左金丸总生物碱胃黏附缓释微球研究

Study on stomach adhesion and sustained releasing microspheres containing total alkaloid from Zuojin pill

关键词:  左金丸  总生物碱  壳聚糖  胃黏附  微球

Key words:  Zuojin pill  total alkaloid from Zuojin pill  chitosan  stomach adhesion  microspheres

摘要:

[目的] 制备载左金丸总生物碱的壳聚糖包裹明胶海藻酸钠载药微球,并考察其释放和胃黏附特性。[方法] 制备胃黏附微球,通过高效液相色谱(HPLC)法测定微球载药量与包封率,通过转篮法测定微球体外释药性能,将微球黏附于大鼠胃黏膜上测其体外生物黏附性。[结果] 微球载药量测定结果:盐酸药根碱2.768 mg/g,盐酸巴马汀3.986 mg/g,盐酸小檗碱21.920 mg/g,吴茱萸碱1.449 mg/g,吴茱萸次碱0.954 mg/g。5种生物碱在8 h内持续释放,微球的胃黏附百分率为89.33%。 [结论] 壳聚糖交联的载左金丸总生物碱微球具有较好的释药性及胃黏附特性。

Abstract:

[Objective] To evaluate the technological feasibility of delivering total alkaloid from Zuojin pill using chitosan coated alginate/gelatin microspheres and determine the release behavior and bioadhesive properties. [Methods] The microspheres were prepared by an emulsification technique. Drug loading, encapsulation yield and release studies were also assessed by HPLC according to the Chinese pharmacopoeia. The bioadhesive property of microspheres was determined when it was adhered on the gastric mucosa of rat in vitro. [Results] The results of practical drug loading efficiency: hydrochloride jatrorrhizine was 2.768 mg/g, hydrochloride palmatine 3.986 mg/g, hydrochloride berberine 21.920 mg/g, evodiamine 1.449 mg/g, rutaecarpine 0.954 mg/g. The results of drug release behavior and bioadhesive properties studies on gastric mucoadhesive microspheres showed that the microspheres were continuously releasing drugs for 8 h and the stomach adhesion percentage was 89.33%. [Conclusion] The results imply that the microspheres are a useful dosage form to increase drug loading for the poorly water-soluble drugs by encapsulating with chitosan. It also indicated that they have satisfactory sustained releasing behavior in simulated gastric fluid.