Acta Pharmaceutica, Vol. 57 No. 4, 2007.
Izvorni znanstveni članak
https://doi.org/10.2478/v10007-007-0035-3
Ketorolac-dextran conjugates: Synthesis, in vitro and in vivo evaluation
SAVITA VYAS
PIYUSH TRIVEDI
SUBHASH CHANDRA CHATURVEDI
Sažetak
Ketorolac is a non-steroidal anti-inflammatory drug. Dextran conjugates of ketorolac (KD) were synthesized and characterized to improve ketorolac aqueous solubility and reduce gastrointestinal side effects. An N-acylimidazole derivative of ketorolac (KAI) was condensed with a model carrier polymer, dextran of different molecular masses (40000, 60000, 110000 and 200000). IR spectral data confirmed formation of ester bonding. Ketorolac contents were evaluated by UV-spectrophotometric analysis. The molecular mass was determined by measuring viscosity using the Mark-Howink-Sakurada equation. In vitro hydrolysis studies were performed in aqueous buffers (pH 1.2, 7.4, 9) and in 80% (V/V) human plasma (pH 7.4). At pH 9, a higher rate of ketorolac release from KD was observed as compared to aqueous buffer of pH 7.4 and 80% human plasma (pH 7.4), following first-order kinetics. In vivo biological screening in mice and rats indicated that conjugates retained analgesic and anti-inflammatory activities with significantly reduced ulcerogenicity compared to the parent drug.
Ključne riječi
ketorolac-dextran conjugates; dextran carrier; NSAIDs
Hrčak ID:
15999
URI
Datum izdavanja:
1.12.2007.
Posjeta: 2.575 *