Transdermal delivery of isoniazid and rifampin in guinea pigs by electro-phonophoresis.
Transdermal delivery of isoniazid and rifampin in guinea pigs by electro-phonophoresis.
复制标题
豚鼠体内异烟肼和利福平的电泳透皮给药
DOI：
10.1080/10717544.2016.1267275
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发表时间：
2017-11
期刊：
影响因子：
6
通讯作者：
Huang H
中科院分区：
文献类型：
--
作者：
Chen S;Han Y;Yu D;Huo F;Wang F;Li Y;Dong L;Liu Z;Huang H
摘要电声导法(EP)已成为临床上常用的给药方法。本研究的目的是用极压法评价异烟肼和利福平对豚鼠皮肤的渗透性，为临床应用该透皮给药系统治疗浅表结核病提供参考依据。将异烟肼和利福平溶液分别经皮给药，给药后0、1/2、1、2、4、6和24 h连续采集局部皮肤和血样，连续给药0.5 h。用高效液相色谱法测定局部皮肤和血液中的药物浓度。经EP透皮给药的豚鼠局部皮肤异烟肼浓度显著高于单纯经皮贴剂给药的豚鼠。然而，对于利福平，单独贴片组与EP组呈现几乎一致的浓度-时间曲线，且两组在持续时间内的浓度都远远高于药物的治疗浓度。EP透皮给药后，异烟肼和利福平在皮肤中的平均峰浓度分别为771.0 ± 163.4 μg/mL和81.2 ± 17.3 μg/mL。在任何时间点均未检测到异烟肼和利福平的血药浓度(低于1 μg/mL的检测下限)。结果表明，EP可显著促进异烟肼在豚鼠皮肤中的渗透，而RIF贴剂在局部皮肤中可达到治疗浓度。我们的工作提出了几种可能的用药方法来有效治疗浅表性结核病。
Abstract Electro-phonophoresis (EP) has been used as a drug delivery approach in clinical fields. The objective of the present study is to evaluate the skin permeability of isoniazid and rifampin in guinea pigs by EP to provide reference basis for clinical applications of such transdermal delivery system in the treatment of patients with superficial tuberculosis. Isoniazid and rifampin solutions were delivered transdermally with or without EP in health guinea pigs for 0.5 h. Local skin and blood samples were collected serially at 0, 1/2, 1, 2, 4, 6 and 24 h after dosing. Drug concentrations in local skin and blood were evaluated by high-performance liquid chromatography. Isoniazid concentrations in local skin of guinea pigs receiving isoniazid through EP transdermal delivery were significantly higher than in animals receiving only isoniazid with transdermal patch. However, for rifampin, patches alone group presented almost uniform concentration versus time curve with that of EP group, and both groups had concentrations much higher than the therapeutic concentration of the drug over sustainable time. After EP transdermal delivery, the mean peak concentrations of isoniazid and rifampin in skin were 771.0 ± 163.4 μg/mL and 81.2 ± 17.3 μg/mL respectively. Neither isoniazid nor rifampin concentration in blood could be detected (below the lower detection limit of 1 μg/mL) at any time point. The present study showed that application of EP significantly enhanced INH penetration through skin in guinea pigs, while RIF patch alone obtained therapeutic concentration in local skin. Our work suggests several possible medication approaches for efficient treatment of superficial tuberculosis.
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DOI：
10.1073/pnas.90.22.10504
发表时间：
1993-11-15
影响因子：
11.1
作者：
PRAUSNITZ, MR;BOSE, VG;WEAVER, JC
通讯作者：
WEAVER, JC
影响因子：
46.9
作者：
Prausnitz, Mark R.;Langer, Robert
通讯作者：
Langer, Robert
影响因子：
4.2
作者：
Paudel KS;Milewski M;Swadley CL;Brogden NK;Ghosh P;Stinchcomb AL
通讯作者：
Stinchcomb AL
影响因子：
3.7
作者：
Kost, J;Pliquett, U;Weaver, J
通讯作者：
Weaver, J
DOI：
10.1016/j.jconrel.2011.01.006
发表时间：
2011-06-30
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Polat BE;Hart D;Langer R;Blankschtein D
通讯作者：
Blankschtein D