摘要
目的研究盐酸索他洛尔脉冲微丸的体外释放特性,根据本类脉冲释放曲线的关键点的比较指导处方优化。方法采用多种数学模型拟合释放曲线,并对各曲线回归方程进行拟合优度测验;同时利用曲线的载荷信息,通过曲线的生长速度函数的一阶和二阶导数得到曲线变化的数学突变点。结果Logistic拟合释放曲线的拟合优度x2及AIC最小,r2最接近于1,说明Logistic拟合效果最好;同时得到比较本类型释放曲线的3个关键点t1=-(lnc2+1.317)/c3,tm=(lnc2)/c3,t2=(1.317-lnc2)/c3,将曲线分为迟释期(0～t1)、突释期(t1～t2)以及减速释放期(t2～∞)。结论通过本类型的曲线拟合及推导,提出可以用模拟曲线的关键点评价不同处方的释放特性,从而指导及优化处方并作进一步研究。
OBJECTIVE To investigate release behavior of sotalol hydrochloride pulsatile pellets in vitro, and to realize pulsatile release mechanism and optimize formulation. METHODS The release profile of sotalol hydrochloride pellets were fitted and compared by employing different kinds of mathematic model. For fitting a good curve regression equation, the adopting x2 and AIC test were used. By first and second derivative of velocity function from growth process of logistic curve, the yielding points displaying the variety of curve were obtained and compared. RESULTS The Logistic model was the best one for fitting the pulsatile release profiles among the several mathematical models. The three key-points were obtained by Logistic curve： t1=-（lnc2＋1.317）/c3,tm=（lnc2）/c3,t2=（1.317-lnc2）/c3. And using two yielding points of the velocity function from the growth process of Logistic model, the release profile was divided into time-delayed release （0-t1）, rupturing release （t1-t2）, decelerating release （t2～∞）. CONCLUSION The regression and prediction indicated that, we can employ the yielding points of the model curve to evaluate the release properties from different formulations. The optimization of the formulation could be guided by the comparison of three key-points.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2009年第5期358-361,共4页
Chinese Pharmaceutical Journal
