Study on different β-cyclodextrin and its derivatives for solubilization and dissolution of entecavir
- VernacularTitle:不同β－环糊精衍生物的恩替卡韦包合物的溶解度和溶出度研究
- Author:
Meisong WANG
;
Haitao WU
;
Min WANG
;
Shengwen CHEN
- Publication Type:Journal Article
- Keywords:
entecavir;
β-cyclodextrin and its derivatives;
inclusion complex;
solubility;
dissolution
- From:
Chinese Journal of Biochemical Pharmaceutics
2015;(3):172-175
- CountryChina
- Language:Chinese
-
Abstract:
Objective To prepared inclusion complex of β-cyclodextrin (β-CD) and its derivatives (methyl -β-cyclode-xtrin, 2,6-dimethyl -β-cyclodextrin, hydroxypropyl -β-cyclodextrin ) with entrcavir, and explore effect of different inclusion complex on the solubility and dissolution of entecavir.Methods Regression equation was established,prepared the inclusion complexes by a magnetic stiring method,grinding method and ultrasonic method.While inclusion rate was an index,the effects of reaction process was inquired by mole ratio, inclusion temperature, inclusion time and stirring rate and the most suitable method and technology of inclusion was optimized.Determinated the solubility with HPLC method and investigated in vitro dissolution with a small cup method.Results The regression equation was A=1.026 ×106C+4248.8, R2 =0.9999 (n=6), in the range of 0.497~4.97 g/mL, linear relationship was good.The best inclusion method was magnetic stirring, the best process conditions were: mole ratio was 1 ︰1, stirring speed was 300 r/min, inclusion time was 4 hours, inclusion temperature was 50 ℃.The four inclusion complexes all were white loose powder materials.The solubility of ETV,β-CD-ETV,HP-β-CD-ETV,RM-β-CD-ETV,2,6-DM-β-CD-ETV were 2.51, 13.4, 18.9, 37.6 and 89.5 g/L.The dissolution rates was ETV<β-CD-ETV
