Formulation approaches to improving the delivery of an antiviral drug with activity against seasonal flu

被引：3

作者：

Sammeta, Srinivasa M. ^{[1
]}

Wang, Li ^{[1
]}

Mutyam, Shravan K. ^{[1
]}

O'Loughlin, Kathleen ^{[1
]}

Green, Carol E. ^{[1
]}

Werner, Milton H. ^{[2
]}

Kelly, Terence ^{[3
]}

Shankar, Gita N. ^{[1
]}

机构：

[1] SRI Int, Biosci Div, Pharmaceut Dev, Menlo Pk, CA 94025 USA

[2] Inhibikase Therapeut Inc, Atlanta, GA USA

[3] Kelly Pharma Res Consulting LLC, Ridgefield, CT USA

来源：

PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY | 2015年 / 20卷 / 02期

关键词：

Bioavailability; co-solvents; cyclodextrins; solubility; Ussing chambers; NOSCAPINE;

D O I：

10.3109/10837450.2013.852574

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The main objective of the present study was to develop formulations of noscapine hydrochloride hydrate with enhanced solubility and bioavailability using co-solvent- and cyclodextrin-based approaches. Different combinations of co-solvents, which were selected on the basis of high-throughput solubility screening, were subjected to in vitro intestinal drug permeability studies conducted with Ussing chambers. Vitamin E tocopherol polyethylene glycol succinate and propylene glycol based co-solvent formulations provided the maximum permeability coefficient for the drug. Inclusion complexes of the drug were prepared using hydroxypropyl-b-cyclodextrin and sulphobutylether cyclodextrins. Pharmacokinetic studies were carried out in male Sprague-Dawley rats for the selected formulations. The relative bioavailabilities of the drug with the co-solvent- and cyclodextrin-based formulations were found to be similar.

引用

页码：169 / 175

页数：7

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