Vincent C M, Laugel C, Marty J P
Dermo-Cosmetic Research Center, Antony, France.
Arzneimittelforschung. 1999 Jun;49(6):509-13. doi: 10.1055/s-0031-1300452.
The objective of the present study was to evaluate in vitro the percutaneous absorption, across human skin, of 5 non-steroidal anti-inflammatory drugs (NSAIDs) formulated as gels: ketoprofen (CAS 22071-15-4), epolamine diclofenac (CAS 15307-86-5), piroxicam (CAS 36322-90-4) and niflumic acid (CAS 4394-00-7) or as emulgel: diclofenac sodium (CAS 15307-79-6) and to compare the different formulations as drug delivery systems. Because the concentrations of the NSAIDs in the different excipients were not identical, the comparison of their diffusional properties was expressed in term of release efficiency (or diffusion efficacy). The results obtained show that, across human skin under standardized experimental conditions, ketoprofen and piroxicam have the best rank order followed by niflumic acid, diclofenac sodium and epolamine diclofenac.
本研究的目的是在体外评估5种制成凝胶剂的非甾体抗炎药(NSAIDs):酮洛芬(CAS 22071-15-4)、依托拉明双氯芬酸(CAS 15307-86-5)、吡罗昔康(CAS 36322-90-4)和尼氟酸(CAS 4394-00-7),以及制成乳胶剂的双氯芬酸钠(CAS 15307-79-6)经人体皮肤的经皮吸收情况,并比较不同制剂作为药物递送系统的差异。由于不同辅料中NSAIDs的浓度不同,其扩散特性的比较以释放效率(或扩散效能)表示。所得结果表明,在标准化实验条件下,经人体皮肤,酮洛芬和吡罗昔康的排名最佳,其次是尼氟酸、双氯芬酸钠和依托拉明双氯芬酸。