Bioequivalence of allopurinol and its metabolite oxipurinol in two tablet formulations

Frías, Jesús; Ruiz, Bibian Pérez; Soto, Altea; Carcas, Antonio J.; Govantes, Carlos; Montuenga, Carlos; Fernández, Ana Patricia

doi:10.1046/j.1365-2710.2001.00329.x

Cited by 12 publications

(11 citation statements)

References 16 publications

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“…Peak concentrations of 2.6 and 2.7 mg/mL were attained at 1.3 and 1.0 hours, respectively, after drug administration, then declined rapidly and were detectable up to 6 hours. The results of this study were in good agreement with the previously published PK data including peak level, elimination rate constant, and half-live 3,5,14,15 which emphasized the validity of the present results.…”

Section: Pharmacokinetic Characteristicssupporting

confidence: 92%

Pharmacokinetics and comparative bioavailability of allopurinol formulations in healthy subjects

Helmy

El-Bedaiwy

2014

Clinical Pharm in Drug Dev

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Allopurinol is the most commonly used urate-lowering therapy in gout. This study was undertaken to evaluate the pharmacokinetics and relative bioavailability of two brands of allopurinol tablets. The in vivo study was established according to a single-center, randomized, single-dose, laboratory-blinded, Two Way, Cross-Over Study with a washout period of 1 week. Under fasting conditions, 24 healthy male volunteers were randomly allocated to receive a single oral dose (200 mg) of either test and reference formulations. Plasma samples were obtained over a 6-hour interval and analyzed for allopurinol by reversed phase liquid chromatography with ultraviolet detection. The 90% confidence intervals for the ratio of log transformed values of Cmax , AUC0-t , and AUCt-∞ of the two treatments were within the acceptable range (0.8-1.25) for bioequivalence. From PK perspectives, the two allopurinol formulations were considered bioequivalent, based on the rate and extent of absorption. No adverse events occurred or were reported after a single 200-mg allopurinol and both formulations were well tolerated.

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Section: Pharmacokinetic Characteristicssupporting

confidence: 92%

Pharmacokinetics and comparative bioavailability of allopurinol formulations in healthy subjects

Helmy

El-Bedaiwy

2014

Clinical Pharm in Drug Dev

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“…Determination of plasma concentrations of oxypurinol highly differs depending on the population studied, the dose and the route of administration, the length of treatment and the time-points after drug intake chosen for measurements (Rodnan et al, 1975; Breithaupt and Tittel, 1982; Berlinger et al, 1985; Murrell and Rapeport, 1986; Emmerson et al, 1987; Day et al, 1988a,b; Graham et al, 1996; Turnheim et al, 1999; Guerra et al, 2001; Kaya et al, 2006; Panomvana et al, 2008; Stocker et al, 2008; Van Dijk et al, 2008; Torrance et al, 2009; Stamp et al, 2011). For instance, Van Dijk et al demonstrated that allopurinol reaches a mean maximal plasma concentration of 41.90 μg/ml within minutes after a dose of 15 mg/kg body weight administered i.v.…”

Section: Discussionmentioning

confidence: 99%

Allopurinol reduces antigen-specific and polyclonal activation of human T cells

Pérez‐Mazliah¹,

Albareda²,

Alvarez³

et al. 2012

Front. Immun.

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Allopurinol is the most popular commercially available xanthine oxidase inhibitor and it is widely used for treatment of symptomatic hyperuricaemia, or gout. Although, several anti-inflammatory actions of allopurinol have been demonstrated in vivo and in vitro, there have been few studies on the action of allopurinol on T cells. In the current study, we have assessed the effect of allopurinol on antigen-specific and mitogen-driven activation and cytokine production in human T cells. Allopurinol markedly decreased the frequency of IFN-γ and IL-2-producing T cells, either after polyclonal or antigen-specific stimulation with Herpes Simplex virus 1, Influenza (Flu) virus, tetanus toxoid and Trypanosoma cruzi-derived antigens. Allopurinol attenuated CD69 upregulation after CD3 and CD28 engagement and significantly reduced the levels of spontaneous and mitogen-induced intracellular reactive oxygen species in T cells. The diminished T cell activation and cytokine production in the presence of allopurinol support a direct action of allopurinol on human T cells, offering a potential pharmacological tool for the management of cell-mediated inflammatory diseases.

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“…Thorough literature survey reveals that few methods were reported for the estimation of AP and OP in human serum using HPLC, [4][5][6][7][8][9] CE, [10,11] electrochemical detection, [12][13][14] ion-exchange chromatography, [15,16] polarographic and voltammetric anodic detection, [17] and micellestabilized room-temperature phosphorescence in real samples. [18] However, these published methods have several limitations.…”

Section: Introductionmentioning

confidence: 99%

Validated Rp-Lc-MS/MS Method for the Simultaneous Determination of Allopurinol and Its Major Metabolite, Oxypurinol, in Human Plasma

Kasawar¹,

Razzak²,

Zaheer³

et al. 2010

Journal of Liquid Chromatography & Related Technologies

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A rapid and highly sensitive LC-MS=MS method was developed and validated for the determination of allopurinol (AP) and its major metabolite, oxypurinol (OP) in human plasma using lamivudine as an internal standard (IS). The analytes were extracted from human plasma by protein precipitation using acetonitrile. The chromatographic separation was employed on ''waters symmetry shield RP 8 , 150 mm Â 3.9 mm, 5 lm'' columns using a mixture of 0.01% formic acid in water and acetonitrile in the ratio of 95:05 (v=v) as the mobile phase. Mass spectrometer in the selected reaction-monitoring mode with negative electro spray was used for the detection and quantification of the analyte. Recovery study was performed showing the accuracy at upper and lower limits of quantification. The stability study was also carried out. The described method was found to be linear over a range of 0.01-10 lg mL À1 with a lower limit of quantification of 0.01 lg mL À1 for both AP and OP. The coefficient of variation for the assay precision was found <6.94, and the accuracy was found >96.03. The extraction recoveries for AP and OP were found to be in between 70 and 80%, the accuracy was found to be in between 95 and 106% in human plasma. The dilution integrity test, hemolysis and anticoagulant effect, and matrix effect studies were reported.

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Bioequivalence of allopurinol and its metabolite oxipurinol in two tablet formulations

Abstract: The two formulations are bioequivalent and therefore interchangeable.

Cited by 12 publications

References 16 publications

Pharmacokinetics and comparative bioavailability of allopurinol formulations in healthy subjects

Pharmacokinetics and comparative bioavailability of allopurinol formulations in healthy subjects

Allopurinol reduces antigen-specific and polyclonal activation of human T cells

Validated Rp-Lc-MS/MS Method for the Simultaneous Determination of Allopurinol and Its Major Metabolite, Oxypurinol, in Human Plasma

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