Intestinal absorption of disodium ethane-1-hydroxy-1,1-diphosphonate (disodium etidronate) using a deconvolution technique.
Intestinal absorption of disodium ethane-1-hydroxy-1,1-diphosphonate (disodium etidronate) using a deconvolution technique.
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使用去卷积技术观察乙烷-1-羟基-1,1-二膦酸二钠（依替膦酸二钠）的肠道吸收。
DOI：
10.1016/0041-008x(73)90219-6
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发表时间：
1973
影响因子：
3.8
通讯作者：
Paul D. Saville
中科院分区：
文献类型：
--
作者：
Robert R. Recker;Paul D. Saville
在9名健康成年男性中静脉和口服给予[14 C]乙烷-1-羟基-1，1-二膦酸二钠（EHDP™，依替膦酸二钠）后获得血清比活度曲线。在I组中，EHDP的口服载体剂量为5 mg/kg，在II组中为30 mg/kg。通过拉普拉斯变换（总吸收百分比，TPA）求解的两条曲线的逆卷积函数、150 min时经口：静脉血清平衡比、经口：静脉尿液回收率（组I）和粪便回收率（组II，100 -粪便回收率）表示每种情况下的吸收（经口给药剂量百分比）。第1组静脉注射示踪剂后24小时尿同位素回收率。在两组中获得了口服同位素后48小时的尿液回收率，在组II中获得了5天的粪便回收率。在组I中，通过去卷积技术计算的平均吸收为1.49%，通过口服：静脉血清平衡比计算的平均吸收为2.95%，通过口服：静脉尿回收率计算的平均吸收为3.35%。静脉注射同位素后的平均尿液回收率为给药剂量的52.0%，口服同位素后为1.80%。在组II中，通过去卷积技术计算的平均吸收率为3.99%，通过经口：静脉血清平衡比计算的平均吸收率为7.19%，通过粪便回收率计算的平均吸收率为10.2%。口服同位素后的尿液回收率平均为3.10%，粪便回收率（不包括1例受试者）为口服剂量的93.0%。第II组的保留率（100 -总回收率，不包括1例受试者）平均为口服剂量的6.9%。结论：I组吸收的最佳估计值为口服：静脉尿回收率（3.35%），II组为口服：静脉150分钟血清平衡率（7.19%）。
Serum specific activity curves were obtained after iv and oral administration of [14C]disodium ethane-1-hydroxy-1,1-diphosphonate (EHDP™, disodium etidronate) in 9 healthy adult males. In group I the oral carrier dose of EHDP was 5 mg/kg and in group II 30 mg/kg. Absorption in each case (percent of oral dose administered) was expressed by an inverse convolution function of the two curves solved by Laplace transforms (total percent absorption, TPA); by the oral:iv serum equilibrium ratio at 150 min; by the oral:iv urine recovery ratio (Group I) and by the fecal recovery (Group II, 100 — fecal recovery). Twenty-four-hr urine isotope recovery after iv tracer was obtained in group 1. Forty-eight hr urine recoveries after oral administration of the isotope were obtained in both groups and 5-day fecal recoveries were obtained in group II. In group I, the mean absorption by the deconvolution technique was 1.49%, by the oral:iv serum equilibrium ratio 2.95% and by the oral:iv urine recovery ratio 3.35%. Mean urine recovery after iv isotope was 52.0% and after oral isotope was 1.80%, of the administered dose. In group II mean absorption by the deconvolution technique was 3.99%, by the oral:iv serum equilibrium ratios, 7.19% and by fecal recovery values 10.2%. Urine recovery after the oral administration of the isotope averaged 3.10%, and fecal recovery (excluding one subject), 93.0% of the oral dose. Retention (100 — total recovery, excluding one subject) in group II averaged 6.9% of the oral dose. It was concluded that the best estimate of absorption in group I was the oral:iv urine recovery ratio (3.35%), and in group II the oral:iv serum equilibrium ratio at 150min (7.19%).