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比较含不溶性药物的黏膜冷冻干燥片和溶剂浇铸膜的体外释放特征。

Comparison of the in vitro release characteristics of mucosal freeze-dried wafers and solvent-cast films containing an insoluble drug.

机构信息

Department of Pharmaceutical, Chemical and Environmental Sciences, School of Science, University of Greenwich at Medway, Central Avenue, Chatham Maritime, Kent, UK.

出版信息

Drug Dev Ind Pharm. 2012 Jan;38(1):47-54. doi: 10.3109/03639045.2011.590496. Epub 2011 Jun 30.

DOI:10.3109/03639045.2011.590496
PMID:21714725
Abstract

Drug release characteristics of freeze-dried wafers and solvent-cast films prepared from sodium carboxymethylcellulose have been investigated and compared. In vitro drug dissolution studies were performed using an exchange cell and drug release was measured by UV spectroscopy at 272 nm using distilled water. The dissolution profiles of hydrochlorothiazide from the wafers and films were compared by determining the rates of drug release, estimated from the % release versus time profiles and calculating their difference (f(1)) and similarity (f(2)) factors. The effects of drug loading, polymer content and amount of glycerol (GLY) (films) on the drug release characteristics of both formulations were investigated. Both the wafers and films showed sustained type release profiles that were best explained by the Korsmeyer-Peppas equation. Changes in the concentration of drug and GLY (films) did not significantly alter the release profiles whilst increasing polymer content significantly decreased the rate of drug release from both formulations. The rate of release was faster from the wafers than the corresponding films which could be attributed to differences in the physical microstructure. The results show the potential of employing both formulations in various mucosal drug delivery applications.

摘要

已研究并比较了由羧甲基纤维素钠制备的冻干片和溶剂浇铸膜的药物释放特性。采用交换池进行体外药物溶出研究,并用蒸馏水在 272nm 处通过紫外分光光度法测量药物释放。通过确定从片剂和薄膜中释放的药物的速率,从%释放与时间曲线来比较氢氯噻嗪的溶解曲线,并计算它们的差异(f(1))和相似性(f(2))因子。研究了药物负载,聚合物含量和甘油(GLY)(薄膜)的量对两种制剂药物释放特性的影响。片剂和薄膜均显示出持续型释放曲线,该曲线最适合用 Korsmeyer-Peppas 方程来解释。药物和 GLY(薄膜)浓度的变化并未明显改变释放曲线,而增加聚合物含量则明显降低了两种制剂的药物释放速率。片剂的释放速率比相应的薄膜快,这可能归因于物理微观结构的差异。结果表明,这两种制剂在各种粘膜药物传递应用中具有潜力。

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