Cui Jing-hao, Qian Ying, Miao Wen-jun, Xia Qi
College of Pharmacy, Soochow University, Suzhou 215123, China.
Zhongguo Zhong Yao Za Zhi. 2008 Aug;33(16):1960-3.
To prepare a novel floating micropellets containing hydroxy propyl-beta-oyclodextrin(puerarin-HP-beta-CD) for gastroretentive dosage form and evaluate its pharmaceutical characteristics in vitro.
The puerarin HP-beta-cyclodextrin inclusion complex was prepared by freeze-drying method. Puerarin and its HP-beta-CD inclusion complex were incorporated into alginate beads, respectively. The effect of methyl cellulose (MC), Mg-Stearate and chitosan on buoyancy and cumulative release rate of puerarin were investigated in simulated gastric fluid.
The spectrums of FTIR and profiles of X-ray powder diffraction of samples proved the formation of inclusion complex between puerarin and HP-beta-CD. Magnesium stearate had a significant effect on the buoyancy of micropellets, and satisfied results were gained by the content with 2%. The solubility of puerarin was increased 65.6-fold by the formation of inclusion complex, the dissolution rate and cumulative release percentage also improved significantly although with the burst release phenomena. The micropellets showed sustained release properties by using puerarin-HP-beta-CD inclusion complex mixed with puerarin (1:1) and treated thoroughly under homogenizer.
The solubility and release rate of puerarin are increased by the formation of inclusion complex with HP-beta-CD and its gastroretentive dosage forms displayed satisfied floating and sustained release characteristics.
制备含羟丙基-β-环糊精（葛根素-HP-β-CD）的新型胃内滞留微丸剂型，并对其体外药学特性进行评价。
采用冷冻干燥法制备葛根素-HP-β-环糊精包合物。将葛根素及其HP-β-CD包合物分别载入海藻酸钠微丸。在模拟胃液中考察甲基纤维素（MC）、硬脂酸镁和壳聚糖对葛根素微丸漂浮性能及累积释放率的影响。
样品的红外光谱和X射线粉末衍射图谱证明葛根素与HP-β-CD形成了包合物。硬脂酸镁对微丸的漂浮性能有显著影响，含量为2%时效果良好。葛根素形成包合物后溶解度提高了65.6倍，溶出速率和累积释放百分率也显著提高，不过存在突释现象。采用葛根素-HP-β-CD包合物与葛根素（1:1）混合并在匀浆器中充分处理后，微丸呈现出缓释特性。
葛根素与HP-β-CD形成包合物后溶解度和释放速率增加，其胃内滞留剂型表现出良好的漂浮和缓释特性。
