摘要
目的测定咪喹莫特的油水分配系数(P),考察油水分配系数与透皮速率常数(J)之间的相关性。方法采用HPLC法测定咪喹莫特的质量分数,摇床法和涡旋法测定油水分配系数,通过Franz扩散池法测定不同pH介质下药物的透皮速率常数,建立lg P与透皮速率常数间的相关模型。结果摇床法和涡旋法所测得的lg P差异不明显,当溶剂介质pH值在4.5~7.4之间时,lg P随pH值增大而增大;lg P与透皮速率常数符合线性方程J=-1.47lg P^2+4.15lg P-1.49,r=0.975 2。结论介质pH值在pH5.8附近时,咪喹莫特的透皮吸收速率常数最大;当介质pH值在4.5~7.4之间时,咪喹莫特的透皮速率常数与lg P有良好线性关系。
Objective To determine the partition coefficient of imiquimod and study the correlation between oil-water partition coefficient（ P） and penetration rate constant（ J）. Methods HPLC method was used to determine the concentration of Imiquimod,and the shaking method and vortex method was used to determine the oil-water partition coefficient. The penetration rate constant in different pH was determined by Franz diffusion cell method. The correlation model between lg P and percutaneous absorption rate was established.Results There was no significant difference between the shaking method and vortex method. When the solvent medium pH was between 4.5 and 7.4,lg P increased with the promotion of pH value. lg P and the penetration rate constant were in line with the linear equation J =- 1.47 lg P2＋ 4.15 lg P- 1.49,r = 0.975 2.Conclusion In the vicinity of pH5.8,the transdermal absorption rate constant J of Imiquimod reached the maximum. When the pH value of medium was between 4. 5 and 7. 4,there was a good linear relationship between the imiquimod penetration rate constant J and lg P.
出处
《广东药学院学报》
CAS
2016年第6期671-674,共4页
Academic Journal of Guangdong College of Pharmacy
基金
广东省科技计划项目(2014A020212417
2013B021800088)
关键词
咪喹莫特
油水分配系数
透皮吸收速率常数
相关性
imiquimod
oil-water partition coefficient
transdermal absorption rate constant
relationship
