- 著者
- Takeo KAWAGUCHI Masahiko SAITO Mineo SANEYOSHI
- 出版者
- The Japanese Cancer Association
- 雑誌
- Japanese Journal of Cancer Research GANN (ISSN:09105050)
- 巻号頁・発行日
- vol.77, no.5, pp.436-439, 1986 (Released:2008-03-17)
- 参考文献数
- 13
The antitumor effect of 5-fluoro-2'-deoxy-uridine (FUdR) esters on L1210 in mice was enhanced by the simultaneous po administration of FUdR esters and acyclothymidine [5-methyl-1-(2'-hydroxyethoxymethyl)uracil]-esters. Acyclothymidine (AcTdR), which strongly inhibits the phospholytic degradation of FUdR, was released from the AcTdR esters by enzymatic hydrolysis. The FUdR esters and AcTdR esters were found to be compatible in terms of their physicochemical properties and susceptibility to enzymatic hydrolysis.
- 著者
- HIRAKU ONISHI TAKEO KAWAGUCHI TSUNEJI NAGAI
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.35, no.8, pp.3370-3374, 1987-08-25 (Released:2009-10-19)
- 参考文献数
- 22
- 被引用文献数
- 7 8
3'- (7-Carboxyheptanoyl) -5-fluoro-2'-deoxyuridine (C6-FUdR) was conjugated to decylenediamine-dextran T70 (T70-C10) or poly-L-lysine (PLL) by using 1-ethyl-3- (3-dimethylaminopropyl) -carbodiimide hydrochloride (EDC). Drug release patterns from the conjugates between C6-FUdR and T70-C10 (T70-C10-C6-FUdR) or PLL (PLL-C6-FUdR) by enzymatic and nonenzymatic processes were investigated at neutral and weakly acidic pHs. Under the nonenzymatic conditions, 5-fluoro-2'-deoxyuridine (FUdR) was released slowly only at neutral pH. This property is similar to that of C6-FUdR. Gradual drug release was observed enzymatically from T70-C10-C6-FUdR at both pHs, while PLL-C6-FUdR did not show enzymatic drug release. However, after the treatment of PLL-C6-FUdR with trypsin, FUdR was released enzymatically from the products; in this case, the release rate of FUdR was faster at neutral pH than at the weakly acidic pH. However, the release of FUdR by enzymatic processing was much slower from these conjugates than from C6-FUdR.