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Levetiracetam: relative bioavailability and bioequivalence of a 10% oral solution (750 mg) and 750-mg tablets.
J Clin Pharmacol. 2003 Dec; 43(12):1370-6.JC

Abstract

Levetiracetam, an antiepileptic drug, is used worldwide as an adjunctive treatment for partial-onset seizures. The availability of a new oral solution formulation would provide an additional treatment option for patients who have difficulty swallowing tablets. A phase I single-center, randomized, open-label, two-way crossover, single-dose study was conducted to confirm that a 10% oral solution of levetiracetam was bioequivalent to the 750-mg oral tablet and to characterize its pharmacokinetics. Each of 24 healthy subjects received a single oral 750-mg dose of the randomized levetiracetam formulation (7.5 mL of 10% solution or 750-mg tablet) on day 1 and a single oral dose of the alternate formulation on day 8. Serial blood samples were collected from 0 to 36 hours after each dose administration for determination of plasma levetiracetam concentrations. Pharmacokinetic parameters were calculated, and bioequivalence of the two formulations was evaluated. The mean levetiracetam plasma concentration-time curves and pharmacokinetic parameters essentially were identical for the oral 10% solution and tablet and consistent with previously reported levetiracetam pharmacokinetics. The 90% confidence limits of the geometric mean ratio of the two formulations for area under the plasma concentration-time curve from time 0 to infinity, area under the plasma concentration-time curve from time 0 to last measurable time point, and maximum plasma concentration were within the 80% to 125% range, demonstrating bioequivalence of the two formulations. Both levetiracetam formulations were well tolerated. The levetiracetam 10% oral solution is a bioequivalent, well-tolerated alternative to the tablet formulation in patients who have difficulty swallowing.

Authors+Show Affiliations

UCB S.A. Parma Sector, Chemin do Foriest, Braine l'Alleud, Belgium.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Journal Article
Randomized Controlled Trial

Language

eng

PubMed ID

14615473

Citation

Coupez, René, et al. "Levetiracetam: Relative Bioavailability and Bioequivalence of a 10% Oral Solution (750 Mg) and 750-mg Tablets." Journal of Clinical Pharmacology, vol. 43, no. 12, 2003, pp. 1370-6.
Coupez R, Straetemans R, Sehgal G, et al. Levetiracetam: relative bioavailability and bioequivalence of a 10% oral solution (750 mg) and 750-mg tablets. J Clin Pharmacol. 2003;43(12):1370-6.
Coupez, R., Straetemans, R., Sehgal, G., Stockis, A., & Lu, Z. S. (2003). Levetiracetam: relative bioavailability and bioequivalence of a 10% oral solution (750 mg) and 750-mg tablets. Journal of Clinical Pharmacology, 43(12), 1370-6.
Coupez R, et al. Levetiracetam: Relative Bioavailability and Bioequivalence of a 10% Oral Solution (750 Mg) and 750-mg Tablets. J Clin Pharmacol. 2003;43(12):1370-6. PubMed PMID: 14615473.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Levetiracetam: relative bioavailability and bioequivalence of a 10% oral solution (750 mg) and 750-mg tablets. AU - Coupez,René, AU - Straetemans,Roel, AU - Sehgal,Geeta, AU - Stockis,Armel, AU - Lu,Zhihong Sarah, PY - 2003/11/15/pubmed PY - 2004/4/13/medline PY - 2003/11/15/entrez SP - 1370 EP - 6 JF - Journal of clinical pharmacology JO - J Clin Pharmacol VL - 43 IS - 12 N2 - Levetiracetam, an antiepileptic drug, is used worldwide as an adjunctive treatment for partial-onset seizures. The availability of a new oral solution formulation would provide an additional treatment option for patients who have difficulty swallowing tablets. A phase I single-center, randomized, open-label, two-way crossover, single-dose study was conducted to confirm that a 10% oral solution of levetiracetam was bioequivalent to the 750-mg oral tablet and to characterize its pharmacokinetics. Each of 24 healthy subjects received a single oral 750-mg dose of the randomized levetiracetam formulation (7.5 mL of 10% solution or 750-mg tablet) on day 1 and a single oral dose of the alternate formulation on day 8. Serial blood samples were collected from 0 to 36 hours after each dose administration for determination of plasma levetiracetam concentrations. Pharmacokinetic parameters were calculated, and bioequivalence of the two formulations was evaluated. The mean levetiracetam plasma concentration-time curves and pharmacokinetic parameters essentially were identical for the oral 10% solution and tablet and consistent with previously reported levetiracetam pharmacokinetics. The 90% confidence limits of the geometric mean ratio of the two formulations for area under the plasma concentration-time curve from time 0 to infinity, area under the plasma concentration-time curve from time 0 to last measurable time point, and maximum plasma concentration were within the 80% to 125% range, demonstrating bioequivalence of the two formulations. Both levetiracetam formulations were well tolerated. The levetiracetam 10% oral solution is a bioequivalent, well-tolerated alternative to the tablet formulation in patients who have difficulty swallowing. SN - 0091-2700 UR - https://www.unboundmedicine.com/medline/citation/14615473/Levetiracetam:_relative_bioavailability_and_bioequivalence_of_a_10_oral_solution__750_mg__and_750_mg_tablets_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0091-2700&date=2003&volume=43&issue=12&spage=1370 DB - PRIME DP - Unbound Medicine ER -