title: Preparation and physicochemical characterization of a solid dispersion of (3, 5, 6-trimethylpyrazin-2-yl) methyl 3-methoxy-4-[(3, 5, 6-trimethylpyrazin-2-yl) methoxy] benzoate (VA-T) and polyvinylpyrrolidone.
abstract: Ischemic brain injury is a major disease which threatens human health and safety. (3, 5, 6-trimethylpyrazin-2-yl) methyl 3-methoxy-4-[(3, 5, 6-trimethylpyrazin-2-yl) methoxy] benzoate (VA-T), a newly discovered lead compound, is effective for the treatment of ischemic brain injury and its sequelae. But the poor solubility of VA-T leads to poor dissolution and limited clinical application. In order to improve the dissolution of VA-T, the pharmaceutical technology of solid dispersions was used in the present study. VA-T/polyvinylpyrrolidone (PVP) solid dispersion was prepared by the solvent method. The dissolution studies were carried out and solid state characterization was evaluated by differential scanning calorimetry (DSC), infrared spectroscopy (IR), x-ray diffraction (XRD) and scanning electron microscopy (SEM). The dissolution rate of VA-T was significantly improved by solid dispersion compared to that of the pure drug and physical mixture. The results of DSC and XRD indicated that the VA-T solid dispersion was amorphous. The IR spectra showed the possible interaction between VA-T and PVP was the formulation of hydrogen bonding. The SEM analysis demonstrated that there was no VA-T crystal observed in the solid dispersions. The ideal drug-to-PVP ratio was 1:5. In conclusion, the solid dispersion technique can be successfully used for the improvement of the dissolution profile of VA-T.
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Sa-Li
authors.initials: SL
authors.lastname: Cao
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Hou
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Bin
authors.initials: B
authors.lastname: Li
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Fu
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Xing-Bin
authors.initials: XB
authors.lastname: Yin
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Xiao-Fang
authors.initials: XF
authors.lastname: Dang
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Chun-Jing
authors.initials: CJ
authors.lastname: Yang
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Jin
authors.initials: J
authors.lastname: Zhang
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Zhang
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Hai-Min
authors.initials: HM
authors.lastname: Lei
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. Electronic address: njtcm@263.net.
authors.forename: Jian
authors.initials: J
authors.lastname: Ni
mesh_terms: D001565:Benzoates / Q000008:administration & dosage / Q000737:chemistry*; D002545:Brain Ischemia / Q000188:drug therapy; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems; D011205:Povidone / Q000737:chemistry*; D012995:Solubility
chemical_list: D001565:Benzoates; D011205:Povidone
keywords: Dissolution; Ischemic stroke; Physicochemical characterization; Solid dispersions; VA-T