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阴极离子电渗疗法后酮洛芬在猪体内的组织渗透情况。

Ketoprofen tissue permeation in swine following cathodic iontophoresis.

作者信息

Panus P C, Ferslew K E, Tober-Meyer B, Kao R L

机构信息

Department of Physical Therapy, College of Public and Allied Health, East Tennessee State University, Johnson City 37614-0624, USA.

出版信息

Phys Ther. 1999 Jan;79(1):40-9.

PMID:9920190
Abstract

BACKGROUND AND PURPOSE

Pharmacokinetic assessment of drug tissue permeation following iontophoresis is limited. The depth of ketoprofen tissue permeation following cathodic iontophoresis (4 mA, 40 minutes) and the stereoselectivity of drug delivery were examined in this study.

SUBJECTS

Ketoprofen (750 mg) was iontophoresed onto one porcine medial thigh, with passive drug permeation conducted on the other thigh.

METHODS

Skin, subcutaneous fascia, and muscle biopsies from the drug delivery sites were harvested and stored separately, and the "R" and "S" ketoprofen enantiomers were determined. Results. Iontophoretic and passive applications yielded equivalent total ketoprofen concentrations in the skin and fascia. In contrast, multivariate analysis demonstrated that the ketoprofen concentration in the first centimeter of muscle following iontophoresis was greater than the drug concentration in the deeper underlying muscle layers and greater than that delivered to any muscle layer following passive delivery. No transcutaneous stereoselective delivery) of ketoprofen was detected.

CONCLUSION AND DISCUSSION

Compared with passive delivery, iontophoresis enhances nonstereoselective ketoprofen permeation into the fascia-muscle interface. With delivery to deeper tissue sites, however, there is no apparent enhancement over passive application.

摘要

背景与目的

离子电渗疗法后药物组织渗透的药代动力学评估有限。本研究检测了阴极离子电渗疗法(4毫安,40分钟)后酮洛芬组织渗透的深度以及药物递送的立体选择性。

对象

将酮洛芬(750毫克)离子电渗到一头猪的内侧大腿上,另一大腿进行被动药物渗透。

方法

从药物递送部位采集皮肤、皮下筋膜和肌肉活检样本并分别储存,测定“R”和“S”酮洛芬对映体。结果。离子电渗和被动应用在皮肤和筋膜中产生的总酮洛芬浓度相当。相比之下,多变量分析表明,离子电渗后肌肉第一厘米处的酮洛芬浓度高于更深层下方肌肉层中的药物浓度,且高于被动递送后递送至任何肌肉层的浓度。未检测到酮洛芬的经皮立体选择性递送。

结论与讨论

与被动递送相比,离子电渗增强了酮洛芬非立体选择性渗透到筋膜 - 肌肉界面。然而,在递送至更深组织部位时,与被动应用相比没有明显增强。

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