46 results about "Milnacipran" patented technology

A once-a-day oral milnacipran modified release formulation has been developed. The formulation comprises an extended release dosage unit (optionally containing the immediate release portion) coated with delayed release coating. The milnacipran composition, when administered orally, first passes through the stomach releasing from zero to less than 10% of the total milnacipran dose and then enters the intestines where drug is released slowly over an extended 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 at 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 need, resulting in diminished incidence or decreased intensity of common milnacipran 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.

The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject comprising administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and a greater inhibition of norepinephrine reuptake than serotonin reuptake, and wherein said compound is not administered adjunctively with phenylalanine or tyrosine. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Methods for treating chronic widespread pain associated with drug therapy or radiation therapy are described. The method generally involves administering a therapeutically effective amount of a dual or tri reuptake inhibitor of a specific type or a pharmaceutically acceptable salt thereof. Preferably the compound is a non-tricyclic dual reuptake inhibitor. The most preferred compound is milnacipran or a bioequivalent or pharmaceutically acceptable salt thereof. Other preferred compounds are duloxetine and venlafaxine or a bioequivalent or pharmaceutically acceptable salt thereof. In yet another embodiment, a therapeutically effective amount of a non-tricyclic triple reuptake inhibitor (“TRI”) compound of a specific type, or a pharmaceutically acceptable salt thereof, is administered. The TRI compounds are characterized by their ability to block the reuptake (and, hence, increase central concentrations of) the three primary brain monoamines: serotonin, noradrenaline, and dopamine.

The present invention is directed to methods for providing long-term treatment of fibromyalgia syndrome (FMS) by administering a dual re-uptake inhibitor to a patient with FMS. More particularly, the present invention is directed to the long-term treatment of FMS by administering a norepinephrine-serotonin reuptake inhibitor (NSRI) to a patient with FMS.

A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tmax of 4-10 hours.

It is intended to provide a milnacipran formulation which is more stable than a conventionally known milnacipran formulation, and a method of stabilizing a milnacipran formulation. The object could be achieved by using a milnacipran-containing composition in which milnacipran or a salt thereof is allowed to exist in a porous carrier, packing a powder containing milnacipran or a salt thereof in an HPMC capsule, or combining an additive which does not cause an interaction with milnacipran with time.

One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

Methods for improving physical function in fibromyalgia syndrome by administering an NSRI such as milnacipran as disclosed.

The present invention discloses a process for preparing optically pure milnacipran and their pharmaceutically acceptable salts, which adopts racemic milnacipran as starting material, tartaric acid derivatives and their compositions as resolving agents to resolve.

The invention discloses a method for preparing optical pure milnacipran and medicinally acceptable salt, which adopts racemic milnacipran as raw material, tartaric acid derivative and composition as resolution agent to resolve.

A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tmax of 4-10 hours.

The present invention discloses a process for preparing optically pure milnacipran and their pharmaceutically acceptable salts, which adopts racemic milnacipran as starting material, tartaric acid derivatives and their compositions as resolving agents to resolve.

The present invention relates to an improved process for the preparation of pharmaceutically acceptable salts of milnacipran by mutual acid radical exchange.

The pharmaceutical composition of the present invention comprises (1) a carbostyril derivative and (2) a serotonin reuptake inhibitor in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof, which is a dopamine-serotonin system stabilizer. The serotonin reuptake inhibitor may be fluoxetine, duloxetine, venlafaxine, milnacipran, citalopram, fluvoxamine, paroxetine, sertraline or escitalopram. The pharmaceutical composition of the present invention is useful for treating patients with mood disorders, particularly depression or major depressive disorder.