复方替加氟胃滞留型缓释片的处方研究

目的：为了延长药物在胃内的滞留时间,研究复方替加氟胃滞留型缓释片的处方。方法：比较不同规格的卡波姆（Carbopol）及羟丙甲纤维素（HPMC）的黏附性及膨胀性,采用3因素3水平L9（3^3）正交设计法以起漂时间、漂浮持续时间、黏附力大小及释放度作为指标选择最佳处方,并进一步考察了影响释放度的因素。采用γ-闪烁扫描技术监测片剂在胃内运行情况。结果：通过正交设计确定处方为：Carbopol 934p 36 mg,HPMC K15M 144 mg,硬脂酸90 mg。该处方能延长胃滞留时间,且释药理想。结论：通过处方研究自制胃滞留型缓释片在胃中滞留时间长,释药平缓。

Formula study on gastric-retention sustained-release tablets of compound tegafur

Aim:To prepare and characterize gastricretention sustained-release tablets of compound tegafur which is expected to prolong its time in stomach,improve targeting,and reduce side effects.Methods:The adhesiveness and expansibility of Carbopol and HPMC of different viscosity were evaluated by adhesion radiometer and expansion cells designed and made by our lab.Orthogonal experimental design was used to aid the optimization of the formula based on the index such as the time to start floating and lasting time,the adhesive force,the drug release rate and its influence factors.In vivo behaviors were evaluated by gamma-scintigraphy.Results:The optimization formula deside by orthogonal experimental design is that Carbopol 934p 36 mg,HPMC K15M 144 mg and stearic acid 90 mg.This formula has long gastic-retention time and delay drug release.Conclusion:The gastric-retention sustained-release tablets could remian in stomach for a long time and delay drug release.