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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 take Epimedium Flavonoids as a model drug and snail enzyme as hydrolase, add preparation agent to prepare biologically enzymatic enteric-coated capsule which can be digested in real time and absorbed in real time, and optimize and evaluate its prescription process. Methods Taking the release of total flavonoids of Epimedium as the evaluation index, the types, dosage, types and dosage of the extenders, the dosage and the amount of the extenders needed to prepare the biomimetic enzyme-solubilized enteric-coated capsules of Epimedium sagittatum flavonoids were screened by UV and single factor experiments Wetting agent and other key factors, and the use of response surface methodology to optimize the formulation of prescriptions, while using HPLC method for enteric-coated capsules of the four main flavonoid glycosides (Epimedium glycosides and epimediesin A, B, C) enzymatic process To inspect. Results Epimedium total flavonoids biomimetic enzymatic enteric-coated capsules optimal prescription Epimedium Flavonoids extract 100 mg, snail enzyme 68 mg, α-lactose 65 mg, low-substituted hydroxypropyl cellulose 11.7 mg, the preparation of The cumulative release rate of total flavonoids in artificial intestinal juice within 45 min was 85.43%, and enzymolysis was complete within the intestinal emptying time (3-6h). Conclusion The prepared epimedium total flavonoids biotransformation enteric-coated capsules are helpful to promote the hydrolysis and transformation of epimedium flavonoids in vivo and provide a research foundation for the development of a new epimedium total flavone preparation.