Esophageal cancer chemotherapy drug carboplatin experimental study

By | March 19, 2012

Experimental study of carboplatin and carboplatin for the 2nd generation platinum anti-cancer drugs, a cell cycle non-specific, similar to the role of agents and burnt. Research by the British Johnson Mathey synthesis, officially put into operation in 1986. Card uranium transplanted tumor in animals leukemia L1210, P388, melanoma B16, ADJ/PC6 plasma cell tumors, colon C26, Mso76 and inhibit Lewis lung cancer. The role of carboplatin and DDP similar, the main target cells can cause DNA cross-linking, obstacles DNA synthesis, while preventing DNA replication, thereby inhibiting tumor cell growth.
The drug is cell cycle non-specific drugs. Intraperitoneal administration of carboplatin in the LDso in mice was 130mg / Zhi, about 10 times the LDso cisplatin. Of renal toxicity in rats or dogs, urea nitrogen and pathological changes in the index, in the corresponding doses of carboplatin were well below the renal toxicity of cisplatin. Gastrointestinal reactions are mild and the dog in the snow Shao minimum emetic dose of DDP is equivalent to 12 times and 16-208 times. Carboplatin caused almost no hearing loss, neurological toxicity is low. Dose-limiting toxicity was reversible myelosuppression.
Most of carboplatin in the body is not bound to plasma proteins, stability is higher. Experimental study of carboplatin and carboplatin in the human body plasma pharmacokinetic models of lead, mostly two-compartment model. Sasaki et al (1989) reported the distribution phase half-life of carboplatin t1/2 to 57min, elimination phase half-life of 14h. China Medical Oncology Hospital Medicine (1991) Human pharmacokinetics determination to do the results, t1/2 to 76min, t1 / are 6.92h, the apparent volume of distribution of VB as 57.78L/ml, Aue shovel under the curve was 84.71mg h / L.
Experimental study of carboplatin in rats after injection CBP20mg/kg carboplatin and protein binding of 20% is reversible within a basically stable in Ih, and to DDP2mg / after, free platinum there is only 5-10min, and the rapid binding protein, that is undetectable to the free platinum 60min. Rabbits after injection of carboplatin, the most in his discharge, and DDP in Ih, 4h, and 21 days from the urine excretion were 32%, 57% and 68%. Experimental and clinical studies have proved that card lifetime of uranium in the body shorter than the DDP. Mainly by renal excretion of carboplatin, a small part of the bile and excreted in feces.

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