title: Enhanced dissolution rate and oral bioavailability of Ginkgo biloba extract by preparing solid dispersion via hot-melt extrusion.
abstract: The aim of this study was to improve the dissolution rate and oral bioavailability of Ginkgo biloba extract (GBE) through the preparation of G. biloba extract solid dispersions (GBE-SD) via hot-melt extrusion (HME). First, we prepared the GBE-SD based on a Kollidon® VA64/Kolliphor® RH40 (85:15) spray dried powder. Then physicochemical properties were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FT-IR). The results indicated that GBE dispersed well in a carrier matrix. Subsequently, we studied the dissolution profile of total flavonoids (TFs) by HPLC-UV and total terpene lactones (TTLs) by HPLC-ELSD. The dissolution percentage of TFs and TTLs was improved within 120min. Finally, we studied the pharmacokinetic characteristics and bioavailability in rats by UPLC-MS/MS. The results showed that the Cmax and AUC0-t of bilobalide (BB), ginkgolide A (GA), ginkgolide B (GB), ginkgolide C (GC), quercetin (QCT), kaempferol (KMF) and isorhamnetin (ISR) in rats were significantly increased after the oral administration of GBE-SD compared with results after the oral administration of GBE. These results suggest that the solid dispersion preparation by HME could serve as a promising formulation approach to enhancing the dissolution rate and oral bioavailability of GBE.
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Wenping
authors.initials: W
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Kang
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Na
authors.initials: N
authors.lastname: Liu
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Yewen
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Li
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Bochen
authors.initials: B
authors.lastname: Zhao
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Yanyan
authors.initials: Y
authors.lastname: Chen
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Lan
authors.affiliation: Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100005, China.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Ma
authors.affiliation: Department of Pharmaceutical Sciences, Beijing University of Chinese Medicine, Beijing 100102, China. Electronic address: qwu@sina.vip.com.
authors.forename: Qing
authors.initials: Q
authors.lastname: Wu
mesh_terms: D000818:Animals; D001682:Biological Availability; D003517:Cyclopentanes / Q000493:pharmacokinetics; D005663:Furans / Q000493:pharmacokinetics; D020441:Ginkgo biloba / Q000737:chemistry*; D046934:Ginkgolides / Q000493:pharmacokinetics; D044949:Kaempferols / Q000493:pharmacokinetics; D007783:Lactones / Q000493:pharmacokinetics; D008297:Male; D015394:Molecular Structure; D010936:Plant Extracts / Q000493:pharmacokinetics*; D011794:Quercetin / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D017207:Rats, Sprague-Dawley; D012995:Solubility
chemical_list: D003517:Cyclopentanes; D005663:Furans; D046934:Ginkgolides; D044949:Kaempferols; D007783:Lactones; D010936:Plant Extracts; C047368:3-methylquercetin; C058295:ginkgolide C; C006552:kaempferol; D011794:Quercetin; C045856:ginkgolide B; C073710:bilobalide; C477042:ginkgolide A
keywords: Bioavailability; Dissolution rate; Ginkgo biloba extract; Hot-melt extrusion; Solid dispersion