别嘌呤醇口服和直肠给药生物利用度的比较

Evaluation on Bioavailability of Single Dose of Allopurinol Rectal Versus Oral Administration

目的探讨比较别嘌呤醇口服和直肠给药两种途径的生物利用度。方法10例淋巴瘤患者随机一次给予别嘌呤醇300mg口服或灌肠,给药前和给药后1、2、3、4、8、24h采血,经高效液相色谱仪监测别嘌呤醇及其主要代谢产物别嘌呤浓度。结果5例口服患者于用药后1～2h达最高血药浓度,为(3.2～6.4)μg/ml。消除半衰期为(2.3±1.3)h。5例经直肠给药患者血浆内未能检测出别嘌呤醇。结论本研究提示经直肠给药吸收甚微,不能取代口服而为临床应用。

Objective To explore the bioavailability of the two means of rectal and oral administration.Methods The bioavailability of allopurinol was studied in 10 patients with lymphoma after a single dose of 300 mg p.o.in comparison with the same dose given by the rectal route.The plasma levels were measured with a high-performance liquid chromatography 1、2、3、4、8、 24 h after administration.Results 5 patients received allopurinol orally and obtained a peak level of 3.2~6.4 μg/ml at 1~2 h,the elimination half-life was (2.3+1.3) h.However,allopurinol was not detected in the 5 patients who received allopurinol as an enema.Conclusion The bioavailability of allopurinol in this formulation is poor after rectal administration.