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电渗涂敷盐酸特比萘芬 1.0%透过猪和人指甲的递送。

Iontophoretic terbinafine HCL 1.0% delivery across porcine and human nails.

机构信息

Huzot Clinic, Clalit Health Services, Ashkelon, Israel.

出版信息

Mycopathologia. 2010 May;169(5):343-9. doi: 10.1007/s11046-009-9265-x. Epub 2009 Dec 13.

DOI:10.1007/s11046-009-9265-x
PMID:20012894
Abstract

BACKGROUND

Onychomycosis is a common disease. Topical treatment is usually not effective due to limitation of trans-nail delivery of antifungal drugs. Successful treatment of deep-seated nail infections remains elusive as the delivery of efficacious levels of antifungal drug to the site of action is very difficult.

OBJECTIVES

To evaluate the influence of several parameters including; the effect of low electrical current, incubation time and the presence of electrolyte (NaCl or KCl) on the penetration of terbinafine through the nail plate into the nail bed, using various formulations and concentrations of terbinafine HCl.

METHODS

Iontophoresis was applied across porcine and human nail in vitro to assess its efficiency in enhancing delivery of terbinafine HCl.

RESULTS

In this study, we have demonstrated that an optimal electrolyte concentration (1% NaCl or KCl) is required for an effective delivery. There is a significant increase in drug delivery into the nail and into the receiving compartment in the presence of 3% DMSO.

CONCLUSIONS

This study demonstrates the efficacy of iontophoresis in enhancing the trans-nail delivery of terbinafine. Clinical studies are needed to evaluate the feasibility, efficacy and safety of iontophoresis of terbinafine in onychomycosis in human.

摘要

背景

甲真菌病是一种常见疾病。由于抗真菌药物向指甲内传递的局限性,局部治疗通常效果不佳。由于很难将有效的抗真菌药物递送至作用部位,深部指甲感染的成功治疗仍然难以实现。

目的

评估多种参数的影响,包括:低电流的影响、孵育时间以及电解质(NaCl 或 KCl)的存在对特比萘芬通过指甲板渗透到甲床的影响,使用不同浓度和配方的盐酸特比萘芬。

方法

将离子电渗疗法应用于体外猪和人指甲,以评估其增强盐酸特比萘芬递送的效率。

结果

在这项研究中,我们已经证明,有效的传递需要最佳的电解质浓度(1%NaCl 或 KCl)。在存在 3%DMSO 的情况下,药物向指甲和接收隔室的递送显著增加。

结论

这项研究证明了离子电渗疗法在增强特比萘芬向指甲内传递方面的有效性。需要进行临床研究,以评估离子电渗疗法在人类甲真菌病中的可行性、疗效和安全性。

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本文引用的文献

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Iontophoretic delivery of terbinafine in onychomycosis: a preliminary study.离子电渗疗法治疗甲真菌病:初步研究。
Br J Dermatol. 2010 Jan;162(1):46-50. doi: 10.1111/j.1365-2133.2009.09414.x. Epub 2009 Jul 20.
2
Trans-ungual iontophoretic delivery of terbinafine.特比萘芬的经甲离子电渗疗法给药
J Pharm Sci. 2009 May;98(5):1788-96. doi: 10.1002/jps.21555.
3
Onychomycosis: rationalization of topical treatment.甲癣:局部治疗的合理化
人指甲板中离子运输的尺寸和电荷依赖性
J Pharm Sci. 2016 Mar;105(3):1201-8. doi: 10.1016/j.xphs.2015.12.011. Epub 2016 Jan 23.
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Transungual permeation: current insights.经皮给药:最新进展。
Drug Deliv Transl Res. 2016 Aug;6(4):426-39. doi: 10.1007/s13346-015-0259-6.
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Preparation, characterization, and in vitro permeation study of terbinafine HCl in poloxamer 407-based thermogelling formulation for topical application.制备、表征及盐酸特比萘芬在泊洛沙姆 407 基热熔胶制剂中的体外渗透研究,用于局部应用。
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Review of antifungal therapy, part II: treatment rationale, including specific patient populations.抗真菌治疗综述,第二部分:治疗原理,包括特定患者群体。
J Dermatolog Treat. 2008;19(3):168-75. doi: 10.1080/09546630701657187.
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Transdermal iontophoresis: impact on skin integrity as evaluated by various methods.经皮离子导入法:通过多种方法评估其对皮肤完整性的影响。
Crit Rev Ther Drug Carrier Syst. 2008;25(4):381-401. doi: 10.1615/critrevtherdrugcarriersyst.v25.i4.30.
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Review of antifungal therapy and the severity index for assessing onychomycosis: part I.抗真菌治疗及评估甲癣严重程度指数综述:第一部分。
J Dermatolog Treat. 2008;19(2):72-81. doi: 10.1080/09546630701243418.
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Mechanistic study of electroosmotic transport across hydrated nail plates: effects of pH and ionic strength.电渗流穿过水合指甲板的机理研究:pH值和离子强度的影响
J Pharm Sci. 2008 Dec;97(12):5186-97. doi: 10.1002/jps.21368.
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Chemical method to enhance transungual transport and iontophoresis efficiency.增强经皮转运及离子导入效率的化学方法。
Int J Pharm. 2008 Jun 5;357(1-2):61-9. doi: 10.1016/j.ijpharm.2008.01.027. Epub 2008 Jan 20.
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Transungual iontophoretic transport of polar neutral and positively charged model permeants: effects of electrophoresis and electroosmosis.极性中性和带正电荷模型渗透剂的经爪离子电渗转运:电泳和电渗的影响
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Combined effects of iontophoretic and chemical enhancement on drug delivery. II. Transport across human and murine skin.离子电渗和化学增强对药物递送的联合效应。II. 跨人和小鼠皮肤的转运
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