阿霉素经肝动脉给药的药代动力学和生物学分布

目的：观察阿霉素以不同剂型肝动脉给药后的药代动力学和生物学分布，方法：２３例肝癌经肝动脉分别注入单纯阿霉素（Ａ组，ｎ＝５），阿霉素与碘油混合液（Ｂ组，ｎ＝５），阿霉素与碘油混合并制成乳剂（Ｃ组，ｎ＝７），或Ｃ组之乳剂加用明胶海绵栓塞（Ｄ组，＝６），用高效液相色谱仪测定阿霉素外周血药浓度，对其中１２例（Ａ，Ｂ，Ｃ和Ｄ组各３例），用ＥＣＴ测定肝脏的放射性强度。结果：肝动脉单纯注入阿霉素，仅形成一过性血

Pharmacokinetics and biodistribution of doxorubicin injected from hepatic artery with different formulation for hepatocellular carcinoma

Aim: To observe the pharmacokinetics and biodistribution of doxorubicin injected from hepatic arterial with different formulation for hepatocellular carcinoma. Methods: Twenty three patients with hepatocellular carcinoma were given an intra arterial injection of doxorubicin alone(group A, n =5), a simple mixture of doxorubicin in aqueous solution with lipiodol(group B, n =5), an emulsion of doxorubicin with lipiodol (group C, n =7), or chemoembolization with the same emulsion followed by gelatin sponge particles (group D, n =6), respectively. The pharmacokinetics and biodistribution of doxorubicin were studied respectively by measurements of the blood level of doxorubicin after injection and by examination of the scintigrams and radioactivity with ECT. Results: Doxorubicin injected alone resulted in a temporarily high level of drug without predominant uptake of organs. The simple mixture of doxorubicin with lipiodol, in which lipiodol did not play the characteristic role as a carrier, only had the effects of doxorubicin and lipiodol separately, and did not have significant difference from doxorubicin alone. The emulsion of doxorubicin with lipiodol lowered the peak concentration of doxorubicin, prolonged its release and remained in tumors for a longer period of time, therefore, targeting of drug to the tumor could be achieved. These ameliorations were more pronounced after embolization with gelatin sponge particles. Conclusion: From the standpoints of pharmacokinetics and biodistribution, the emulsion of doxorubicin with lipiodol associated with gelatin sponge embolization is the best method of transcatheter hepatic arterial chemoembolization for hepatocellular carcinoma.