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Azone(月桂氮酮,Laurocapram),化学名1-十二烷基氮杂环庚烷-2-酮,是Nelson公司开发的一种新型高效透皮吸收促进剂。 Azone为无色、无臭、无毒(小鼠LD_(50)>8 g/kg)和无刺激性的油状液体,有润滑性,易于涂展。不溶于水,易溶于大多数有机溶媒中。化学性质稳定,室温避光可贮藏6年。在许多杀菌剂、抗生素和甾体等药物的外用制剂中,加入少量Azone,可明显增加这些药物穿透皮肤的能力而提高疗效。它有广阔的应用前景。为目前颇引人注目和重视的一种透皮吸收促进剂。一、Azone的合成方法 Azone为N-烷基己内酰胺衍生物,关于它的合成一般以己内酰胺为起始原料与烃化
Azone (Laurocapram), the chemical name of 1-dodecylazacycloheptan-2-one, is Nelson’s new and highly effective transdermal absorption enhancer. Azone is a colorless, odorless, non-toxic (LD_ (50)> 8 g / kg for mice) and non-irritating oily liquid that is lubricious and easy to spread. Insoluble in water, soluble in most organic solvents. Chemical stability, dark at room temperature can be stored for 6 years. In many topical preparations such as bactericides, antibiotics and steroids, the addition of a small amount of Azone can significantly increase the ability of these drugs to penetrate the skin and improve the curative effect. It has broad application prospects. It is a transdermal absorption enhancer that attracts much attention and attention at present. First, Azone synthesis Azone is N-alkyl caprolactam derivatives, for its synthesis is generally caprolactam as the starting material and alkylation