基于漂浮和膨胀的盐酸二甲双胍胃滞留型缓释片研究  

Gastric retentive metformin hydrochloride sustained release tablets based on floatation and expansion

作　　者：潘阳 李伟 黄侃 童伟勤 PAN Yang;LI Wei;HUANG Kan;TONG Wei-qin(Bostal Drug Delivery Co.,Ltd.,Guangzhou 510530;China Pharmaceutical University,Nanjing 210009)

机构地区：[1]广州玻思韬控释药业有限公司,广州510530 [2]中国药科大学,南京210009

出　　处：《中南药学》2023年第3期600-606,共7页Central South Pharmacy

基　　金：广东省重点领域研发计划项目-新药创制核心技术研发及应用(No.2019B020201011)。

摘　　要：目的设计一种基于漂浮和膨胀的盐酸二甲双胍胃滞留型缓释片,以期获得胃滞留特性。方法通过片芯厚度控制本品的漂浮性能,片芯内填充高膨胀性辅料,以实现其膨胀性能;片芯外包具有高度延展性的缓释衣,使其能承受片芯的膨胀。以成品的密度、膨胀性能和药物溶出行为作为评价指标,与已上市的胃滞留制剂(胃漂浮型)1 g盐酸二甲双胍缓释片(商品名:Glumetza)进行对比,评估本品在体内的胃滞留能力。结果本品密度小于1 g·mL^(-1),可立即起漂;在pH 1.2 HCl介质中,2 h内最小两个维度的尺寸均大于12 mm,能膨胀至与Glumetza一致的尺寸;溶出曲线与Glumetza相似,均为一级释放模型。结论本品具有良好的漂浮和膨胀性能,在不大幅度增加片尺寸的前提下,成为一种兼顾良好吞咽性和胃滞留潜能的新型缓释片。Objective To obtain an floatable and expandable sustained release tablets with good gastric retentive capacity.Methods The floatation and expandsion were respectively controlled by the thickness of tablet core and the high expandable excipients.The flexibility of sustained release film was strong enough to support the expansion of the tablet core.The gastric retention of the final product was evaluated by comparing with the marketed gastric product Glumetza on density,expansion and in vitro dissolution.Results The tablets floated immediately as the density was lower than 1 g·mL^(-1).The minor and minimum dimension were both higher than 12 mm at 2 h.The dissolution profile between self-developed formulation and Glumetza were extremely similar,both obeying the first-order dynamic equation.Conclusion The floatation and expansion of gastric retentive tablets are strong.Without greatly increasing the size of tablets,they can be a novel sustained release tablets with easy swallowing and gastric retention.

关 键 词：漂浮 膨胀 胃滞留 盐酸二甲双胍缓释片 

分 类 号：R94[医药卫生—药剂学]