摘要
卡铂(Carboplatin)是我国正在研制的第二代铂类抗癌药,具有抗癌作用强,肾毒性小的特点。进行了6例住院肿瘤病人单次I.V.卡铂(400mg/sqM)的药动学研究。用无火焰原子吸收光谱测定血浆中的总铂(total Pt)及血浆离心超滤液的游离铂(free Pt)。同时用高压液相色谱(HPLC)测定血浆离心超滤液的卡铂。结果显示:卡铂与血浆中游离铂的血药一时间曲线拟合均符合一室开放模型,两条曲线平行下降,半衰期分别为1.01和1.61hr,清除率分别为12.59和8.35L/sp M.hr.分布容积分别为18.27和17.43L/sp M.,提示血浆free Pt基本反映卡铂的处置规律。而血浆总铂的衰减为二室模型,分布相半衰期(tl/2α)为1.27hr,消除相半衰期(tl/2β)为48.92hr,清除率为2.79L/sq M.hr。给药后0—24h内尿总铂的累积排泄相当于给药剂量的72.44±12.64％。
Carboplatin is a second-generation platinum coordination compound w-hich was found to be less nephrotoxic and shown the same antitumor activity as cisplatin. The pharmacokineties of carboplatin were investigeted in 6 cancer patients after single, IV bolus dose of 400 mg/sq M. Total plasma and urine platinum and plasma ultrafilterable platinum (free platinum) concentrations were determined by flameless atomic absorption spectrometry. Carboplatin was analyzed in ultrafiltrates by a specific and sensitive, high-perfo rmance liquid chromatoraghic procedure. Total plasma platinum, which represented carboplatin, protein-bound platinum and metabolites, declined biexponentially with a rapid-phase half-life of 1.27 hr, a slow-phase half-life of 48.92 hr and total body clerance of 2.79 L/sp M.hr. Plasma ultrafilterable platinum and carbop,latin. concentrations declned monoex ponentially. The plasma concentration profiles of carboplatin paralled reasonably close of total filterable species, (carboplatin Tl/2=1.01 hr, Cl=12.59 L/sq M. hr; free platinum Tl/2=1.61 hr, Cl=8.35 L/sq M.hr) and volumes of distribution were 18.27 and 17.43 L/sq M,respectively. Of the administered dose, 72 44 ±12.64% was recovered in urine over 24 hr period after injection.
出处
《癌症》
SCIE
CAS
CSCD
北大核心
1990年第6期452-455,共4页
Chinese Journal of Cancer
