Restricted accessReview articleFirst published online 1987-4
Review : Polymer Drugs and Polymeric Drugs: Part 3-Synthesis and Hydrolysis of Acryloyl and Methacryloyl Type Polymeric Drugs Containing 5-Fluorouracil and Theophylline
Acryloyl and methacryloyl derivatives of 5-fluorouracil and theophylline were synthesized by the reaction of trimethylsilylated 5-fluorouracil or theophylline with acryloyl chloride or methacryloyl chloride. Polymerization and copoly merization of derivatives with vinyl monomers gave polymeric drugs contain ing pharmaceutically active 5-fluorouracil or theophylline. Under mild conditions, these acryloyl and methacryloyl type polymeric drugs were found to undergo amide hydrolysis to release the 5-fluorouracil or theophylline.
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References
1.
Takemoto, K.Polymeric Drugs. L. G. Donaruma and O. Vogl, eds. New York: Academic Press, p. 103 (1978).
2.
Pitha, J., M. Akashi and M. Draminski.Biomedical Polymer: Polymeric Materials and Pharmaceuticals for Biomedical Use. E. P. Goldberg and A. Nakajima, eds. New York :Academic Press, p. 271 (1978).
3.
Akashi, M., K. Beppu, I. Kikuchi and N. Miyauchi.J. Macromol. Sci.-Chem., A23:1233 (1986).
4.
Akashi, M., M. Wada, S. Yanase and N. Miyauchi.J. Polym. Sci., Polym. Lett. Ed., in press.
5.
Tada, M.Chem. Lett., 129 (1975 ).
6.
Ozaki, S., Y. Ike, H. Mizuno, K. Ishikawa and H. Mori.Bull. Chem. Soc. Jpn., 50:2406 (1975).
7.
Umrigar, P.P. , S. Ohashi and G.B. Butler.J. Polym. Sci. Polym. Chem. Ed., 17:351 (1979).
8.
Gebelein, C.G., R.M. Morgan, R. Glowacky and W. Baig.Biomedical and Dental Applications of Polymers, 191 (1981).
9.
Hartsough, R.R. and C.G. Gebelein.Polym. Mater. Sci. Eng., 51:131 (1984).
10.
Buur, A. and H. Bundgaad.Int. J. Pharm., 21:349 (1984).
11.
Ouchi, T., H. Yuyama and O. Vogl.Makromol. Chem. Rapid Commun., 6:815 (1985).
12.
Akashi, M., Y. Tanaka, H. Iwasaki and N. Miyauchi.Angew. Makromol. Chem., 147:207 (1987).
13.
Akashi, M., Y. Inaki and K. Takemoto.Makromol. Chem., 178:353 (1977).
