Controlled release of di:hydro-Ergotamine methane sulphonate - from micro-granules coated with anionic and cationic methacrylic! polymers and a plasticiser

摘要

Microgranules for oral administration to man or animals liberate dihydroergotamine methane sulphonate (I) in a controlled manner, independently of the pH. The microgranules have a spherical inert support, (I) fixed on the support, and a coating which is a mixt. of two methacrylic acid polymers, one cationic and one anionic, and a plasticiser. The inert support is spherical and has a diameter of 800 to 1000 microns. It is made from talc, sucrose, maizestarch, and polyvinyl pyrrolidone. Usually 0.0139 to 0.0147 mg. of (I) is fixed to this support. The coating film, which is 1 to 2% of the mass of the uncoated material, comprises 70 to 80 percent anionic methacrylic acid polymer, 30 to 20% cationic methacrylic acid polymer, and 1 to 2% ethyl phthalate. Used for treatment of migraines, orthostatic syndrome, chronic venous insufficiency, neurovegetative disorders, atonic constipation, dysmenorrhoea, and catamenial migraine.