Design and development of formulations of zolmitriptan for the treatment of migraine

Abstract

Orally disintegrating tablets (ODTs) are getting popularity over conventional tablets due to newlinetheir convenience in administration and suitability for patients having dysphagia. There is newlinean increasing demand for more patient compliant dosage form and a novel method is the newlinedevelopment orally disintegrating tablets which dissolve or disintegrates instantly on the newlinepatient tongue or buccal mucosa. It is suited for tablets undergoing high first pass newlinemetabolism and is used for improving bioavailability with reducing dosing frequency to newlineminimize side effect and make it more cost effective. The Zolmitriptan is a serotonin (5- newlineHT1) agonist used for the treatment of migraine with or without aura. The half-life of newlineZolmitriptan is 2.5 to 3 hrs and it undergoes hepatic metabolism, the absolute oral newlinebioavailability is about 40 to 50%. Hence the main objective of the study was to formulate newlineoral disintegrating tablets of Zolmitriptan to achieve a better dissolution rate and further newlineimproving the bioavailability of the drug. Orally disintegrating tablets prepared by direct newlinecompression and using Spray Dried Lactose, Avicel pH 102, Crospovidone XL-10, newlineCroscarmellose Sodium, Sodium Starch Glycolate, Aspartame, Peppermint, Magnesium newlineStearate were prepared and evaluated for the preformulation parameters such as newlineOrganoleptic properties, bulk density, Tapped density, compressibility, Hausner s Ratio, newlineangle of repose, Drug-Excipients compatibility study etc. The prepared batches of tablets newlinewere evaluated for Physical appearance, Thickness, hardness, weight variation, friability, newlinedisintegration time and in-vitro dissolution profile was found satisfactory. To achieve our newlinegoal, nine formulations of ODTs were prepared and optimized. Optimized formulation newlineshowed minimum disintegration time and maximum dissolution rate with drug release. newline