Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability
To improve the stability and oral bioavailability of Z-ligustilide (LIG), the inclusion complex of LIG with hydroxypropyl- β-cyclodextrin (HP-β-CD) was prepared by the kneading method and characterized by UV-Vis spectroscopy, differential thermal analysis (DTA) and Fourier transform infrared (FTIR)...
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Sciendo
2014-06-01
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Series: | Acta Pharmaceutica |
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Online Access: | http://www.degruyter.com/view/j/acph.2014.64.issue-2/acph-2014-0012/acph-2014-0012.xml?format=INT |
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author | Lu Yapeng Liu Siyuan Zhao Yu Zhu Li Yu Shuqin |
author_facet | Lu Yapeng Liu Siyuan Zhao Yu Zhu Li Yu Shuqin |
author_sort | Lu Yapeng |
collection | DOAJ |
description | To improve the stability and oral bioavailability of Z-ligustilide (LIG), the inclusion complex of LIG with hydroxypropyl- β-cyclodextrin (HP-β-CD) was prepared by the kneading method and characterized by UV-Vis spectroscopy, differential thermal analysis (DTA) and Fourier transform infrared (FTIR) spectroscopy. LIG is capable of forming an inclusion complex with HP-b-CD and the stoichiometry of the complex was 1:1. Stability of the inclusion complex against temperature and light was greatly enhanced compared to that of free LIG. Further, oral bioavailability of LIG and the inclusion complex in rats were studied and the plasma drug concentration-time curves fitted well with the non-compartment model to estimate the absolute bioavailability, which was 7.5 and 35.9 %, respectively. In conclusion, these results show that LIG/HP-β-CD complexation can be of great use for increasing the stability and biological efficacy of LIG |
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id | doaj.art-32a9d5ee84d84303bca9ae3fee5333b4 |
institution | Directory Open Access Journal |
issn | 1330-0075 1846-9558 |
language | English |
last_indexed | 2024-12-22T17:01:07Z |
publishDate | 2014-06-01 |
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spelling | doaj.art-32a9d5ee84d84303bca9ae3fee5333b42022-12-21T18:19:20ZengSciendoActa Pharmaceutica1330-00751846-95582014-06-0164221122210.2478/acph-2014-0012acph-2014-0012Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailabilityLu Yapeng0Liu Siyuan1Zhao Yu2Zhu Li3Yu Shuqin4Institute of Nautical Medicine, Nantong University, Nantong 226001, ChinaSchool of Life Sciences, Nantong University, Nantong 226007, ChinaInstitute of Nautical Medicine, Nantong University, Nantong 226001, ChinaInstitute of Nautical Medicine, Nantong University, Nantong 226001, ChinaJiangsu Key Laboratory for Supramolecular Medicinal Materials and Applications College of Life Sciences, Nanjing Normal University, Nanjing 210046, ChinaTo improve the stability and oral bioavailability of Z-ligustilide (LIG), the inclusion complex of LIG with hydroxypropyl- β-cyclodextrin (HP-β-CD) was prepared by the kneading method and characterized by UV-Vis spectroscopy, differential thermal analysis (DTA) and Fourier transform infrared (FTIR) spectroscopy. LIG is capable of forming an inclusion complex with HP-b-CD and the stoichiometry of the complex was 1:1. Stability of the inclusion complex against temperature and light was greatly enhanced compared to that of free LIG. Further, oral bioavailability of LIG and the inclusion complex in rats were studied and the plasma drug concentration-time curves fitted well with the non-compartment model to estimate the absolute bioavailability, which was 7.5 and 35.9 %, respectively. In conclusion, these results show that LIG/HP-β-CD complexation can be of great use for increasing the stability and biological efficacy of LIGhttp://www.degruyter.com/view/j/acph.2014.64.issue-2/acph-2014-0012/acph-2014-0012.xml?format=INTZ-ligustilidehydroxypropyl-β-cyclodextrininclusion complexstabilitybioavailability |
spellingShingle | Lu Yapeng Liu Siyuan Zhao Yu Zhu Li Yu Shuqin Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability Acta Pharmaceutica Z-ligustilide hydroxypropyl-β-cyclodextrin inclusion complex stability bioavailability |
title | Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability |
title_full | Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability |
title_fullStr | Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability |
title_full_unstemmed | Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability |
title_short | Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability |
title_sort | complexation of z ligustilide with hydroxypropyl β cyclodextrin to improve stability and oral bioavailability |
topic | Z-ligustilide hydroxypropyl-β-cyclodextrin inclusion complex stability bioavailability |
url | http://www.degruyter.com/view/j/acph.2014.64.issue-2/acph-2014-0012/acph-2014-0012.xml?format=INT |
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