2012 Fiscal Year Final Research Report
Potential use of supramolecular cyclodextrins for the design of patient- friendly super-generic drug formulations
| Project/Area Number |
22590164
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Medical pharmacy
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| Research Institution | Sojo University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
IOHARA Daisuke 崇城大学, 薬学部, 助手 (40454954)
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| Project Period (FY) |
2010 – 2012
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| Keywords | 親水性シクロデキストリン / 包接複合体 / グリメピリド / 次世代型口腔内崩壊錠 / 嚥下性向上 / 放出制御, スーパージェネリック製剤 |
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| Research Abstract |
2-Hydroxybutyl-β-CyD (HB-β-CyD) is a new hydroxyalkylated β-CyD derivative that has one more methylene group in the substituent of 2-hydroxypropyl-β-cyclodextrin (HP-β-CyD). Some physicochemical and biological properties of HB-β-CyD, such as surface activity, moisture sorption, hemolytic activity and solubilizing ability for poorly water-soluble drugs were studied in comparison with those of HP-β-CyD. Then, a combined use of various CyDs and stearoxy ether of hydroxypropylmethylcellulose (SangeloseR) was investigated to improve usability of orally disintegrating tablets (ODTs). Glimepiride, a potent third generation hypoglycemic agent for type 2 diabetes was used as a model drug, because it is poorly water-soluble with long linear structure and biological half life is short. Solubility and NMR studies demonstrated that glimepiride formed water-soluble complexes with CyDs, where the magnitude of the stability constant increased in the order of HB-β-CyD > HP-β-CyD > β-CyD > γ-CyD D
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