Heasman P A, Ward A, Barrett A W, Seymour R A, Edwards G
Dental School, University of Newcastle upon Tyne, U.K.
J Periodontal Res. 1990 Mar;25(2):88-92. doi: 10.1111/j.1600-0765.1990.tb00897.x.
The aim of this study was to determine whether the non-steroidal anti-inflammatory drug, flurbiprofen, which has been shown to be an inhibitor of alveolar bone loss in human periodontal disease, is present in human crevicular fluid (CF) following oral dosing. A method is described whereby routine high-performance liquid chromatography is used to detect the drug in only 20 microliters of CF. 5 volunteers abstained from toothbrushing for 21 days to induce experimental gingivitis and increase the resting flow of CF. 100 mg of flurbiprofen was taken by each volunteer on d 21-28. On d 21 and 28, serum and CF samples were taken prior to dosing and afterwards at 1, 2, 4 and 6 hours. On d 21 the mean peak concentration of the drug in serum was about 11 micrograms/ml and was found between 1-2 h after dosing. The respective values for CF (d 21) were 0.32 micrograms/ml and 4 h. On d 28 flurbiprofen was detected in both fluids prior to dosing. The mean peak concentrations after dosing had increased to 13.13 micrograms/ml (serum) and 0.46 micrograms/ml (CF) although the levels of the drug in CF remained relatively constant throughout the observation period on d 28. The results indicate that flurbiprofen may be detected in human CF after oral administration and that the levels are in excess of the plasma level, which in beagles has been shown to inhibit alveolar bone loss in periodontal disease.
本研究的目的是确定口服给药后,已被证明可抑制人类牙周病中牙槽骨丧失的非甾体抗炎药氟比洛芬是否存在于人类龈沟液(CF)中。本文描述了一种方法,即使用常规高效液相色谱法仅在20微升的龈沟液中检测该药物。5名志愿者连续21天不刷牙以诱发实验性牙龈炎并增加龈沟液的静息流量。在第21 - 28天,每位志愿者服用100毫克氟比洛芬。在第21天和第28天,在给药前以及给药后1、2、4和6小时采集血清和龈沟液样本。在第21天,血清中药物的平均峰值浓度约为11微克/毫升,在给药后1 - 2小时出现。龈沟液(第21天)的相应值为0.32微克/毫升和4小时。在第28天,给药前在两种液体中均检测到氟比洛芬。给药后的平均峰值浓度分别增至13.13微克/毫升(血清)和0.46微克/毫升(龈沟液),尽管在第28天的整个观察期内龈沟液中药物水平保持相对恒定。结果表明,口服给药后可在人类龈沟液中检测到氟比洛芬,且其水平超过血浆水平,在比格犬中已表明该血浆水平可抑制牙周病中的牙槽骨丧失。