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用于持续眼部给药的自组装纳米结构

Self assembling nanostructures for sustained ophthalmic drug delivery.

作者信息

Khopade A J, Jain N K

机构信息

Department of Pharmaceutics, Bharati Vidyapeeth's Poona College of Pharmacy, Pune, India.

出版信息

Pharmazie. 1995 Dec;50(12):812-4.

PMID:8584558
Abstract

Nanopseudolatex was prepared for sustained ophthalmic delivery. It was prepared by a solvent injection method without the use of any stabilizer. The acrylate copolymers Eudragit RLPM and RSPM were used as carrier materials. Their formation was confirmed by electron microscopy. The system was extensively characterized for particle size, viscosity, sedimentation volume, encapsulation efficiency, in vitro release profile and pharmacodynamic properties. The particle size was found to be stirring rate dependent above the injection rate of 1 ml/min. Only at slow stirring rates it was temperature dependent. There was no sedimentation for about 60 d. The viscosity was 23-27 cps which was particle size dependent. The results show an excellent encapsulation efficiency of about 94-98%. Release studies showed slow and consistent drug release from the formulation. However, Eudragit RSPM showed comparatively longer release than Eudragit RLPM nanosuspensions. Using this method we have developed a new formulation of diclofenac diethyl ammonium which showed increased therapeutic efficacy as compared with eye drops.

摘要

纳米伪乳胶是为眼科药物的持续递送而制备的。它是通过溶剂注射法制备的,未使用任何稳定剂。丙烯酸酯共聚物Eudragit RLPM和RSPM用作载体材料。通过电子显微镜确认了它们的形成。该系统对粒径、粘度、沉降体积、包封率、体外释放曲线和药效学性质进行了广泛表征。发现粒径在注射速率高于1 ml/min时与搅拌速率有关。仅在缓慢搅拌速率下,粒径才与温度有关。大约60天内没有沉降。粘度为23 - 27 cps,这与粒径有关。结果显示包封率极佳,约为94 - 98%。释放研究表明制剂中的药物释放缓慢且持续。然而,Eudragit RSPM显示出比Eudragit RLPM纳米混悬液释放时间相对更长。使用这种方法,我们开发了双氯芬酸二乙铵的新制剂,与滴眼液相比,其治疗效果有所提高。

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