苦参降血糖活性部位分散片剂型探究.docVIP

苦参降血糖活性部位分散片剂型探究 　　[摘要] 目的 对具有显著降糖活性的苦参乙酸乙酯部位进行分散片处方工艺研究，为工业化生产和临床应用奠定基础。方法 以分散片硬度、崩解度为考察指标，通过正交试验确定最佳处方工艺。采用转篮法测定溶出度，并计算累积溶出度百分率。结果 最佳处方工艺为主药量25%，1.0%阿斯巴甜作为矫味剂，1.4～1.6 mL/100 g浓度的蒸馏水作为润湿剂，0.5%硬脂酸镁作为润滑剂，2.0%PVPP作为崩解剂，MCC-预胶化淀粉（3?U1）作为填充剂。苦参分散片的累?e溶出度平均值为82.65%。结论 苦参分散片处方工艺合理可行，可用于苦参分散片的制备及质量控制 [关键词] 苦参；处方工艺；抗糖尿病；分散片 [中图分类号] R944 [文献标识码] A [文章编号] 1673-7210（2017）04（a）-0017-05 [Abstract] Objective To investigate the dispersible tablets of the ethylacetate extract of Sophora flavescens Ait.， which will be laying the basic foundation for its industrial production and clinical study. Methods The orthogonal experiment design was performed to determine the optimized formulation with hardness and disintegration as examine indexes. The rotation basket was applied to determine the dissolution， and the accumulative dissolution percentage was calculated. Results The optimized formulation was shown as follows： the content of extracts in tablets was 25%， 1.0% aspartame was used as sweetener， 1.4-1.6 mL/100 g of distilled water was used as wetting agent， 0.5% magnesium stearate was used as lubricant， 2.0% PVPP was used as disintegrant， and MCC-pregelatinized starch （3?U1） was used as filler. The average value of accumulative dissolution percentage was 82.65%. Conclusion The preparation is reasonable and feasible， which can be used in the preparation and the quality control of Sophora flavescens dispersible tablets. [Key words] Sophora flavescens； Preparation； Antidiabetic； Dispersible tablets 苦参Sophora flavescens Ait.为豆科槐属植物，味苦，性寒，具清热解毒、祛风杀虫等功效，主治湿热泻痢，肠风便血，黄疽，水肿等症[1]。近年报道苦参用于治疗非典和肿瘤[2]及杀虫剂的开发[3-4]。苦参主要含生物碱和黄酮两类成分，具多种活性[5-6]，其中苦参碱、氧化苦参碱为主的苦参碱制剂已经上市，主要用来治疗急、慢性病毒性肝炎，肿瘤等疾病[7-10]。但对于苦参黄酮的研究相对较少，近来发现富含苦参乙酸乙酯部位中黄酮具有良好的降糖活性[11]，此外Sato等从苦参乙酸乙酯部位中分离的九种黄酮化合物具有钠-葡萄糖协同转运（SGLT）抑制作用[12]。黄秋云等从苦参乙酸乙酯部位分离的异黄酮苷F对蔗糖酶、异麦芽糖酶、麦芽糖酶活性的IC50分别为 26.7 μmol/L、20 μmol/L、5.34 μmol/L，比儿茶素的活性强37～187倍，对大鼠摄入葡萄糖后血糖值上升的ED50为40 μg/kg，比儿茶素（800 μg/kg）强20倍，还可抑制醛糖还原酶（AR）的活性，IC50为11 μmol/L[13]。以上文献数据表明苦参降血糖活性主要