非渗透性胶囊体的制备及性质考察

Preparation and Property Evaluation of Impermeable Capsule Body

目的:制备柱塞控制型脉冲释药胶囊组成中的非渗透性胶囊体(ICB),并对其性质进行考察。方法:以乙基纤维素(EC)为材料,二氯甲烷、无水乙醇、乙酸乙酯为混合溶剂,采用灌注法制备ICB;分别考察混合溶剂比例、EC溶液浓度及EC黏度3种因素对ICB成型性的影响;在5种释放介质中通过体外释放试验对所制囊体的非渗透性进行考察。结果:3种因素最优水平分别为4∶0.8∶0.2、11.5%、45cp;由此制备的ICB光洁透明、开口圆整、柔韧性及塑性好,且在不同介质中72h内药物累积释放率均≤0.60%。结论:所制备的ICB非渗透性良好,为进一步制备柱塞型脉冲释药胶囊奠定了基础。

OBJECTIVE： To prepare impermeable capsule body （ICB） which is constituent of plug controlled pulsatile cap- sule, and to evaluate its properties. METHODS： ICB was prepared by filling method with ethyl cellulose （EC） using dichlorometh- ane, ethanol, ethyl acetate as mixed solvent. The effects of factors on the formability had been tested, including the ratio of mixed solvent, concentration of EC and viscosity of EC. The impermeability of ICB was examined in five release mediums in vitro. RE- SULTS： With the optimized formulation （dichloromethane-ethanol-ethyl acetate ratio of4：0.8：0.2, EC concentration of 11.5%, EC viscosity of 45 cp）, the ICB was transparent with round opening, well hardness and tenacity. The accumulative drug release of drugs within 72 h was no more than 0.6% in different mediums. CONCLUSION： ICB have been prepared successfully, which pro- vide foundation for the preparation of plug controlled pulsatile capsule.