Fate of the analgesic and anti-inflammatory drug K 4277 after oral administration to man

Fuccella, L. M.; Goldaniga, Giancarlo; Moro, E.; Tamassia, V.; Tosolini, G. P.; Valzelli, G

doi:10.1007/bf00644742

Cited by 26 publications

(7 citation statements)

References 4 publications

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“…The propionic acid moiety of pirprofen is shared by several other clinically active antiinflammatory compounds: fenoprofen,7 naproxen, 8 indoprofen, 3 and ibuprofen. 1 The synthesis and biological activity of pirprofen has been described by Carney and associates.…”

Section: Wasvary5 Preliminary Clinical Studiesmentioning

confidence: 99%

Disposition of pirprofen, a new anti‐inflammatory drug

Luders¹,

Maggio‐Cavaliere²,

Egger³

et al. 1977

Clin Pharma and Therapeutics

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Plasma and urine concentrations of 2-(3-chloro-4[3-pyrrolinyl]phenyl) propionic acid, pirprofen, a new nonsteroidal anti-inflammatory compound, are described for normal male volunteers receiving one or more doses of the drug. Orally administered pirprofen is rapidly and almost completely absorbed from the gastrointestinal tract, resulting in maximum plasma levels in 1 to 2 hr. Mean peak levels are 23 microng/ml after an oral pirprofen dose of 200 mg; lower doses given proportionally lower levels. Administration 1 hr after a meal slightly delays the peak plasma level, but the extent of absorption is not affected significantly. Administration of pirprofen, 150 mg, 4 times daily, or 200 mg, 3 times daily, results in nearly identical plasma levels at steady-state. Pirprofen has an apparent elimination half-life of about 7 hr. The results obtained from a 200-mg pirprofen-14C dose indicate that excretion of the drug occurs primarily by the renal route in the form of metabolites and is essentially complete within 24 hr. In urine, less than 5% of the administered dose is accounted for as unchanged drug.

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Section: Wasvary5 Preliminary Clinical Studiesmentioning

confidence: 99%

Disposition of pirprofen, a new anti‐inflammatory drug

Luders¹,

Maggio‐Cavaliere²,

Egger³

et al. 1977

Clin Pharma and Therapeutics

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“…Keyphrases o Indoprofen-analysis, high-performance liquid chromatography, human milk 0 High-performance liquid chromatography-analysis, indoprofen, human milk o Anti-inflammatory agentsindoprofen, high-performance liquid chromatographic analysis, human milk 0 Milk, human-analysis, indoprofen, high-performance liquid chromatography Indoprofen, 4-( 1,3-di hydro-1 -oxo-2H-isoindol-2-y1)a-methylbenzeneacetic acid (I), has been reported to have analgesic activity in animals and humans (1)(2)(3)(4). In an earlier report (5), a reversed-phase high performance liquid chromatographic (HPLC) method was presented for the quantitation of drug levels in plasma and urine samples.…”

Section: (1947)mentioning

confidence: 99%

High‐Performance Liquid Chromatographic Microdetermination of Indoprofen in Human Milk

Lakings

Lizarraga

Haggerty

et al. 1979

Journal of Pharmaceutical Sciences

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“…Pranoprofen, 2-(5H-[1] benzopyrano-[2, 3-b]-pyridin-7-yl) propionic acid, has been widely used to treat diseases such as rheumatoid arthritis owing to its analgesic and anti-inflammatory properties (Fuccela et al, 1973;Luders et al, 1977). It was reported that pranoprofen is strongly bound to plasma protein (Kato et al, 1976) and shows rapid absorption and a urinary recovery of over 90% after the oral administration of a marketed conventional tablet to humans (Yoshio et al, 1990).…”

Section: Introductionmentioning

confidence: 99%

Enhanced Bioavailability by Transdermal Administration of Pranoprofen Gels Containing Octanoic Acid to Rats

Shin¹

2008

Biomolecules and Therapeutics

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− The pharmacokinetic parameters and bioavailability of pranoprofen from the gel were measured to determine the enhancing effect of octanoic acid on the transdermal absorption of pranoprofen in rats. 8 mg/kg of pranoprofen was administered from gel with octanoic acid (the enhancer group) or that without octanoic acid (the control group) via the transdermal route, and the results were compared with those obtained from the intravenously (0.5 mg/kg, IV group) or orally administered group (4 mg/kg, oral group). The AUC of the control, the enhancer, the IV, and the oral groups were 20.2±5.1, 50.7±12.7, 19.9±2.5, and 70.5±17.6 ug/ml·h respectively. The average C max of the control and the enhancer group were 0.93±0.23 and 2.82±0.71 ug/ml, respectively, and the mean T max of the control and the enhancer group was 7.00 h. The relative bioavailability of the transdermally administered pranoprofen gel containing octanoic acid was approximately 2.50 times higher than the control group, showing a relatively constant, sustained blood concentration with minimal fluctuation. This suggests that it might be feasible to develop a pranoprofen gel preparation containing an enhancer for the transdermal administration, which is more convenient dosage form than the oral dosage forms.

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Fate of the analgesic and anti-inflammatory drug K 4277 after oral administration to man

Cited by 26 publications

References 4 publications

Disposition of pirprofen, a new anti‐inflammatory drug

Disposition of pirprofen, a new anti‐inflammatory drug

High‐Performance Liquid Chromatographic Microdetermination of Indoprofen in Human Milk

Enhanced Bioavailability by Transdermal Administration of Pranoprofen Gels Containing Octanoic Acid to Rats

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