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Effect of current profile on the stability and transdermal iontophoretic delivery of lhrh and nafarelin in vitro

机译:目前概况对LHRH和NAFARLIN体外稳定性和透皮离子电渗递送的影响

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Transdermal iontophoresis is a potential method to administer therapeutically actigve peptides into the systemic circulation because most peptides are ineffective when taken orally~1. Especially the stability and biological activity of peptides are a concern. In this study, stability and iontophoretic transdermal permeation of two decapeptides, luteinizing hormone releasing hormone (LHRH) and Nafarelin, were evalauted. Nafarelin is an agonist analogue of LHRH: the sixth amino acid of LHRH, glycine, is replaced by D-naphthylalanine that makes the molecule more lipophilic and biologically more active.~2 The aim of this study was to evalaute the stability of LHRH and Nafarelin in buffer solution, with electrical current, and in the presence of skin metabolizing enzymes. The effect of different current profiles - direct current (DC), pulsed DC with different on/off ratios, and alternating current (AC) with differnet +/- duty cycles - on the trandermal iontophoresis of these peptides was measued. The influence of the peptides and current profile on the permeation of neutrla sugar, mannitol, during the iontophoresis was also determined.
机译:透皮离子电渗疗法是向系统循环中施用治疗性致肽的潜在方法,因为大多数肽在口服〜1时无效。特别是肽的稳定性和生物活性是一个问题。在该研究中,评估两种疏水肽,腐蚀激素释放激素(LHRH)和Nafarelin的稳定性和离子渗透压透皮渗透。 Nafarelin是LHRH的激动剂模拟:LHRH,甘氨酸的第六氨基酸由D-萘葡萄酒取代,使分子更加亲脂性和生物学上更活跃。〜2本研究的目的是评估LHRH和NAFARLIN的稳定性在缓冲溶液中,具有电流,并且在存在皮肤代谢酶。不同电流型材 - 直流(DC),具有不同开/关比的脉冲DC,以及具有不同+/-占空比的交流(AC)的效果测量了这些肽的组成+/-占空比的交流(AC)。还测定了肽和电流谱对离子电渗透渗透血症期间Neutrla糖渗透的影响。

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