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局部应用抗肿瘤药治疗皮肤癌或牛皮癣可防止或至少降低药物的全身毒性,但大多药物由于理化性质难以透皮吸收而无效。丝裂霉素(Ⅰ)药物透皮性能差,将其制成N-取代的亲酯性低融点前体衍生物试图能透皮后经酶或化学转化成母体药而发挥作用。七种前体药为:苄基(Ⅱ),苯甲酰(Ⅲ),苄羰基(Ⅳ),羧苄基(Ⅴ),羧丙基(Ⅵ),羧戊基(Ⅶ),羧壬基(Ⅷ),测定了这些化合物的溶解度和在辛醇-水的分配系数。为比较丝裂霉素及其前体药透皮性能,将浓度为
Topical application of antineoplastic agents for the treatment of skin cancer or psoriasis prevents or at least reduces the systemic toxicity of the drug, but most drugs are ineffective because of their poor physical and chemical properties. Mitomycin (I) drugs have poor transdermal properties and are made into N-substituted pro-lipophilic low melting point precursor derivatives that attempt to transdermally act via enzymatic or chemical conversion to parent drug. The seven prodrugs are benzyl (Ⅱ), benzoyl (Ⅲ), benzyloxycarbonyl (Ⅳ), carbobenzyl (Ⅴ), carboxypropyl (Ⅷ), the solubility of these compounds and their partition coefficient in octanol-water were determined. To compare mitomycin and its prodrugs transdermal properties, the concentration of