茶碱（ThH）的N-烷基-N-烷氧基羰基氨基甲基（NANAOCAM）前药的局部递送。
Topical delivery of N-alkyl-N-alkyloxycarbonylaminomethyl (NANAOCAM) prodrugs of theophylline (ThH).
作者信息
Majumdar Susruta, Sloan K B
机构信息
Department of Medicinal Chemistry, University of Florida, Gainesville, FL 32610, USA.
出版信息
Int J Pharm. 2007 Mar 6;332(1-2):64-71. doi: 10.1016/j.ijpharm.2006.09.034. Epub 2006 Sep 26.
N(7)-(N-Alkyl-N-alkyloxycarbonyl) aminomethyl (NANAOCAM) prodrugs of theophylline (ThH) have been synthesized and characterized by their solubilities in isopropyl myristate (S(IPM)), solubilities in water (S(AQ)), partition coefficients between IPM and pH 4.0 buffer (K(IPM:4.0)) and by their ability to penetrate hairless mouse skin from IPM (J(MIPM)). The most lipid soluble and water soluble member, N-methyl-N-ethyloxy-carbonylaminomethyltheophylline, gave the highest flux through hairless mouse skin from IPM compared to ThH. The flux of NANAOCAM prodrugs of ThH can be accurately predicted by the Roberts-Sloan (RS) equation.
已合成了茶碱（ThH）的N(7)-(N-烷基-N-烷氧基羰基)氨甲基（NANAOCAM）前药，并通过它们在肉豆蔻酸异丙酯中的溶解度（S(IPM)）、在水中的溶解度（S(AQ)）、在肉豆蔻酸异丙酯和pH 4.0缓冲液之间的分配系数（K(IPM:4.0)）以及它们从肉豆蔻酸异丙酯渗透无毛小鼠皮肤的能力（J(MIPM)）对其进行了表征。最具脂溶性和水溶性的成员，N-甲基-N-乙氧基羰基氨甲基茶碱，与ThH相比，从肉豆蔻酸异丙酯中通过无毛小鼠皮肤的通量最高。ThH的NANAOCAM前药的通量可以通过罗伯茨-斯隆（RS）方程准确预测。
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