Dextrans - potential polymeric drug carriers for flurbiprofen

• Published in: Pharmazie Vol. 58; no. 6; pp. 389 - 391
• Main Authors: Shrivastava, S. K., Jain, D. K., Trivedi, P.
• Format: Journal Article
• Language: English
• Published: Eschborn Govi-Verlag 01.06.2003; Govi
• Subjects: Animals; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - adverse effects; Anti-Inflammatory Agents, Non-Steroidal - chemistry; Biological and medical sciences; Bones, joints and connective tissue. Antiinflammatory agents; Carrageenan; Chemical Phenomena; Chemistry, Physical; Chromatography, High Pressure Liquid; Colon - metabolism; Dextrans - chemistry; Drug Carriers - chemistry; Drug Delivery Systems; Edema - chemically induced; Edema - pathology; Edema - prevention & control; Flurbiprofen - administration & dosage; Flurbiprofen - adverse effects; Flurbiprofen - chemistry; Hydrolysis; Magnetic Resonance Spectroscopy; Medical sciences; Pharmacology. Drug treatments; Rats; Spectrophotometry, Infrared; Stomach Ulcer - chemically induced; Rat; Toxicity; Drug carrier; Gastrointestinal; Molecular weight property relation; Arylpropionic acid derivatives; Ulcer; Chemical synthesis; Flurbiprofen; Subacute; Control release polymer; Acute; Rodentia; Oral administration; Inflammation; Biological activity; Non steroidal antiinflammatory agent; Dextran; Vertebrata; Chemotherapy; Chronic; Mammalia; Treatment; Animal; Conjugated compound; Polysaccharide
• ISSN: 0031-7144

Dextrans have been used as carrier for flurbiprofen. Conjugates of flurbiprofen were synthesized by preparing their acylimidazol derivatives which were condensed in situ with dextrans of different molecular weight (40000, 60000, 110000 and 200000). The structures of the synthesized conjugates were confirmed by IR and NMR spectroscopy. The degrees of substitution were obtained between 8.0 to 9.5% and molecular weight was determined by Mark-Howin Sakurada viscosity equation. A hydrolysis study was performed in different buffer solutions (pH 1.2, 7.4, 9.0) and 80% human plasma (pH 7.4). The hydrolysis followed first order kinetics. Much faster hydrolysis was observed at pH 9.0 compared to buffer solution pH 7.4 and 80% human plasma (pH 7.4). The biological evaluation for acute and chronic anti-inflammatory activity was performed and the results were found to be comparable with the parent drug. The conjugates showed remarkable reduction in ulcerogenicity compared to parent flurbiprofen.