Antipyretic, Analgesic and Anti-inflammatory Activities of Ketoprofen β-Cyclodextrin Inclusion Complexes in Animals(Pharmacology)

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Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) orally effective in treating fever, pain, and inflammation but gastrointestinal side effects were observed. Preparation of ketoprofen β-cyclodextrin inclusion complexes was to increase the solubility and reduce the irritation. The complexes were prepared and preliminarily confirmed using X-ray diffraction and dissolution test. Antipyretic, analgesic and anti-inflammatory models were induced by 10% yeast using rabbits, 0.8% acetic acid using mice and 1% carrageenin using rats, respectively. Results showed that the dissolution rate of ketoprofen was significantly improved by complexation. X-Ray diffraction pattern of the complexes exhibited a diffuse pattern that differed from that of physical mixture of ketoprofen and β-cyclodextrin. Ketoprofen markedly inhibited the fever reactions at a single dose of 2 mg/kg as follows : 64.53% (inhibition rate %) at Ih for ketoprofen, 73.04% at 1 h for ketoprofen β-cyclodextrin inclusion complexes, respectively. Alleviating pain reaction rates following a single dose of 8 mg/kg at 20 min were 39.25% for the inclusion complexes and 26.72% for ketoprofen, respectively. Inhibition rates to rat edema following a single dose of 5 mg/kg at 1 h were 39.47% for the inclusion complexes and 23.86% for ketoprofen. Results for antipyretic, analgesic and anti-inflammatory activities showed that the rapid and stronger effects were found in the treatment group of ketoprofen β-cyclodextrin inclusion complexes in comparison with those of free ketoprofen.
公益社団法人日本薬学会の論文
2004-10-01

Antipyretic, Analgesic and Anti-inflammatory Activities of Ketoprofen β-Cyclodextrin Inclusion Complexes in Animals(Pharmacology)

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