CA3095341A1 - Levodopa fractionated dose composition and use - Google Patents
Levodopa fractionated dose composition and use Download PDFInfo
- Publication number
- CA3095341A1 CA3095341A1 CA3095341A CA3095341A CA3095341A1 CA 3095341 A1 CA3095341 A1 CA 3095341A1 CA 3095341 A CA3095341 A CA 3095341A CA 3095341 A CA3095341 A CA 3095341A CA 3095341 A1 CA3095341 A1 CA 3095341A1
- Authority
- CA
- Canada
- Prior art keywords
- levodopa
- carbidopa
- patient
- layer
- tablet
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 title claims abstract description 22
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 title claims abstract description 22
- 229960004502 levodopa Drugs 0.000 title claims abstract description 22
- 239000000203 mixture Substances 0.000 title claims description 23
- 238000011282 treatment Methods 0.000 claims abstract description 53
- 208000018737 Parkinson disease Diseases 0.000 claims abstract description 52
- IVTMXOXVAHXCHI-YXLMWLKOSA-N (2s)-2-amino-3-(3,4-dihydroxyphenyl)propanoic acid;(2s)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1.NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 IVTMXOXVAHXCHI-YXLMWLKOSA-N 0.000 claims abstract description 11
- 229940052036 carbidopa / levodopa Drugs 0.000 claims abstract description 9
- 238000000034 method Methods 0.000 claims description 25
- 239000003937 drug carrier Substances 0.000 claims description 22
- 230000004044 response Effects 0.000 claims description 21
- 239000004480 active ingredient Substances 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 20
- 238000009472 formulation Methods 0.000 claims description 9
- 229960004205 carbidopa Drugs 0.000 claims description 8
- 238000011272 standard treatment Methods 0.000 claims description 7
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 6
- 230000002265 prevention Effects 0.000 claims description 4
- 229940085760 carbidopa 25 mg Drugs 0.000 claims description 3
- TZFNLOMSOLWIDK-JTQLQIEISA-N carbidopa (anhydrous) Chemical compound NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 TZFNLOMSOLWIDK-JTQLQIEISA-N 0.000 claims 3
- 229940080381 levodopa 100 mg Drugs 0.000 claims 3
- 230000000149 penetrating effect Effects 0.000 claims 3
- 229940097987 carbidopa 10 mg Drugs 0.000 claims 1
- 229940015929 carbidopa 12.5 mg Drugs 0.000 claims 1
- 201000002886 generalized dystonia Diseases 0.000 claims 1
- 229940067290 levodopa 50 mg Drugs 0.000 claims 1
- 238000002638 palliative care Methods 0.000 claims 1
- 238000001802 infusion Methods 0.000 abstract description 7
- 238000001990 intravenous administration Methods 0.000 abstract description 5
- 230000000116 mitigating effect Effects 0.000 abstract description 2
- 239000003826 tablet Substances 0.000 description 80
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 64
- 229960003638 dopamine Drugs 0.000 description 24
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 24
- 229940001089 sinemet Drugs 0.000 description 17
- 208000024891 symptom Diseases 0.000 description 17
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 16
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 16
- 210000004556 brain Anatomy 0.000 description 12
- 238000007906 compression Methods 0.000 description 12
- 230000006835 compression Effects 0.000 description 12
- 239000003814 drug Substances 0.000 description 12
- 235000019359 magnesium stearate Nutrition 0.000 description 12
- 229920000881 Modified starch Polymers 0.000 description 11
- 201000010099 disease Diseases 0.000 description 11
- 239000008108 microcrystalline cellulose Substances 0.000 description 11
- 229940016286 microcrystalline cellulose Drugs 0.000 description 11
- 208000012661 Dyskinesia Diseases 0.000 description 9
- 229940079593 drug Drugs 0.000 description 9
- 239000008187 granular material Substances 0.000 description 9
- 230000003291 dopaminomimetic effect Effects 0.000 description 8
- 238000002156 mixing Methods 0.000 description 8
- 230000008569 process Effects 0.000 description 8
- 238000002560 therapeutic procedure Methods 0.000 description 8
- 230000000694 effects Effects 0.000 description 7
- 238000005469 granulation Methods 0.000 description 7
