Pak C Y, Skurla C, Brinkley L, Sakhaee K
J Clin Pharmacol. 1984 Jan;24(1):19-26. doi: 10.1002/j.1552-4604.1984.tb01809.x.
The time course, dose frequency schedule, and dose-response relationship of the citraturic response to orally administered potassium citrate was examined in 22 normal volunteers and 21 patients with uric acid or calcium nephrolithiasis. The slow-release (wax matrix) preparation of potassium citrate produced a rapid and sustained rise in urinary citrate lasting for up to 12 hours following a single oral administration. Probably owing to this prolonged action, the slow-release preparation when given in a twice-daily or thrice-daily schedule at a dosage of 60 meq or 3.78 Gm citrate/day virtually eliminated the normally wide circadian fluctuation in urinary citrate and maintained urinary citrate at a higher, more constant level throughout the day. The liquid preparation of potassium citrate was less effective in this regard. However, the two preparations of potassium citrate caused an equivalent rise in total 24-hour urinary citrate. When 24-hour excretions of citrate were examined, urinary citrate was shown to reach its peak level by the second day of potassium citrate treatment and to return to the pretreatment level by the second day after the treatment was stopped. The rise in urinary citrate produced by treatment was directly proportional to the dose of potassium citrate. In most hypocitraturic patients with renal stones, potassium citrate 60 meq/day restored normal urinary citrate (greater than 320 mg/day).
在22名正常志愿者和21名尿酸或钙肾结石患者中,研究了口服柠檬酸钾后枸橼酸尿反应的时间进程、给药频率方案和剂量反应关系。柠檬酸钾缓释(蜡基质)制剂单次口服给药后,尿枸橼酸盐迅速且持续升高,持续长达12小时。可能由于这种延长的作用,当以每日两次或三次的给药方案,以60毫当量或3.78克柠檬酸盐/天的剂量给予缓释制剂时,实际上消除了尿枸橼酸盐通常较大的昼夜波动,并使尿枸橼酸盐在一整天内维持在较高且更恒定的水平。柠檬酸钾液体制剂在这方面效果较差。然而,两种柠檬酸钾制剂使24小时尿枸橼酸盐总量有同等程度的升高。当检查24小时枸橼酸盐排泄量时,发现尿枸橼酸盐在柠檬酸钾治疗的第二天达到峰值水平,并在治疗停止后的第二天恢复到治疗前水平。治疗引起的尿枸橼酸盐升高与柠檬酸钾剂量成正比。在大多数肾石症低枸橼酸尿患者中,60毫当量/天的柠檬酸钾可使尿枸橼酸盐恢复正常(大于320毫克/天)。