| 論文名 |
Inclusion complex of colchicine in hydroxypropyl-β-cyclodextrin tenders better solubility and improved pharmacokinetics. |
| 著者 |
Ritu Chauhan
Jitender Madan
Dinesh Kaushik
Satish Sardana
Ravi Shankar Pandey
Rakesh Sharma
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| キーワード |
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| 出版年月 |
1970年1月 |
| 発表先 |
Pharm Dev Technol. Mar-Apr 2013;18(2):313-22. |
| WEBサイト |
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| 論文概要（和文） |
ヒドロキシプロピル-β-シクロデキストリンへのコルヒチンの包接複合体は、溶解性を改善し、薬物動態を改善します。 |
| 論文概要（英文） |
Context: Colchicine (CLC) causes cell death by destabilizing the tubulin unit. However, it ionizes at physiological pH resultant low bioavailability and therapeutic efficacy. Objectives: We have attempted to augment the bioavailability of CLC by fabricating the inclusion complex with hydroxypropyl-β-cyclodextrin (HP-β-CD). Materials and methods: CLC-HP-β-CD inclusion complex was prepared and evaluated with Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, scanning electron microscopy, (1)H nuclear magnetic resonance ((1)H NMR) spectroscopy and rotating frame overhauser enhancement spectroscopy (ROESY). Oral bioavailability of CLC-HP-β-CD inclusion complex was analyzed using high performance liquid chromatography method. Results and discussion: Our phase-solubility data indicated the formation of a stable complex with K(c) ~0.31 mM(-1) at pH 7.4. (1)H NMR ascertains that NHCOCH(3) moiety of CLC enters in the HP-β-CD cavity and deshielded the H-3 and H-5 protons. ROESY also correlates the H(f) and H(g) of CLC with H-3 and H-5 protons of HP-β-CD and indicates that H(f) and H(g) protons of CLC are present either as cis and/or trans form in CLC-HP-β-CD inclusion complex. Pharmacokinetic studies showed a 1.82-fold increase in absolute bioavailability of CLC upon complexation. Conclusion: CLC-HP-β-CD inclusion complex may potentially be used as a viable formulation of CLC. |