- 230000003179 granulation Effects 0.000 description 7
- 210000002569 neuron Anatomy 0.000 description 7
- 239000008194 pharmaceutical composition Substances 0.000 description 7
- 230000000541 pulsatile effect Effects 0.000 description 7
- 230000008901 benefit Effects 0.000 description 6
- 230000002354 daily effect Effects 0.000 description 6
- 208000035475 disorder Diseases 0.000 description 6
- 238000002360 preparation method Methods 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 229920002472 Starch Polymers 0.000 description 5
- QTAOMKOIBXZKND-PPHPATTJSA-N carbidopa Chemical compound O.NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 QTAOMKOIBXZKND-PPHPATTJSA-N 0.000 description 5
- 208000017763 cutaneous neuroendocrine carcinoma Diseases 0.000 description 5
- 239000000314 lubricant Substances 0.000 description 5
- 239000000546 pharmaceutical excipient Substances 0.000 description 5
- 102000005962 receptors Human genes 0.000 description 5
- 108020003175 receptors Proteins 0.000 description 5
- 235000019698 starch Nutrition 0.000 description 5
- 230000000638 stimulation Effects 0.000 description 5
- 238000003860 storage Methods 0.000 description 5
- 102000015554 Dopamine receptor Human genes 0.000 description 4
- 108050004812 Dopamine receptor Proteins 0.000 description 4
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 4
- 239000001913 cellulose Substances 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- 238000005520 cutting process Methods 0.000 description 4
- 238000004049 embossing Methods 0.000 description 4
- 230000003203 everyday effect Effects 0.000 description 4
- 230000006870 function Effects 0.000 description 4
- 230000000977 initiatory effect Effects 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 230000001242 postsynaptic effect Effects 0.000 description 4
- 239000008213 purified water Substances 0.000 description 4
- 238000011160 research Methods 0.000 description 4
- 208000011580 syndromic disease Diseases 0.000 description 4
- 238000005550 wet granulation Methods 0.000 description 4
- 206010061818 Disease progression Diseases 0.000 description 3
- 208000006083 Hypokinesia Diseases 0.000 description 3
- 208000002740 Muscle Rigidity Diseases 0.000 description 3
- 235000021355 Stearic acid Nutrition 0.000 description 3
- 206010044565 Tremor Diseases 0.000 description 3
- VREFGVBLTWBCJP-UHFFFAOYSA-N alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 description 3
- 230000000648 anti-parkinson Effects 0.000 description 3
- 239000000939 antiparkinson agent Substances 0.000 description 3
- 239000011230 binding agent Substances 0.000 description 3
- 235000010980 cellulose Nutrition 0.000 description 3
- 229920002678 cellulose Polymers 0.000 description 3
- 210000003169 central nervous system Anatomy 0.000 description 3
- 230000005750 disease progression Effects 0.000 description 3
- JRURYQJSLYLRLN-BJMVGYQFSA-N entacapone Chemical compound CCN(CC)C(=O)C(\C#N)=C\C1=CC(O)=C(O)C([N+]([O-])=O)=C1 JRURYQJSLYLRLN-BJMVGYQFSA-N 0.000 description 3
- 229960003337 entacapone Drugs 0.000 description 3
- 238000005194 fractionation Methods 0.000 description 3
- 230000005021 gait Effects 0.000 description 3
- 239000000499 gel Substances 0.000 description 3
- 230000007774 longterm Effects 0.000 description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 3
- 230000000737 periodic effect Effects 0.000 description 3
- 239000008107 starch Substances 0.000 description 3
- 239000008117 stearic acid Substances 0.000 description 3
- 239000000454 talc Substances 0.000 description 3
- 229910052623 talc Inorganic materials 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- 206010052804 Drug tolerance Diseases 0.000 description 2
- 206010020751 Hypersensitivity Diseases 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 206010030312 On and off phenomenon Diseases 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- 235000010443 alginic acid Nutrition 0.000 description 2
- 229920000615 alginic acid Polymers 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 230000001684 chronic effect Effects 0.000 description 2
- 229960000913 crospovidone Drugs 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 230000018109 developmental process Effects 0.000 description 2
