Levy Sharon, Furst Katharine, Chern Wendy
Dermik Laboratories, Berwyn, Pennsylvania, USA.
Cutis. 2002 Aug;70(2 Suppl):14-21.
Recent in vitro and in vivo studies compared the absorption of a 0.5% fluorouracil cream with that of a 5% fluorouracil cream, following topical application to the skin. Both studies demonstrated that fluorouracil is minimally absorbed into the systemic circulation. Despite a one-tenth concentration difference between formulations, the cumulative amount of fluorouracil excreted in the urine of patients treated with the 0.5% cream was one fortieth that of patients treated with the 5% cream. Interestingly, higher percentages of fluorouracil were retained in the skin following application of the 0.5% cream compared with the 5% cream, suggesting that delivery of the 0.5% cream may be more targeted to the affected area. Other studies have demonstrated that the 0.5% cream is as effective as the 5% cream for the treatment of actinic keratoses (AKs) and has a more favorable tolerability profile. Therefore, this new 0.5% fluorouracil cream may be a safer, yet equally effective treatment alternative.
最近的体外和体内研究比较了0.5%氟尿嘧啶乳膏和5%氟尿嘧啶乳膏经皮肤局部应用后的吸收情况。两项研究均表明,氟尿嘧啶极少被吸收进入体循环。尽管两种制剂的浓度相差十分之一,但使用0.5%乳膏治疗的患者尿液中排出的氟尿嘧啶累积量仅为使用5%乳膏治疗患者的四十分之一。有趣的是,与5%乳膏相比,使用0.5%乳膏后皮肤中保留的氟尿嘧啶百分比更高,这表明0.5%乳膏的给药可能更具靶向性。其他研究表明,0.5%乳膏在治疗光化性角化病(AKs)方面与5%乳膏同样有效,且耐受性更好。因此,这种新型0.5%氟尿嘧啶乳膏可能是一种更安全但同样有效的治疗选择。