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补骨脂素的生物药剂学、药代动力学及药理学

Biopharmaceutics, pharmacokinetics and pharmacology of psoralens.

作者信息

Stolk L M, Siddiqui A H

机构信息

Department of Pharmacy, Academic Medical Centre, Amsterdam, The Netherlands.

出版信息

Gen Pharmacol. 1988;19(5):649-53. doi: 10.1016/0306-3623(88)90122-x.

Abstract

The psoralen derivative 8-methoxypsoralen (8-MOP) and to a lesser extent some other psoralens, including 5-methoxypsoralen (5-MOP) and 4,5',8-trimethylpsoralen (TMP) have acquired a place in the treatment of psoriasis and other dermatoses. They are only active when combined with long-wave ultraviolet light: PUVA therapy (Psoralen plus UVA). Successful PUVA therapy depends on sufficiently high psoralen concentrations coinciding with the time of irradiation. The use of oral or rectal pharmaceutical formulations with 8-MOP dissolved in liquid is preferable to conventional tablets or capsules. Since no formulation of 5-MOP with fast and predictable absorption is available 8-MOP should be preferred in PUVA therapy. The effectiveness of oral TMP is doubtful, because of low serum concentrations, probably due to malabsorption.

摘要

补骨脂素衍生物8-甲氧基补骨脂素(8-MOP)以及在较小程度上的其他一些补骨脂素,包括5-甲氧基补骨脂素(5-MOP)和4,5',8-三甲基补骨脂素(TMP),在银屑病和其他皮肤病的治疗中占据了一席之地。它们只有在与长波紫外线结合时才具有活性:即光化学疗法(补骨脂素加紫外线A)。成功的光化学疗法取决于在照射时补骨脂素浓度足够高。使用将8-MOP溶解在液体中的口服或直肠药物制剂优于传统片剂或胶囊。由于没有可快速且可预测吸收的5-MOP制剂,在光化学疗法中应首选8-MOP。口服TMP的有效性存疑,因为血清浓度较低,这可能是由于吸收不良所致。

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