Guy Richard H, Kuma Hidekazu, Nakanishi Masaru
University of Bath, Department of Pharmacy & Pharmacology, Claverton Down, Bath, BA2 7AY, U.K.
Hisamitsu Pharmaceutical Co., Inc., R&D Division, Kannondai 1-25-11, Tsukuba, Ibaraki, Japan.
Eur J Dermatol. 2014 May-Jun;24(3):365-71. doi: 10.1684/ejd.2014.2332.
Topical administration of ketoprofen to treat local subcutaneous pain significantly reduces gastrointestinal and cardiovascular adverse effects associated with oral delivery. However, this benefit must be weighed against the risk of photosensitisation/phototoxicity.
To substantiate the safety and efficacy of topical ketoprofen delivery from a patch.
Experiments were performed, and published information analysed, (a) to confirm the superior skin permeability and pharmacological activity of ketoprofen, and (b) to demonstrate the lower incidence of ketoprofen photosensitisation/phototoxicity when delivered from a topical patch.
Ketoprofen's photodegradation products were more photoallergic than the drug itself. The period post-ketoprofen treatment that skin should be protected from UV radiation (while the drug is cleared from the application site) was estimated.
Photosensitisation to ketoprofen can be mitigated by a patch formulation, which protects the drug from direct UV exposure during skin application, and reduces the formation of even more photoallergic photodegradation products.
局部应用酮洛芬治疗局部皮下疼痛可显著降低与口服给药相关的胃肠道和心血管不良反应。然而，这种益处必须与光敏化/光毒性风险相权衡。
证实贴剂局部递送酮洛芬的安全性和有效性。
进行实验并分析已发表的信息，(a) 以确认酮洛芬具有更好的皮肤渗透性和药理活性，(b) 以证明从局部贴剂递送时酮洛芬光敏化/光毒性的发生率较低。
酮洛芬的光降解产物比药物本身更具光过敏性。估计了酮洛芬治疗后皮肤应免受紫外线辐射的时间段（即药物从应用部位清除期间）。
贴剂制剂可减轻对酮洛芬的光敏反应，该制剂可在皮肤应用期间保护药物免受直接紫外线照射，并减少更具光过敏性的光降解产物的形成。
