Statistically designed enzymatic hydrolysis of an icariin/β-cyclodextrin inclusion complex optimized for production of icaritin

Autor: Xin Jin, Zhenhai Zhang, E. Sun, Songlin Li, Xiaobin Jia
Jazyk: angličtina
Rok vydání: 2012
Předmět:
Zdroj: Acta Pharmaceutica Sinica B, Vol 2, Iss 1, Pp 83-89 (2012)
Druh dokumentu: article
ISSN: 2211-3835
2211-3843
DOI: 10.1016/j.apsb.2011.12.004
Popis: This study focuses on the preparation and enzymic hydrolysis of an icariin/β-cyclodextrin inclusion complex to efficiently generate icaritin. The physical characteristics of the inclusion complex were evaluated by differential scanning calorimetry (DSC). Enzymatic hydrolysis was optimized for the conversion of icariin/β-cyclodextrin complex to icaritin by Box–Behnken statistical design. The inclusion complex formulation increased the solubility of icariin approximately 17-fold, from 29.2 to 513.5 μg/mL at 60 °C. The optimum conditions were predicted by Box–Behnken statistical design as follows: 60 °C, pH 7.0, the ratio of enzyme/substrate (1:1.1) and reaction time 7 h. Under the optimal conditions the conversion of icariin was 97.91% and the reaction time was decreased by 68% compared with that without β-CD inclusion. Product analysis by melting point, ESI-MS, UV, IR, 1H NMR and 13C NMR confirmed the authenticity of icaritin with a purity of 99.3% and a yield of 473 mg of icaritin from 1.1 g icariin.
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