采用热熔挤出法制备伏格列波糖口溶膜剂,以拉伸性能和溶化时间为指标,筛选优化处方。结果以聚氧乙烯N10为成膜材料、5%甘油为增塑剂的膜剂可在20 s 内溶化,体外溶出行为与已在日本上市的膜剂相似。对正常大鼠蔗糖负荷后高血糖的体内试验表明,自制膜剂与国外膜剂以及国内上市的分散片的降血糖效果相当。
Abstract
The voglibose oral dissolvable films were prepared by hot melt extrusion method. The formulation was optimized with the tensile properties and the dissolvable time as the evaluation parameters. The optimal product with polyoxyethylene N10 as carrier and 5% glycerol as plasticizer could dissolve within 20 s and showed a similar dissolution behavior to the voglibose OD Film 0.2?QQ? marketed in Japan. The in vivo experiment on postprandial hyperglycemia
in normal rats demonstrated that the voglibose oral dissolvable films had equivalent hypoglycemic effect with the commercial voglibose films in Japanese market and its dispersible tablets in domestic market.
关键词
伏格列波糖 /
口溶膜剂 /
热熔挤出 /
溶出 /
降血糖
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Key words
voglibose; /
oral dissolvable film /
hot melt extrusion /
dissolution /
hypoglycemic effect
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参考文献
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脚注
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基金
国家“重大新药创制”科技重大专项(2011ZX0940-403-3)
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