星点设计 -效应面法优化杜仲漂浮型脉冲释放片处方的研究

目的 采用星点设计-效应面法优化杜仲漂浮型脉冲释放片的处方.方法 在前期单因素试验的基础上,以包衣层材料中羟丙甲纤维素(HPMCK15M)、乳糖、碳酸氢钠的百分含量为考察因素,以释药时滞和起漂时间为考察指标,采用Design-Ex-pert 8.06软件进行试验设计,对指标与因素之间进行多元线性和二次多项式方程拟合,通过效应面法优化最佳处方为:HPMCK15M、乳糖、碳酸氢钠分别占包衣层质量的35％、20％、20％,并对其进行验证.结果 各指标与因素之间二次多项式方程拟合良好,相关系数R2分别为0.9655和0.9668,采用优化处方制备的杜仲漂浮型脉冲释放片具有脉冲释药和快速漂浮特性,各指标实测值与预测值偏差+1.94％和-3.77％.结论 星点设计-效应面法可用于本制剂处方的优化,所制得的杜仲漂浮型脉冲释放片具有体外定时脉冲释药特性.

Optimization on formulation of Eucommia ulmoides floating pulse drug delivery tablets by central composite design-response surface method

Objective To optimize the formulation of Eucommia ulmoides floating pulse drug delivery tablets by central composite design-response surface method.Methods On the basis of the previous single factor tests, the percentage of H ydroxypropyl Methycel. lulose (HPMCK15M), lactose and sodium bicarbonate (NaHCO3) in the coating material was taken as the investigation factor, the lag timeof drug release and the time of floating as the investigation index, and the Design-Expert 8.06 software was applied for central compos. ite design. The data were simulated using multi-linear equation and second-order polynomial equation. The possibly optimal formula.tion of coating layer was predicted by response surface method: the best ratios of HPMCK15, lactoseand sodium bicarbonate were 35%, 20%, and 20%, respectively, which was then validated.Results The investigation factor and index agreed well with second-order poly. nomial equation and R2 were 0.965 5 and 0.966 8. The floating pulse release tablets prepared with the optimized formulation had thecharacteristics of rapid floating and pulse release. The deviation between the measured values and the predicted values of each indexwas within +1.94% and .3.77%.Conclusions The central composite design-response surface method can be used to optimize the for. mulation of this preparation. The prepared floating pulse release tablet of Eucommia ulmoides has the characteristics of in vitro timed pulse release.