不同物料参数及配比对模型丸剂体外溶出的影响

Dissolution of Chinese Medicine Pills on Model Parameters and Ratio for Different Materials

目的:初步探讨不同物料参数及配比与中药丸剂有效性关系,通过改变物料配比改变中药丸剂的生物有效性。方法:选取不同物料的代表药物并测定其物料参数,以均匀设计法自拟12个处方并制备模型丸剂,用HPLC法测定处方中苦参碱含量,根据Weibull分布提取溶出参数,用SPSS 20.0处理数据。结果:不同物料配比的模型丸剂中苦参碱在不同时间点的溶出百分率不同,如2 min时处方1的溶出百分率最低(2.78%),处方12的溶出百分率最高(39.00%);240 min时处方1的溶出百分率最低(82.90%),处方12的溶出百分率最高(99.26%)。结论:纤维类、淀粉类、矿物类对丸剂溶出有明显促进溶出作用,树脂类、油脂类、蛋白类对丸剂溶出有明显的阻滞作用,而多糖类对丸剂溶出影响不显著。吸湿率、吸水率、吸水膨胀率、比黏度等物料参数与体外溶出也有相关性。

Objective ： To explore different materials of parameters and the ratio of Chinese medicine pills effectiveness relationship by changing the ratio of materials to change the biological effectiveness of Chinese medicine pills. Methods ： We selected different materials behalf drug and determine the material parameters to uniform design from the proposed 12 model formulations and preparations of pills. The prescription matrine was determined by HPLC elution profile extraction parameters Weibull and the processing data was analyzed with SPSS 20.0. Results ： Different material ratio of the model pill at different time points of dissolution percentage was different. The 2 min dissolution percentage of prescription 1 was the lowest （2.78%） and the dissolution pereentageof prescription 12 was the highest（39.00% ）. The 240 min dissolution percentage of prescription 1 was the lowest percentage （ 82.90% ） and that of prescription 12 was the highest （99. 26% ）. Conclusion： Fiber, starch and minerals have significantly promoted effect on dissolution of the pills and resins, fats and proteins significantly block the pill dissolution. The polysaccharides effect on dissolution was not significant. Moisture absorption, water absorption, water swelling, viscosity and other materials are also relevant in vitro dissolution.