- 210000005064 dopaminergic neuron Anatomy 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 210000001198 duodenum Anatomy 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 230000037406 food intake Effects 0.000 description 2
- 230000036541 health Effects 0.000 description 2
- 230000003483 hypokinetic effect Effects 0.000 description 2
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 230000017311 musculoskeletal movement, spinal reflex action Effects 0.000 description 2
- 210000005036 nerve Anatomy 0.000 description 2
- 210000001428 peripheral nervous system Anatomy 0.000 description 2
- 229940068196 placebo Drugs 0.000 description 2
- 239000000902 placebo Substances 0.000 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 229940069328 povidone Drugs 0.000 description 2
- 230000000750 progressive effect Effects 0.000 description 2
- 230000002829 reductive effect Effects 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 238000004904 shortening Methods 0.000 description 2
- 235000012222 talc Nutrition 0.000 description 2
- 238000004448 titration Methods 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 1
- 206010067484 Adverse reaction Diseases 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 102100038238 Aromatic-L-amino-acid decarboxylase Human genes 0.000 description 1
- 101710151768 Aromatic-L-amino-acid decarboxylase Proteins 0.000 description 1
- 206010006100 Bradykinesia Diseases 0.000 description 1
- 102000004031 Carboxy-Lyases Human genes 0.000 description 1
- 108090000489 Carboxy-Lyases Proteins 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 208000002603 Dopa-responsive dystonia Diseases 0.000 description 1
- 102100027346 GTP cyclohydrolase 1 Human genes 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 101000862581 Homo sapiens GTP cyclohydrolase 1 Proteins 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 208000015592 Involuntary movements Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 206010061296 Motor dysfunction Diseases 0.000 description 1
- 208000016285 Movement disease Diseases 0.000 description 1
- 206010034156 Pathological fracture Diseases 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 241000288906 Primates Species 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 208000005793 Restless legs syndrome Diseases 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 208000005250 Spontaneous Fractures Diseases 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- 102000019355 Synuclein Human genes 0.000 description 1
- 108050006783 Synuclein Proteins 0.000 description 1
- 240000008042 Zea mays Species 0.000 description 1
- 235000016383 Zea mays subsp huehuetenangensis Nutrition 0.000 description 1
- 235000002017 Zea mays subsp mays Nutrition 0.000 description 1
- 230000001594 aberrant effect Effects 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 238000004364 calculation method Methods 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 230000006727 cell loss Effects 0.000 description 1
- 238000013329 compounding Methods 0.000 description 1
- 239000000039 congener Substances 0.000 description 1
- 239000012059 conventional drug carrier Substances 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 238000011461 current therapy Methods 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 230000003412 degenerative effect Effects 0.000 description 1
- 230000002939 deleterious effect Effects 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 230000003292 diminished effect Effects 0.000 description 1
- 238000006073 displacement reaction Methods 0.000 description 1
- 230000004771 dopaminergic neurodegeneration Effects 0.000 description 1
- 238000007580 dry-mixing Methods 0.000 description 1
- 229940009579 duopa Drugs 0.000 description 1
- 238000013265 extended release Methods 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 description 1
- 238000009478 high shear granulation Methods 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000000366 juvenile effect Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007942 layered tablet Substances 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 235000009973 maize Nutrition 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 238000003801 milling Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 150000004682 monohydrates Chemical class 0.000 description 1
