复方灯黄胶囊的制备工艺及药效学研究

Optimal formulation and pharmacodynamics of compound Erigeron Breviscapus-Rheum capsules

目的采用水溶性聚维酮K30(PVP K30)作为载体,制备灯盏花-大黄固体分散体胶囊(复方灯黄胶囊),并考察其对糖尿病大鼠肾功能的影响。方法采用溶剂法制备复方灯黄固体分散体,通过考察不同灯盏花-大黄提取物-PVP K30比例对有效成分溶解度的影响,以优选最优处方;采用单侧肾切除及链脲菌素(STZ)诱导大鼠糖尿病肾病模型,通过生化指标及肾脏病理组织评价复方灯黄胶囊治疗糖尿病肾病大鼠的药效。结果灯盏花-大黄提取物与PVP K30的最佳比例为1∶6;与糖尿病组比较,复方灯黄胶囊可显著降低模型大鼠的血总胆固醇、血三酰甘油、血尿素氮、血肌酐、内生肌酐清除率、肾指数及尿微量白蛋白水平(P<0.01),减少肾小球面积及系膜堆积。结论复方灯黄胶囊对糖尿病肾病具有显著的防治作用。

Objective To prepare solid dispersion capsules containing compound Erigeron BreviscapusRheum（ EBR） and polyvinyl pyrrolidone K30（ PVP K30） and investigate the effects of EBR solid dispersion capsules on renal function of diabetic nephropathy in rats. Methods The EBR solid dispersion was prepared by the solvent method. The influence of different ratio of PVP K30 and EBR on the solubility of EBR solid dispersion was applied to optimize the formulation. The diabetic nephropathy model was established by uninephrectomy and interperitoneal injection of streptozotocin. Biochemical criterion and pathological tissue of kidney were used to evaluate the effect of compound EBR capsules on the pharmacodynamics of diabetic nephropathy in rats. Results The formulation was optimized with EBR and PVP K30 in the ratio of 1 ∶ 6. The total cholesterol, triglycerides, blood urea nitrogen, serum creatinine,creatinine clearance,urine albumin and kidney index of rats（ P〈0. 01） were significantly decreased, the glomerular area and the mesangial accumulation was also reduced in the compound EBR capsules group comparing with the diabetes rats group. Conclusion EBR capsules can effectively treat and prevent the disease of diabetic nephropathy and retard progression of diabetic nephropathy.