Drug Delivery System
Online ISSN : 1881-2732
Print ISSN : 0913-5006
ISSN-L : 0913-5006
[Feature articles] “:Species difference problem on formulation design” Editor:Hiroshi Kikuchi
Species differences in oral bioavailability enhancement of lipid based formulation
Masaaki ImonoKatsuji Sugita
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2017 Volume 32 Issue 5 Pages 389-395

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Abstract
Improvement of oral absorption for poorly water-soluble compounds is a major concern to the pharmaceutical industry. Although various formulation studies have been investigated to overcome the issue of poorly water-soluble compounds, the performance difference of the formulations between animal species is still not well known. This article is designed to contribute further research on oral bioavailability (BA) enhancements by lipid based formulation among animal species. Compound A was used as a poorly water-soluble drug. The lipid based formulation of Compound A was prepared by lipid and lecithin, and administered to rats, dogs and monkeys. Oral absorption of the lipid based formulation was dramatically enhanced, but the effect of the formulation on BA was different among the animal species. The BA enhancement ratios of the lipid formulation to conventional formulation, in rats, dogs and monkeys were 2.2, 6.3 and 3.5, respectively. Pharmacokinetic analysis suggested that the difference of gastro-intestinal and hepatic first pass metabolisms affected the performance of the lipid based formulation of Compound A.
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© 2017 The Japan Society of Drug Delivery System
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