医药导报2012，Vol.31Issue(11)：1396-1400,5.DOI:10.3870/yydb.2012.11.002
盐酸伐昔洛韦多晶型的溶解性质与药动学研究
Solubility and Pharmacokinetics Study of Valacyclovir Hydrochloride
摘要
Abstract
Objective To study the bioavailability and solubility of valacyclovir hydrochloride for enhancing quality standards. Methods The solubility was determined and compared for the crystal form 1 , IV, Ⅷ of valacyclovir hydrochloride, the latter of which were administered to SD rats at the dose of 100 mg o kg-1. And a HPLC method was established to test the plasma level of valacyclovir hydrochloride. Results The form VU was the most soluble form among the three forms in the six solvents. The indirect pharmaeokinetic parameters of acyclovir,as the metabolites of the form I , Ⅳ ,Ⅷ of valacyclovir hydrochloride were as follows; Cmax was (10. 304±5. 246) , (9. 321 ±3. 701 ) and ( 10. 365±6. 787) mg ·L-1 , respectively(P>0. 05); AUC0→t was (20. 167 + 1. 775) , (22. 337±5. 166) and (20.289 + 7.845) mgoL-1 o h,respectively (P>0.05). Conclusion There is certain difference in solubility of valacyclovir hydrochloride among form I ,form FV and form Ⅷ, but no significant difference is found in biological actions in the body among them.and (20.289 + 7.845) mg·L-1· h,respectively (P>0.05). Conclusion There is certain difference in solubility of valacyclovir hydrochloride among form I ,form IV and form VI, but no significant difference is found in biological actions in the body among them.关键词
伐昔洛韦,盐酸/多晶型/溶解度/药动学Key words
Valacyclovir, hydrochloride/ Polymorphs/ Solubility/ Pharmaeokinetic分类
医药卫生引用本文复制引用
胡帆,赵睿,张丽,宋俊科,吕扬,杜冠华..盐酸伐昔洛韦多晶型的溶解性质与药动学研究[J].医药导报,2012,31(11):1396-1400,5.基金项目
科技重大专项"重大新药创制""药物晶型研发关键技术研究"(2009ZX09501-021) （2009ZX09501-021）
卫生行业科研专项(200802041,200902008) （200802041,200902008）
中药制造过程新技术国家重点实验室(SKL2010M0402) （SKL2010M0402）
