淫羊藿总黄酮仿生酶解肠溶胶囊的制备及评价  

Preparation and evaluation of bionic enzymatic Epimedium flavonoids-loaded enteric-coated capsules

作　　者：刘聪燕[1,2] 高霞[1,2] 黄萌萌[1,2] 彭静[1,2] 陈彦[1,2] 

机构地区：[1]南京中医药大学附属中西医结合医院,江苏南京210028 [2]江苏省中医药研究院中药组分与微生态研究中心,江苏南京210028

出　　处：《中草药》2016年第20期3610-3617,共8页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81173557)

摘　　要：目的以淫羊藿总黄酮为模型药物,蜗牛酶为水解酶,加入制剂辅料制备可实时酶解、实时吸收的淫羊藿总黄酮仿生酶解肠溶胶囊,对其处方工艺进行优化和评价。方法以淫羊藿总黄酮释放度为评价指标,采用UV法和单因素实验筛选制备淫羊藿总黄酮仿生酶解肠溶胶囊所需的填充剂种类、用量,崩解剂种类、用量及润湿剂种类等关键因素,并采用响应面法优化其制剂处方,同时采用HPLC法对肠溶胶囊中4种主要黄酮苷(淫羊藿苷及朝藿定A、B、C)的酶解过程进行考察。结果淫羊藿总黄酮仿生酶解肠溶胶囊的最优处方为淫羊藿总黄酮提取物100 mg,蜗牛酶68 mg,α-乳糖65 mg,低取代羟丙纤维素11.7 mg,该制剂在人工肠液中45 min内的总黄酮累积释放率可达85.43%,同时能够在肠道排空时间内(3-6h)酶解完全。结论所制备的淫羊藿总黄酮仿生酶解肠溶胶囊有利于促进淫羊藿总黄酮在体内的水解转化,为研发高效的淫羊藿总黄酮新制剂提供研究基础。Objective To prepare and evaluate bionic enzymatic Epimedium flavonoids-loaded enteric-coated capsules, composed of Epimedium flavonoids as drug, snail enzyme as hydrolase and common formulation accessories, which is in favor of in vivo real-time enzymolysis and real-time absorption ofEpimedium flavonoids. Methods The UV method and single factor experiment were applied to investigating the effects of key factors such as filling agents species and dosage, disintegrating agents species and dosage, wetting agents species and drying temperature on the cumulative release degree ofEpimedium flavonoids. Response surface method was used to optimize the prescription for bionic enzymatic Epimedium flavonoids-loaded enteric-coated capsules, and the enzymatic process of the four Epimedium flavonoids （icariin and epimendin A, B, C） was also evaluated by HPLC. Results The optimal formulation for the bionic enzymatic Epimedium flavonoids-loaded enteric-coated capsules was composed of 100 mg Epimedium fiavonoids extract, 68 mg snail enzyme, 65 mg α-lactose, and 11.7 mg low-substituted hydroxypropyl cellulose. This enteric-coated capsules showed a cumulative Epimedium flavonoids release rate of 85.43 % within 45 min in simulated intestinal fluid and a complete enzymolysis within the intestine emptying time （3-6 h）. Conclusion The bionic enzymatic Epimedium flavonoids-loaded enteric-coated capsules show an advantage in improving hydrolysis and anti-osteoporosis efficacy of Epimedium flavonoids, providing some research ideas for improving the oral bioavailability of other flavonoids.

关 键 词：淫羊藿总黄酮 蜗牛酶 肠溶胶囊 仿生酶解 黄酮苷 淫羊藿苷 朝藿定A 朝藿定B 朝藿定C 

分 类 号：R283.6[医药卫生—中药学]