Hobbs D C, Connolly A G
J Pharmacokinet Biopharm. 1978 Dec;6(6):477-85. doi: 10.1007/BF01062104.
Using a newly developed sensitive gas chromatograph-mass spectrometer assay for benzquinamide, pharmacokinetics have been determined in man following the administration of intramuscular, oral, and rectal suppository doses. Drug is absorbed most rapidly from the intramuscular dose and least rapidly from suppositories. The mean apparent elimination half-life is 1.0-1.6 hr from all formulations. Benzquinamide is 33-39% bioavailable from the capsule and suppository formulations, relative to the intramuscular formulation. A high correlation between capsule and suppository bioavailabilities suggests that first-pass metabolism may account for at least part of the incomplete availability.
使用新开发的用于测定苄喹酰胺的灵敏气相色谱-质谱分析法，已测定了人体在肌内注射、口服和直肠栓剂给药后的药代动力学。药物从肌内注射剂量吸收最快，从栓剂吸收最慢。所有制剂的平均表观消除半衰期为1.0 - 1.6小时。相对于肌内注射制剂，苄喹酰胺从胶囊和栓剂制剂的生物利用度为33% - 39%。胶囊和栓剂生物利用度之间的高度相关性表明，首过代谢可能至少部分解释了生物利用度不完全的原因。
