GB2624861A — Sustained release pharmaceutical compositions comprising pregabalin or pharmaceutically acceptable salts thereof

USPTO Abstract

A sustained release film-coated tablet for once-daily dosing, comprising 20-80 %w/w pregabalin or pharmaceutically acceptable salt thereof, at least two release retarding agents, film coating material and one or more pharmaceutically acceptable excipients. Preferably, the release retarding agent is hydroxy ethyl cellulose, a carbomer, or a combination of polyvinyl acetate, povidone, sodium lauryl sulfate and silica. The pharmaceutically acceptable excipients may be diluents and/or lubricants, a preferred diluent is mannitol and a preferred lubricant is magnesium stearate. The film coating material may be selected from vinyl polymers such as polyvinyl pyrrolidone, polyvinyl alcohol, polyvinyl acetate; cellulosics; acrylates and methacrylates; and natural gums and resins. A process of preparing the pregabalin once-daily dosage is also disclosed comprising sieving the ingredients, blending all but the magnesium stearate lubricant, adding the magnesium stearate lubricant and blending, then compressing into a tablet and coating the tablet. The tablet exhibits a drug dissolution profile wherein 10-30 % of the total amount of pregabalin is released at 1 hour and not less than 85 % of the total amount of pregabalin is released at 24 hours. The tablet is for use in treating/preventing neuropathic pain, epilepsy, fibromyalgia, diabetic peripheral neuropathy, postherpetic neuralgia or generalized anxiety disorder.