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目的:为提高黄芩苷在固体制剂中的溶出度及生物利用度,设计筛选了黄芩苷自乳化系统的处方并评价其在胶囊剂中的溶出度。方法:采用正交试验对黄芩苷自乳化系统处方进行优化,以乳化速度、粒径及透光率为指标进行综合评价,确定最佳处方。结果:正交法筛选出黄芩苷自乳化系统的最佳处方用量(质量)比为:黄芩苷∶聚山梨酯80∶橄榄油∶甘油=0.15∶1∶1∶1.5。结论:按最佳处方制备的黄芩苷自乳化系统可明显改善黄芩苷的溶解性能,有效地提高了黄芩苷在人工胃液中的溶出度。
OBJECTIVE: To improve the dissolution and bioavailability of baicalin in solid preparations, we designed and characterized the baicalin self-emulsifying system and evaluated its dissolution in capsules. Methods: The orthogonal test was used to optimize the prescription of baicalin self-emulsifying system. The optimum prescription was determined by the comprehensive evaluation of emulsifying speed, particle size and light transmittance. Results: The optimum prescription dosage (mass) ratio of baicalin self-emulsifying system screened by orthogonal test was baicalin: polysorbate 80: olive oil: glycerol = 0.15:1:1:1.5. CONCLUSION: Baicalin self-emulsifying system prepared according to the best prescription can obviously improve the solubility of baicalin and effectively improve the dissolution of baicalin in artificial gastric juice.