摘要
(目的)测定阿昔洛韦在不同pH介质中的平衡溶解度及在正辛醇-水/缓冲体系中的表观油水分配系数,为阿昔洛韦新剂型研究提供基础。(方法)采用高效液相色谱法测定阿昔洛韦在不同pH介质中的平衡溶解度,采用摇瓶法测定阿昔洛韦在正辛醇-水/缓冲体系中的表观油水分配系数。(结果)在37℃下,阿昔洛韦在pH值为1.0、1.2、1.4、1.6、1.8、2.0、2.2、3.0、4.0、4.5、5.8、6.8、7.4、8.0的缓冲液和水中,平衡溶解度分别为14.91、10.62、8.28、5.14、3.52、2.30、1.97、2.16、1.58、1.61、1.18、1.19、1.10、1.02、1.02 mg·mL^(-1),平均表观油水分配系数(P_(O/W))分别为0.0222、0.0259、0.0046、0.0252、0.0075、0.0558、0.0190、0.0157、0.0146、0.0129、0.0138、0.0382、0.0214、0.0129和0.0753。(结论)阿昔洛韦微溶于水,在pH 1.0~8.0范围内平衡溶解度随pH值的增大而减小;阿昔洛韦的表观油水分配系数小,亲脂性小,提示阿昔洛韦为低渗透性药物。
(Objective)To determine the equilibrium solubility of acyclovir in different pH media and its apparent oil/water distribution coefficient in n-octanol-water/buffering system,so as to provide a basis for the study of new dosage forms of acyclovir.(Methods)The equilibrium solubility of acyclovir in different pH media was determined by HPLC,and the apparent oil/water distribution coefficient of acyclovir in n-octanol-water/buffering system was determined by shaking flask method.(Results)At 37℃,the equilibrium solubility of acyclovir in pH 1.0,1.2,1.4,1.6,1.8,2.0,2.2,3.0,4.0,4.5,5.8,6.8,7.4,8.0 buffer and water was 14.91,10.62,8.28,5.14,3.52,2.30,1.97,2.16,1.58,1.61,1.18,1.19,1.10,1.02 and 1.02 mg/mL,and the average apparent oil/water distribution coefficient(P_(O/W))was 0.0222,0.0259,0.0046,0.0252,0.0075,0.0558,0.0190,0.0157,0.0146,0.0129,0.0138,0.0382,0.0214,0.0129 and 0.0753.(Conclusion)Acyclovir is slightly soluble in water,and the equilibrium solubility decreases with the increase of pH value in the range of pH 1.0~8.0.The apparent oil/water distribution coefficient and lipophilicity of acyclovir are small,suggesting that acyclovir is a low permeability drug.
作者
谢娜娜
黄玉香
林水森
谢志新
Xie Nana;Huang Yuxiang;Lin Shuisen;Xie Zhixin(Department of Pharmacy,Quanzhou Medical College,Quanzhou 362100,China)
出处
《云南化工》
CAS
2021年第12期66-68,共3页
Yunnan Chemical Technology
基金
福建省中青年教师教育科研项目(编号:JAT171159),泉州医学高等专科学校校级课题(编号:XJ1425A)。
关键词
阿昔洛韦
平衡溶解度
表观油水分配系数
acyclovir
equilibrium solubility
apparent oil/water distribution coefficient
