzed by ANOVA and two-sided one-tailed t-tests, indicating that the two formulations were bioequivalent. The relative bioavailability of guaifenesin sustained release tablets was (107.1 ± 8.0)% and (0-∞) was (108.3 ± 9.0)%, respectively. CONCLUSION: The guaifenesin sustained-release tablets have a slow-release effect in Beagle dogs and are bioequivalent to the reference tablets of guaifenesin-normal tablets.