transdermal drug delivery systems - 山东大学课 .pptVIP

10. Transdermal Drug Delivery Systems 经皮给药系统 Contents Factors affecting percutaneous absorption Percutaneous absorption enhancer Design features of transdermal drug delivery system Percutaneous absorption model Advantages and disadvantages of TDDSs Examples of transdermal drug deliver systems General clinical considerations in the use of TDDSs Transdermal drug delivery systems (TDDSs) facilitate the passage of therapeutic quantities of drug substances through the skin and into the general circulation for their systemic effect. 经皮给药系统能促进具治疗量的药物透过皮肤，进入体循环发挥系统作用。 For transdermal drug delivery, it is considered ideal if the drug penetrates through the skin to the underlying blood supply without drug buildup in the dermal layers. 理想的经皮给药系统时，药物渗透入皮肤后，能够进入血液而不在皮下蓄积。 Macroflux? E-TRANS? Benefits of TDDSs Eliminates potential pain associated with injections No first pass metabolism in liver Eliminates gastrointestinal side effect Improves patient compliance due to simpler, pain free delivery Potential for home administration I. Factors affecting percutaneous absorption 1. Drug concentration is an important factor. （药物浓度是一个重要因素。） 2. The larger the area of application, the more drug is absorbed. （当药物应用面积增大，经皮吸收的药物量增加。） 3. The aqueous solubility of a drug determines the concentration presented to the absorption site, and the partition coefficient influences the rate of transport across the absorption site. 药物的水溶性决定了吸收部位的浓度，分配系数影响吸收部位的药物转运速率。 Drugs generally penetrate the skin better in their un-ionized form. Nonpolar drugs tend to across the cell barrier through the lipid-rich regions, whereas the polar drugs favor transport between cells. 非解离型的药物透皮效果好。非极性药物易通过富含脂质的部位跨越细胞屏障，而极性药物则通过细胞转运。 4. Drugs with molecular weights of 100 to 800 and adequate lipid and aqueous solubility can permeate skin. The ideal molecular weight of a drug for transdermal drug delivery is believed to be 400 or less. 分子量在100和800之间并且具有一定的脂溶性和水溶性的药物能渗透入皮肤。理想的经皮吸收系统的药物分子量应为400或更小。 5. Hy