Eckenberger P, Bisler H, Panse P
Abteilung Klinische Entwicklung, Luitpold Pharma, München.
Arzneimittelforschung. 1993 Apr;43(4):469-74.
The feasibility of the bilateral vein stripping model for the investigation of the transcutaneous absorption of a non-steroidal antirheumatic drug (NSAID) was examined. After application of a 1% solution of indomethacin (Elmetacin, CAS 53-86-1) at one leg (steady state) plasma and vein tissue of both sides was taken at the same time. The mean indomethacin plasma levels of 19 female patients were 7 ng/ml, in the vein tissue of the application side 280 ng/g and at the opposite side 80 ng/g. The tissue levels in the veins are in the same range as in the target tissues of transcutaneous antirheumatic therapy. Therefore the model is considered useful for the investigations of the pharmacokinetics of topically applied NSAID.
研究了双侧静脉剥脱模型用于非甾体类抗炎药(NSAID)经皮吸收研究的可行性。在一条腿上涂抹1%的吲哚美辛溶液(消炎痛,CAS 53-86-1)(达到稳态后),同时采集两侧的血浆和静脉组织。19名女性患者的吲哚美辛平均血浆水平为7 ng/ml,涂抹侧静脉组织中为280 ng/g,对侧为80 ng/g。静脉中的组织水平与经皮抗风湿治疗的靶组织中的水平处于同一范围。因此,该模型被认为可用于局部应用NSAID的药代动力学研究。