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经皮离子导入技术下 2.5%及 5%盐酸利多卡因的渗透效果。

Effective permeation of 2.5 and 5% lidocaine hydrochloride in human skin using iontophoresis technique.

机构信息

Centre for Biomedical Engineering, Indian Institute of Technology Delhi, New-Delhi, India.

Department of Burns and Plastic Surgery, Vardhman Mahavir Medical College & Safdarjung Hospital, New-Delhi, India.

出版信息

Int J Dermatol. 2018 Nov;57(11):1335-1343. doi: 10.1111/ijd.14107. Epub 2018 Jul 6.

DOI:10.1111/ijd.14107
PMID:29978889
Abstract

BACKGROUND

Lidocaine Hydrochloride (HCL) is one of the commonest topical local anesthetic drugs. The permeation of the lidocaine can be enhanced by iontophoresis (IOP). The purpose of this study was to evaluate the permeability of 2.5 and 5% lidocaine permeation in ex vivo human skin using different IOP waveform.

METHODS

Continuous and modulated IOP at the current density of 0.5 mA/cm were applied across human skin (n = 3) in donor chamber of vertical diffusion cell at 2.5 and 5% lidocaine concentration. High Performance Liquid Chromatography was used to determine lidocaine concentration.

RESULTS

Findings revealed that lidocaine concentration increased effectively in a time-dependent manner in both modulated and continuous IOP at 2.5 and 5% lidocaine concentration. Compared to the passive group, the flux of lidocaine with modulated and continuous IOP were higher of about six and ten-fold, respectively. However, no significant difference was observed between continuous and modulated IOP groups at both lidocaine concentrations. At 2.5% lidocaine concentration, the permeation time taken by modulated and continuous IOP to attain therapeutic levels of 142 and 164 μg/cm , respectively, was approximately 10 minutes. At 5% lidocaine, the therapeutic permeation of 129 and 147 μg/cm , respectively, was achieved at approximately 5 minutes after applying iontophoresis waveform.

CONCLUSION

Study shows that modulated IOP can be a promising alternative method in clinical settings aside from continuous IOP. Based on the clinical requirements, IOP can be used at 2.5 and 5% lidocaine concentration depending on need of relatively short or very short onset action.

摘要

背景

盐酸利多卡因(HCL)是最常见的局部麻醉药之一。离子电渗(IOP)可以增强利多卡因的渗透。本研究旨在评估不同 IOP 波形下 2.5%和 5%利多卡因在离体人皮肤上的渗透情况。

方法

在垂直扩散池供体室中,以 0.5 mA/cm 的电流密度对 2.5%和 5%利多卡因浓度的人皮肤施加连续和调制 IOP。采用高效液相色谱法测定利多卡因浓度。

结果

结果表明,在 2.5%和 5%利多卡因浓度下,调制和连续 IOP 均能有效地使利多卡因浓度随时间呈依赖性增加。与被动组相比,调制和连续 IOP 的利多卡因通量分别提高了约 6 倍和 10 倍。然而,在两种利多卡因浓度下,连续和调制 IOP 组之间没有观察到显著差异。在 2.5%利多卡因浓度下,调制和连续 IOP 分别达到治疗水平 142 和 164 μg/cm 所需的渗透时间约为 10 分钟。在 5%利多卡因浓度下,调制和连续 IOP 分别在应用离子电渗波形后约 5 分钟达到治疗渗透的 129 和 147 μg/cm 。

结论

研究表明,调制 IOP 除了连续 IOP 之外,在临床环境中可能是一种有前途的替代方法。根据临床需要,可根据需要较短或极短的起效时间,在 2.5%和 5%利多卡因浓度下使用 IOP。

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