Evard D, Aubry J P, Le Quintrec Y, Cheymol G, Cheymol A
Br J Clin Pharmacol. 1984 Oct;18(4):632-7. doi: 10.1111/j.1365-2125.1984.tb02518.x.
Pindolol kinetics and bioavailability were studied after a single dose (oral 5 mg; intravenous 3 mg) in nine patients with malabsorption (two with villous atrophies, seven with short bowel syndromes) and in six healthy volunteers. After oral administration no significant differences were observed in bioavailability (59.4 +/- 6.2% in patients vs 79.5 +/- 8.6% in controls) and for most plasma and urinary pharmacokinetic parameters between the experimental and control groups as a whole. However, detailed analysis revealed decreased absorption for pindolol in two out of nine patients. After i.v. administration, apparent distribution volume was smaller (V: 2.10 +/- 0.25 l kg-1 vs 3.05 +/- 0.31 l kg-1) and global elimination constant was larger (ke: 1.43 +/- 0.46 h-1 vs 0.56 +/- 0.10 h-1), in patients with malabsorption than in controls (P less than 0.05). The smaller weight of patients and pharmacokinetic modifications due to the pathology could account for this.
对9例吸收不良患者(2例绒毛萎缩、7例短肠综合征)和6名健康志愿者单次给药(口服5mg;静脉注射3mg)后,研究了吲哚洛尔的动力学和生物利用度。口服给药后,实验组和对照组整体之间的生物利用度(患者为59.4±6.2%,对照组为79.5±8.6%)以及大多数血浆和尿液药代动力学参数均未观察到显著差异。然而,详细分析显示,9例患者中有2例吲哚洛尔吸收减少。静脉注射给药后,吸收不良患者的表观分布容积较小(V:2.10±0.25l·kg⁻¹ 对比 3.05±0.31l·kg⁻¹),总体消除常数较大(ke:1.43±0.46h⁻¹ 对比 0.56±0.10h⁻¹),与对照组相比差异有统计学意义(P<0.05)。患者体重较轻以及病理导致的药代动力学改变可能是其原因。