[Time course of oxipurinol levels in plasma following single dose and chronic administration of allopurinol in different pharmaceutical preparations (author's transl)].
Oxipurinol plasma levels and plasma elimination half-life were investigated in five healthy volunteers after oral administration of 300 mg allopurinol in customary (A 300) and in slow-release preparation (A ret) in a double blind cross-over study. After a single oral dose of 300 mg allopurinol in customary preparation maximum oxipurinol plasma levels were 5.24 microgram/ml. After allopurinol in slow-release preparation maximum oxipurinol levels were 2.22 microgram/ml. 24-h oxipurinol plasma levels were 3.78 microgram/ml after A 300 and 2.08 microgram/ml after A ret, respectively. Chronic oral administration of a daily dose of 300 mg allopurinol resulted in accumulation of oxipurinol until day 8. 24-h steady-state levels of oxipurinol were found to be 9.98 microgram/ml after A 300 and 7.14 microgram/ml after A ret. All oxipurinol plasma levels on A 300 exceeded those on A ret. The time course of oxipurinol plasma levels after a single oral dose of allopurinol suggests that oxipurinol elimination from plasma follows an exponential function (first-order elimination). Plasma elimination half-life of oxipurinol was 42.65 h after administration of A 300 and 49.91 h after administration of A ret. The difference between the elimination half-lives is statistically not significant.
D000328:Adult; D000493:Allopurinol / Q000008:administration & dosage / Q000378:metabolism*; D003692:Delayed-Action Preparations; D004311:Double-Blind Method; D006207:Half-Life; D006801:Humans; D010117:Oxypurinol / Q000097:blood*; D011743:Pyrimidines / Q000097:blood*; D013997:Time Factors
D003692:Delayed-Action Preparations; D011743:Pyrimidines; D000493:Allopurinol; D010117:Oxypurinol
Verlauf der Oxipurinol-Spiegel im Plasma nach akuter und chronischer Gabe von Allopurinol in verschiedenen galenischen Zubereitungen.