Jensen K M, Grenabo L
Acta Pharmacol Toxicol (Copenh). 1985 Nov;57(5):322-7. doi: 10.1111/j.1600-0773.1985.tb00052.x.
The pharmacokinetics of indomethacin was studied after intravenous and intramuscular injection of 50 mg and administration of rectal solution and suppositories of 100 mg to 8 volunteers. Peak plasma concentrations of indomethacin occurred 20 min. after administration of the rectal solution (3.7 micrograms X ml-1), 40 min. after intramuscular injection (2.7 micrograms X ml-1), and 60 min. after suppositories (3.7 micrograms X ml-1). The bioavailability after the two rectal forms was found to be almost the same, about 80%. After intramuscular injection the bioavailability was calculated to be complete. These results suggest that indomethacin administered as a rectal solution or as intramuscular injection may be an alternative to intravenous administration when an early plasma peak of the drug is required.
对8名志愿者静脉注射50毫克、肌肉注射50毫克、直肠给药100毫克溶液和栓剂后,研究了吲哚美辛的药代动力学。直肠溶液给药后20分钟出现吲哚美辛血浆峰浓度(3.7微克/毫升),肌肉注射后40分钟(2.7微克/毫升),栓剂给药后60分钟(3.7微克/毫升)。发现两种直肠剂型给药后的生物利用度几乎相同,约为80%。肌肉注射后的生物利用度经计算为完全。这些结果表明,当需要药物早期血浆峰浓度时,直肠溶液或肌肉注射给药的吲哚美辛可能是静脉给药的替代方法。