Chaplin M D
Syntex Research, Palo Alto, California.
Am J Obstet Gynecol. 1992 Feb;166(2):762-5. doi: 10.1016/0002-9378(92)91710-r.
The bioavailability of a single dose of intranasal nafarelin was evaluated in 15 healthy female volunteers. Each subject received a 400 micrograms intranasal and a 25 micrograms intravenous dose of nafarelin separated by at least 7 days. Blood samples were obtained frequently after each dose for determination of nafarelin plasma levels. After intravenous administration, time to maximum concentration (Tmax) was 2 minutes, and maximum serum concentration (Cmax) was 8.2 +/- 2.09 (SD) ng/ml. For intranasal nafarelin, mean Tmax was 18.4 +/- 7.9 minutes (range, 5 to 40 minutes), and Cmax was 2.04 +/- 1.29 ng/ml (range, 0.49 to 5.7 ng/ml). Systemic bioavailability of nafarelin ranged from 1.15% to 5.62% and averaged 2.82% +/- 1.23%. Nafarelin's bioavailability is adequate to achieve the desired therapeutic effect because of its inherent high biologic potency and its pharmacokinetic properties. Nafarelin is readily absorbed by the nasal mucosa, and therapeutic blood levels are rapidly achieved and maintained for a prolonged period of time.
在15名健康女性志愿者中评估了单剂量鼻内使用那法瑞林的生物利用度。每位受试者接受400微克鼻内剂量和25微克静脉剂量的那法瑞林，给药间隔至少7天。每次给药后频繁采集血样以测定那法瑞林的血浆水平。静脉给药后，达峰时间（Tmax）为2分钟，最大血清浓度（Cmax）为8.2±2.09（标准差）纳克/毫升。对于鼻内使用那法瑞林，平均Tmax为18.4±7.9分钟（范围为5至40分钟），Cmax为2.04±1.29纳克/毫升（范围为0.49至5.7纳克/毫升）。那法瑞林的全身生物利用度范围为1.15%至5.62%，平均为2.82%±1.23%。那法瑞林因其固有的高生物活性及其药代动力学特性，其生物利用度足以实现预期的治疗效果。那法瑞林很容易被鼻黏膜吸收，能迅速达到并维持治疗所需的血药浓度。
