Development of a novel prediction method for oral absorption of drugs from lipid based formulation

2020 Fiscal Year Final Research Report

• Project/Area Number: 18K06808
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 47060:Clinical pharmacy-related
• Research Institution: Hiroshima International University
• Principal Investigator: Tanaka Yusuke 広島国際大学, 薬学部, 講師 (10435068)
• Project Period (FY): 2018-04-01 – 2021-03-31
• Keywords: 消化管吸収 / 過飽和溶解 / 脂質分散製剤 / BCS / IVIVC

Outline of Final Research Achievements

The aim of this study is to clarify absorption mechanisms after oral administration of drugs from various lipid-based formulations (LBFs). In in vitro digestion study, various solubilization behavior of drugs was observed depending on compositions of LBFs. However, the oral absorption of drugs in vivo were different than expectation from the results of in vitro digestion study. From a series of analysis, this discrepancy may be caused by ①lowered free concentration in the gastrointestinal tract owing to incorporation of drugs into the undigested lipid, ②improved re-solubilization of amorphous precipitate and ③different solubilization capacity of colloidal species composed of bile components and digestion products. The present study revealed detailed absorption mechanisms from LBFs with different compositions. Our findings may be useful for evaluation of drug absorption for from LBFs.

Free Research Field

薬剤学

Academic Significance and Societal Importance of the Research Achievements

脂質分散製剤(LBF)は薬物の溶解性を改善する手法として極めて有用である。しかし、LBFからの薬物吸収機構は十分に解明されていないため、可溶化技術としてLBFを選択しにくいことが問題となっている。本課題ではLBFからの薬物吸収機構を明らかにした。これにより、LBFからの薬物吸収性を予測することが可能になるものと期待される。従って、これまで優れた薬効を有していたにもかかわらず、低溶解性のため開発途中でドロップアウトしていたような化合物を開発することができ、また、LBF処方の最適化が容易となるため、優れたLBFの開発が可能となる。