Objective: To study the concentration change of chemotherapeutic agents in plasma and tissue after intraarterial and intravenous injection.

Methods: Ten mature female New Zealand rabbits were divided randomly into two groups. Fluorouracil, etopiside, and cisplatin were injected into the rabbits through the ear vein in one group and through the internal iliac artery in the other group. Blood samples and the uterus tissue specimens were collected at various time points after injection. Drug concentration in plasma and tissue was determined by high performance liquid chromatography (HPLC) method. The data were analyzed by the pharmacokinetic program 3P97.

Results: Regular concentration change of the three drugs in plasma and tissue was observed after the intravenous and intraarterial injection, which met the two - compartment model. The pharmacokinetic parameters of the three drugs after intravenous and intraarterial injection were different. The peak concentration in plasma after intraarterial injection was lower than that after intravenous injection and the peak concentration and area under curve (AUC) value in tissue after intraarterial injections were higher than those after intravenous injection.

Conclusion: Intraarterial chemotherapy has advantages to intravenous chemotherapy in fluorouracil, etopiside and cisplatin. These advantages depend on the drug pharmacological properties.

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