CA2503201A1 — Modified release compositions of milnacipran

USPTO Abstract

A once-a-day oral milnacipran modified release formulation has been develope d. The formulation comprises an extended release dosage unit (Optionally containing the immediate release portion) coated with delayed release coatin g. The milnacipran composition, when administered orally, first passes through the stomach releasing from zero to less than 10% of the total milnacipran do se and then enters the intestines where drug is released slowly over an extende d period of time. The release profile is characterized by a 0.05-4 hours lag time period during which less than 10% of the total milnacipran dose is released followed by a slow or extended release of the remaining drug over a defined period of time. The composition provides in vivo drug plasma levels characterized by Tmax 4-10 hours and an approximately linear drop-off thereafter and Cmax below 3000 ng/ml, preferably below 2000 ng/ml, and most preferably below 1000 ng/ml. The composition allows milnacipran to be delivered over approximately 24 hours, when administered to a patient in nee d, resulting in diminished incidence or decreased intensity of common milnacipr an side effects such as sleep disturbance, nausea, vomiting, headache, tremulousness, anxiety, panic attacks, palpitations, urinary retention, orthostatic hypotension, diaphoresis, chest pain, rash, weight gain, back pain, constipation, vertigo, increased sweating, agitation, hot flushes, tremors, fatigue, somnolence, dyspepsia, dysoria, nervousness, dry mouth, abdominal pain, irritability, and insomnia.