Structure of supersaturated solution of poorly water-soluble drug indexed by mobility and diffusibility and the correlation with membrane permeability

2014 Fiscal Year Final Research Report

• Project/Area Number: 24590045
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Physical pharmacy
• Research Institution: Chiba University
• Principal Investigator: MORIBE Kunikazu 千葉大学, 薬学研究科(研究院), 教授 (50266350)
• Co-Investigator(Kenkyū-buntansha): YAMAMOTO Keiji 千葉大学, 大学院薬学研究院, 名誉教授 (50110341) ; HIGASHI Kenjirou 千葉大学, 大学院薬学研究院, 助教 (40451760)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: 固体分散体 / 過飽和

Outline of Final Research Achievements

The decrease of the substituent ratio of succinoyl group in HPMC-AS promoted the inhibition effect of drug crystallization. NMR measurements revealed that HPMC-AS suppressed the molecular mobility of drug and formed the hydrophobic interaction with drug. The molecular interaction between drug and HPMC-AS was strongest in acetyl group and weakest in succinoyl group of HPMC-AS, indicated by saturation transfer difference (STD)-NMR measurements. The molecular interaction between drug and HPMC-AS revealed by NMR measurement showed good correlation with the inhibitory effect of drug crystallization.

Free Research Field

製剤学