Nakamura K, Katagai K, Mori K, Higo N, Sato S, Yamamoto K
R&D Planning Department, Hisamitsu Pharmaceutical Co., Inc., Nishigotanda 6-25-8, Shinagawa-ku, 141-0031, Tokyo, Japan.
Int J Pharm. 2001 May 7;218(1-2):93-102. doi: 10.1016/s0378-5173(01)00615-9.
Using the pulse depolarization-iontophoresis (PDP-IP) system, salmon calcitonin (sCT), a drug for the treatment of osteoporosis, was transdermaly administered in rats. While absorption of sCT was not observed after passive transdermal administration, the serum sCT concentration was confirmed at a dose of 0.2-4 microg when the PDP-IP system was employed. The results indicated that PDP-IP could enhance transdermal absorption of peptide drugs. Also noted was the increased amount of absorption of sCT along with an increase in the dose. We investigated the influence of electrical parameters (current, frequency) in PDP-IP on the transdermal absorption of sCT. An optimal current for drug absorption was found within the range of transported current (0.1-1.0 mA) employed for PDP-IP. In comparison with the results obtained at 0.1 mA, the drug absorption increased, along with an increase in transported current, when the current was set at 0.5 mA, while the drug absorption decreased at 1.0 mA in comparison. The decrease in drug absorption was assumed to be attributable to the structural destruction of skin by application of excessive current. There was no change in skin resistance attributable to the frequency; nor was there any influence of the frequency on the amount of drug absorption.
利用脉冲去极化离子导入（PDP - IP）系统，将治疗骨质疏松症的药物鲑降钙素（sCT）经皮给予大鼠。被动经皮给药后未观察到sCT的吸收，但采用PDP - IP系统时，在0.2 - 4微克剂量下可确认血清sCT浓度。结果表明，PDP - IP可增强肽类药物的经皮吸收。还注意到sCT的吸收量随剂量增加而增加。我们研究了PDP - IP中的电参数（电流、频率）对sCT经皮吸收的影响。在用于PDP - IP的传输电流（0.1 - 1.0毫安）范围内发现了药物吸收的最佳电流。与在0.1毫安时获得的结果相比，当电流设定为0.5毫安时，药物吸收随传输电流增加而增加，而相比之下在1.0毫安时药物吸收减少。药物吸收的减少被认为是由于施加过大电流导致皮肤结构破坏。皮肤电阻未因频率而改变；频率对药物吸收量也没有任何影响。
