Medicaments contg. 5HT antagonists - formulated as anhydrous compsns. for dissolving in water, esp. for migraine treatment

摘要

Anhydrous non-effervescent pharmaceutical compsns. for dissolving in an aq. medium before oral admin. contain a 5HT1 receptor antagonist (I) as active ingredient and are free of Mg stearate. Pref. (I) is selected from 3-(2-dimethyl aminoethyl) -N-methyl-1H-indole 5-methanesulphonamide (Ia), N-methyl-3-(1-methyl -4-piperidinyl)-1H indole-5-ethanesulphonamide (Ib) and their salts and solvates, esp. (Ia) succinate. The compsns. comprises (by wt.) 10-45% (Ia) succinate, 40-80% lactose and 5-15% aspartame. They are in unit dose form and contain 1-200mg active ingredient. USE/ADVANTAGE - The comspsn. may be used to treat migraine and other vascular headaches. The compsns. have good stability and formulation properties and dissolve rapidly in water to give solns. with good bioavailability and a rapid action.