Wilimzig C, Latz R, Vierling W, Mutschler E, Trnovec T, Nyulassy S
Datapharm GmbH, Munich, Germany.
Eur J Clin Pharmacol. 1996;49(4):317-23. doi: 10.1007/BF00226334.
Magnesium plasma concentrations were measured in healthy probands before and after administration of trimagnesium dicitrate by the oral and intravenous routes. There was a notable circadian fluctuation of the plasma concentration with a peak in the evening hours. After oral administration of 12 and 24 mmol magnesium, a long-lasting, statistically significant increase in plasma magnesium concentration measured as the increase in area under the curve (AUC) between 0 and 12 h, of 3.1% and 4.6%, respectively, was found. After intravenous administration of 4 and 8 mmol magnesium, AUCs increased by 9.5% and 16.1%, respectively. The decline in the plasma magnesium concentration after i.v. administration was compatible with a three-compartment model with a terminal half-time of about 8 h. Although no absolute value of the oral bioavailability of trimagnesium dicitrate could be determined from the data, our results may be important in helping to elucidate the influence of magnesium preparations on the plasma magnesium concentration. By comparing the effects of different preparations, it should be possible to estimate the relative oral bioavailability and the bioequivalence of these preparations.
在健康受试者中,通过口服和静脉途径给予柠檬酸三镁前后,测量其血浆镁浓度。血浆浓度存在显著的昼夜波动,在傍晚时分达到峰值。口服12和24毫摩尔镁后,以曲线下面积(AUC)在0至12小时之间的增加来衡量,血浆镁浓度出现持久且具有统计学意义的升高,分别为3.1%和4.6%。静脉注射4和8毫摩尔镁后,AUC分别增加了9.5%和16.1%。静脉注射后血浆镁浓度的下降符合三室模型,终末半衰期约为8小时。尽管从这些数据中无法确定柠檬酸三镁的口服生物利用度绝对值,但我们的结果可能有助于阐明镁制剂对血浆镁浓度的影响。通过比较不同制剂的效果,应该能够估计这些制剂的相对口服生物利用度和生物等效性。