He Wei, Huang Shijing, Zhou Chunyan, Cao Lin, Yao Jing, Zhou Jianping, Wang Guangji, Yin Lifang
State Key Laboratory of Natural Medicines, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, People's Republic of China.
AAPS PharmSciTech. 2015 Apr;16(2):344-53. doi: 10.1208/s12249-014-0229-1. Epub 2014 Oct 16.
A combination therapy of metformin hydrochloride (MH) and repaglinide (RG) achieves a perfect glycemic control; however, the combination formulation of immediate release must be taken several times a day, compromising the therapeutic benefits and causing inconveniences to the patients. Herein, a bilayer matrix tablet that aimed at continuously releasing both MH and RG over time was developed, in which the two drugs were formulated into two separated layers. The tablets were prepared by wet granulation method, and the optimized formulation was obtained by evaluating the factors that affected the drug release. The bilayer tablets simultaneously released the two drugs over 12 h; and a better in vivo performance with a steady plasma concentration, markedly lower Cmax, prolonged Tmax, and perfect absorption was obtained. Summarily, the bilayer matrix tablets sustained both MH and RG release over time, thereby prolonging the actions for diabetic therapy and producing better health outcomes.
盐酸二甲双胍（MH）和瑞格列奈（RG）联合疗法可实现完美的血糖控制；然而，速释联合制剂必须一天服用数次，这会影响治疗效果并给患者带来不便。在此，研发了一种双层基质片，旨在使MH和RG随时间持续释放，其中两种药物被制成两个分开的层。该片剂通过湿法制粒法制备，并通过评估影响药物释放的因素获得了优化配方。双层片在12小时内同时释放两种药物；并在体内表现出更好的性能，具有稳定的血浆浓度、显著更低的Cmax、延长的Tmax和完美的吸收。总之，双层基质片可使MH和RG随时间持续释放，从而延长糖尿病治疗的作用时间并产生更好的健康结果。
