Macromolecular prodrugs of a hydrophilic polymer [α,β-poly( N- hydroxyethyl)-DL-aspartamide (PHEA)] was used as a drug carrier. Three poly- (HEA)-NSAID adducts were studied: poly(HEA)-Alclofenac, poly(HEA)-Keto profen, and poly(HEA)-Ibuprofen. Prodrugs with different drug content were synthesized both as water-soluble and water-insoluble agents. Hydrolysis of water-soluble adducts in a simulated gastric juice was studied.
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References
1.
Otterness, I.G. and M.L. Bliven.1985. In Nonsteroidal Anti-Inflammatory Drugs . J. G. Lombardino, ed. New York: John Wiley & Sons.
2.
Cavallini, L. and G. Lucchetti.1975. Gazz. Med. Ital. , 134(1):7.
3.
Adams, S.S., R.G. Bough, E.E. Cliffe, B. Lessel and R.F.N. Mills.1969. Toxicol. Appl. PharmacoL, 15(2):310.
4.
Dumitriu, S. , M. Popa and M. Dumitriu.1989. J. Bioactive Compat. Polym., 4:57.
5.
Hashida, M., Y. Takakura, S. Matsumoto, H. Sasaki, A. Kato, T. Kojima, S. Muranishi and H. Sezaki.1983. Chem. Pharm. Bull., 31(6):2055.
6.
Kopeček, J.1990. J. Controlled Release , 11:279.
7.
Bennet, D.B. , N.W. Adams, X. Li , J. Feijen and S.W. Kim.1988. J. Bioactive Compat. Polym., 3:44.
8.
Cecchi, R., L. Rusconi, M.C. Tanzi, F. Danusso and P. Ferruti.1981. J. Med. Chem., 24:622.
9.
Azori, M., J. Pató, É. Csákvári and F. Tüdós.1986. Makromol. Chem., 187:2073.
10.
Harboe, E., C. Larsen, M. Johansen and H.P. Olesen.1989. Int. J. Pharm., 53:157.
11.
Giammona, G. , B. Carlisi and S. Palazzo.1987. J. Polym. Sci., Polym. Chem. Ed., 25:2813.
12.
Antoni, G., C. Arezzini, F. Cocola, G. Gazzei and P. Neri.1979. Il Farmaco Ed. Pr., 34(4):146.
13.
Rypáček, F., J. Drobník, V. Chmelar and J. Kálal.1982. Plugers Arch., 392:211.
14.
Duncan, R., D. Starling, F. Rypáček, J. Drobník and J.B. Lloyd.1982. Biochim. Biophys. Acta, 717:248.
15.
Rypáček, F., J. Drobník and J. Kálal.1980. Analytical Biochemistry, 104: 141.
16.
Giammona, G. , G. Puglisi, B. Carlisi, R. Pignatello, A. Spadaro and A. Caruso.1989. Int. J. Pharm., 57:55.
17.
Castelli, F. , G. Giammona, G. Puglisi, B. Carlisi and S. Gurrieri.1990. Int. J. Pharm., 59:19.
18.
Lambelin, G. , J. Roba, C. Gillet and N.P. Buu-Hoi.1970. Arzneim. Forsch. (Drug Res.), 20:610.
19.
Julou, L., C. Guyonnet, R. Ducrot, C. Garrett, M.C. Bordone, G. Maignan and J. Pasquet.1971. J. Pharmacol. ( Paris), 2:18.
20.
Julou, L., C. Guyonnet, R. Ducrot, J. Fournel and J. Pasquet.1976. Scand. J. Rheumatol. Suppl., 14:33.
21.
Kubota, T., H. Komatsu, H. Kawamoto and T. Yamada.1979. Arch. Int. Pharmacodin., 237:169.