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离子电渗疗法中对流溶剂流的表征

Characterization of convective solvent flow during iontophoresis.

作者信息

Delgado-Charro M B, Guy R H

机构信息

Department of Pharmacy, University of California, San Francisco 94143-0446.

出版信息

Pharm Res. 1994 Jul;11(7):929-35. doi: 10.1023/a:1018910715229.

DOI:10.1023/a:1018910715229
PMID:7937551
Abstract

During iontophoresis under neutral pH conditions, there is a net convective flow of volume (electroosmosis) from anode to cathode leading to the enhanced transport of dissolved polar (but uncharged) solutes in the same direction. The objective of this study was to address the following unresolved questions with respect to electroosmotic transport: [1] Whether the efficiency of electroosmotic transport is solute size-dependent and, if so, how severe is this dependence? [2] Is electroosmosis linearly related to current density in the same way that the iontophoretic flux of charged species appears to be? [3] Are positively charged permeants able to influence their own electrotransport across the skin (by modifying the net charge on the membrane and altering, as a result, the permselectivity) and, if so, why and to what extent? Electroosmosis was assessed from the iontophoreically driven fluxes of mannitol, sucrose and lactose across hairless mouse skin in vitro. It was found that:- (a) The electroosmotic transport rate of mannitol is similar to that of the disaccharides, sucrose and lactose, when examined under identical conditions. The dependence of electroosmotic flux upon molecular size requires study of solutes having a wider range of MW than those considered here. (b) Electroosmotic flow from anode-to-cathode increases with applied current density; similarly, convective flow in the opposite direction diminishes with increasing current density. Apparently, there is correlation between the net movement of solvent and the total flux of ions across the skin. (c) The permselectivity of skin can be 'neutralized' by driving, iontophoretically, a cationic, lipophilic peptide (specifically the leutinizing hormone releasing hormone (LHRH) analog, Nafarelin) into the membrane.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在中性pH条件下的离子电渗疗法过程中,存在从阳极到阴极的净体积对流(电渗),导致溶解的极性(但不带电)溶质沿相同方向的转运增强。本研究的目的是解决以下关于电渗转运的未解决问题:[1]电渗转运效率是否取决于溶质大小,如果是,这种依赖性有多严重?[2]电渗是否与电流密度呈线性关系,就像带电物质的离子电渗通量那样?[3]带正电荷的渗透剂是否能够影响其自身跨皮肤的电转运(通过改变膜上的净电荷并因此改变渗透选择性),如果是,原因是什么以及程度如何?通过体外测定甘露醇、蔗糖和乳糖经离子电渗驱动穿过无毛小鼠皮肤的通量来评估电渗。结果发现:- (a)在相同条件下检测时,甘露醇的电渗转运速率与二糖蔗糖和乳糖相似。电渗通量对分子大小的依赖性需要研究分子量范围比此处考虑的更宽的溶质。(b)从阳极到阴极的电渗流随施加的电流密度增加而增加;同样,相反方向的对流随电流密度增加而减小。显然,溶剂的净移动与跨皮肤的离子总通量之间存在相关性。(c)通过离子电渗将阳离子亲脂性肽(具体为促黄体生成素释放激素(LHRH)类似物那法瑞林)驱动到膜中,可以“中和”皮肤的渗透选择性。(摘要截断于250字)

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本文引用的文献

1
The role of electroosmotic flow in transdermal iontophoresis.电渗流在经皮离子电渗疗法中的作用。
Adv Drug Deliv Rev. 2001 Mar 1;46(1-3):281-305. doi: 10.1016/s0169-409x(00)00138-1.
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Iontophoresis of nafarelin across human skin in vitro.那法瑞林经人皮肤体外离子电渗疗法。
Pharm Res. 1996 May;13(5):798-800. doi: 10.1023/a:1016072205371.
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Flow-through system effects on in vitro analysis of transdermal systems.流通系统对透皮系统体外分析的影响。
交流电流频率和渗透促进剂对人体表皮膜的影响。
Int J Pharm. 2009 May 8;372(1-2):24-32. doi: 10.1016/j.ijpharm.2008.12.036. Epub 2009 Jan 4.
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Simultaneous transdermal extraction of glucose and lactate from human subjects by reverse iontophoresis.通过反向离子电渗法同时从人体受试者中经皮提取葡萄糖和乳酸。
Int J Nanomedicine. 2008;3(2):211-23. doi: 10.2147/ijn.s1728.
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The influence of iontophoresis on acyclovir transport and accumulation in rabbit ear skin.离子导入法对阿昔洛韦在兔耳皮肤中转运和蓄积的影响。
Pharm Res. 2005 Sep;22(9):1519-24. doi: 10.1007/s11095-005-5884-1. Epub 2005 Aug 24.
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Transdermal iontophoretic delivery of vapreotide acetate across porcine skin in vitro.醋酸伐普肽经皮离子电渗法在体外猪皮中的递送
Pharm Res. 2005 Aug;22(8):1305-12. doi: 10.1007/s11095-005-5276-6. Epub 2005 Aug 3.
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Transdermal delivery of timolol and atenolol using electroporation and iontophoresis in combination: a mechanistic approach.联合使用电穿孔和离子电渗法经皮递送噻吗洛尔和阿替洛尔:一种机制研究方法。
Pharm Res. 2003 Dec;20(12):1946-51. doi: 10.1023/b:pham.0000008041.86042.c0.
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Iontophoretic delivery of ropinirole hydrochloride: effect of current density and vehicle formulation.盐酸罗匹尼罗的离子电渗给药:电流密度和载体配方的影响。
Pharm Res. 2001 Dec;18(12):1714-20. doi: 10.1023/a:1013322613436.
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Pharm Res. 2001 Dec;18(12):1701-8. doi: 10.1023/a:1013318412527.
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Pharm Res. 2001 Mar;18(3):311-5. doi: 10.1023/a:1011050829531.
Pharm Res. 1993 Oct;10(10):1521-6. doi: 10.1023/a:1018943929902.
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A new system for in vitro studies of iontophoresis.
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Transport mechanisms in iontophoresis. III. An experimental study of the contributions of electroosmotic flow and permeability change in transport of low and high molecular weight solutes.离子电渗疗法中的转运机制。III. 关于电渗流和渗透率变化对低分子量和高分子量溶质转运贡献的实验研究。
Pharm Res. 1990 Mar;7(3):222-9. doi: 10.1023/a:1015809725688.
8
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