Drug Development and Industrial Pharmacy 2001-01-01

Activity profile of glycolamide ester prodrugs of ibuprofen.

A K Bansal, R K Khar, R Dubey, A K Sharma

文献索引：Drug Dev. Ind. Pharm. 27(1) , 63-70, (2001)

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摘要

Glycolamide esters of ibuprofen (I), namely, unsubstituted (II), N,N dimethyl (III), and N,N diethyl (IV), were synthesized and studied for different physicochemical, pharmacological, and toxicological properties. They were comparable with I in respect of anti-inflammatory and analgesic activity but did not exhibit reduction in the ulcerogenicity on oral administration. However, all three exhibited significantly better topical activity in carrageenan-induced rat paw edema assay. In the same assay, they provided significant protection against inflammation when applied at a site remote to the inflammation site.