魔芋葡甘聚糖超多孔复合水凝胶作为胃滞留给药载体的研究

Superporous hydrogel composite of Konjac glucomanan as gastroretentive drug carriers

目的:考察魔芋葡甘聚糖超多孔复合水凝胶(KGM-SPHC)作为胃滞留给药载体的性能。方法:比较加入KGM前后体系对大鼠胃黏膜的黏附力及其体外溶胀和溶蚀行为,制备载苦参碱的缓释胶囊并考察其体外释放度和犬口服后的药物动力学特征。结果:KGM的加入改善了体系的黏膜黏附力,体外溶胀性能增强、溶蚀更缓慢;体系遇水10 s内迅速起漂并长时间(>17 h)持续漂浮;与普通胶囊相比,载药缓释胶囊体外缓释特征显著,犬口服后体内达峰时间和平均滞留时间显著延长。结论:KGM-SPHC兼有膨胀、漂浮、黏附等性能,是一种优良的胃滞留给药载体。

OBJECTIVE To evaluate the properties of Konjac glucomannan superporous hydrogel compaosite （KGM-SPHC） as gastroretentive drug carrier. METHODS The adhesive force, swelling and erosion kinetics of KGM-SPHC and SPH were compared in vitro. Matrine-loaded sustained release capsules were prepared and investigated on their in vitro release profiles and in vivo pharmacokinetics after oral administration in Beagle dogs. RESULTS The adhesive force of SPH was improved byadding KGM. KGM-SPHC showed better swelling and erosion performance than single SPH, and the system floated up in less than 10 seconds and kept floating for more than 17 h. Matrine-loaded KGM-SPHC capsules showed sustained release profile in vitro, and prolonged and MRT＇ in vivo as well. CONCLUSION With its excellent properties of floating, swelling and bio adhesion, KGM-SPHC could be used as an ideal carrier for gastroretentive drug delivery systems.