正交试验法优化利多卡因传递体

Orthogonal Design Test to Optimize Lidocaine Transfersomes

筛选利多卡因传递体得到制备药物的最佳配比。为利用排列整齐的水平-因素指标对利多卡因传递体试验进行整体设计、综合比较、统计分析,实现通过少数的实验次数找到较好的生产条件,以达到最高生产工艺效果。采用正交试验法优化利多卡因传递体配比的药物量,以包封率和载药量作为考察指标,采用L9(34)正交试验优化利多卡因传递体的处方。这样能对该实验各关键因素变化范围内均衡抽样,使每次试验都具有较强的代表性。由于正交表具备均衡分散的特点,保证了全面实验的某些要求,往往能够较好或更好地达到研究目的。试验结果表明,利多卡因传递体的最佳处方是A2B3C1D2组合,即卵磷脂:胆固醇为2:1;卵磷脂:利多卡因为3:1;甲醇:氯仿为1:1;超声时间为10min。用此处方配比得到的利多卡因传递体的平均粒径为(81.1±3.1)nm。包封率为(80.95±0.5)%,载药量为(1.87±0.03)%。由此,经过正交试验法优选利多卡因传递体处方在配比上得到的药物质量最佳,载药量适宜大小适中、稳定性好,能够为以后的利多卡因传递体透皮给药提供实验依据。

Screening of lidocaine transfersomes is to obtain the best ratio of preparation and to achieve good performance for production processes. The level-factor indicators shown in Table 1 are used as orthogonal rows, comprehensive comparison and statistical analysis are carried out to determine the best conditions through a limited number of experiments. Lidocaine transfersomes volume ratio is obtained with encapsulation efgiciency and drug loading as the inspection targets, in L9（3^4） orthogonal test. Each test has a good representation. The orthogonal table with a balanced dispersion characteristics of a comprehensive experiment can ensure some key requirements. The experimental results show that Lidocaine transfersomes A2B3C1D2 is the best combination of prescription, that is, lecithin： cholesterol 2：1; lecithin： lidocaine 3：1; methanol： chloroform 1：1; ultrasonic time of 10 min. This ratio has been used here to convey the body of lidocaine with the average particle size of （81.1±3.1） nm, with encapsulation efficiency of （80.95±0.5）% for the drug loading （1.87±0.03）%. Therefore, through the orthogonal tests we get prescription drugs of the best quality, with drug loading suitable for moderate size and good stability.