Berner G, Wagener H H
Forschungslaboratorien der Firma Dolorgiet GmbH, St. Augustin/Bonn.
Arzneimittelforschung. 1987 Jul;37(7):814-6.
The percutaneous penetration of an ibuprofen cream at 5% (Dolgit Creme) was tested in guinea pigs. Already 20 min after application of the cream on the shaved skin high ibuprofen concentrations of about 10 micrograms/g were found in the subcutaneous and in the muscular tissue. The plasma concentrations reached only one tenth of the values ascertained in the tissues. 2 h after application the concentrations in the tissue increased by 50%, whereas the increase of the plasma concentrations was more significant. The results confirm in agreement with kinetic studies in man that ibuprofen penetrates from the tested formulation directly and very quickly in deeper tissues. The deviation of the active ingredient over the systemic circulation is improbable.
对5%布洛芬乳膏(Dolgit Creme)在豚鼠身上的经皮渗透情况进行了测试。在将乳膏涂抹于剃毛后的皮肤上仅20分钟后,就发现皮下和肌肉组织中布洛芬浓度很高,约为10微克/克。血浆浓度仅达到在组织中测定值的十分之一。涂抹后2小时,组织中的浓度增加了50%,而血浆浓度的增加更为显著。结果与人体动力学研究一致,证实布洛芬可从受试制剂直接且非常迅速地渗透到更深层组织中。活性成分在体循环中出现偏差的可能性不大。