title: Improvement in solubility and bioavailability of puerarin by mechanochemical preparation.
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.
authors.affiliation: Key Laboratory of Pharmaceutical Engineering of Ministry of Education, Zhejiang University of Technology, Hangzhou, P.R. China.
authors.forename: Jie
authors.initials: J
authors.lastname: Xie
authors.forename: Fan
authors.initials: F
authors.lastname: Yang
authors.forename: Xiangjun
authors.initials: X
authors.lastname: Shi
authors.forename: Xingyi
authors.initials: X
authors.lastname: Zhu
authors.forename: Weike
authors.initials: W
authors.lastname: Su
authors.forename: Ping
authors.initials: P
authors.lastname: Wang
mesh_terms: D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D007529:Isoflavones / Q000138:chemical synthesis* / Q000378:metabolism*; D008297:Male; D055595:Mechanical Phenomena; D010316:Particle Size; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000378:metabolism*; D014961:X-Ray Diffraction
chemical_list: D007529:Isoflavones; D014665:Vasodilator Agents; C033607:puerarin