Santi P, Colombo P, Bettini R, Catellani P L, Minutello A, Volpato N M
Pharmaceutical Department, University of Parma, Italy.
Pharm Res. 1997 Jan;14(1):63-6. doi: 10.1023/a:1012055401038.
The aim of the work was to study iontophoretic transdermal administration of salmon calcitonin (sCt) in rabbits, with particular attention to drug reservoir composition. A dry sCt disc, to be dissolved on the application site, was used for preparing the reservoir for transdermal iontophoresis. As a reference drug reservoir, a pad wetted with drug solution was used.
Experiments were done in rabbits depositing 100 IU of salmon calcitonin on skin and applying anodal iontophoresis. Serum calcium concentration was measured during iontophoresis, passive diffusion and after i.v. administration. Parameters such as pH value and reservoir type were examined.
Transdermal iontophoresis of sCt elicited a decrease in the serum calcium level, whereas, in the absence of electric current, no significant fall was measured. Using the reservoir prepared from drug solution, anodal iontophoresis at pH 4.2 was more effective than at pH 7.4, probably due to higher sCt net positive charge. Using the reservoir prepared from dry disc, similar kinetics and extent of drug effect were observed at both pH values. The reservoir prepared from solid drug deposit concentrated sCt next to the skin.
Anodal iontophoresis for transdermal calcitonin administration shows therapeutical applicability. The type of reservoir is an important parameter affecting sCt transdermal iontophoresis.
本研究旨在探讨鲑鱼降钙素(sCt)在兔体内的离子导入透皮给药情况,尤其关注药物储库的组成。使用一种在给药部位溶解的干燥sCt圆盘来制备透皮离子导入的储库。作为对照药物储库,使用浸湿药物溶液的药垫。
对兔进行实验,将100 IU鲑鱼降钙素涂抹于皮肤,并施加阳极离子导入。在离子导入、被动扩散过程中以及静脉注射后测量血清钙浓度。检测诸如pH值和储库类型等参数。
sCt的透皮离子导入引起血清钙水平下降,而在无电流情况下,未测得显著下降。使用由药物溶液制备的储库时,pH 4.2时的阳极离子导入比pH 7.4时更有效,这可能是由于sCt的净正电荷更高。使用由干燥圆盘制备的储库时,在两个pH值下观察到相似的药物作用动力学和程度。由固体药物沉积物制备的储库使sCt在皮肤附近浓缩。
用于透皮给予降钙素的阳极离子导入显示出治疗适用性。储库类型是影响sCt透皮离子导入的一个重要参数。