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氟康唑β-环糊精包合物眼用膜剂的制备：体内外评价

Preparation of Fluconazole β-Cyclodextrin Complex Ocuserts: In Vitro and In Vivo Evaluation.

作者信息

Abdul Ahad Hindustan, Sreeramulu J, Padmaja B Suma, Reddy M Narasimha, Prakash P Guru

机构信息

Department of Pharmaceutics, College of Pharmacy, Sri Krishnadevaraya University, Andhra Pradesh, Anantapur 515003, India.

出版信息

ISRN Pharm. 2011;2011:237501. doi: 10.5402/2011/237501. Epub 2011 Aug 25.

DOI:10.5402/2011/237501
PMID:22389846
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3263730/
Abstract

The main purpose of the present study was to develop ocuserts of Fluconazole β-CD (beta-cyclodextrin) complex and to evaluate both in vitro and in vivo. Fluconazole was made complex with β-CD, and the release rate was controlled by HPMC K(4)M and ethyl cellulose polymers using dibutyl Phthalate as permeability enhancer. Drug-polymer interactions were studied by Fourier transform infrared spectroscopic studies. The formulated ocuserts were tested for physicochemical parameters of in vitro release and in vivo permeation in rabbits. The optimized formulations (F-5 and F-8) were subjected to stability studies. The formulated ocuserts were found to have good physical characters, thickness, diameter, uniformity in weight, folding endurance, less moisture absorption, and controlled release of drug both in vitro and in vivo. The optimized formulations retained their characteristics even after stability studies. The study clearly showed that this technique was an effective way of formulating ocuserts for retaining the drug concentration at the intended site of action for a sufficient period of time and to elicit the desired pharmacological response.

摘要

本研究的主要目的是开发氟康唑β-环糊精复合物眼用控释膜，并进行体外和体内评价。氟康唑与β-环糊精制成复合物，以邻苯二甲酸二丁酯作为渗透促进剂，通过羟丙甲纤维素K(4)M和乙基纤维素聚合物控制释放速率。通过傅里叶变换红外光谱研究药物-聚合物相互作用。对所制备的眼用控释膜进行体外释放和家兔体内渗透的理化参数测试。对优化后的制剂（F-5和F-8）进行稳定性研究。结果发现，所制备的眼用控释膜具有良好的物理特性，如厚度、直径、重量均匀性、耐折性、低吸湿性，并且在体外和体内均能实现药物的控释。即使经过稳定性研究，优化后的制剂仍保持其特性。该研究清楚地表明，这种技术是制备眼用控释膜的有效方法，能够在预期作用部位维持足够长时间的药物浓度，并引发所需的药理反应。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2216/3263730/b70167459740/PHARMACEUTICS2011-237501.013.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2216/3263730/27739b140ce5/PHARMACEUTICS2011-237501.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2216/3263730/a5bb72486f50/PHARMACEUTICS2011-237501.008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2216/3263730/b70167459740/PHARMACEUTICS2011-237501.013.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2216/3263730/4096bae9eb74/PHARMACEUTICS2011-237501.002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2216/3263730/b70167459740/PHARMACEUTICS2011-237501.013.jpg

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