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使用大鼠对含普伐他汀钠微胶囊的制剂及药代动力学评价

Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats.

作者信息

Puttegowda Venkatesh Dinnekere, Karki Roopa, Goli Divakar, Jha Sajal Kumar, Mudagal Manjunatha Panduranga

机构信息

Department of Pharmaceutics & Pharmacology, Acharya and B. M. Reddy College of Pharmacy, Soldevanahalli, Bengaluru 560107, India.

Department of Pharmaceutics, School of Pharmacy, Guru Nanak Institutions Technical Campus, Ibrahimpatnam, Telangana, India.

出版信息

Scientifica (Cairo). 2016;2016:7623193. doi: 10.1155/2016/7623193. Epub 2016 Aug 9.

Abstract

Pravastatin Sodium has a cholesterol lowering agent. It has shorter half-life and undergoes first-pass metabolism. Frequent dose is required in case of conventional dosage form. The purpose of the study is to formulate and evaluate microcapsules containing Pravastatin Sodium by complex with cholestyramine resins coated with Eudragit RLPO and Eudragit RSPO polymers for achieving control release. Complexation of drug on resin was carried out by batch method. Microencapsulation was carried out by nonaqueous solvent evaporation method. Pharmacokinetic studies were done by using rats. The intermediate stability studies were carried out on the most satisfactory formulations. FTIR, X-ray diffraction, and DSC spectra of drug, drug-resinates, and polymers revealed no chemical interaction. The % DEE and % yield were observed for formulations of f1 to f7 that were varied from 97.1 ± 0.8 to 98.9 ± 0.5% and 95.0 ± 3.25 to 98.8 ± 7.1%, respectively. Most satisfactory formulation, f6, showed drug release up to 72.6%. No changes in % DEE and % CDR were observed after stability studies. Microcapsules of f6 formulation achieved best performance regarding in vitro drug release and from pharmacokinetic evaluation mean residence time was found to be 6.3 h, thus indicated, Pravastatin Sodium microcapsules were released and absorbed slowly over a prolonged period of time.

摘要

普伐他汀钠是一种降胆固醇药物。它的半衰期较短,会经历首过代谢。对于传统剂型,需要频繁给药。本研究的目的是制备并评估含有普伐他汀钠的微胶囊,该微胶囊通过与用Eudragit RLPO和Eudragit RSPO聚合物包衣的消胆胺树脂形成复合物来实现控释。药物与树脂的络合采用分批法进行。微囊化采用非水溶剂蒸发法进行。使用大鼠进行药代动力学研究。对最满意的制剂进行中间稳定性研究。药物、药物树脂酸盐和聚合物的傅里叶变换红外光谱(FTIR)、X射线衍射和差示扫描量热法(DSC)光谱显示无化学相互作用。观察到f1至f7制剂的包封率(% DEE)和产率分别在97.1±0.8%至98.9±0.5%和95.0±3.25%至98.8±7.1%之间变化。最满意的制剂f6显示药物释放率高达72.6%。稳定性研究后,未观察到包封率和累积释放率(% CDR)的变化。f6制剂的微胶囊在体外药物释放方面表现最佳,药代动力学评估显示平均驻留时间为6.3小时,因此表明,普伐他汀钠微胶囊在较长时间内缓慢释放和吸收。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39b4/4993944/e7cef56b74b4/SCIENTIFICA2016-7623193.001.jpg

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