Consentrations of 5-Fluorouracil in Portal Vain after p.o. Administration by the Sutained Release Type

Shigeru Sato, Yoshimasa Ootani, Yoshiki Hiki, Akira Kakita

Department of Surgery, Kitasato University School of Medicine

We have produced the sustained release type 5-Fluorouracil (5-Fu) for the purpose of the inhibition of liver metastasis of the gastrointestinal tract carcinomas and evaluated its hemodynamics. After 10 mg/kg of sustained release type 5-Fu (Sustained release group) had been administered into the rabbit duodenum, the blood sample was taken from the portal vein with specific intervals. The concentration of 5-Fu reached the plateau three hourse after the administration and the high concentration higher than 700 ng/ml was maintined. The concentration of the peripheral blood sample which was taken simultaneously was lower than 100 ng/ml. On the other hand, the portal concentration of presently available 5-Fu (Control group, 10 mg/kg) reached the maximum concentration of 2600 mg/ml followed by the straight lined decrease. The mean retaining time (MRT) was 3.6 hours in sustaiend release group and 1.9 hours in control group. We conclude that our sustained release type 5-Fu maintain high portal concentration and the low peripheral concentration for the prolonged time. It is effective for the local treatment of liver metastasis which is targetting portal vein.

Reprint requests
Sigeru Sato Department of Surgery, Sagamidai Hospital
6-24-28 Sagamigaoka, Zama, 228-0001 JAPAN

Accepted
December 3, 1997

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