奥沙普秦-氢化磷脂复合物的研究及体外透皮试验

Studies on preparation of oxaprozin-hydrogenated phospholipid complex and its skin permeation test in vitro

目的 制备奥沙普秦 氢化磷脂复合物。考察复合物的摩尔比及奥沙普秦、奥沙普秦氢化磷脂物理混合物与奥沙普秦 氢化磷脂复合物三者的体外透皮渗透情况。方法 采用差热分析及扫描电镜研究复合物的理化性质 ;通过连续递变实验测定复合物的组成摩尔比 ;用改进Franz扩散池进行离体鼠皮渗透实验。结果 奥沙普秦 氢化磷脂复合物在正辛醇中的脂溶性明显增加 ,差热分析图谱显示形成了新的物相 ;透皮实验表明其渗透速率、增渗倍数及 1 2h累积渗透量均大于奥沙普秦及其物理混合物。结论 奥沙普秦与氢化磷脂的最佳摩尔比为 1∶1 ;

OBJECTIVE: To prepare the complex between oxaprozin and hydrogenated phospholipid. To study the compositon ratio of the complex and the skin permeation in vitro of oxaprozin, physical mixture and complex of oxaprozin and hydrogenated phospholipid respectively. METHODS: The physico-chemical properties of the complex were confirmed by differential scanning calorimetry (DSC) and scanning electron microscope (SEM) respectively. The composition ratio was determined by continuous variation method. The rat skin permeation test in vitro was performed by modified Franz diffusion pool. RESULTS: The lipophilic property of the complex was raised in n-octyl. The profiles of DSC showed that it appeared a new physical phase after the interaction of oxaprozin and hydrogenated phospholipid in specific conditions. It produced higher diffusion ratio, enhancement multiple and cumulative permeation in 12 h than the plain oxaprozin and uncomplexed mixture. CONCLUSIONS The optimal composition ratio of oxaprozin and hydrogenated phospholipid was 1:1 (mol:mol). The ability of permeation was strengthened after oxaprozin was formed into phospholipid complex.