HRP20240303T1 - Osmotski oblici doziranja koji sadrže deutetrabenazin i postupci njihove upotrebe - Google Patents
Osmotski oblici doziranja koji sadrže deutetrabenazin i postupci njihove upotrebe Download PDFInfo
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- HRP20240303T1 HRP20240303T1 HRP20240303TT HRP20240303T HRP20240303T1 HR P20240303 T1 HRP20240303 T1 HR P20240303T1 HR P20240303T T HRP20240303T T HR P20240303TT HR P20240303 T HRP20240303 T HR P20240303T HR P20240303 T1 HRP20240303 T1 HR P20240303T1
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- deutetrabenazine
- microparticles
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- 239000002552 dosage form Substances 0.000 title claims 36
- MKJIEFSOBYUXJB-VFJJUKLQSA-N (3r,11br)-3-(2-methylpropyl)-9,10-bis(trideuteriomethoxy)-1,3,4,6,7,11b-hexahydrobenzo[a]quinolizin-2-one Chemical compound C1CN2C[C@@H](CC(C)C)C(=O)C[C@@H]2C2=C1C=C(OC([2H])([2H])[2H])C(OC([2H])([2H])[2H])=C2 MKJIEFSOBYUXJB-VFJJUKLQSA-N 0.000 title claims 24
- 229950005031 deutetrabenazine Drugs 0.000 title claims 24
- 230000003204 osmotic effect Effects 0.000 title claims 3
- 239000011859 microparticle Substances 0.000 claims 22
- 239000003795 chemical substances by application Substances 0.000 claims 7
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 7
- -1 poly(vinyl methyl) Polymers 0.000 claims 6
- 239000011248 coating agent Substances 0.000 claims 5
- 238000000576 coating method Methods 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 239000002357 osmotic agent Substances 0.000 claims 4
- 229920000642 polymer Polymers 0.000 claims 4
- 208000012661 Dyskinesia Diseases 0.000 claims 3
- 239000011230 binding agent Substances 0.000 claims 3
- 238000007789 sealing Methods 0.000 claims 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 2
- 206010008748 Chorea Diseases 0.000 claims 2
- 208000000269 Hyperkinesis Diseases 0.000 claims 2
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 claims 2
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 claims 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
- 229920002301 cellulose acetate Polymers 0.000 claims 2
- 208000012601 choreatic disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 238000004090 dissolution Methods 0.000 claims 2
- 239000013583 drug formulation Substances 0.000 claims 2
- 229910017053 inorganic salt Inorganic materials 0.000 claims 2
- 239000008363 phosphate buffer Substances 0.000 claims 2
- 239000011148 porous material Substances 0.000 claims 2
- 235000002639 sodium chloride Nutrition 0.000 claims 2
- LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 claims 2
- 229920003176 water-insoluble polymer Polymers 0.000 claims 2
- 229920003169 water-soluble polymer Polymers 0.000 claims 2
- FYGDTMLNYKFZSV-URKRLVJHSA-N (2s,3r,4s,5s,6r)-2-[(2r,4r,5r,6s)-4,5-dihydroxy-2-(hydroxymethyl)-6-[(2r,4r,5r,6s)-4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxan-3-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1[C@@H](CO)O[C@@H](OC2[C@H](O[C@H](O)[C@H](O)[C@H]2O)CO)[C@H](O)[C@H]1O FYGDTMLNYKFZSV-URKRLVJHSA-N 0.000 claims 1
- 229920001817 Agar Polymers 0.000 claims 1
- 206010001540 Akathisia Diseases 0.000 claims 1
- 229920000856 Amylose Polymers 0.000 claims 1
- 229920002498 Beta-glucan Polymers 0.000 claims 1
- 229920001747 Cellulose diacetate Polymers 0.000 claims 1
- DQEFEBPAPFSJLV-UHFFFAOYSA-N Cellulose propionate Chemical compound CCC(=O)OCC1OC(OC(=O)CC)C(OC(=O)CC)C(OC(=O)CC)C1OC1C(OC(=O)CC)C(OC(=O)CC)C(OC(=O)CC)C(COC(=O)CC)O1 DQEFEBPAPFSJLV-UHFFFAOYSA-N 0.000 claims 1
- 229920002284 Cellulose triacetate Polymers 0.000 claims 1
- 239000001856 Ethyl cellulose Substances 0.000 claims 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 1
- 229930182556 Polyacetal Natural products 0.000 claims 1
- 229920000954 Polyglycolide Polymers 0.000 claims 1
- 229920001710 Polyorthoester Polymers 0.000 claims 1
- 208000001431 Psychomotor Agitation Diseases 0.000 claims 1
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 claims 1
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 208000016620 Tourette disease Diseases 0.000 claims 1
- 206010044565 Tremor Diseases 0.000 claims 1
