维生素a酸类和类维生素a酸化合物的前药

文档序号:1826440 发布日期:2021-11-12 浏览:12次 >En<

阅读说明:本技术 维生素a酸类和类维生素a酸化合物的前药 (Prodrugs of retinoids and retinoid-like compounds ) 是由 于崇曦 于 2007-01-15 设计创作,主要内容包括:本发明涉及维生素A酸类和类维生素A酸化合物的前药。具体而言,本发明涉及具有通式(31)“结构式31”的结构的带有正电荷的维生素A酸类及类维生素A酸化合物的前药的设计与合成。所述化合物可由维生素A酸及其相关化合物与合适的醇、硫醇、或胺通过偶合剂反应得到。实验结果表明超过90%的前药能在几分钟内变回母药。在治疗中,这些前药能透皮给药用于任何治疗,避免维生素A酸类及类维生素A酸化合物的大多数副作用。前药的控释透皮给药系统可以使血液中维生素A酸类及类维生素A酸化合物的浓度稳定在最佳的治疗浓度,提升疗效并减少维生素A酸类及类维生素A酸化合物的副作用。这些前药透皮给药的另一大好处是使用更加方便,特别是对于儿童给药。(The present invention relates to prodrugs of retinoids and retinoid-like compounds. In particular, the present invention relates to the design and synthesis of positively charged pro-drugs of retinoids and retinoid-like compounds having the general formula (31) &#39;Structure 31&#39;. The compounds can be obtained by reacting retinoic acid and related compounds with suitable alcohols, thiols, or amines via coupling reagents. Experimental results indicate that more than 90% of the prodrug can change back to the parent drug within minutes. In therapy, these prodrugs can be administered transdermally for any kind of treatment, avoiding most of the side effects of retinoids and retinoid-like compounds. The controlled-release transdermal drug delivery system of the prodrug can stabilize the concentration of the vitamin A acids and the retinoid acid compounds in blood at the optimal treatment concentration, improve the curative effect and reduce the side effects of the vitamin A acids and the retinoid acid compounds. Another great benefit of transdermal administration of these prodrugs is that it is more convenient to use, especially for children.)

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