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具有相反溶解度的药物和聚合物单层膜的配方。

Formulation of monolayered films with drug and polymers of opposing solubilities.

作者信息

Perumal V A, Lutchman D, Mackraj I, Govender T

机构信息

School of Pharmacy and Pharmacology, University of KwaZulu-Natal, Durban 4000, South Africa.

出版信息

Int J Pharm. 2008 Jun 24;358(1-2):184-91. doi: 10.1016/j.ijpharm.2008.03.005. Epub 2008 Mar 13.

Abstract

The aim of this study was to prepare and characterise monolayered multipolymeric films (MMFs) comprising of a hydrophilic drug (Propranolol HCl) (PHCl) and polymers of opposing solubilities. Films were prepared by emulsification and casted by a new approach using a silicone-molded tray with individual wells. MMFs comprising of PHCl with Eudragit 100 (EUD100) and Chitosan (CHT), i.e. films with drug and polymers of opposing solubilities were successfully prepared (PHCl:EUD100:CHT; 1:10:0.5) and demonstrated uniform and reproducible drug content (100.71+/-2.66%), thickness (0.442+/-0.030 mm), mucoadhesivity (401.40+/-30.73 mN) and a controlled drug release profile. Drug release followed Higuchi's square-root model. Maximum swelling of the films occurred after 1h and 28.26% of the films eroded during the 8-h test period. Mechanical testing revealed that the MMFs displayed a greater abrasion resistance, were more elastic and also required more energy to break, rendering them tougher and more suitable for buccal delivery than the monopolymeric PHCl:EUD100 film. The inclusion of CHT to the film led to a more porous surface morphology. The surface pH of the films remained constant at neutral pH. This study confirmed the potential of the above MMFs as a promising candidate for buccal delivery of PHCl.

摘要

本研究的目的是制备并表征由亲水性药物(盐酸普萘洛尔)(PHCl)和具有相反溶解性的聚合物组成的单层多聚膜(MMF)。通过乳化法制备薄膜,并采用一种新方法,使用带有单个孔的硅树脂模制托盘进行浇铸。成功制备了由PHCl与Eudragit 100(EUD100)和壳聚糖(CHT)组成的MMF,即由具有相反溶解性的药物和聚合物组成的薄膜(PHCl:EUD100:CHT;1:10:0.5),并证明其药物含量均匀且可重现(100.71±2.66%)、厚度(0.442±0.030 mm)、粘膜粘附性(401.40±30.73 mN)以及具有可控的药物释放曲线。药物释放遵循Higuchi平方根模型。薄膜在1小时后出现最大溶胀,在8小时测试期内28.26%的薄膜发生侵蚀。机械测试表明,MMF表现出更大的耐磨性、更具弹性,并且断裂需要更多能量,使其比单一聚合物PHCl:EUD100薄膜更坚韧,更适合口腔给药。向薄膜中加入CHT导致表面形态更具多孔性。薄膜的表面pH在中性pH下保持恒定。本研究证实了上述MMF作为盐酸普萘洛尔口腔给药的有前景候选物的潜力。

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