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醋氯芬酸壳聚糖微球的体外与体内评价。

Chitosan microspheres of aceclofenac: in vitro and in vivo evaluation.

机构信息

Indukaka Ipcowala College of Pharmacy, Vithal Udyognagar, New Vallabh Vidyanagar, Anand.

出版信息

Pharm Dev Technol. 2010 Sep-Oct;15(5):442-51. doi: 10.3109/10837450903286503.

Abstract

The objective of this investigation was to achieve controlled drug release of Aceclofenac (ACE) microspheres and to minimize local side-effects in the gastrointestinal tract (GIT). Sustained release chitosan microspheres containing ACE were prepared using double-emulsion solvent evaporation method (O/W/O). Chitosan microspheres were prepared by varying drug to polymer ratio (1:3, 1:4, 1:5 and 1:6). Microspheres were characterized for morphology, swelling behavior, mucoadhesive properties, FTIR and DSC study, drug loading efficiency, in vitro release, release kinetics, and in vivo study was performed on rat model. ACE-loaded microspheres were successfully prepared having production yield, 57-70% w/w. Drug encapsulation efficiency was ranging from 53-72% w/w, Scanning electron microscopy (SEM) revealed particle size of microspheres was between 39 and 55 mum. FTIR spectra and DSC thermograms demonstrated no interaction between drug and polymer. The in vitro release profiles of drug from chitosan microspheres showed sustained-release pattern of the drug in phosphate buffer, pH 6.8. In vitro release data showed correlation (r2 > 0.98), good fit with Higuchi/Korsmeyer-Peppas models, and exhibited Fickian diffusion. ACE microspheres demonstrated controlled delivery of aceclofenac and apparently, no G.I.T. erosion was noticed.

摘要

本研究旨在实现醋氯芬酸(ACE)微球的控制释放,并最大程度地减少胃肠道(GIT)的局部副作用。采用复乳溶剂蒸发法(O/W/O)制备了载有 ACE 的壳聚糖微球。通过改变药物与聚合物的比例(1:3、1:4、1:5 和 1:6)来制备壳聚糖微球。对微球进行形态学、溶胀行为、粘膜粘附性能、FTIR 和 DSC 研究、载药量、体外释放、释放动力学以及大鼠模型的体内研究进行了表征。成功制备了载有 ACE 的微球,产率为 57-70%w/w。药物包封效率在 53-72%w/w 之间,扫描电子显微镜(SEM)显示微球的粒径在 39-55 微米之间。FTIR 谱和 DSC 热图表明药物与聚合物之间没有相互作用。壳聚糖微球中药物的体外释放曲线显示药物在 pH 6.8 的磷酸盐缓冲液中呈现持续释放模式。体外释放数据显示相关性(r2>0.98),与 Higuchi/Korsmeyer-Peppas 模型拟合良好,并表现出菲克扩散。ACE 微球显示出对醋氯芬酸的控制释放,显然没有观察到胃肠道侵蚀。

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