Wagener H H, Vögtle-Junkert U
Dolorgiet Arzneimittel GmbH & Co. KG, St. Augustin/Bonn.
Arzneimittelforschung. 1996 Mar;46(3):299-301.
For some 10 years it has been usual practice to determine tissue drug concentrations following the application of topical antirheumatic agents. However, testing the measured drug concentrations for their therapeutic relevance continues to be difficult. An appropriate reference parameter is, for example, the IC50 of the inhibition of the prostaglandin synthesis. Moreover, tissue concentrations should be compared with those achieved following oral administration of clinically effective doses. Based upon practical experience with ibuprofen (CAS 15687-27-1) following both topical and oral administrations, it is illustrated how such studies and the tissue concentrations found could be evaluated and interpreted taking into particular consideration the sample size calculation and the therapeutic relevance of the results.
在过去约10年中，测定局部应用抗风湿药物后组织中的药物浓度已成为常规做法。然而，测试所测药物浓度的治疗相关性仍然困难。例如，一个合适的参考参数是前列腺素合成抑制的IC50。此外，应将组织浓度与口服临床有效剂量后所达到的浓度进行比较。基于布洛芬（CAS 15687-27-1）局部和口服给药后的实际经验，说明了如何评估和解释此类研究以及所发现的组织浓度，特别要考虑样本量计算和结果的治疗相关性。
