Pharmacokinetics of Single-Dose Administration of Naproxen at 10:00 and 22:00 Hours

Rao, B. Ramesh; Rambhau, D.; Rao, V. V. Sarveswar

doi:10.3109/07420529309059703

Cited by 14 publications

(6 citation statements)

References 10 publications

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“…Regarding the Anaprox® formulation, a bioavailability study by Haberer et al (Haberer et al, 2010) and a bioequivalence (BE) study by Setiawati et al(Setiawati et al, 2009) To investigate the bioavailability of naproxen free acid, Rao et al administered 500 mg of pure drug powder filled in hard capsules together with a glass of water to twelve Indian healthy male volunteers, aged between 18 and 22 years, who had fasted overnight. (Rao et al, 1993) In all studies, no concomitant administration of any other drugs was permitted for at least 1 week before the study and food was withheld until 3 hours post-dose.…”

Section: In Vivo Studiesmentioning

confidence: 99%

“…The performance of the developed PBPK model was verified by simulation of several clinical studies after oral administration and by comparison with the mean observed pharmacokinetic profiles already available in the literature. (Charles and Mogg, 1994;Haberer et al, 2010;Rao et al, 1993;Setiawati et al, 2009;Zhou et al, 1998) Virtual populations were selected to closely match the enrolled individuals in the respective in vivo clinical trials with respect to sample size, ethnicity, gender ratio, and age and weight range. Reported volumes of concomitant liquid intake, dosage form type and sampling schedule were also included in the study design.…”

Section: Verification Of Pbpk Model and Clinical Trial Simulationsmentioning

confidence: 99%

“…In vivo mean PK parameters (SD) tmax (h) Cmax (mg/L) AUC (mg/L•h) (Charles and Mogg, 1994) Naprosyn® 500 mg 1.50 a 71.4 a 1211 a (Zhou et al, 1998) Naprosyn® 2 x 250 mg 2.6 (1.5) 87.3 (15.5) 1428 (193) (Haberer et al, 2010) Anaprox® 550 mg 1.48 75.2 1294 (Setiawati et al, 2009) Anaprox® 550 mg 1.00 (0.5-2) 72.0 (11.2) 1013 (186) (Rao et al, 1993) IR Naproxen 500 mg 1.36 (0.81) 69.2 (20.9) 1435 312Haberer et al…”

Section: Reference Formulation and Dosementioning

confidence: 99%

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Establishing virtual bioequivalence and clinically relevant specifications using in vitro biorelevant dissolution testing and physiologically-based population pharmacokinetic modeling. case example: Naproxen

Loisios-Konstantinidis

Cristofoletti

Fotaki

et al. 2020

European Journal of Pharmaceutical Sciences

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Background: Physiologically-based population pharmacokinetic modeling (popPBPK) coupled with in vitro biopharmaceutics tools such as biorelevant dissolution testing can serve as a powerful tool to establish virtual bioequivalence and set clinically relevant specifications. One of several applications of popPBPK modeling is in the emerging field of virtual bioequivalence (VBE), where it can be used to streamline drug development by implementing model-informed formulation design and to inform regulatory decision-making e.g., with respect to evaluating the possibility of extending BCS-based biowaivers beyond BCS Class I and III compounds in certain cases. Methods: In this study, Naproxen, a BCS class II weak acid was chosen as the model compound. In vitro biorelevant solubility and dissolution experiments were performed and the resulting data were used as an input to the PBPK model, following a stepwise workflow for the confirmation of the biopharmaceutical parameters. The naproxen PBPK model was developed by implementing a middleout approach and verified against clinical data obtained from the literature. Once confidence in the performance of the model was achieved, several in vivo dissolution scenarios, based on model-based analysis of the in vitro data, were used to simulate clinical trials in healthy adults. Inter-occasion variability (IOV) was also added to critical physiological parameters and mechanistically propagated through the simulations. The various trials were simulated on a "worst/best case" dissolution scenario and average bioequivalence was assessed according to Cmax, AUC and tmax. Results: VBE results demonstrated that naproxen products with in vitro dissolution reaching 85% dissolved within 90 minutes would lie comfortably within the bioequivalence limits for Cmax and AUC. Based on the establishment of VBE, a dissolution "safe space" was designed and a clinically relevant specification for naproxen products was proposed. The interplay between formulation-related and drug-specific PK parameters (e.g., t1/2) to predict the in vivo performance was also investigated. Conclusion: Over a wide range of values, the in vitro dissolution rate is not critical for the clinical performance of naproxen products and therefore naproxen could be eligible for BCS-based biowaivers 3 based on in vitro dissolution under intestinal conditions. This approach may also be applicable to other poorly soluble acidic compounds with long half-lives, providing an opportunity to streamline drug development and regulatory decision-making without putting the patient at a risk.

