Development and Characterization of Taste-Masked Sublingual Tablet of Almotriptan Malate or Migraine

Abstract

The objective of the study was to develop fast disintegrating taste masked sublingual tablet of Almotriptan Malate to achieve rapid onset of action in management of migraine. Migraine is chronic neurobiological disease which is triggered by increase in excitability of the central nervous system. Almotriptan Malate is selective 5-HT receptor agonist. The conventional tablet shows slow onset of action about 1-2 hours, because poor absorption through gastric mucosa having systemic availability 69% to 70% due to metabolism of drug by MAO inhibitors present in GIT. Furthermore, oral delivery shows side effect which can be minimize by sublingual route by providing drug release into oral cavity to achieve direct systemic absorption. Drug have 469.55 molecular weight and 6.25 mg dose which make it appropriate for sublingual drug delivery. In this study various taste masking agents, disintegrating agents and diluents were explore.Taste masking of drug was achieved by Tulsion 339 which shows 93.55% drug loading in ratio of 1:4 in pH 7 at 6.5 hr. The result shows that Tulsion 339 was capable of releasing up to 91.54 % drug within 15 minutes in simulated saliva fluid 6.8 pH.fast disintegration of the tablet was achieved by Kyron T 314. 2% Kyron T 314 was capable to disintegrate tablet within 14 seconds. 40:60 ration of Mannitol and Avicel PH 102 shows good flow properties, compressibility and lesser disintegration time. The tablets were formulate by using direct compression and characterize by performing various precompression and postcompression tests.It was saw that disintegrating time and drug release profile of the tablet was majorly affected by the amount of diluents and disintegrating agents used. Optimized formula shown 89.62 % drug release in 5 minutes. The study shown that prepared sublingual tablet of Almotriptan Malate will increase onset of action was well as bioavailability of the drug by avoiding hepatic metabolism