当前位置： SCI文献检索 > INTERNATIONAL JOURNAL OF PHARMACEUTICS期刊下所有文献 > Positively charged self-nanoemulsifying oily formulations of olmesartan medoxomil: Systematic development, in vitro, ex vivo and in vivo evaluation.

Positively charged self-nanoemulsifying oily formulations of olmesartan medoxomil: Systematic development, in vitro, ex vivo and in vivo evaluation.

Abstract：

:The current research work explores the potential applications of cationic self-nanoemulsifying oily formulations (CSNEOFs) for enhancing the oral bioavailability of olmesartan medoxomil. Initial preformulation studies, risk assessment and factor screening studies revealed selection of oleic acid, Tween 40 and Transcutol HP as the critical factors. Systematic optimization of SNEOFs was carried out employing D-optimal mixture design and evaluating them for responses viz. emulsification efficiency, globule size and in vitro drug release. The CSNEOFs were prepared from the optimized SNEOFs by adding oleylamine as cationic charge inducer. In vitro cell line studies revealed markedly better drug uptake along with safer and biocompatible nature of CSNEOFs than free drug suspension. In situ perfusion, and in vivo pharmacokinetic and pharmacodynamic studies in Wistar rats revealed significant improvement in the biopharmaceutical performance of the drug from CSNEOFs and SNEOFs vis-à-vis the marketed formulation. Successful establishment of various levels of in vitro/in vivo correlations (IVIVC) substantiated high degree of prognostic ability of in vitro dissolution conditions in predicting the in vivo performance. In a nutshell, the present studies report successful development of CSNEOFs of olmesartan medoxomil with distinctly improved biopharmaceutical performance.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Beg S,Sharma G,Thanki K,Jain S,Katare OP,Singh B

doi

10.1016/j.ijpharm.2015.07.048

subject

Has Abstract

pub_date

2015-09-30 00:00:00

pages

466-82

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(15)30066-1

journal_volume

493

pub_type

杂志文章

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