Fukuda H, Honda C, Wadabayashi N, Kobayashi T, Yoshino K, Hiratsuka J, Takahashi J, Akaizawa T, Abe Y, Ichihashi M, Mishima Y
Department of Nuclear Medicine and Radiology, Institute of Development, Aging and Cancer, Tohoku University, Japan.
Melanoma Res. 1999 Feb;9(1):75-83. doi: 10.1097/00008390-199902000-00010.
To optimize the neutron dose for boron neutron capture therapy (BNCT), the boron-10 (10B) concentration kinetics of 10B-p-boronophenylalanine (BPA) were analysed in 22 melanoma patients with primary or metastatic melanomas who received BPA and subsequently underwent BNCT or surgery. The blood concentration in nine patients receiving 179.7+/-14.9 mg/kg BPA increased with time during intravenous infusion, peaked at the end of administration and decreased thereafter. The peak values at the end of administration were 9.4 2.6 microg 10B/g blood, and half-lives for the initial and second components of the blood clearance were 2.8 and 9.2 h, respectively. Skin concentrations in the 10 patients varied from case to case; however, skin-to-blood ratios were relatively constant at 1.31+/-0.22 during the 6 h after the end of administration. Boron concentrations in the tumours resected from the seven patients who were operated on decreased in parallel to the blood values, the tumour-to-blood ratio being relatively constant at 3.40+/-0.83. The present analytical data of BPA pharmacokinetics support our previous approach for optimizing the timing of irradiation and setting the neutron flux large enough for tumour eradication but still tolerable for normal skin.
为优化硼中子俘获疗法（BNCT）的中子剂量，对22例患有原发性或转移性黑色素瘤的患者进行了分析，这些患者接受了对硼苯丙氨酸（BPA）治疗，随后接受了BNCT或手术，分析了其中硼-10（¹⁰B）的浓度动力学。9例接受179.7±14.9mg/kg BPA治疗的患者，静脉输注期间血药浓度随时间升高，给药结束时达到峰值，随后下降。给药结束时的峰值为9.4±2.6μg¹⁰B/g血液，血液清除初始成分和第二成分的半衰期分别为2.8小时和9.2小时。10例患者的皮肤浓度因病例而异；然而，给药结束后6小时内，皮肤与血液的比值相对恒定，为1.31±0.22。7例接受手术患者切除肿瘤中的硼浓度与血液值平行下降，肿瘤与血液的比值相对恒定，为3.40±0.83。目前BPA药代动力学的分析数据支持我们之前优化照射时间和设定足够大的中子通量以根除肿瘤但仍能耐受正常皮肤的方法。
