Takada M, Usui N, Suzuki M, Furugen Y, Yamamoto T
Department of Obstetrics and Gynecology, Juntendo University School of Medicine, Tokyo.
Nihon Sanka Fujinka Gakkai Zasshi. 1993 Feb;45(2):99-105.
CDDP was administered to 36 patients with ovarian cancer by one of three routes: i.v., ip, or ia, and its pharmacokinetics was studied. 1) With an initial dose of 100 mg/body the peak values for blood free-pt were 1.63 +/- 0.78 micrograms/ml (S.D.) in the i.v. group, 0.61 +/- 0.53 micrograms/ml (S.D.) in the ip group, and 1.62 +/- 0.78 micrograms/ml (S.D.) in the ia group. The area under the curve (AUC) was 2.56 +/- 0.72 micrograms.hr/ml (S.D.), 1.84 +/- 0.75 micrograms.hr/ml(S.D.), and 2.70 +/- 0.51 micrograms.hr/ml (S.D.), respectively. 2) The free-pt level of the ascitic fluid in the ip group was 25.3 +/- 28.1 micrograms/ml (S.D.) just after the injection of 100 mg/body. 3) The ovarian tissue level following the initial CDDP dose of 100 mg/body was the highest in the ia group, next highest in the ip group, and lowest in the i.v. group. In some cases, the ovarian tissue level was markedly elevated after repeated ip injections. Deep-middle layer concentrations in ovarian tissue were not so low in the ip group as in the i.v. or ia group. As noted above, the blood free-pt peak was low following ip administration, but the ovarian tissue level was higher following ip administration than following i.v. though lower than following ia administration. These findings suggest that ip administration of CDDP may be useful in treating large tumor masses. Good results are expected particularly following repeated ip therapy, which sometimes provided a markedly high tissue level.
36例卵巢癌患者通过静脉注射（i.v.）、腹腔注射（ip）或动脉注射（ia）这三种途径之一接受顺铂（CDDP）治疗，并对其药代动力学进行了研究。1）初始剂量为100mg/体时，静脉注射组血游离铂（free-pt）峰值为1.63±0.78μg/ml（标准差），腹腔注射组为0.61±0.53μg/ml（标准差），动脉注射组为1.62±0.78μg/ml（标准差）。曲线下面积（AUC）分别为2.56±0.72μg·hr/ml（标准差）、1.84±0.75μg·hr/ml（标准差）和2.70±0.51μg·hr/ml（标准差）。2）腹腔注射组在注射100mg/体后即刻，腹水中游离铂水平为25.3±28.1μg/ml（标准差）。3）初始顺铂剂量为100mg/体时，动脉注射组卵巢组织水平最高，腹腔注射组次之，静脉注射组最低。在某些情况下，腹腔重复注射后卵巢组织水平明显升高。腹腔注射组卵巢组织深层中间层浓度不像静脉注射组或动脉注射组那样低。如上所述，腹腔给药后血游离铂峰值较低，但腹腔给药后卵巢组织水平高于静脉给药，尽管低于动脉给药。这些发现表明，顺铂腹腔给药可能对治疗大肿瘤块有用。特别是腹腔重复治疗后有望取得良好效果，有时腹腔重复治疗可使组织水平显著升高。
