Comparative pharmacokinetic study of a single dose of two prolonged-release formulations of diclofenac in healthy subjects

Biasi, Giovanni; Canova, Nadia; Palazzini, Emesto; Marcolongo, Roberto

doi:10.1016/s0011-393x(98)85104-7

Cited by 4 publications

(3 citation statements)

References 4 publications

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“…In Fig. 5a are presented the AUC 0-∞ versus dose data for diclofenac (29)(30)(31)(32)(33)(34). It is obvious that there is AUC 0-∞ -dose proportionality for the first segment of the plot after oral administration of diclofenac (dose range from 12.5 up to 100 mg).…”

Section: Applicationsmentioning

confidence: 99%

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Elucidating the Role of Dose in the Biopharmaceutics Classification of Drugs: The Concepts of Critical Dose, Effective In Vivo Solubility, and Dose-Dependent BCS

et al. 2012

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Section: Applicationsmentioning

confidence: 99%

“…Plots of (a) diclofenac and (b) ketoprofen (S enantiomer) presenting AUC vs dose data after oral (•) and iv (∇) administration (data taken from refs(29)(30)(31)(32)(33)(34)(35)(36)(37).…”

mentioning

confidence: 99%

Elucidating the Role of Dose in the Biopharmaceutics Classification of Drugs: The Concepts of Critical Dose, Effective In Vivo Solubility, and Dose-Dependent BCS

et al. 2012

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“…Several methods have been used for assay of DS in plasma, among which high-performance liquid chromatography (HPLC) is commonly adopted (Yong et al, 2005;El-Samaligy et al, 2004;Su et al, 2003;Biasi et al, 1998;Hosny et al, 1997;Hosny, 1996). The time taken for a single sample in an HPLC system is many times longer than that in UPLC-MS/MS.…”

Section: Introductionmentioning

confidence: 99%

A new rapid ultra‐performance liquid chromatography method for the pharmacokinetic and bioavailability study of diclofenac sodium aqueous injection and lipid microsphere injection in rats

Cui

Xia

Guan

et al. 2009

Biomedical Chromatography

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A novel, rapid and selective ultra performance liquid chromatography mass spectrometric method had been developed for the pharmacokinetic study of diclofenac sodium (DS) after single intravenous injection of DS aqueous injection and DS lipid microsphere (LM) injection in rats. Ketoprofen (KP) was used as internal standard. Samples were treated by a one-step liquid liquid extraction. Separation was performed on an Acquity UPLC BEH C(18) column (50 x 2.1 mm i.d., 1.7 mum). The mobile phase consisted of acetonitrile-0.1% ammonium hydroxide aqueous solution (20 : 80, v/v) initially in the gradient mode. The detection was carried out by means of electrospray ionization mass spectrometry in negative ion mode with multiple-reaction monitoring mode. Standard curves showed good linearity (r > 0.99) from the plasma concentration of 0.1-50 microg/mL. The lower limit of quantification was 0.1 microg/mL. The intra- and inter-day precisions and the accuracy all satisfied the acceptance criteria. The developed method was validated and successfully applied to the pharmacokinetics study of DS aqueous injection and LM injection. The results showed that the two preparations were bioequivalent in rats.

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Comparative in vitro dissolution and in vivo bioequivalence of two diclofenac enteric coated formulations

Basmenji¹,

Valizadeh

Zakeri–Milani

2012

Arzneimittelforschung

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The aim of this study was the comparison of in vitro dissolution and in vivo bioavailability of two different brands of diclofenac sodium (CAS 15307-86-5) enteric coated tablets in healthy male Iranian volunteers in a single-dose, randomized, open-label, single blind study, which was conducted according to a crossover design in healthy volunteers. A washout interval of two weeks was selected between administrations to each subject in this study. Serial venous blood samples over 10 h after each administration to measure diclofenac sodium concentration in serum were obtained, and placed into tubes containing sodium heparin. Then the plasma was separated and kept frozen at -20 degrees C for subsequent analysis with a modified HPLC method with UV detection. In addition, the in vitro dissolution study was performed on the brands. For the test and reference formulation, mean Cmax values were 2257.3 (ng/ml) and 2156 (ng/ml), respectively. The mean AUC(0)tau and AUC(0)infinity were 5726.1 (ng x h/ml) and 5917.8 (ng x h/ml) for the test and 5689.9 (ng x h/ml) and 5967.4 (ng x h/ml) for the reference formulation, respectively. Results show that the 90% confidence intervals for the ratio of test and reference products in Cmax (101.4-114.9%), AUC(0)tau (96.3-109.1%) and AUC(0)infinity (94.7-107.3%) were all within the 80-125% interval proposed by the FDA and EMA. Both formulations released > 80% of drug within 30 min in buffer pH = 6.8 medium. Therefore the diclofenac sodium enteric coated tablets of the test and reference formulations are bioequivalent in terms of rate and extent of absorption.

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Comparative pharmacokinetic study of a single dose of two prolonged-release formulations of diclofenac in healthy subjects

Cited by 4 publications

References 4 publications

Elucidating the Role of Dose in the Biopharmaceutics Classification of Drugs: The Concepts of Critical Dose, Effective In Vivo Solubility, and Dose-Dependent BCS

Elucidating the Role of Dose in the Biopharmaceutics Classification of Drugs: The Concepts of Critical Dose, Effective In Vivo Solubility, and Dose-Dependent BCS

A new rapid ultra‐performance liquid chromatography method for the pharmacokinetic and bioavailability study of diclofenac sodium aqueous injection and lipid microsphere injection in rats

Comparative in vitro dissolution and in vivo bioequivalence of two diclofenac enteric coated formulations

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