Oral melphalan kinetics
Oral melphalan kinetics
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口服马法兰动力学
DOI：
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发表时间：
1979
期刊：
影响因子：
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通讯作者：
T. Moon
中科院分区：
文献类型：
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作者：
D. Alberts;Sai Y. Chang;H.;T. L. Evans;T. Moon
口服美法仑后的全身利用度尚不清楚。大多数患者接受固定的口服剂量方案。我们研究了14例患者单次口服美法仑后的处置。另外5名患者在静脉注射相同剂量后也进行了研究。口服美法仑的平均血浆终末相半衰期（t1/2）为90 ±17 min。平均血药浓度-时间曲线下面积（CXT）为53 ± 33 µg · min/ml。在前24小时内，口服美法仑的尿排泄率平均为10.9 ± 4.9%。在口服和静脉注射美法仑（0.6 mg/kg）后，研究的5名患者的CXT比率（口服：静脉注射）范围在0.25和0.89之间，平均为0.56。在14例空腹患者口服给药后，美法仑首次出现在血浆中的时间在15分钟和6小时之间变化。在骨髓瘤患者口服美法仑，没有发现美法仑在血浆或尿液中长达24小时。一些情况下，肿瘤对口服美法仑的反应失败可能是由于生物利用度不足，而不是固有的肿瘤抵抗。
The systemic availability of melphalan after oral administration is not well known. Most patients are put on a fixed oral dosage regimen. We have studied the disposition of melphalan in 14 patients after single oral doses. Five were also studied after receiving the same dose intravenously. Oral melphalan had a mean plasma terminal phase half‐life (t½) of 90 ±17 min. The mean area under the plasma concentration: time curve (CXT) was 53 ± 33 µg · min/ml. Urinary excretion of oral melphalan averaged 10.9 ± 4.9% during the first 24 hr. The CXT ratio (oral: intravenous) for the 5 patients studied after both oral and intravenous melphalan (0.6 mg/kg) ranged between 0.25 and 0.89 and averaged 0.56. After oral dosing in 14 fasting patients, the time at which melphalan first appeared in the plasma varied between 15 min and 6 hr. In a myeloma patient who took oral melphalan, no melphalan was found in plasma or urine up to 24 hr. Some instances of failure of tumor response to oral melphalan may be due to inadequate bioavailability rather than inherent tumor resistance.