New Technologies Noven Pharmaceuticals Inc., Florida, USA.
Eur Rev Med Pharmacol Sci. 2011 Jul;15(7):823-30.
The mechanism of action of non-steroidal anti-inflammatory drugs (NSAIDs), to which ketoprofen belongs, is based on their cyclo-oxigenase (COX) inhibiting action, concerning both subtype COX-1 constitutive isoform and COX-2 inducible isoform. Ketoprofen administration may be carried out by oral and parenteral routes as well as by topical application, which includes transdermic patch use. Following a synthetic description of the results obtained by several investigators on ketoprofen use, the Authors present a new formulation of the ketoprofen patch obtained by the so called DermaLight Technology.
According to such a technique, the active principle is dissolved in oil components and dispersed inside an anhydrous polymeric matrix made up of styrene-isoprene-styrene (SIS), which is an elastic and flexible material that provides a gentle adhesion to the skin, maintains an elevated ketoprofen concentration and induces a strong thrust that favours the crossing of the skin by the drug; in addition, the patch is fit to be applied to the various areas of the body, including the joints.
Patch adhesiveness reduces skin irritation due to multiple applications and to long-term use, as the DermaLight Technology minimises keratinocytes exfoliation. In pharmacokinetic studies carried out on pigs ketoprofen has been demonstrated to reach deep tissues, where the drug was detected in much higher concentrations, with respect to plasma levels, 12 hours following its application. Experimental studies carried out on rats have shown that ketoprofen patch significantly reduces the edema induced by chronic inflammation. The ulcerogenic effect of ketoprofen patch is then compared with that shown by oral administration of the drug. UD50 values of ketoprofen patch were 49.9 mg/kg and 48.9 mg/kg for the stomach and the small intestine, respectively, whereas UD50 values of oral ketoprofen were 3.6 mg/kg and 3.7 mg/kg, respectively.
The Authors conclude by stating that ketoprofen patch is both a good alternative and a safe modality of administration, with special reference to patients who are prone to gastrointestinal disorders.
属于非甾体抗炎药（NSAIDs）的酮洛芬的作用机制基于其环氧化酶（COX）抑制作用，涉及到组成型同工酶 COX-1 和诱导型同工酶 COX-2。酮洛芬可以通过口服和肠胃外途径以及局部应用（包括透皮贴剂的使用）进行给药。在对几位研究人员关于酮洛芬使用的结果进行综合描述后，作者提出了一种新的酮洛芬贴剂配方，该配方采用所谓的 DermaLight 技术获得。
根据该技术，将活性成分溶解在油成分中，并分散在由苯乙烯-异戊二烯-苯乙烯（SIS）组成的无水聚合基质中，SIS 是一种弹性和柔性材料，对皮肤提供温和的附着力，保持较高的酮洛芬浓度，并产生强烈的推力，有利于药物穿过皮肤；此外，该贴剂适用于身体的各个部位，包括关节。
由于多次应用和长期使用，贴剂的粘性会降低皮肤刺激，因为 DermaLight 技术可最大限度减少角质形成细胞的剥落。在对猪进行的药代动力学研究中，已经证明酮洛芬可以到达深层组织，在这些组织中，药物的浓度比血浆水平高得多，在应用 12 小时后即可检测到。在对大鼠进行的实验研究中，已经表明酮洛芬贴剂可以显著减轻慢性炎症引起的水肿。然后将酮洛芬贴剂的溃疡形成作用与口服给药的效果进行比较。酮洛芬贴剂的 UD50 值分别为胃和小肠的 49.9 mg/kg 和 48.9 mg/kg，而口服酮洛芬的 UD50 值分别为 3.6 mg/kg 和 3.7 mg/kg。
作者总结称，酮洛芬贴剂既是一种良好的替代治疗方法，也是一种安全的给药方式，特别是对于易患胃肠道疾病的患者。
