SYNTHESIS AND PHARMACOKINETIC BEHAVIOR OF ESTER DERIVATIVES OF 4-ISOBUTYLPHENYL-2-PROPIONIC ACID (IBUPROFEN) WITH END-HYDROXYLATED POLY(N-VINYL PYRROLIDINONE) AND POLY(N-ACRYLOYL MORPHOLINE) OLIGOMERS

Four derivatives of 4-isobutylphenyl-2-propionic acid (Ibuprofen), in which the drug was bound by ester linkages to poly(ethylene glycols) ( PEG 2000-I), monomethoxy poly(ethylene glycols) (PEG 1900-I), poly(N-v inyl pyrrolidinone) (PVP-I) and poly(N-acryloyl morpholine) (PACM-I), all having approximatively the same number average molecular weight (( M) over bar(n) similar or equal to 2:2000), were prepared and tested f or their pharmacokinetic properties after oral administration. It was found that the two end-hydroxylated amphiphilic oligomers of polyvinyl ic structure, PACM and PVP, whose physico-chemical properties are comp arable to those of PEGs especially as regards solvent affinity, have i n principle a similar potential as promoieties for preparing oligomeri c prodrugs.