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目的:考察戊己胃漂浮缓释片中4种成分的体外释放规律及其在家兔胃内的滞留时间。方法:采用浆法测定戊己胃漂浮缓释片的体外释放度,以含0.8%聚山梨酯-80的0.1 mol·mL-1盐酸溶液为释放介质,运用HPLC测定戊己胃漂浮缓释片中盐酸小檗碱、吴茱萸碱和吴茱萸次碱、芍药苷在12 h内的体外累积释放率,色谱条件为Thermo-ODS2-Hypersil色谱柱(4.6 mm×250 mm,5μm),流动相乙腈(A)-0.05 mol·L-1磷酸二氢钾(B)梯度洗脱(0~20 min,11%A;22~44 min,28%A;46~70 min,40%A),检测波长225 nm;对数正态分布模型、威布尔分布函数和Higuich方程进行溶出动力学模拟,利用γ-闪烁照相法考察戊己胃漂浮缓释片在家兔胃内的滞留时间。结果:4种成分的体外释放均符合Higuchi模型,戊己胃漂浮缓释片可在家兔胃内滞留6 h。结论:饱腹状态下,戊己胃漂浮缓释片在家兔胃内的滞留时间明显长于禁食状态下,提示食物可能对该制剂在胃内的滞留时间具有显著性影响。
OBJECTIVE: To investigate the in vitro release patterns of four components in pentosidine floating tablets and its residence time in rabbit stomach. Methods: The in vitro release of pentoxylamine floating sustained-release tablets was determined by using the plasma method. The 0.1 mol · mL -1 hydrochloric acid solution containing 0.8% polysorbate-80 as the release medium and the pentoxylamine floating sustained-release tablets The results showed that the cumulative release rates of berberine hydrochloride, evodiamine, rutaecarpine and paeoniflorin in 12 h were in vitro. The chromatographic conditions were Thermo-ODS2-Hypersil column (4.6 mm × 250 mm, 5 μm) ) Gradient of -0.05 mol·L -1 potassium dihydrogen phosphate (B) (0-20 min, 11% A; 22-44 min, 28% A; 46-70 min, 40% A) nm logarithmic normal distribution model, Weibull distribution function and Higuich equation. The residence time of pentoxylamine floating sustained-release tablets in rabbit stomach was investigated by γ-scintigraphy. Results: The in vitro release of four components were in accordance with Higuchi model, and the pentoxylamine floating sustained release tablets could be retained in the stomach of rabbits for 6 h. CONCLUSION: In full stomach condition, the retention time of edema sustained release tablets in rabbits stomach is significantly longer than that in fasting condition, suggesting that food may have a significant effect on the retention time of the preparation in the stomach.