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目的测定溴吡斯的明缓释片的体外释放和体内药代动力学,并研究其体内外相关性。方法按《中国药典》2010版二部附录XD释放度测定第二法,以磷酸缓冲液为释放介质,采用紫外分光光度法测定溴吡斯的明的累积释放百分率。6只新西兰兔采用自身交叉给药方案,单剂量口服溴吡斯的明缓释片和普通片后,采用HPLC-紫外色谱法测定不同时间点的体内血药浓度。结果溴吡斯的明缓释片12 h体外累积释放率达98.6%,其体内药动学参数如下:tmax为(4.001±0.004)h;Cmax为(15.442±0.215)mg/L;AUC0-∞为200.557±3.357。Loo-Riegelman法计算溴吡斯的明缓释片体内外的相关性,其体内累积吸收百分率与体外累积释放百分数X建立的线性回归方程为:fa=0.485 1 fr+3.837 7,r=0.986 5,大于临界值r6,0.01(P<0.01)。结论溴吡斯的明缓释片释放行为的体内外相关性显著,通过体外释放行为可预测其体内释放动力学。
Objective To determine the in vitro release and in vivo pharmacokinetics of dibenzamine sustained release tablets and to study its in vitro and in vivo correlation. Methods According to “Chinese Pharmacopoeia” 2010 edition two appendix XD release determination of the second method, with phosphate buffer as the release medium, the use of UV spectrophotometry Determination of the cumulative release percentage of pyridostigmine. Six New Zealand rabbits adopted their own cross-over regimen. After a single oral dose of pyridostigmine sustained-release tablets and ordinary tablets, the HPLC-UV method was used to determine the in vivo plasma concentrations at different time points. Results The cumulative release rate of meclizine sustained-release tablets in 12 h was 98.6%. The in vivo pharmacokinetic parameters were as follows: tmax was (4.001 ± 0.004) h; Cmax was (15.442 ± 0.215) mg / L; AUC0-∞ 200.557 ± 3.357. The linear regression equation established by Loo-Riegelman method for the in vitro and in vivo dosages of dibenzopyr sustained release tablets was established as follows: fa = 0.485 1 fr + 3.837 7, r = 0.986 5 , Greater than the critical value r6, 0.01 (P <0.01). Conclusion The in vitro and in vivo correlations of the release behavior of pyridostigmine in sustained release tablets are significant. The in vivo release kinetics can be predicted by in vitro release behavior.