Pharmaceutics Research Laboratory, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya, Bilaspur (C.G.) 495 009, India.
Mol Pharm. 2011 Dec 5;8(6):2273-81. doi: 10.1021/mp2001395. Epub 2011 Oct 21.
The aim of present study was to develop stomach specific floating beads of metformin hydrochloride for effective management of type 2 diabetes mellitus. The beads were evaluated for surface morphology, particle size, tapped density, true density, percent porosity, drug entrapment efficiency, percent yield, differential scanning calorimetry, in vitro floating ability and in vitro drug release. Stability studies were performed at 25 and 40 °C up to 45 days. Effectiveness of the formulations was evaluated in vivo by hypoglycemic response in both normal and diabetic albino rats. The beads were grossly spherical in shape, and average particle diameter of beads was found to be in the size range of 861.34 to 991.75 μm. Percent entrapment was found to be in the range of 77.61 to 82.48%. Beads demonstrated favorable in vitro floating ability. All the formulations followed a non-Fickian release mechanism. It was found that there was no significant effect on floating ability of aged beads since it floated up to an 8 h study period. In vivo studies on diabetic rats showed that the hypoglycemic effect induced by the metformin hydrochloride loaded alginate beads was significantly greater (P < 0.05) and more prolonged than that induced by the nonfloating beads. The results clearly demonstrated the ability of the formulation to maintain blood glucose level and improved the patient compliance by enhancing, controlling and prolonging the systemic absorption of metformin hydrochloride.
本研究旨在开发盐酸二甲双胍的胃溶型漂浮珠，以有效治疗 2 型糖尿病。对珠粒进行了表面形态、粒径、振实密度、真密度、孔隙率、药物包封效率、收率、差示扫描量热法、体外漂浮能力和体外药物释放进行评价。在 25 和 40°C 下进行了 45 天的稳定性研究。通过正常和糖尿病白化大鼠的降血糖反应评价了制剂的有效性。珠粒呈大体球形，平均粒径在 861.34 到 991.75 μm 范围内。包封率在 77.61%到 82.48%之间。珠粒表现出良好的体外漂浮能力。所有配方均遵循非菲克扩散机制。研究发现，老化珠粒的漂浮能力没有显著影响，因为它在 8 小时的研究期间仍能漂浮。在糖尿病大鼠的体内研究表明，载盐酸二甲双胍的海藻酸钠珠粒诱导的降血糖作用明显大于（P<0.05）且持续时间更长，比非漂浮珠粒诱导的降血糖作用更长。结果清楚地表明，该制剂能够通过增强、控制和延长盐酸二甲双胍的全身吸收，维持血糖水平并提高患者的顺应性。
