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不同纤维素丙烯酸酯和甲基丙烯酸酯聚合物负载醋氯芬酸微球的设计、表征及体外评价

Design, characterization and in-vitro evaluation of different cellulosic acrylic and methacrylic polymers loaded aceclofenac microspheres.

作者信息

Dewan Irin, Miah Salim, Islam S M Ashraful, Rana Sohel

机构信息

Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka, Bangladesh.

Department of Pharmacy, Jahangirnagar University, Savar, Dhaka, Bangladesh.

出版信息

Pak J Pharm Sci. 2014 Sep;27(5):1241-8.

Abstract

The aspire of this attempt was to design and evaluate aceclofenac loaded sustained release microspheres by emulsion solvent evaporation method, using different polymers like Ethyl cellulose (EC), Kollidon SR (KSR), Eudragit RS 100, Eudragit RL 100 and Hydroxypropylmethyl Cellulose (HPMC K100M). Microspheres were prepared using different stirring rate (1200, 1500, 2000rpm) and larger microspheres were obtained with lower stirring rate. Performance of microspheres was evaluated in terms of in vitro dissolution study which was allowed according to USP paddle method using Phosphate Buffer (pH 6.8) for 8 hours. UV-spectrophotometric method was used to calculate the drug content and the maximum and minimum release of aceclofenac from microspheres was observed 96.08% and 46.41% for formulation F18 and F5 after 8 hours respectively. Dissolution data were fitted by different mathematical models such as the zero order plot, first order plot, Higuchi plot, Hixon-Crowel plot and korsemeyer plot. Korsemeyer model has found to best fitted with release data. Scanning electron microscopic technique was performed to obtain the particle size and morphological changes due to different polymers. Fourier Transform Infra-red (FT-IR) spectroscopy was performed to find out any interaction of drug with the polymers. The drug might be released by both diffusion and erosion as data were best fitted with Korsemeyer model. So it has been demonstrated that aceclofenac microspheres containing different cellulosic, acrylic and methacrylic loaded polymers may be excellent candidates for consideration in drug delivery systems.

摘要

本研究旨在通过乳液溶剂蒸发法,使用不同的聚合物,如乙基纤维素(EC)、聚乙烯吡咯烷酮缓释型(KSR)、丙烯酸树脂RS 100、丙烯酸树脂RL 100和羟丙基甲基纤维素(HPMC K100M),设计并评估载有醋氯芬酸的缓释微球。使用不同的搅拌速率(1200、1500、2000转/分钟)制备微球,较低的搅拌速率可获得较大的微球。根据美国药典桨法,使用磷酸盐缓冲液(pH 6.8)进行8小时的体外溶出研究,以评估微球的性能。采用紫外分光光度法计算药物含量,8小时后,F18和F5制剂中醋氯芬酸的最大释放率和最小释放率分别为96.08%和46.41%。溶出数据通过不同的数学模型进行拟合,如零级图、一级图、Higuchi图、Hixon-Crowel图和Korsemeyer图。发现Korsemeyer模型与释放数据拟合最佳。采用扫描电子显微镜技术观察不同聚合物对微球粒径和形态的影响。通过傅里叶变换红外(FT-IR)光谱法研究药物与聚合物之间的相互作用。由于数据与Korsemeyer模型拟合良好,药物可能通过扩散和侵蚀两种方式释放。因此,已证明含有不同纤维素、丙烯酸和甲基丙烯酸负载聚合物的醋氯芬酸微球可能是药物递送系统中值得考虑的优秀候选者。

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