Smith I J, Hinson J L, Johnson V A, Brown R D, Cook S M, Whitt R T, Wilson J T
Department of Pharmacology, Louisiana State University Medical Center, Shreveport 71130.
J Clin Pharmacol. 1989 Feb;29(2):174-84. doi: 10.1002/j.1552-4604.1989.tb03309.x.
The plasma and milk disposition of flurbiprofen (FB) was assessed in healthy women during the early post-partum period after multiple doses of FB. The results confirmed that a pragmatic study design is an attainable requirement for definitive statements about the excretion of FB in transitional milk. Nine doses of FB (50 mg per dose) were administered during three days. Paired milk and plasma samples were obtained during this period of dosing as well as after the last dose. The plasma data were used to derive an equation, which was then used to simulate cumulative plasma profiles for multiple doses given at unequal time intervals. The observed data corresponded to the simulated cumulative profiles of FB in plasma. The plasma elimination half-life of FB during early lactation was slightly prolonged (mean 4.8 hrs) as compared to reported values for normal adult men. The peak plasma concentrations of FB were comparable to those reported for healthy volunteers. In 10 of 12 women (3-5 days post-partum) the FB concentration in breast milk was less than 0.050 micrograms/ml. In two women the milk concentrations of FB were 0.06, 0.07 and 0.07 micrograms/ml as found in only three samples. We conclude that, on the basis of dose found in milk, FB is safe for women breast feeding their infants in the early post-partum period.
在多次服用氟比洛芬（FB）后的产后早期，对健康女性的血浆和乳汁中氟比洛芬的处置情况进行了评估。结果证实，对于明确阐述过渡乳中FB的排泄情况而言，实用的研究设计是一项可实现的要求。在三天内给予九剂FB（每剂50毫克）。在此给药期间以及最后一剂后采集配对的乳汁和血浆样本。利用血浆数据推导出一个方程式，然后用该方程式模拟在不等时间间隔给予多剂药物后的累积血浆曲线。观察到的数据与血浆中FB的模拟累积曲线相符。与正常成年男性的报告值相比，早期哺乳期FB的血浆消除半衰期略有延长（平均4.8小时）。FB的血浆峰值浓度与健康志愿者的报告值相当。在12名女性中的10名（产后3 - 5天），母乳中FB的浓度低于0.050微克/毫升。在两名女性中，仅在三个样本中发现乳汁中FB的浓度分别为0.06、0.07和0.07微克/毫升。我们得出结论，基于乳汁中发现的剂量，FB对产后早期进行母乳喂养的女性是安全的。
