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.
10.1016/S1875-5364(15)30090-X
- Author:
Sa-Li CAO
1
;
Peng HOU
1
;
Bin LI
1
;
Jing FU
1
;
Xing-Bin YIN
1
;
Xiao-Fang DANG
1
;
Chun-Jing YANG
1
;
Jin ZHANG
1
;
Hui ZHANG
1
;
Hai-Min LEI
1
;
Jian NI
2
Author Information
1. School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
2. School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. Electronic address: njtcm@263.net.
- Publication Type:Journal Article
- Keywords:
Dissolution;
Ischemic stroke;
Physicochemical characterization;
Solid dispersions;
VA-T
- MeSH:
Benzoates;
administration & dosage;
chemistry;
Brain Ischemia;
drug therapy;
Chemistry, Pharmaceutical;
methods;
Drug Delivery Systems;
Povidone;
chemistry;
Solubility
- From:
Chinese Journal of Natural Medicines (English Ed.)
2015;13(11):861-866
- CountryChina
- Language:English
-
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.
