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Improvement in solubility and bioavailability of puerarin by mechanochemical preparation
Jie Xie1, Fan Yang, Xiangjun Shi
1Key Laboratory of Pharmaceutical Engineering of Ministry of Education, Zhejiang University of Technology, Hangzhou, P.R. China.
Abstract:
An efficient and solvent-free procedure was developed to improve the solubility and bioavailability of the poorly water-soluble drug puerarin by mechanochemical technology. The stable inclusion complex of puerarin and 2-hydroxypropyl-β-cyclodextrin (HPCD) was prepared by a ball mill under the following conditions: equimolar ratio of puerarin to HPCD; rotational speed of 250 rpm; milling time of 90 min; steel balls of 22 mm diameter. The solid complex was characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffractometry (XRD), and fourier transformation-infrared spectroscopy (FT-IR). Mechanochemical action could result in enhanced molecular encapsulation, homogeneous distribution and amorphization of the drug. In comparison to puerarin, a 1.64-fold increase in absolute bioavailability was obtained. The solubility of the inclusion complex was 25.33-fold higher and the drug release amount reached 79.44% at 15 min, 2.76-fold higher.
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