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    • 1. 发明申请
    • HIGH PENETRATION PRODRUG COMPOSITIONS OF RETINOIDS AND RETINOID-RELATED COMPOUNDS
    • 雷诺霉素和与雷公藤相关的化合物的高渗透性原料组合物
    • US20160184253A1
    • 2016-06-30
    • US14877788
    • 2015-10-07
    • SUZHOU TECHFIELDS MEDICAL LTD.
    • Chongxi YU
    • A61K31/21A61K31/216A61K31/4453G01N33/50
    • A61K31/215A61K31/21A61K31/216A61K31/221A61K31/4453A61K47/54C07C219/10C07C2601/16C07C2602/10G01N33/502
    • The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    • 本发明提供了能够穿过具有高穿透效率的生物屏障的类视黄醇和类视黄醇相关化合物的新型高渗透组合物(HPC)或高渗透前药(HPP)的组合物。 HPP在穿过生物屏障后能够转化为亲本活性药物或药物代谢物,因此可以对母体药物或代谢物可以进行的处理。 此外,HPP能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域,从而进行新的治疗。 HPP可以通过各种施用途径施用于受试者,例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。