- 230000007659 motor function Effects 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 231100000189 neurotoxic Toxicity 0.000 description 1
- 230000002887 neurotoxic effect Effects 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229920003124 powdered cellulose Polymers 0.000 description 1
- 235000019814 powdered cellulose Nutrition 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 238000011809 primate model Methods 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 238000004393 prognosis Methods 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- -1 salt stearate Chemical class 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 229910021487 silica fume Inorganic materials 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000003523 substantia nigra Anatomy 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000005062 synaptic transmission Effects 0.000 description 1
- 230000015883 synaptic transmission, dopaminergic Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
Classifications
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
-
- 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
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Psychology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862650012P | 2018-03-29 | 2018-03-29 | |
| US62/650,012 | 2018-03-29 | ||
| PCT/US2019/024464 WO2019191353A1 (en) | 2018-03-29 | 2019-03-28 | Levodopa fractionated dose composition and use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3095341A1 true CA3095341A1 (en) | 2019-10-03 |
Family
ID=68060752
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3095341A Pending CA3095341A1 (en) | 2018-03-29 | 2019-03-28 | Levodopa fractionated dose composition and use |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US11033521B2 (enExample) |
| EP (1) | EP3773532A4 (enExample) |
| JP (2) | JP2021517128A (enExample) |
| CN (1) | CN111954523A (enExample) |
| BR (1) | BR112020017422A2 (enExample) |
| CA (1) | CA3095341A1 (enExample) |
| WO (1) | WO2019191353A1 (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111954523A (zh) * | 2018-03-29 | 2020-11-17 | 艾维制药有限责任公司 | 左旋多巴分次剂量组合物及用途 |
| WO2022044045A1 (en) * | 2020-08-26 | 2022-03-03 | Rubicon Research Private Limited | Modified release formulations of levodopa |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5061494A (en) * | 1990-06-14 | 1991-10-29 | The Upjohn Comany | Tri-scored drug tablet |
| CN1960712B (zh) * | 2004-05-21 | 2011-04-20 | 阿库-伯雷克技术公司 | 包含多个片段的刻痕药片 |
| US7838031B2 (en) | 2004-05-21 | 2010-11-23 | Lawrence Solomon | Method of administering a partial dose using a segmented pharmaceutical tablet |
| JP5395355B2 (ja) * | 2004-05-21 | 2014-01-22 | アキュ−ブレイク テクノロジーズ インコーポレーテッド | ２個またはそれ以上の単位セグメントを含む医薬錠剤 |
| US8506999B2 (en) | 2005-05-23 | 2013-08-13 | Accu-Break Technologies, Inc. | Pharmaceutical tablets comprising a plurality of segments |
| US20070275060A1 (en) * | 2005-08-05 | 2007-11-29 | Osmotica Costa Rica Sociedad Anonima | Extended release solid pharmaceutical composition containing carbidopa and levodopa |
| AU2005338350A1 (en) | 2005-11-18 | 2007-05-24 | Solapharm, Inc. | Segmented pharmaceutical dosage forms |
| MX2008015339A (es) * | 2006-05-31 | 2008-12-16 | Solvay Pharm Gmbh | Administracion intestinal a largo plazo durante 24 horas de levodopa/carbidopa. |
| US20080131492A1 (en) * | 2006-06-23 | 2008-06-05 | Spherics, Inc. | Dosage forms for movement disorder treatment |
| UA106877C2 (uk) * | 2008-08-22 | 2014-10-27 | Вокхардт Рісерч Сентер | Фармацевтична композиція ентакапону або його солей пролонгованого вивільнення |
| RU2678839C2 (ru) * | 2009-05-19 | 2019-02-04 | Неуродерм Лтд | Композиции для непрерывного введения ингибиторов допа-декарбоксилазы |
| BR112015022390A8 (pt) * | 2013-03-13 | 2019-11-26 | Neuroderm Ltd | uso de carbidopa, levodopa e um inibidor de comt para a preparação de uma composição para tratamento de doença de parkinson |