- NNLVGZFZQQXQNW-ADJNRHBOSA-N [(2r,3r,4s,5r,6s)-4,5-diacetyloxy-3-[(2s,3r,4s,5r,6r)-3,4,5-triacetyloxy-6-(acetyloxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6s)-4,5,6-triacetyloxy-2-(acetyloxymethyl)oxan-3-yl]oxyoxan-2-yl]methyl acetate Chemical compound O([C@@H]1O[C@@H]([C@H]([C@H](OC(C)=O)[C@H]1OC(C)=O)O[C@H]1[C@@H]([C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O1)OC(C)=O)COC(=O)C)[C@@H]1[C@@H](COC(C)=O)O[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]1OC(C)=O NNLVGZFZQQXQNW-ADJNRHBOSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 239000008272 agar Substances 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 150000001720 carbohydrates Chemical class 0.000 claims 1
- 229920006217 cellulose acetate butyrate Polymers 0.000 claims 1
- 229920003086 cellulose ether Polymers 0.000 claims 1
- 229920006218 cellulose propionate Polymers 0.000 claims 1
- 206010008129 cerebral palsy Diseases 0.000 claims 1
- 238000013270 controlled release Methods 0.000 claims 1
- 229920001577 copolymer Polymers 0.000 claims 1
- 239000006185 dispersion Substances 0.000 claims 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 1
- 229920001249 ethyl cellulose Polymers 0.000 claims 1
- 235000019325 ethyl cellulose Nutrition 0.000 claims 1
- 229960004502 levodopa Drugs 0.000 claims 1
- INHCSSUBVCNVSK-UHFFFAOYSA-L lithium sulfate Inorganic materials [Li+].[Li+].[O-]S([O-])(=O)=O INHCSSUBVCNVSK-UHFFFAOYSA-L 0.000 claims 1
- 229910001629 magnesium chloride Inorganic materials 0.000 claims 1
- 235000011147 magnesium chloride Nutrition 0.000 claims 1
- 229910052943 magnesium sulfate Inorganic materials 0.000 claims 1
- 235000019341 magnesium sulphate Nutrition 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920000747 poly(lactic acid) Polymers 0.000 claims 1
- 239000002745 poly(ortho ester) Substances 0.000 claims 1
- 229920006324 polyoxymethylene Polymers 0.000 claims 1
- 229910000160 potassium phosphate Inorganic materials 0.000 claims 1
- 235000011009 potassium phosphates Nutrition 0.000 claims 1
- OTYBMLCTZGSZBG-UHFFFAOYSA-L potassium sulfate Chemical compound [K+].[K+].[O-]S([O-])(=O)=O OTYBMLCTZGSZBG-UHFFFAOYSA-L 0.000 claims 1
- 229910052939 potassium sulfate Inorganic materials 0.000 claims 1
- 235000011151 potassium sulphates Nutrition 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000001488 sodium phosphate Substances 0.000 claims 1
- 229910000162 sodium phosphate Inorganic materials 0.000 claims 1
- 229910052938 sodium sulfate Inorganic materials 0.000 claims 1
- 235000011152 sodium sulphate Nutrition 0.000 claims 1
- 238000001370 static light scattering Methods 0.000 claims 1
- 238000009492 tablet coating Methods 0.000 claims 1
- 239000002700 tablet coating Substances 0.000 claims 1
- RBTVSNLYYIMMKS-UHFFFAOYSA-N tert-butyl 3-aminoazetidine-1-carboxylate;hydrochloride Chemical compound Cl.CC(C)(C)OC(=O)N1CC(N)C1 RBTVSNLYYIMMKS-UHFFFAOYSA-N 0.000 claims 1
- ILJSQTXMGCGYMG-UHFFFAOYSA-N triacetic acid Chemical compound CC(=O)CC(=O)CC(O)=O ILJSQTXMGCGYMG-UHFFFAOYSA-N 0.000 claims 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 claims 1
- 239000003021 water soluble solvent Substances 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4747—Quinolines; Isoquinolines spiro-condensed
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/2004—Excipients; Inactive ingredients
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
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- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- Bioinformatics & Cheminformatics (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Psychology (AREA)
- Inorganic Chemistry (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
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Claims (19)
1. Osmotski oblik doziranja za davanje deutetrabenazina jednom dnevno subjektu kojem je to potrebno, naznačen time što sadrži:
a. jezgru tablete koja se sastoji od aktivnog sloja i potisnog sloja, pri čemu aktivni sloj sadrži određenu količinu mikročestica deutetrabenazina i sredstvo za kontrolu oslobađanja aktivnog sloja, te pri čemu potisni sloj sadrži osmotsko sredstvo i sredstvo za kontrolu oslobađanja potisnog sloja, i izborno brtvenu ovojnicu tablete na vanjskoj površini jezgre tablete;
b. polupropusni sloj koji okružuje jezgru tablete;
c. otvor koji se proteže kroz polupropusni sloj u jezgru tablete; i
d. izbornu prevlaku s trenutnim oslobađanjem izvan polupropusnog sloja koja sadrži drugu količinu mikročestica deutetrabenazina.
