In vitro and in situ characterization of triterpene glycosides from Cimicifuga racemosa extract
Cimicifuga racemosa products are widely used in the treatment of climacteric symptoms. The aim of this study was to evaluate C racemosa extract Ze 450 according to Biopharmaceutics Classification System (BCS). Triterpene glycosides served as analytical marker and were evaluated for solubility and ab...
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| Main Authors: | , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
4 August 2017
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| In: |
Journal of pharmaceutical sciences
Year: 2017, Volume: 106, Issue: 12, Pages: 3642-3650 |
| ISSN: | 1520-6017 |
| DOI: | 10.1016/j.xphs.2017.07.023 |
| Online Access: | Verlag, Volltext: http://dx.doi.org/10.1016/j.xphs.2017.07.023 Verlag, Volltext: http://www.sciencedirect.com/science/article/pii/S0022354917305580 
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| Author Notes: | Lucia Disch, Kristina Forsch, Beate Siewert, Jürgen Drewe, Gert Fricker |
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| 520 | |a Cimicifuga racemosa products are widely used in the treatment of climacteric symptoms. The aim of this study was to evaluate C racemosa extract Ze 450 according to Biopharmaceutics Classification System (BCS). Triterpene glycosides served as analytical marker and were evaluated for solubility and absorption properties. pH-dependent thermodynamic solubility was tested via shake flask method, and dissolution performance of a herbal medicinal product containing C racemosa extract Ze 450 was assessed. Absorption was estimated by in vitro permeation through Caco-2 monolayers. Furthermore, different intestinal segments were screened for absorption performance using an in situ rat model. Over a physiological pH range, triterpene glycosides exhibited pH-dependent solubility with highest concentration at pH 7.5. Dissolution profiles showed rapid dissolution of actein and 23-epi-26-deoxyactein. Furthermore, 23-epi-26-deoxyactein as surrogate for contained triterpene glycosides showed a high permeability through Caco-2 monolayers. Results of in situ rat model showed absorption capacity for 23-epi-26-deoxyactein in duodenum, jejunum, ileum, and colon. The results indicate high bioavailability of triterpene glycosides from C racemosa extract Ze 450. With regard to BCS, triterpene glycosides can be classified into BCS class I (high solubility, high permeability). | ||
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