磷酸川芎嗪透皮贴剂制备及辛夷挥发油促渗作用考察

Primarily exploration of the preparation of Ligustrazine Phosphate Transdermal Patches and the effect on permeation Enhancing of volatile oil of Flos Magnoliae

目的制备磷酸川芎嗪透皮贴剂,并考察辛夷挥发油对贴剂中磷酸川芎嗪经皮渗透的影响。方法选择Eudragit E100、丁二酸、邻苯二甲酸二乙酯3个因素,采用L9(34)正交试验设计,以累积渗透量和初黏力为指标优选磷酸川芎嗪贴剂的基质配比;用改良的Franz扩散池进行透皮吸收实验,比较3%、5%、7%辛夷挥发油对贴剂中磷酸川芎嗪的促渗作用。结果磷酸川芎嗪透皮贴剂的最佳制备工艺为A2B1C3(Eudragit E100:丁二酸:邻苯二甲酸二乙酯=1.60∶0.05∶0.6)。在贴剂处方中加入辛夷挥发油促渗剂后,药物累积渗透量增加,3%、5%、7%辛夷组的12h累积平均渗透量分别是3 720.114、5 470.13、4115.408μg.cm-2.h-1,其增渗倍数分别为1.123、1.601、1.209。结论优选出的基质配比可制备质量较佳的磷酸川芎嗪透皮贴剂,黏着力符合要求,5%辛夷挥油对磷酸川芎嗪透皮贴剂有明显促透皮作用。

OBJECTIVE To prepare Ligustrazine Phosphate （LP） transdermal patches, and to investigate the effect of volatile oil of Flos Magnoliae（FM） on permeation degree of LP from transdermal patches. METHODS The best preparation technology of LP patches was explored with L9 （3^4） orthogonal design by using Eudragit E100, Suceinic Acid, Diethyl phthalate as three elements. The cumulative permeation quantity and the initial adhesive force were taken as the targets to choose the optimum proportion of matrix of LP patches. A test of penetration through rats skin was conducted by using an improved Franz diffusion cell to compare the effects of 3% , 5% , 7% volatile oil of FM on enhancing permeation degree of LP from the transdermal patches. RESULTS The optimum proportion of LP transdermal patches was A2 B1 C3 （Eudragit E100 ：Succinic Acid ：Diethyl phthalate = 1.60： 0. 05： 0. 6）. The cumulative permeation quantity increased after adding the volatile oil of FM to the patches. The average cumulative permeation quantity of LP with 3%, 5%, 7% volatile oil of RZ in 12h were 3 720. 11, 5470. 13, 4 115.41 （ μg . cm-2 , h-1） respectively, and the enhancing times of each was 1. 123, 1. 601, 1. 209 resPectively. CONCLUSION The optimum proportion of matrix selected could be used to make LP transdermal patches that had good quality, and the adhesive force matched requirement. 5% volatile oil of Flos FM had obviously effect on enhancing permeation degree of LP from the patches.