Relation between plasma concentration and therapeutic efficacy of a new anti-inflammatory compound, benoxaprofen (LRCL 3794) in rats with adjuvant-induced arthritis

Chatfield, David H.; Cashin, C. H.; Kitchen, E. A.; Green, John N.

doi:10.1111/j.2042-7158.1977.tb11339.x

Cited by 6 publications

(2 citation statements)

References 4 publications

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“…Single-dose studies in several animal species have shown that the compound is well absorbed after oral administration . In the adjuvant arthritis test conducted in rats, it has been shown that with steady-state plasma levels of 5 gg/ml there is a 30% reduction in secondary lesions as measured by paw volume, and with plasma levels of 35 jg/ml the reduction is 70% (Chatfield, Cashin, Kitchen & Green, 1977). Therefore initial studies in human volunteers were planned with the object of establishing the oral dose of benoxaprofen which would produce plasma concentrations in the range 5-35 ig/ml and to provide other data useful in the design of the initial clinical trials.…”

Section: Introduction Methodsmentioning

confidence: 99%

Preliminary studies of absorption and excretion of benoxaprofen in man.

Smith¹,

Goulbourn²,

Burt³

et al. 1977

Brit J Clinical Pharma

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1 Benoxaprofen is a new acidic anti‐inflammatory compound which was well absorbed after oral administration to man. 2 Single doses of 100, 200 and 400 mg produced mean peak concentrations in the plasma of 13.0, 33.5 and 45.3 microgram respectively, and the plasma half‐life of the compound was between 30 and 35 hours. 3 Multiple dosing with 25 and 50 mg every 24 h achieved an equilibrium conentration in the plasma after 6‐8 days, while dosing with 100 mg every 12 h enabled equilibrium to be reached in 3‐6 days. Plasma concentrations between 35 and 45 microgram/ml were achieved by giving 100 mg doses every 12 hours. 4 Absorption of benoxaprofen was delayed when the drug was given with food, but the total amount absorbed remained the same. 5 The effect of milling the material to small particle size (19 micron) was to increase the rate of absorption compared to that of unmilled material (58 micron). 6 Benoxaprofen was well tolerated by healthy male subject in the doses given.

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Section: Introduction Methodsmentioning

confidence: 99%

Preliminary studies of absorption and excretion of benoxaprofen in man.

Smith¹,

Goulbourn²,

Burt³

et al. 1977

Brit J Clinical Pharma

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show abstract

“…The title compound, known as benoxaprofen, is one of a series of related compounds prepared by Dunwell, Evans, Hicks, Cashin & Kitchen (1975) that have some anti-inflammatory activity. Subsequent Work by Cashin, Dawson & Kitchen (1977) and Chatfield, Cashin, Kitchen & Green (1977) and others established its use as a non-steroidal anti-inflammatory agent. Benoxaprofen was marketed as a drug but subsequently withdrawn in 1982.…”

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confidence: 99%