Suppr超能文献

酮咯酸氨丁三醇速溶片的制剂与药代动力学

Formulation and pharmacokinetics of ketorolac tromethamine fast dissolving tablets.

作者信息

Mettu S R, Veerareddy P R

机构信息

Department of Pharmaceutics, Jyothishmathi Institute of Pharmaceutical Sciences, Andhra Pradesh, India.

出版信息

Drug Res (Stuttg). 2013 Nov;63(11):586-90. doi: 10.1055/s-0033-1348258. Epub 2013 Jun 18.

Abstract

OBJECTIVE

The current study is intended to develop the fast dissolving tablets of Ketorolac tromethamine using different superdisintegrants to improve the dissolution rate and absorption rate to produce the bioavailability enhancement and rapid onset of action.

METHODS

In this, Ketorolac tromethamine fast dissolving tablets were prepared using different superdisintegrants and evaluated for different physical parameters, in vitro dissolution studies and in vivo pharmacokinetics to demonstrate the bioavailability enhancement. RESULTS & DISCUSSIONS: From the in vitro drug release studies, in case of optimized formulation, the cumulative percent drug release in 15 min (Q15) was found to be 94.34±1.68 where as the conventional tablets showed 28.78±0.82 in 15 min. The initial dissolution rate and dissolution efficiency of optimized formulation was 6.29%/min and 53.43 but it was 1.92%/min and 14.03 in conventional tablets. From the in vivo pharmacokinetic evaluation, the optimized formulation showed peak plasma concentration (Cmax) as 1 248.39 ng/ml at 1 h Tmax, but they were found to be 988.22 ng/ml at 2 h Tmax, in case of conventional tablets. The area under the curve for the optimized and conventional tablets was 3 890.68 and 3 173.07 ng-h/ml.

CONCLUSIONS

Hence the development of fast dissolving tablets using superdisintegrants was a good approach to improve the dissolution rate and absorption rate of Ketorolac tromethamine.

摘要

目的

本研究旨在使用不同的超级崩解剂开发酮咯酸氨丁三醇速溶片,以提高其溶出速率和吸收速率,从而增强生物利用度并实现快速起效。

方法

在此研究中,使用不同的超级崩解剂制备了酮咯酸氨丁三醇速溶片,并对其进行了不同物理参数、体外溶出度研究和体内药代动力学评估,以证明生物利用度的提高。结果与讨论:从体外药物释放研究来看,对于优化后的制剂,15分钟时的累积药物释放百分比(Q15)为94.34±1.68,而传统片剂在15分钟时为28.78±0.82。优化制剂的初始溶出速率和溶出效率分别为6.29%/分钟和53.43,而传统片剂分别为1.92%/分钟和14.03。从体内药代动力学评估来看,优化后的制剂在1小时达峰时间(Tmax)时的血浆峰浓度(Cmax)为1248.39纳克/毫升,而传统片剂在2小时Tmax时为988.22纳克/毫升。优化片剂和传统片剂的曲线下面积分别为3890.68和3173.07纳克-小时/毫升。

结论

因此,使用超级崩解剂开发速溶片是提高酮咯酸氨丁三醇溶出速率和吸收速率的一种良好方法。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验