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关于2-氯-2'-脱氧腺苷(CdA)的生物利用度。食物和奥美拉唑的影响。

On the bioavailability of 2-chloro-2'-deoxyadenosine (CdA). The influence of food and omeprazole.

作者信息

Albertioni F, Juliusson G, Liliemark J

机构信息

Department of Clinical Pharmacology, Karolinska Hospital, Stockholm, Sweden.

出版信息

Eur J Clin Pharmacol. 1993;44(6):579-82. doi: 10.1007/BF02440863.

Abstract

The pharmacokinetics of oral CdA (0.24 mg/kg) was studied in 4 patients (1 with hairy cell leukaemia and 3 with B-cell chronic lymphocytic leukaemia) to determine any effect of food and fasting with and without omeprazole. Food intake did not significantly influence the bioavailability of CdA (42% after food intake vs 46% while fasting) but it did reduce the maximum plasma concentration (Cmax) by 40%; 83 compared to 116 nM while fasting. The time to reach maximum concentration (tmax) was delayed about 0.8 h after food intake. Pretreatment with omeprazole did not significantly influence the bioavailability of CdA (51% vs 46% without), or the interindividual variability in bioavailability in the fasting state (C. V. 0.26 with and C. V. 0.27 without). In conclusion, there was a small, though not statistically significant reduction in the bioavailability of CdA after food intake. Omeprazole did not significantly improve the bioavailability of CdA.

摘要

对4例患者(1例毛细胞白血病患者和3例B细胞慢性淋巴细胞白血病患者)进行了口服2 - 氯脱氧腺苷(CdA,0.24mg/kg)的药代动力学研究,以确定食物、禁食以及同时使用奥美拉唑对其的影响。食物摄入对CdA的生物利用度没有显著影响(进食后为42%,禁食时为46%),但确实使血浆最大浓度(Cmax)降低了40%;禁食时为116nM,进食后为83nM。进食后达到最大浓度的时间(tmax)延迟了约0.8小时。奥美拉唑预处理对CdA的生物利用度没有显著影响(使用时为51%,未使用时为46%),对禁食状态下生物利用度的个体间变异性也没有显著影响(使用时变异系数为0.26,未使用时为0.27)。总之,进食后CdA的生物利用度有小幅降低,但无统计学意义。奥美拉唑未显著提高CdA的生物利用度。

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