Fuglsang G, Hertz B, Holm E B, Borgström L
Department of Pediatrics, Viborg Hospital, Denmark.
Biopharm Drug Dispos. 1990 Jan-Feb;11(1):85-90. doi: 10.1002/bdd.2510110109.
The study aimed at finding the absolute bioavailability of terbutaline of a newly developed CR-granulate. Eight asthmatic children, aged 8-13 years, were given 3 mg of terbutaline as the CR-granulate, concomitant with the intravenous administration of 0.100 mg of deuterium-labelled terbutaline. The labelling of the intravenous dose made possible a separation, in the analytical step, of terbutaline originating from the intravenous and oral administration. Maximal plasma concentration, 8.7 (range: 4.9-15.2) nmol l-1, was reached after 4.7 (2.2-6.0) h. Absolute bioavailability was 10.8 (7.63-16.4) per cent. The parameter values were similar to those found after administration of terbutaline CR-tablets to adults. The CR-formulation is easily swallowed and can be dosed twice daily. Thus it should be a good alternative to elixir or plain tablets, dosed three times a day.
该研究旨在确定一种新开发的控释颗粒剂特布他林的绝对生物利用度。八名8至13岁的哮喘儿童服用了3毫克控释颗粒剂特布他林,同时静脉注射0.100毫克氘标记的特布他林。静脉给药剂量的标记使得在分析步骤中能够分离出来自静脉注射和口服给药的特布他林。4.7(2.2 - 6.0)小时后达到最大血浆浓度8.7(范围:4.9 - 15.2)纳摩尔/升。绝对生物利用度为10.8(7.63 - 16.4)%。这些参数值与给成人服用特布他林控释片后得到的值相似。这种控释制剂易于吞咽,且可每日给药两次。因此,它应该是每日给药三次的酏剂或普通片剂的良好替代品。