2. Oblik doziranja prema zahtjevu 1, naznačen time što sredstvo za kontrolu oslobađanja aktivnog sloja sadrži polimer koji ima viskoznost od 50-150 mPa s ili 55-90 mPa s; izborno pri čemu polimer sredstva za kontrolu oslobađanja aktivnog sloja sadrži polietilen oksid koji ima prosječnu molekularnu težinu od 100.000 daltona do 500.000 daltona u količini od 60% do 98% težine, temeljeno na ukupnoj težini aktivnog sloja.
3. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što aktivni sloj nadalje sadrži najmanje jedno od:
a. antioksidans aktivnog sloja prisutan u količini od 0,001% do 1% težine, temeljeno na ukupnoj težini aktivnog sloja; i
b. vezivo aktivnog sloja koje je prisutno u količini od 2% do 20% težine, temeljeno na ukupnoj težini aktivnog sloja.
4. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što osmotsko sredstvo sadrži anorgansku sol, ugljikohidrat ili bilo koju njihovu smjesu; izborno pri čemu osmotsko sredstvo sadrži anorgansku sol odabranu između magnezijevog sulfata, magnezijevog klorida, kalijevog sulfata, natrijevog klorida, natrijevog sulfata, litijevog sulfata, natrijevog fosfata, kalijevog fosfata ili bilo koje njihove smjese i prisutna je u količini od 5% do 50% težine, na temelju ukupne težine oblika doziranja.
5. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što sredstvo za kontrolirano oslobađanje potisnog sloja sadrži polimer koji ima viskoznost od 5500-7500 mPa s i prisutno je u količini od 50% do 80% težine, temeljeno na ukupnoj težini potisnog sloja.
6. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što težinski omjer osmotskog sredstva i sredstva za kontrolu oslobađanja potisnog sloja u potisnom sloju iznosi 1:2 - 1:3,5 ili 1:2 - 1:2,5.
7. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što potisni sloj nadalje sadrži najmanje jedno od:
a. vezivo potisnog sloja; i
b. farmaceutski prihvatljivo pomoćno sredstvo.
8. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što polupropusni sloj sadrži polimer topiv u vodi, polimer netopljiv u vodi ili bilo koju njihovu smjesu; izborno pri čemu polupropusni sloj sadrži u vodi netopljivi polimer odabran između celuloznog acetata, celuloznog diacetata, celuloznog triacetata, celuloznog propionata, celuloznog acetat butirata, celuloznih etera poput etil celuloze, agar acetata, amiloznog triacetata, betaglukan acetata, kopolimera poli(vinil metil) etera, poli(ortoestera), poliacetala i selektivno propusnih derivata poli(glikolne kiseline), poli(mliječne kiseline), polimera celuloznog acetata ili bilo koje njihove smjese u količini od 80% do 99,9% težine, temeljeno na težini polupropusnog sloja.
9. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što polupropusni sloj sadrži sredstvo za stvaranje pora; izborno pri čemu sredstvo za stvaranje pora sadrži šećer topiv u vodi, sol topljivu u vodi, otapalo topljivo u vodi, polimer topiv u vodi ili bilo koju njihovu smjesu i prisutno je u polupropusnom sloju u količini od 0,1% do 20% težine polupropusnog sloja.
10. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što je težinski omjer polupropusnog sloja i jezgre tablete 1:8-1:10.
11. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što otvor ima promjer od 0,1 mm do 1 mm.
12. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što nadalje sadrži polupropusni sloj za brtvljenje na vanjskoj površini polupropusnog sloja.
13. Oblik doziranja prema zahtjevu 12, naznačen time što svaki od brtvene prevlake jezgre tablete i nepropusne prevlake polupropusnog sloja neovisno sadrži vezivo u količini do 20% težine, temeljeno na ukupnoj težini oblika doziranja.
14. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što obuhvaća prevlaku za trenutno oslobađanje izvan polupropusne membrane, pri čemu prevlaka za trenutno oslobađanje sadrži 0,1% do 30% težine mikročestica deutetrabenazina, temeljeno na ukupnoj težini oblika doziranja ili 0,2 % do 5 % težine mikročestica deutetrabenazina, temeljeno na ukupnoj težini oblika doziranja ili 0,3 % do 2 % težine mikročestica deutetrabenazina, temeljeno na ukupnoj težini oblika doziranja.
15. Oblik doziranja prema zahtjevu 14, naznačen time što oblik doziranja sadrži:
a. ukupnu količinu od 6 mg mikročestica deutetrabenazina pri čemu ovojnica za trenutačno oslobađanje sadrži 0,1% do 0,5% težine mikročestica deutetrabenazina, temeljeno na ukupnoj težini oblika doziranja, ili
b. ukupnu količinu od 12 mg mikročestica deutetrabenazina pri čemu ovojnica za trenutačno oslobađanje sadrži 0,5% do 1% težine mikročestica deutetrabenazina, temeljeno na ukupnoj težini oblika doziranja, ili
c. ukupnu količinu od 24 mg mikročestica deutetrabenazina, pri čemu ovojnica za trenutačno oslobađanje sadrži 1% do 2% težine mikročestica deutetrabenazina, bazirano na ukupnoj težini oblika doziranja.
16. Oblik doziranja prema bilo kojem od zahtjeva 1-14, naznačen time što doziranje sadrži od 6 mg do 48 mg deutetrabenazina u obliku mikročestica deutetrabenazina i pri čemu je 70%-80% ukupne količine mikročestica deutetrabenazina prisutnih u obliku doziranja prisutno unutar aktivnog sloja i pri čemu je 20%-30% ukupne količine mikročestica deutetrabenazina prisutnih u obliku doziranja, prisutno unutar ovojnice za trenutno oslobađanje; izborno pri čemu oblik doziranja sadrži:
a) ukupnu količinu od 6 mg mikročestica deutetrabenazina, pri čemu je ukupna količina mikročestica deutetrabenazina 0,5% do 3% težine, temeljeno na ukupnoj težini oblika doziranja, ili
b) ukupnu količinu od 12 mg mikročestica deutetrabenazina, pri čemu je ukupna količina mikročestica deutetrabenazina 1% do 5% težine, temeljeno na ukupnoj težini oblika doziranja, ili
c) ukupnu količinu od 24 mg mikročestica deutetrabenazina, pri čemu je ukupna količina mikročestica deutetrabenazina 5% do 10% težine, temeljeno na ukupnoj težini oblika doziranja.
17. Oblik doziranja prema bilo kojem od prethodnih zahtjeva, naznačen time što mikročestice deutetrabenazina imaju veličinu čestica od 1 µm do 30 µm u promjeru, poželjno s D90 od 15 µm, D50 10 µm, i/ili D10 od 3 µm, mjereno dinamičkim ili statičkim raspršenjem svjetlosti vodene disperzije pripravka mikročestica.
18. Osmotski oblik doziranja prema bilo kojem od prethodnih zahtjeva naznačen time što se koristi u liječenju hiperkinetičkog poremećaja kretanja; izborno pri čemu je hiperkinetički poremećaj pokreta koreja, akatizija, diskinezija, tremor, tik, koreja povezana s Huntingtonovom bolešću, tardivna diskinezija, tik povezan s Touretteovim sindromom, diskinezija izazvana levodopom kod Parkinsonove bolesti ili diskinezija u cerebralnoj paralizi.
