论文部分内容阅读
美国在航天用药途径方面进行了研究,其航天员已开始用经皮肤吸收的东茛菪碱防治空间运动病。药物经皮吸收和转运有较大的优越性,不仅避免肝脏的首过代谢,减少毒副作用,而且具有长效等特点,致使经皮给药在航天、航空、航海等特殊环境下,更具有重要意义。为了提高药物经皮吸收利用率,常使用助渗剂,增加皮肤对药物的通透性。随着高效皮肤渗透促进剂Azone 的出现,一系列新型助渗剂不断合成。因此助渗剂助渗效果的评价显得非常重要。过去评价助渗剂助渗效果常规方法是测定助渗剂对某种药物经离体皮肤渗透速率的影响。渗透速率的测定,不仅需要特殊的试验装置,同时需要建立检测渗透小室接收液中药物浓度的方法。这种检测方法的建立至少要花费2～3个月的时间,还需要昂贵的仪器相匹配。随着经皮给药的迅速发展和助渗剂的大量出现,皮肤药理的研究中迫切需要建立一种快速、无创、准确的评价助渗剂的方法。为此,根据Fick 定律我们进行了实验分析,找出了在助渗剂作用下皮肤生理功能改变而引起的电学特性变化的规律;用助渗指数对助渗剂的助渗效果进行了定量的描述;并进行了专用仪器EWC—1型测量仪的研制。我们利用EWC—1型测量仪和紫外可见分光光度计,研究了溶剂、助渗剂对小鼠皮肤助渗指数和药物经皮渗透作用的影响。发现了一种助渗剂对皮肤助渗指数的影响和它对药物的助渗作用具有一致关系,因此只要用EWC-1型测量仪测量被评价的助渗剂在体助渗指数的变化就可以快速预告该助渗剂的助渗效果,从而建立了助渗剂快速、无创的评价方法。该方法与常规方法相比具有省时、省力、操作简单、安全等特点。该方法在皮肤药理、毒理等研究中具有重要实用价值。
The United States has conducted research on space medicine routes and its astronauts have begun to use scopolamine absorbed through the skin to prevent and control space motion sickness. Drug percutaneous absorption and transport have greater advantages, not only to avoid the first liver metabolism, reduce side effects, but also has long-lasting characteristics, resulting in transdermal delivery in aerospace, aviation, navigation and other special circumstances, more Significance. In order to improve the percutaneous absorption and utilization of drugs, often use penetration enhancers, increase the skin permeability of the drug. With the advent of Azone, a highly effective skin penetration enhancer, a series of new penetration enhancers continue to be synthesized. Therefore, it is very important to evaluate the permeation aid effect. In the past, the conventional method for evaluating the effect of aids to aid penetration was to determine the effect of a penetration enhancer on the rate of penetration of a drug through the skin. Penetration rate measurement, not only requires a special test device, at the same time need to establish a method of detecting drug concentration in the receiving chamber of the permeate cell. This method of detection will take at least 2 to 3 months to build and will require expensive equipment to match. With the rapid development of transdermal delivery and the large number of penetration enhancers, there is an urgent need to establish a rapid, noninvasive and accurate method to evaluate the penetration enhancers in dermal pharmacology. Therefore, according to Fick’s law, we conducted an experimental analysis to find out the change of the skin’s physiological function under the action of the penetration enhancer, and the change of the electrical characteristics was also studied. The osmotic infiltration index was used to quantify the permeation enhancement effect of the penetration enhancer Description; and conducted a special instrument EWC-1-type measuring instrument development. We use EWC-1 type measuring instrument and UV-visible spectrophotometer to study the effects of solvent and osmotic agent on mouse skin penetration index and drug transdermal penetration. It has been found that the influence of a penetration enhancer on the skin penetration index and its effect on the permeation of the drug have a consistent relationship. Therefore, as long as the variation of the somatotropic osmotic index evaluated by the EWC-1 meter is measured It can quickly predict the infiltration aid effect of the infiltration aid, thus establishing a rapid and non-invasive evaluation method of the infiltration aid. Compared with the conventional method, the method has the advantages of time saving, labor saving, simple operation, safety and the like. The method in the skin pharmacology, toxicology and other research has important practical value.