Dunky A, Nitsche V, Eberl R
Wien Klin Wochenschr. 1981 Jan 23;93(2):65-8.
The efficacy of a retard preparation of allopurinol is verified by biochemical, pharmacological and clinical investigations. The action of a 300 mg allopurinol tablet, with normal release and absorption parameters, is based on the specific activity of oxypurinol, a metabolite which is formed from allopurinol according to a biotransformation process. The inhibitory action of oxypurinol on xanthine oxidase amounts to only 1/5th of that of allopurinol. On the other hand allopurinol shows an extremely short half life, so that a slow-release preparation of allopurinol seems the better way of administration to get adequate uricostatic efficacy by a single dose over a 24-hour period.
别嘌醇缓释制剂的疗效已通过生化、药理学和临床研究得到证实。一片300毫克普通释放和吸收参数的别嘌醇片的作用,是基于氧嘌呤醇的特定活性,氧嘌呤醇是别嘌醇通过生物转化过程形成的一种代谢产物。氧嘌呤醇对黄嘌呤氧化酶的抑制作用仅为别嘌醇的五分之一。另一方面,别嘌醇的半衰期极短,因此别嘌醇缓释制剂似乎是更好的给药方式,通过单次给药在24小时内获得足够的尿酸抑制疗效。