Effects of Food on Oxaprozin Bioavailability

Chiang, Soong T.; Knowles, John A.; Hubsher, Jerome A.; Ruelius, Hans W.; Walker, Bruce K.

doi:10.1002/j.1552-4604.1984.tb02790.x

Cited by 13 publications

(1 citation statement)

References 11 publications

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“…It was separated and identified both by thin layer chromatography 4 and gas chromatography 5 . A number of liquid chromatographic (LC) methods were reported for the determination of OXA [6][7][8][9] in biological fluids. There is a LC method for the quantitative determination of OXA and its impurities in the bulk drug 10 .…”

Section: Introductionmentioning

confidence: 99%

Simple Extractive Colorimetric Determination of Oxaprozin by Acid‐Dye Complexation Methods in Solid Dosage Form

Ganesh¹,

Thangabalan

Patil³

et al. 2008

Journal of Chemistry

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A simple and sensitive extractive spectrophometric method has been described for the assay of oxaprozin (OXA) either in pure form or in pharmaceutical solid dosage form. The developed method involves formation of colored chloroform extractable ion-pair complex of OXA with bromocresol green in aqueous acidic medium. The extracted complexes showed absorbance maxima at 421 nm. Beer's law is obeyed in the concentration range of 10-50 μg mL-1. This method has been applied to the determination of drug in commercial tablets. Results of analysis were validated statistically. The excipients present in the formulations do not interfere with the assay procedure.

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Section: Introductionmentioning

confidence: 99%

Simple Extractive Colorimetric Determination of Oxaprozin by Acid‐Dye Complexation Methods in Solid Dosage Form

Ganesh¹,

Thangabalan

Patil³

et al. 2008

Journal of Chemistry

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A quantitative approach to probe the dependence and correlation of food-effect with aqueous solubility, dose/solubility ratio, and partition coefficient (LogP) for orally active drugs administered as immediate-release formulations

Singh

2005

Drug Dev. Res.

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The purpose of the present review was to systematically evaluate if aqueous solubility, dose/solubility ratio, and partition coefficient (Log P ) could be used as useful parameters to quantitatively probe the dependence and correlation of in vivo food effects with these physicochemical properties of orally active drugs administered as immediate-release (IR) formulations. Mean AUC data obtained under fasted and fed states of over 100 structurally diverse orally active drugs with different physicochemical properties were obtained from the primary literature. Correlations of AUC ratio (Fed/Fasted) with aqueous solubility, dose/solubility ratio, and Log P were derived and statistically evaluated by Pearson's correlation test (two-tailed). A negative correlation was obtained between the logarithm of the aqueous solubility and the AUC ratio (r 5 À0.5982, N 5 93), whereas a positive correlation existed between AUC ratio and Log P (r 5 0.5147, N 5 110) and between AUC ratio and dose/solubility ratio (r 5 0.5511, N 5 87). All these correlations were significant (Po0.0001). Based on this study, the estimated range within which a drug is not expected to be significantly affected by food falls between 0.148-89.39 mg/ml for aqueous solubility and between 0.23-624 ml for the dose:solubility ratio. The corresponding range of Log P for expecting a lack of food-effect lies between À1.13 and 2.98. Quantitatively, the effect of food was most pronounced for lipophilic, poorly water-soluble drugs (with only a few exceptions), irrespective of whether the drug is acidic, basic, or neutral. It is concluded that aqueous solubility, dose/solubility ratio, and partition coefficient can be used as useful parameters to probe the dependence and correlation of food-effect with these physicochemical parameters for immediate-release formulations. Drug Dev. Res. 65:55-75, 2005.

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Oxaprozin and Piroxicam, Nonsteroidal Antiinflammatory Drugs with Long Half‐Lives: Effect of Protein‐Binding Differences on Steady‐State Pharmacokinetics

Karim¹,

Noveck

McMahon

et al. 1997

The Journal of Clinical Pharma

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The nonsteroidal antiinflammatory drugs (NSAIDs) oxaprozin and piroxicam have long elimination half-lives (t 1/2 approximately 55 hours), permitting once-daily dose regimens. The protein-binding characteristics of these drugs, however, vary widely. This study examines the effect of these binding differences on the drugs' disposition kinetics at steady state. A total of 52 participants (26 young healthy volunteers, and 26 elderly osteoarthritic patients, 15 men and 37 women (2 of them poor metabolizers of debrisoquine [CYP2D6]) completed the two-period, two-treatment, randomized, single-dose and 21-day, once-daily multiple-dose, cross-over study. Doses of oxaprozin and piroxicam were 1,200 mg once daily and 20 mg once daily, respectively. Mean single-dose kinetic parameters of oxaprozin versus piroxicam did not differ more than +/-14% (t1/2, 53.0 versus 57.4 hours; apparent oral clearance adjusted for 70-kg body weight [Clpo], 0.139 versus 0.121 L/hr; apparent volume of distribution adjusted for 70-kg body weight [Vd/F]; 10.2 L versus 9.13 L). Protein binding was plasma-concentration dependent with oxaprozin (range, 10-400 mg/L) but not with piroxicam (range, 1-30 mg/ L). Steady-state conditions were established within 3 days with oxaprozin but took almost 12 days with piroxicam. Compared with the single-dose values, steady-state Clpo (Clpo,ss) and Vd/F of total drug increased with oxaprozin by almost 127% but remained within +/-10% with piroxicam. Post-steady-state apparent t 1/2 of the total and unbound drugs of approximately 62 hours were similarly prolonged with piroxicam but differed substantially with oxaprozin (50.6 hours [total drug] versus 23.8 hours [unbound drug]). Single dose Clpo (Clpo,sd) values of both NSAIDs were significantly correlated in the study populations. With both NSAIDs, Clpo in the two poor metabolizers of debrisoquine was within +/-20% of mean values for the population. Clinically important age- and gender-dependent decreases were not observed in the weight-adjusted, Clpo,sd or Vd/F values of the total drug for either NSAID. Clearances of the two NSAIDs were significantly correlated, suggesting that a common P450 isozyme (most likely CYP2C9, in that piroxicam is a known substrate of this isozyme) may be at least partly involved in the oxidative metabolism of these NSAIDs.

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Effects of Food on Oxaprozin Bioavailability

Cited by 13 publications

References 11 publications

Simple Extractive Colorimetric Determination of Oxaprozin by Acid‐Dye Complexation Methods in Solid Dosage Form

Simple Extractive Colorimetric Determination of Oxaprozin by Acid‐Dye Complexation Methods in Solid Dosage Form

A quantitative approach to probe the dependence and correlation of food-effect with aqueous solubility, dose/solubility ratio, and partition coefficient (LogP) for orally active drugs administered as immediate-release formulations

Oxaprozin and Piroxicam, Nonsteroidal Antiinflammatory Drugs with Long Half‐Lives: Effect of Protein‐Binding Differences on Steady‐State Pharmacokinetics

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