透皮贴剂应用后治疗作用的可能性

E. G. Kuznetsova, O. M. Kuryleva, L. A. Salomatina, S. V. Kursakov, V. Y. Belov, Z. Z. Gonikova, Y. Basok, V. Sevastianov
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引用次数: 0

摘要

背景。随着关于皮肤结构和功能特性的科学知识的增加,在透皮给药过程中,药物可能积聚在真皮层的深层,随后扩散到血液中,即使在透皮治疗系统(TTS),也称为透皮贴片被移除后。目的:定量测定TTS应用后动物皮肤中残留的原料药成分。材料和方法。研究选择了两种先前开发的含有俄罗斯制造的药物物质的透皮贴剂:氨基二氢酞嗪二酮钠(免疫调节剂)和双(1-乙烯基咪唑- n)双乙酸锌(一氧化碳解毒剂)。本研究以体重2.5 - 3kg的雄性栗鼠为研究对象。每种物质分别在取下贴片后立即、4小时后、取下后第1周、第2周和第3周进行5个系列的实验。采用高效液相色谱法和原子吸收光谱法定量测定皮肤中残留药物。结果。在与氨基二氢酞嗪二酮钠TTS接触24小时的皮瓣中,取下贴片后立即检出药物0.516 mg。在接下来的两周内,皮肤中的药物物质减少,免疫调节剂在前4小时显著减少至0.41 mg。在与双乙酸锌(1-乙烯咪唑- n)接触24小时的皮瓣中,取下贴片后立即出现约1mg的药物。在去除透皮贴片4小时后,皮肤中活性物质的数量几乎保持不变。在第1周和第2周,解毒剂的用量略有下降,分别为~0.7 mg和~0.25 mg。结论。对于氨基二氢酞嗪二酮钠的透皮应用,即使在透皮贴片被移除后,皮肤也可以作为药物仓库并延长药物的效果。而双(1-乙烯基咪唑- n)双乙酸锌则没有发现这种作用,这显然是由于药物在生物组织中的溶解度不同所致。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
On the possibility of therapeutic action after transdermal patch application
Background. As scientific knowledge about the peculiarities of the structure and functional properties of the skin increased, it became clearer that during transdermal administration, drug may accumulate in the deep layers of the dermis and subsequently get diffused into the bloodstream even after the transdermal therapeutic system (TTS), also called transdermal patch, had been removed. Objective: to quantify active drug substances remaining in an animal skin after TTS application. Materials and methods. Two previously developed transdermal patches containing Russian-made drug substances were chosen for the study: aminodihydrophthalazinedione sodium (immunomodulator) and bis(1-vinylimidazole-N) zinc diacetate (antidote for carbon monoxide). The study was performed on male Chinchilla rabbits weighing 2.5–3 kg. Five series of experiments were performed for each substance: immediately after removal of the patch, 4 hours later, at week 1, 2 and 3 after removal. High-performance liquid chromatography and atomic absorption spectroscopy methods were used to quantify residual drug substances left in the skin. Results. In the skin flap that was in contact with the aminodihydrophthalazinedione sodium TTS for 24 hours, 0.516 mg of the drug was detected immediately after removal of the patch. Over the next two weeks, the drug substance in the skin decreased with the immunomodulator significantly reducing to 0.41 mg in the first 4 hours. In the skin flap that had been in contact with zinc bis(1-vinylimidazole-N) diacetate for 24 hours, about 1 mg of the drug was present immediately after patch removal. Four hours after removal of the transdermal patch, the quantity of active substance in the skin remained practically unchanged. At week 1 and 2, the quantity of the antidote decreased slightly to ~0.7 mg and ~0.25 mg, respectively. Conclusion. For transdermal application of aminodihydrophthalazinedione sodium, the skin can act as a drug depot and prolong the effect of this drug even after the transdermal patch had been removed. No such effect was found in the case of bis(1-vinylimidazole-N) zinc diacetate, which is apparently due to the different solubility of the drugs in the biotissue.
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