Lipid-based formulations for improving oral absorption of poorly water-soluble drugs

2018 Fiscal Year Final Research Report

• Project/Area Number: 16K18967
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Medical pharmacy
• Research Institution: Setsunan University
• Principal Investigator: Higashino Haruki 摂南大学, 薬学部, 助教 (60736784)
• Project Period (FY): 2016-04-01 – 2019-03-31
• Keywords: 自己乳化型製剤 / 難水溶性薬物 / 過飽和溶解

Outline of Final Research Achievements

As one of the formulation techniques to improve oral absorption of poorly water-soluble drugs, lipid-based formulation (LBF) attracts much attention from the pharmaceutical companies. In this study, the performance of LBFs in the gastrointestinal (GI) tract, such as the release of loaded drugs along with the dilution by the GI fluid and the digestion of lipid components by lipase was investigated in vitro and in vivo.
As the results, medium-chain (MC) lipids were rapidly digested by lipase and released drugs induced the supersaturation. This step contributed to the increase in the absorption rate and the systemic exposure of drugs in vivo. Therefore, in order to design the potent LBFs for poorly water-soluble drugs, release profiles of drugs from LBFs should be observed carefully under various conditions.

Free Research Field

消化管吸収

Academic Significance and Societal Importance of the Research Achievements

近年の医薬品開発では、難水溶性を示す候補化合物の数が増えている。一方、これら化合物を実際の経口製剤として開発する場合、投与後、消化管内で速やかに溶解し体内に吸収される必要がある。本研究では、難水溶性薬物の溶解性を改善させる手法の一つである自己乳化型製剤を調製し、経口投与後の消化管内での薬物の放出性や血中曝露量の改善効果に関する検討を行い、吸収メカニズムの一つとして過飽和溶解の関与を明らかにした。