白及纯化物/氧化魔芋葡甘聚糖胃漂浮片的制备优化与评价

Preparation and Evaluation of Purified Bletilla Striata/oxidized Konjac Glucomannan Gastric Floating Tablets

以盐酸环丙沙星为模式药物,采用不同浓度乙醇纯化白及,通过测试白及纯化物/氧化魔芋葡甘聚糖胃漂浮片的漂浮性能和释药性能优化白及纯化物和氧化魔芋葡甘聚糖的配方比例,通过测试载药材料孔隙率、形貌、分子量和胃漂浮片的溶胀率、溶蚀率分析其体外释药机制。结果表明:用体积分数70%乙醇纯化得到的白及纯化物,其多糖质量分数最高,为84.88%,表观黏度最大,为22.25 mPa·s,分子量为2.372×10^(5) g/mol;当氧化魔芋葡甘聚糖与白及纯化物质量比为8∶2时,其孔隙率为77.40%,制备的胃漂浮片立即起漂,续漂时间大于12 h;2 h的药物累积释放率最小,为22.80%,12 h药物累积释放率为89.05%;药物释放指数为0.64,其释药机制为Fick扩散和骨架溶蚀协同作用。在氧化魔芋葡甘聚糖与白及纯化物质量比为8∶2时可获得漂浮性和释药性最佳的白及纯化物/氧化魔芋葡甘聚糖胃漂浮片。

In order to optimize the ratio of purified Bletilla striata and oxidized konjac glucomannan in formula,this study adopted ciprofloxacin hydrochloride as model drug to test the floating performance and drug release performance of Bletilla striata purified with different concentration of ethanol/oxidized konjac glucomannan gastric floating tablets.The mechanism of drug release in vitro was analyzed by measuring the porosity,morphology and molecular weight of drug-loaded material as well as swelling rate and dissolution rate of gastric floating tablet.The results show that the Bletilla striata,whose molecular weight is 2.372×10^(5)(g/mol)and is purified with 70%ethanol,obtain the maximum polysaccharide content of 84.88%and the maximum apparent viscosity of 22.25 mPa·s.When the ratio of oxidized konjac glucomannan and purified Bletilla striata is 8∶2,the porosity reach 77.40%,moreover,the gastric floating tablets float immediately with floating state lasting for more than 12 h.The minimum cumulative drug release rate was 22.80%at 2 h and the maximum is 89.05%at 12 h.The release exponent(n=0.64)indicate that the release of this formulation is the joint result of Fick diffusion and matrix erosion.Thus,we conclude that the developed gastric floating tablets with oxidized konjac glucomannan and purified Bletilla striata ratio of 8∶2 possess proper desired floating periods with sustained-release characteristics.