Progress in pharmaceutical development presentation with improved pharmacokinetics: a new formulation for valproate

Abstract

Successful long-term treatment of patients with epilepsy requires selection of an appropriate antiepileptic regimen, optimal dosing and patient compliance. Recent advances in our understanding of the biological basis of epilepsy and in the choice of treatment options are transforming the global management of these patients. If the achievement of seizure freedom remains the primary goal of any antiepileptic treatment, issues associated with drug acceptability and tolerability, and with quality of life of patients, have gained increasing attention as major determinants of ultimate therapeutic success. Sustained-release formulations of antiepileptic drugs can be very helpful in achieving treatment objectives. Stable serum levels without marked peak-to-trough fluctuations, reduced frequency of dosing and the possibility of dosing flexibility may all improve compliance, patient satisfaction and ultimately quality of life. The efficacy of sodium valproate for the treatment of most types of epilepsy has been demonstrated extensively and this drug remains the mainstay of treatment for many clinical situations. Among the various valproate formulations, extended-release tablets have shown improved patient compliance and satisfaction. However, the tablet size and the limited dosing flexibility could be unsuitable for individualized treatment in special populations such as children, the elderly and patients with swallowing difficulties. A new sustained-release formulation of sodium valproate consisting of tasteless microspheres that can be sprinkled on semi-solid food such as yoghurt or jam has been developed. A stick pack presentation allows individualized dosing and greater convenience.