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首页> 外文会议>International Pharmaceutical Symposium >Transdermal Delivery of Praziquantel: Effect of Solvents on Permeation across Rabbit Skin
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Transdermal Delivery of Praziquantel: Effect of Solvents on Permeation across Rabbit Skin

机译：Praziquantel的透皮递送：溶剂对兔皮肤渗透的影响

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In order to explore a new way for transdermal delivery of praziquantel (PZQ), the effect of solvents on permeation across rabbit skin was investigated. The solubility of PZQ in five different solvents, ethylene glycol monophenyl ether (EGPE), 1, 4dioxane, tetrahydrofuran (THF), DMSO (DMS O), oleic acid (OA), were measured by Nicolet Evolution 300 ultraviolet-visible spectrophotometer. The determination of n-octanol/water partition coefficient of PZQ contained in five different solutions and assay of serum concentration following PZQ transdermal administration on rabbits were performed by HPLC with Agilent 1100 system. The results indicated that the transdermal absorption of drug was related with solubility, partition coefficient and the lipophilic character of the solvents. The optimal solvent for PZQ transdermal delivery is EGPE. The solubility of PZQ in it is above 400mg·mL-1, the apparent partition coefficient of PZQ in the solution is 0.895 (log P value). After transdermal administration of the solutions, the Cmax of PZQ in blood is 18.36μg·mL-1, the area under the serum concentration-time curve (AUC) is 1174.22μg·mL-1, 5 times compared with the value documented. Therefore, EGPE will be the excellent solvent for PZQ transdermal delivery.
机译：为了探讨吡喹酮递送的新方法（PZQ），研究了溶剂对兔皮肤渗透的影响。 PZQ在五种不同溶剂中的溶解度，乙二醇二苯基醚（EGPE），1,4diOx烷，四氢呋喃（THF），DMSO（DMS O），油酸（DMS O），Nicolet Evolution 300紫外线可见分光光度计测量。通过HPLC与Agilent 1100系统进行PZQ透皮给药后含有五种不同溶液和血清浓度的测定的N-辛醇/水分配系数。结果表明，药物的透皮吸收与溶剂的溶解度，分配系数和溶剂的亲脂性特征有关。用于PZQ透皮递送的最佳溶剂是EGPE。 PZQ在其上的溶解度高于400mg·mL-1，溶液中PZQ的表观分配系数为0.895（log p值）。在透皮施用溶液后，血液中PZQ的Cmax为18.36μg·mL-1，血清浓度 - 时间曲线（AUC）下的面积为1174.22μg·mL-1，与记录值相比5次。因此，EGPE将是PZQ透皮递送的优异溶剂。

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