International journal of pharmaceutics, 2001-10, Vol.228 (1), p.129-138
2001
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Details
- Autor(en) / Beteiligte
- Titel
- Macromolecular prodrugs. IX. Synthesis of polymer-fenoprofen conjugates
- Ist Teil von
- International journal of pharmaceutics, 2001-10, Vol.228 (1), p.129-138
- Ort / Verlag
- Amsterdam: Elsevier B.V
- Erscheinungsjahr
- 2001
- Quelle
- Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)
- Beschreibungen/Notizen
- Synthesis of several polymer-fenoprofen conjugates is described. Fenoprofen was first chemically modified into benzotriazolide 2 and amino acid amide derivatives: glycine fenoprofenamide ( 3a) and β-alanine fenoprofenamide ( 3b) and their benzotriazolides 6a and 6b. Compounds 2 and 6 readily reacted with polyhydroxy aspartamide-type polymers, i.e. poly[α,β-( N-2-hydroxyethyl- dl-aspartamide)] (PHEA) and poly[α,β-( N-3-hydroxypropyl- dl-aspartamide)] (PHPA) forming conjugates 5, 8a, b and 9a, b, respectively. Conjugate 11 was obtained by partial aminolysis of poly- dl-(2,5-dioxo-1,3-pyrrolidinediyl) (PSI) with 2-aminoethyl fenoprofenamide ( 3c), followed by total aminolysis with 2-hydroxyethylamine. The synthesised polymer-drug conjugates differed in type of covalent bounding, type and/or length of spacer and drug-loading.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0378-5173eISSN: 1873-3476DOI: 10.1016/S0378-5173(01)00822-5Titel-ID: cdi_proquest_miscellaneous_71198996
- Format
- –
- Schlagworte
- Analgesics, Anti-Inflammatory Agents, Non-Steroidal - chemistry, Biological and medical sciences, Bones, joints and connective tissue. Antiinflammatory agents, Chromatography, Thin Layer, Fenoprofen, Fenoprofen - chemistry, General pharmacology, Macromolecular prodrug, Magnetic Resonance Spectroscopy, Medical sciences, Neuropharmacology, Pharmaceutical technology. Pharmaceutical industry, Pharmacology. Drug treatments, Poly[α,β-( N-2-aminoethyl- dl-aspartamide]-poly[α,β-( N-2-hydroxyethyl- dl-aspartamide)]-copolymer, Poly[α,β-( N-2-hydroxyethyl- dl-aspartamide)], Poly[α,β-( N-3-hydroxypropyl- dl-aspartamide)], Polyhydroxyethyl Methacrylate - analogs & derivatives, Polymer-drug conjugate, Prodrugs, Spacer, Spectrophotometry, Infrared, Spectrophotometry, Ultraviolet