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Section: In Vivo Studiesmentioning

confidence: 99%

Section: Verification Of Pbpk Model and Clinical Trial Simulationsmentioning

confidence: 99%

Section: Reference Formulation and Dosementioning

confidence: 99%

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Establishing virtual bioequivalence and clinically relevant specifications using in vitro biorelevant dissolution testing and physiologically-based population pharmacokinetic modeling. case example: Naproxen

Loisios-Konstantinidis

Cristofoletti

Fotaki

et al. 2020

European Journal of Pharmaceutical Sciences

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“…34 The proposed doses of febuxostat for the management of hyperuricemia in gout patients are 80 mg and 120 mg of febuxostat once daily. 15 Although assessment of the chronokinetics of indomethacin and naproxen 35 was not part of the study objectives, the pharmacokinetic data obtained from AM and PM dosing of indomethacin and naproxen provided additional information about the effect of the time of dosing on the pharmacokinetics of indomethacin and naproxen. The chronokinetic data for both indomethacin and naproxen indicate that even though PM dosing compared to AM dosing caused a delay in t max and a slight decrease in C max mean values, AUC 12 mean values were not affected and remained relatively unchanged for both indomethacin and naproxen.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic Interactions of Concomitant Administration of Febuxostat and NSAIDs

Khosravan¹,

Wu²,

Joseph‐Ridge³

et al. 2006

The Journal of Clinical Pharma

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To evaluate the effect of febuxostat on the pharmacokinetics of indomethacin and naproxen and vice versa, 2 multiple-dose, 3-period crossover studies were performed in healthy subjects. In study 1, subjects received febuxostat 80 mg once daily, indomethacin 50 mg twice daily, or both. In study 2, subjects received febuxostat 80 mg, naproxen 500 mg twice daily, or both. Twenty-four-hour blood samples were collected on day 5 in study 1 and day 7 in study 2. In study 1, 90% confidence intervals of geometric mean ratios for maximum plasma concentration (Cmax) and area under the curve (AUC) were within the 0.80 to 1.25 no-effect range for febuxostat and indomethacin. In study 2, 90% confidence intervals for febuxostat C(max) and AUC extended above that range, with increases of 28% and 40% in Cmax and AUC24, respectively. However, 90% confidence intervals for naproxen C(max) and AUC were within the 0.80 to 1.25 range. Febuxostat had no effect on the plasma pharmacokinetics of indomethacin and naproxen. Similarly, indomethacin had no effect on the plasma pharmacokinetics of febuxostat. Although naproxen caused an increase in plasma exposure to febuxostat, this increase is not expected to be clinically significant. Therefore, based on the plasma pharmacokinetic data in healthy subjects, febuxostat may be administered with indomethacin or naproxen with no dose adjustments for febuxostat, indomethacin, or naproxen.

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“…Ollagnier et al (1987) reported that the peak plasma concentration of ketoprofen was twice as high after drug administration at 07 00 h compared with administration at any other time, and t max was much longer after drug administration at 01 00 h compared with 13 00 h. Mustofa et al (1991) and Nagamahender et al (1995) found that the peak serum diclofenac concentration and the AUC value were signi®cantly lower during the night compared with the day. Rao et al (1993)…”

Section: Discussionmentioning

confidence: 99%

Chronopharmacokinetics of Sumatriptan in Healthy Human Subjects

Poondru

Devaraj

Boinpally

et al. 2000

Journal of Pharmacy and Pharmacology

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Rhythms in the onset and symptoms of several diseases are well established. Migraine is a disorder that exhibits periodicity in its symptoms and so chronotherapy may be beneficial in treating the problem. Designing a chronotherapeutic schedule requires chronopharmacokinetic and chronopharmacodynamic data of the drugs prescribed. We have studied the chronopharmacokinetics of sumatriptan, a drug of choice in migraine treatment. Twelve healthy male volunteers were treated with 100 mg sumatriptan orally at 0700, 1300, 1900 and 0100 h in a randomized 4 x 4 Latin square crossover design, with a wash-out period of one week. Serum samples were analysed by high performance liquid chromatography with an electrochemical detector. Pharmacokinetic parameters were calculated using noncompartmental methods. The pharmacokinetic parameters were analysed using analysis of variance and a two-tailed paired t-test at the probability of 95%. The mean peak serum concentration following the 0700 h administration (Cmax; 59.09 +/- 10.53 ng mL(-1)) was significantly (P < 0.05; n = 12) higher than after the 1900 h administration (Cmax 41.88 +/- 12.21 ngmL(-1)). The mean area under the serum concentration-time curve from time zero to the last time-point (AUCo-t), the area under the serum concentration-time curve from zero to infinity (AUC 0-infinity), and the area under the first moment curve (AUMC) were significantly (P < 0.05; n = 12) higher following the 0700 and 0100 h administrations than after the 1900 h administration. Following administration at 0700 h, the mean oral clearance (CLs/f; 781 +/- 186 mL h(- 1) kg(-1)) and the apparent volume of distribution (Vd/f; 2,379 +/- 684) were significantly lower (P < 0.05; n = 12) than after the 1900 h administration (CLs/f 1,208 +/- 458 mL h(-1) kg(-1), Vd/f 4,655 +/- 2,096 mL kg(-1)). The mean Vd/f value was again lower after the 1300h administration than after the 1900 h administration (2,763 +/- 1,417 vs 4,655 +/- 2,096 mL kg(-1); P < 0.05; n = 12). The variations may be due to the time dependent changes in the extent of absorption and/or circadian variations in hepatic blood flow.

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Pharmacokinetics of Single-Dose Administration of Naproxen at 10:00 and 22:00 Hours

Cited by 14 publications

References 10 publications

Establishing virtual bioequivalence and clinically relevant specifications using in vitro biorelevant dissolution testing and physiologically-based population pharmacokinetic modeling. case example: Naproxen

Establishing virtual bioequivalence and clinically relevant specifications using in vitro biorelevant dissolution testing and physiologically-based population pharmacokinetic modeling. case example: Naproxen

Pharmacokinetic Interactions of Concomitant Administration of Febuxostat and NSAIDs

Chronopharmacokinetics of Sumatriptan in Healthy Human Subjects

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