US2021322429A1PendingUtilityA1

Stabilized formulations of cns compounds

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Assignee: SUPERNUS PHARMACEUTICALS INCPriority: Mar 31, 2010Filed: Jun 25, 2021Published: Oct 21, 2021
Est. expiryMar 31, 2030(~3.7 yrs left)· nominal 20-yr term from priority
Inventors:Rong-Kun ChangMichael L. VieiraLikan LiangPadmanabh P. BhattAustin B. HuangSachin V. Patel
A61K 9/2072A61P 25/00A61K 9/1623A61K 9/4866A61K 9/2018A61K 9/2027A61K 9/0004A61K 9/2054A61K 9/2866A61K 9/2886A61K 31/5377A61K 9/4858A61K 9/209A61K 9/16A61K 9/1635A61P 25/20A61K 9/4808A61P 25/18
72
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Claims

Abstract

Formulations of molindone having superior stability and methods of administering same are provided. The formulations may be immediate, modified, or otherwise delayed release formulations of molindone.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A method of treating a central nervous system (CNS) disorder comprising administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical formulation comprising molindone, wherein said formulation provides a linear increase of a plasma concentration of molindone in the subject with an administered dose of molindone. 
     
     
         2 . The method of  claim 1 , wherein the pharmaceutical formulation is an extended release formulation. 
     
     
         3 . The method of  claim 1 , wherein the said formulation provides a linear increase of the plasma concentration of molindone in the subject with the administered dose of molindone, which is from 3 mg to 36 mg of molindone. 
     
     
         4 . The method of  claim 2 , wherein said extended release formulation is a tablet. 
     
     
         5 . The method of  claim 2 , wherein said administering provides a therapeutically effective blood concentration of molindone in the subject for 6 to 24 hours after the administering. 
     
     
         6 . The method of  claim 2  wherein said administering provides a therapeutically effective blood concentration of molindone in the subject for 8 to 24 hours after the administering. 
     
     
         7 . The method of  claim 1 , wherein the CNS disorder comprises at least one of impulsive aggression, aggression and other conduct disorder. 
     
     
         8 . The method of  claim 1 , wherein molindone is a single active pharmaceutical ingredient in the pharmaceutical formulation and wherein the pharmaceutical formulation comprises
 (a) a modified-release formulation comprising a matrix of a homogeneous admixture of:   (i) molindone,   (ii) at least one release controlling polymer, wherein the release controlling polymer consists of one or more non-pH-dependent polymers selected from the group consisting of hydroxypropyl cellulose, hypromellose (hydroxypropyl methyl cellulose), methyl cellulose, polyethylene oxide, acacia, carbomer homopolymer type A NF; carbomer homopolymer type B NF, hydroxyethyl cellulose, carrageenan, tragacanth, xanthan gum, povidone, alginic acid and salts thereof, polyvinyl alcohol, carboxymethylcellulose; ethylcellulose, cellulose acetate, cellulose acetate butyrate, poly(ethyl acrylate-co-methyl methacrylate) ethyl acrylate methyl methacrylate copolymer, poly (ethyl acrylate-co-methyl methacrylate-cotrimethylammonioethyl methacrylate chloride), polyvinyl acetate, and cellulose acetate propionate, and   (iii) at least one stabilizer selected from the group consisting of acidifying agents and hydrophobizing agents;   wherein the total amount of water content in the formulation is not more than 5% by weight of the formulation.   
     
     
         9 . The method of  claim 8 , wherein the modified release formulation is an extended release formulation. 
     
     
         10 . The method of  claim 1 , wherein said administering is performed once a day. 
     
     
         11 . The method of  claim 1 , wherein said administering is performed twice a day. 
     
     
         12 . The method of  claim 9 , comprising an extended release component comprising from 5% to 95% by weight of the formulation of a non-pH-dependent polymer. 
     
     
         13 . The method of  claim 8 , wherein the pharmaceutical formulation further comprises an additional formulation comprising molindone, which is an immediate release, an extended release or a delayed release formulation. 
     
     
         14 . The method of  claim 12 , wherein the additional formulation is an immediate release formulation. 
     
     
         15 . The method of  claim 8 , wherein the pharmaceutical formulation is an osmotic formulation. 
     
     
         16 . The method of  claim 8 , wherein the pharmaceutical formulation comprises an acidifying agent as the stabilizer. 
     
     
         17 . The method of  claim 16 , wherein the acidifying agent is selected from the group consisting of fumaric acid, citric acid, malic acid, tartaric acid, ascorbic acid, edetic acid, aspartic acid, adipic acid, alginic acid, benzoic acid, butanedioic acid, erythorbic acid, lactic acid, malic acid, maleic acid, glutamic acid, sorbic acid, succinic acid, hydrochloric acid (dilute) nitric acid (dilute), phosphoric acid (dilute), sulfuric acid (dilute), acacia, aluminum phosphate, aluminum sulfate, ammonium alum, ammonium chloride, carbomers, edetate calcium disodium, edetate disodium, methacrylic acid copolymers, poly(methyl acrylate-co-methyl methacrylate-co-methacrylic acid), polycarbophils, polydextrose, potassium alum, potassium phosphate monobasic, sodium metabisulfite, sodium phosphate monobasic, sodium starch glycolate, zinc acetate, zinc sulfate and pharmaceutical grade ion exchange resins. 
     
     
         18 . The method of  claim 8 , wherein the pharmaceutical formulation comprises a hydrophobizing agent. 
     
     
         19 . The method of  claim 18 , wherein the hydrophobizing agent is selected from the group consisting of magnesium stearate, stearic acid, glyceryl behenate, and glyceryl stearate, glyceryl palm itostearate, waxes and hydrogenated vegetable oils. 
     
     
         20 . The method of  claim 8 , wherein the pharmaceutical formulation further comprises a pharmaceutically acceptable excipient selected from the group consisting of bulking agents, fillers, lubricants, wetting and solubility enhancing agents and dispersants. 
     
     
         21 . The method of  claim 1 , wherein molindone is a racemic mixture of (+)-enantiomer and (−)-enantiomer. 
     
     
         22 . The method of  claim 1 , wherein molindone is in the form of (+)-enantiomer. 
     
     
         23 . The method of  claim 1  wherein molindone is in the form of (−)-enantiomer. 
     
     
         24 . The method of  claim 8 , wherein the pharmaceutical formulation comprises the stabilizer and molindone, respectively, in a weight ratio of 0.1:1 to 50:1. 
     
     
         25 . The method of  claim 8 , wherein the pharmaceutical formulation comprises the stabilizer and molindone, respectively, in a weight ratio of 0.25:1 to 40:1. 
     
     
         26 . The method of  claim 1 , wherein the pharmaceutical formulation is in a dosage form selected from tablets, osmotic tablets, matrix tablets, mini tablets, capsules, beads, granules, powders, caplets, troches, sachets, cachets, pouches, gums and sprinkles. 
     
     
         27 . The method of  claim 1 , wherein the subject is a human being.

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