Journal of Pharmaceutical Sciences p. 1578 - 1581 (1994)
Update date:2022-08-03
Topics:
De Caprariis
Palagiano
Bonina
Montenegro
D'Amico
Rossi
Five indomethacin oligoethylene ester derivatives (3-7) were synthesized and evaluated for their anti-inflammatory, analgesic, and ulcerogenic activity after oral administration. The molecular weight of the oligoethylene glycols used for synthesizing esters 3-7 ranged from 106 to 282. The chemical and enzymatic stabilities of esters 3-7 were evaluated in pH 7.4 and 2.0 buffers and in human plasma, respectively. All the prodrugs showed a good stability both in pH 7.4 phosphate buffer and in pH 2.0 buffer, and they were readily hydrolyzed by human plasma. Esters 3-7 showed an anti-inflammatory activity, determined as the percent inhibition of carrageenan-induced edema, similar to that of indomethacin, although at higher doses. From writhing test results, we observed that all the prodrugs exhibited better or similar analgesic activity compared to indomethacin. Esters 3-7 were significantly less irritating to the gastric mucosa than indomethacin, after oral administration, and esters 3-5 did not show any ulcerogenic activity, although they were administered at higher doses than indomethacin.
View MoreAnhui Sunsing Chemicals Co.,Ltd
website:http://www.sunsingchem.com
Contact:0086-566-2023179
Address:Jin An industry park, Chizhou economic technical development zone, Anhui
Shifang Taifeng New Flame Retardant Co., Ltd
Contact:02884721008
Address:tingjiang industrial park, hefeng town
Contact:+1-284-4950244
Address:Box 3069, Road Town, Tortola, British Virgin Islands
Zhangjiagang Golden Reach Fine Chemical Co.,LTD.
Contact:+86-512-6585 6968
Address:Changfu Road, Dongsha Chemical Industry Park, Zhangjiagang City, Jiangsu Province, China
Zhejiang Chemicals Import & Export Corporation
Contact:86-571-87043088
Address:No.37,Qingchun Road,Hangzhou,China
Doi:10.1021/ja962736v
(1996)Doi:10.1021/jo00334a018
(1981)Doi:10.1007/BF00765592
(1981)Doi:10.1016/S0040-4039(01)90462-9
(1981)Doi:10.1016/S0022-1139(00)81440-2
(1982)Doi:10.1055/s-1981-29451
(1981)