44 results about "Milnacipran" patented technology

A once-a-day oral milnacipran pulsatile release composition has been developed that releases the drug in spaced apart “pulses”. The dosage forms are comprised of first, second and optional third dosage units, with each dosage unit having a different drug release profile. This dosage form provides in vivo drug plasma levels characterized by C_max below 3000 ng/ml, preferably below 2000 ng/ml, and most preferably below 1000 ng/ml. The composition provides pulsatile release of milnacipran to produce a therapeutic effect 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 attention deficit/hyperactivity disorder (AD/HD) and associated tic disorders in an animal subject comprising administering an effective amount of an anti-AD/HD compound or a pharmaceutically acceptable salt thereof. The anti-AD/HD compound useful in the present invention is characterized by ant-AD/HD and anti-tic properties and exhibits at least two distinct pharmacological activities. In particular, the use of milnacipran to treat AD/HD and comorbid tic and psychiatric disorders is disclosed.

Discolsed herein are compositions and methods for treatment of genitourinary disorders (e.g., urge incontinence). The compositions may generally include a dual-acting SNRI-NMDA antagonist (e.g., bicifadine and/or milnacipran). Alternatively, the compositions may generally include an SNRI and an NMDA antagonist.

Methods for the prevention or treatment of stress-related disorders by administering a therapeutically effective amount of a dual serotonin/norepinephrine reuptake inhibitor to an individual under stress are described. A triple monoamine reuptake inhibitor for serotonin/noradrenaline/dopamine may also be administered to an individual at risk for a stress-related disorder. In a preferred embodiment the compound is milnacipran and is prophylactically administered at an effective amount to delay or prevent stress-related disorders in an individual at risk.

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 T_max of 4-10 hours.

Methods for treating fatigue associated with fibromyalgia by administering high-dose milnacipran to a patient suffering from such fatigue are provided. Also provided are methods for the long-term treatment of fatigue associated with FMS by administering milnacipran to a patient suffering from such fatigue.

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 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.

The present invention relates to the method for synthesizing the pharmaceutically acceptable acid addition salt of (1S,2R)-milnacipran, it comprises following successive steps: (a) phenylacetonitrile and (R)-epichlorohydrin Reaction under the condition that alkali exists, after alkali treatment, acid treatment, obtain lactone; (b) under the condition that Lewis acid-amine complex exists, this lactone and MNEt2 (M represents alkali metal) or NHEt2 reaction, obtain Amide alcohol; (c) the amide alcohol reacts with thionyl chloride to obtain amide chloride; (d) the chloride amide reacts with phthalimide salt to obtain phthalimide derivatives; (e) hydrolyzing the phthalimide group of the phthalimide derivative to obtain (1S, 2R)-milnacipran; (f) in the presence of a pharmaceutically acceptable acid (1S,2R)-milnacipran is salted in a suitable solvent system under the same conditions.

Methods for treating cognitive dysfunction associated with fibromyalgia by administering high-dose milnacipran to a patient suffering from such cognitive dysfunction are provided. Also provided are methods for the long-term treatment of cognitive dysfunction associate with FMS by administering milnacipran to a patient suffering from such cognitive dysfunction.

The invention provides a Milnacipran composition transferred through noses and brains, which contains a Milnacipran original drug or a pharmaceutically acceptable salt thereof and pharmaceutically necessary auxiliary materials. The composition transferred through the noses and the brains can target to a brain tissue, quickly take effect, reduce adverse reaction of the whole body, and is convenient to use.

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.

The invention relates to a slow-release composition containing L-milnacipran and a preparation method thereof. The composition contains the L-milnacipran serving as an active ingredient or pharmaceutically acceptable salt thereof. The composition is characterized by also comprising high-viscosity hydroxypropyl methylcellulose serving as a hydrophilic gel slow-release skeleton material and acrylic resin serving as a pH adjustor, wherein the composition comprises the following components in parts by weight: 10 to 70 parts of L-milnacipran or pharmaceutically acceptable salt, 5 to 30 parts of hydroxypropyl methylcellulose, and 3.5 to 7.5 parts of acrylic resin; and during preparation, the L-milnacipran, the hydroxypropyl methylcellulose and the acrylic resin are bound to be mixed uniformly. The composition can realize consistency of release behaviors in artificial gastric juice and artificial intestinal juice and keep 12-hour continuous release effect, and is low in preparation loss, high in efficiency, high in stability, easy to operate and easy to popularize.

The present invention develops methods for treating or preventing depression secondary to atypical pain (DSP). The methods generally comprise administering an effective amount of a monoamine reuptake inhibitor to treat or prevent the symptoms of DSP. In a preferred embodiment, a therapeutically effective dose of a specific type of dual serotonin norepinephrine reuptake inhibitor (SRNI) compound or a pharmaceutically acceptable salt thereof is administered. Most preferably the SNRI compounds are non-tricyclic SNRIs, wherein the serotonin reuptake inhibition is stronger than norepinephrine reuptake inhibition; NSRIs, wherein the norepinephrine reuptake inhibition is stronger than serotonin reuptake inhibition inhibition. The most preferred compound is milnacipran or a bioequivalent or pharmaceutically acceptable salt thereof. Other preferred compounds are duloxetine, venlafaxine or bioequivalent or pharmaceutically acceptable salts thereof. In another embodiment, a therapeutically effective amount of a particular type of non-tricyclic triple reuptake inhibitor ("TRI") compound, or a pharmaceutically acceptable salt thereof, is administered. TRI compounds are characterized by blocking the reuptake (and thus increasing central concentrations) of three major brain monoamines: serotonin, norepinephrine and dopamine.

The invention provides a levomilnacipran hydrochloride sustained release capsule. The sustained release capsule is prepared from a levomilnacipran hydrochloride drug application pill core and a sustained release coating, wherein the weight ratio of the sustained release coating to the levomilnacipran hydrochloride drug application pill core is at (15-35) to (65-85). According to the method disclosed by the invention, a mixed coating liquid of a pH non-dependent material and a pH dependent material is coated on the core material of levomilnacipran hydrochloride. A pH value in a human body from stomach to small intestine is gradually increased to about 7 from 1.2, and the pH dependent material in a coating membrane provided by the invention is gradually dissolved in the intestine which is higher than 5 in pH value, so that small pores are formed in the membrane; therefore, the permeability of the coating membrane in the intestines is enhanced, and subsequently, the purpose of improving release of drugs in the intestine is achieved. The preparation method disclosed by the invention is simple and convenient, applicable to industrial production and is relatively high in practical value.