19. Oblik doziranja prema bilo kojem od zahtjeva 1 do 17 za upotrebu prema zahtjevu 18, naznačen time što liječenje uključuje davanje oblika doziranja, pri čemu se: ne više od 15% formulacije lijeka oslobađa nakon 2 sata kada se testira u 500 mL kiselog fosfatnog pufera na pH 3,0 korištenjem USP II aparata za otapanje; ili ne više od 60% formulacije lijeka se oslobađa nakon 8 sati kada se testira u 500 mL kiselog fosfatnog pufera na pH 3,0 korištenjem USP II aparata za otapanje.
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| EP21737870.2A EP4153136B1 (en) | 2020-06-10 | 2021-06-10 | Osmotic dosage forms comprising deutetrabenazine and methods of use thereof |
| PCT/US2021/036778 WO2021252741A1 (en) | 2020-06-10 | 2021-06-10 | Osmotic dosage forms comprising deutetrabenazine and methods of use thereof |
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| US3173876A (en) | 1960-05-27 | 1965-03-16 | John C Zobrist | Cleaning methods and compositions |
| US3276586A (en) | 1963-08-30 | 1966-10-04 | Rosaen Filter Co | Indicating means for fluid filters |
| US3546142A (en) | 1967-01-19 | 1970-12-08 | Amicon Corp | Polyelectrolyte structures |
| US3541006A (en) | 1968-07-03 | 1970-11-17 | Amicon Corp | Ultrafiltration process |
| US3541005A (en) | 1969-02-05 | 1970-11-17 | Amicon Corp | Continuous ultrafiltration of macromolecular solutions |
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US3916899A (en) | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| GB1478759A (en) | 1974-11-18 | 1977-07-06 | Alza Corp | Process for forming outlet passageways in pills using a laser |
| US4200098A (en) | 1978-10-23 | 1980-04-29 | Alza Corporation | Osmotic system with distribution zone for dispensing beneficial agent |
| US4327725A (en) | 1980-11-25 | 1982-05-04 | Alza Corporation | Osmotic device with hydrogel driving member |
| US5082668A (en) | 1983-05-11 | 1992-01-21 | Alza Corporation | Controlled-release system with constant pushing source |
| US4783337A (en) | 1983-05-11 | 1988-11-08 | Alza Corporation | Osmotic system comprising plurality of members for dispensing drug |
| US4612008A (en) | 1983-05-11 | 1986-09-16 | Alza Corporation | Osmotic device with dual thermodynamic activity |
| US20030161882A1 (en) * | 2002-02-01 | 2003-08-28 | Waterman Kenneth C. | Osmotic delivery system |
| US20070031496A1 (en) * | 2005-08-04 | 2007-02-08 | Edgren David E | Osmotic dosage forms comprising semipermeable membranes with polymer blends providing improved properties |
| US20120208773A1 (en) * | 2008-08-12 | 2012-08-16 | Valeant International (Barbados) Srl | Pharmaceutical compositions with tetrabenazine |
| US8524733B2 (en) | 2008-09-18 | 2013-09-03 | Auspex Pharmaceuticals | Benzoquinoline inhibitors of vesicular monoamine transporter 2 |
| EP2464340A2 (en) * | 2009-08-12 | 2012-06-20 | Valeant International (Barbados) SRL | Pharmaceutical compositions with tetrabenazine |
| BR112015005894B1 (pt) * | 2012-09-18 | 2022-03-29 | Auspex Pharmaceuticals, Inc | Composto, composição farmacêutica, método para tratar um distúrbio mediado por vmat2 e formulação farmacêutica de liberação prolongada |
| US10479787B2 (en) * | 2016-04-22 | 2019-11-19 | Lupin Limited | Process for preparation of tetrabenazine and deutetrabenazine |
| US20170312226A1 (en) * | 2016-04-28 | 2017-11-02 | Ascent Pharmaceuticals, Inc. | Pharmaceutical dosage forms |
| AU2018236336B2 (en) * | 2017-03-15 | 2022-02-24 | Auspex Pharmaceuticals, Inc. | Analogs of deutetrabenazine, their preparation and use |
| EP3836926A4 (en) * | 2018-08-15 | 2022-05-04 | Neurocrine Biosciences, Inc. | METHODS OF ADMINISTRATION OF CERTAIN VMAT2 INHIBITORS |
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