| HK1211836A1 (en) * | 2013-03-28 | 2016-06-03 | Omniactive Health Technologies Limited | Neuroprotective effect of carotenoids in brain |
| RU2017120184A (ru) * | 2014-11-28 | 2018-12-28 | БИАЛ - ПОРТЕЛА ЭНД Ка, С.А. | Лекарства для замедления течения болезни паркинсона |
| WO2018034626A1 (en) * | 2016-08-18 | 2018-02-22 | İlko İlaç Sanayi Ve Ticaret Anonim Şirketi | Antiparkinson tablet formulation with improved dissolution profile |
| CN111954523A (zh) * | 2018-03-29 | 2020-11-17 | 艾维制药有限责任公司 | 左旋多巴分次剂量组合物及用途 |
-
2019
- 2019-03-28 CN CN201980023074.8A patent/CN111954523A/zh active Pending
- 2019-03-28 EP EP19775769.3A patent/EP3773532A4/en not_active Withdrawn
- 2019-03-28 JP JP2020546876A patent/JP2021517128A/ja active Pending
- 2019-03-28 CA CA3095341A patent/CA3095341A1/en active Pending
- 2019-03-28 BR BR112020017422-0A patent/BR112020017422A2/pt unknown
- 2019-03-28 WO PCT/US2019/024464 patent/WO2019191353A1/en not_active Ceased
- 2019-12-18 US US16/719,203 patent/US11033521B2/en active Active
-
2021
- 2021-03-31 US US17/219,253 patent/US11439613B2/en active Active
-
2022
- 2022-07-08 JP JP2022110134A patent/JP2022133449A/ja active Pending
- 2022-08-26 US US17/896,808 patent/US11819485B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20210220308A1 (en) | 2021-07-22 |
| JP2021517128A (ja) | 2021-07-15 |
| US20200121626A1 (en) | 2020-04-23 |
| EP3773532A1 (en) | 2021-02-17 |
| US20230233496A1 (en) | 2023-07-27 |
| US11439613B2 (en) | 2022-09-13 |
| US11819485B2 (en) | 2023-11-21 |
| JP2022133449A (ja) | 2022-09-13 |
| EP3773532A4 (en) | 2022-11-02 |
| CN111954523A (zh) | 2020-11-17 |
| BR112020017422A2 (pt) | 2020-12-22 |
| US11033521B2 (en) | 2021-06-15 |
| WO2019191353A1 (en) | 2019-10-03 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US4962121A (en) | Method and composition for treating neurological diseases such as migraine | |
| US8426470B2 (en) | Method for alleviating signs and symptoms of spasticity | |
| US11318144B2 (en) | Compositions and methods for treating Alzheimer's disease and Parkinson's disease | |
| EA012964B1 (ru) | Фармацевтические составы модафинила | |
| JPH06508836A (ja) | 光学的に純粋なｒ（＋）オンダンセトロンを使用する嘔吐、吐き気および他の障害の治療のための方法および組成物 | |
| EP1435943B1 (en) | Use of 2-oxo-1-pyrrolidine derivatives for the preparation of a drug for treating dyskinesia | |
| US11819485B2 (en) | Levodopa fractionated dose composition and use | |
| JPH05213741A (ja) | デプレニル／ｌ−ドーパ／カルビドーパ含有の医薬組成物 | |
| KR20160111013A (ko) | 신경질환의 치료를 위한 바클로펜, 아캄프로세이트 및 중쇄 트리-글리세리드의 조합 | |
| WO2006051154A1 (en) | Treatment of restless legs syndrome | |
| US3557292A (en) | Compositions and methods for treating parkinson's disease with combinations of l-3,4-dihydroxyphenylalanine and a hydrazine | |
| CA3074563A1 (en) | Sublingual epinephrine tablets | |
| EP1784177B1 (de) | Formulierung für l-tryptophan mit carbidopa/ benserazid | |
| KR102693607B1 (ko) | 하지 불안 증후군을 치료하기 위한 치료제 | |
| US7915262B2 (en) | Combination preparations comprising SLV308 and a dopamine agonist | |
| CA2840521C (en) | Pharmaceutical composition for treating premature ejaculation and method for treating premature ejaculation | |
| HK40037691A (en) | Levodopa fractionated dose composition and use | |
| CN102670597B (zh) | 5-(4-羟基-3-甲氧基苯亚甲基)罗丹宁在制备治疗帕金森氏病药物中的用途 | |
| JPH06509073A (ja) | 光学的に純粋なｓ（−）オンダンセトロンを使用する嘔吐、吐き気および他の障害の治療のための方法および組成物 | |
| WO2008010768A1 (en) | Method of treating and diagnosing restless legs syndrome and periodic limb movements during sleep and means for carrying out the method | |
| WO2014005721A1 (en) | Use of (r)-phenylpiracetam for the treatment of parkinson's disease | |
| CN110101690B (zh) | 一种神经细胞保护剂及其在癫痫防治中的应用 | |
| KR101473998B1 (ko) | 에페리손 함유 필름코팅정제 | |
| CA2654719A1 (en) | Combination preparations comprising slv308 and a l-dopa | |
| GB2321190A (en) | Medicament pack for treating Parkinson's Disease |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20220908 |
|
| EEER | Examination request |
Effective date: 20220908 |
|
| EEER | Examination request |
Effective date: 20220908 |
|
| EEER | Examination request |
Effective date: 20220908 |
|
| EEER | Examination request |
Effective date: 20220908 |
|
| EEER | Examination request |
Effective date: 20220908 |