异硫氰酸苄基酯包合物胃漂浮片的制备

Preparation of Stomach buoyant tablets containing benzyl isothiocyanate inclusions

目的掩盖异硫氰酸苄基酯的刺激性气味,提高稳定性,延长其在体内的作用时间。方法先采用饱和水溶液法将异硫氰酸苄基酯用2-羟丙基-β-环糊精包合,再以HPMC为主的凝胶骨架材料将该包合物制备成胃漂浮片,采用正交设计优化处方。结果得到包封率为80%的包合物,以及在模拟人工胃液中能立即起漂且持漂时间达8 h的胃漂浮缓释片剂。结论制备的异硫氰酸苄基酯包合物胃漂浮片的漂浮性能良好,且能掩盖其刺激性气味,达到缓释效果。

OBJECTIVE To conceal the pungent odor of benzyl isothiocyanate, improve stability and prolong the time of action in vivo. METHODS At first, Benzyl isothiocyanate was included in modified 2 - hydroxypropyl - β - cyclodextrin （2 - HP - β - CD） by saturated solution stirring method, then HPMC was used as the main material of gel matrix to prepare the Stomach buoyant tablets. Orthogonal design was adopted to optimize prescription. RESULTS The result of encapsulation rate could reach 80% and the tablet optimized prescription soak in the acidic mediums （pill. 0 ）, in which immediate float could prolong the drug release time, comparing to that from BITC without 2 - HP - β - CD. CONCLUSION Isothiocyanate inclusion complexes of Stomach buoyant tablets shows buoyancy during the whole release process, and it provides the sustained release properties.