HRP20250268T1 - Farmaceutska kombinacija i pripravak, te kombinirana priprema koja sadrži aktivator glukokinaze i hipoglikemički lijek biguanid kao i metoda pripreme i njihova uporaba - Google Patents
Farmaceutska kombinacija i pripravak, te kombinirana priprema koja sadrži aktivator glukokinaze i hipoglikemički lijek biguanid kao i metoda pripreme i njihova uporaba Download PDFInfo
- Publication number
- HRP20250268T1 HRP20250268T1 HRP20250268TT HRP20250268T HRP20250268T1 HR P20250268 T1 HRP20250268 T1 HR P20250268T1 HR P20250268T T HRP20250268T T HR P20250268TT HR P20250268 T HRP20250268 T HR P20250268T HR P20250268 T1 HRP20250268 T1 HR P20250268T1
- Authority
- HR
- Croatia
- Prior art keywords
- hms5552
- solid dispersion
- metformin hydrochloride
- eudragit
- opadry
- Prior art date
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- 229940124828 glucokinase activator Drugs 0.000 title claims 14
- 238000002360 preparation method Methods 0.000 title claims 4
- 238000000034 method Methods 0.000 title claims 3
- 239000003814 drug Substances 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- HMUMWSORCUWQJO-QAPCUYQASA-N (2s)-2-[3-(2-chlorophenoxy)-5-oxo-2h-pyrrol-1-yl]-n-[1-[(2r)-2,3-dihydroxypropyl]pyrazol-3-yl]-4-methylpentanamide Chemical compound C=1C(=O)N([C@@H](CC(C)C)C(=O)NC2=NN(C[C@@H](O)CO)C=C2)CC=1OC1=CC=CC=C1Cl HMUMWSORCUWQJO-QAPCUYQASA-N 0.000 claims 81
- 239000007962 solid dispersion Substances 0.000 claims 60
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 38
- 229960004329 metformin hydrochloride Drugs 0.000 claims 36
- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical compound Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 claims 36
- 229920003139 Eudragit® L 100 Polymers 0.000 claims 26
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 26
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 239000003826 tablet Substances 0.000 claims 15
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 14
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 14
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- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 14
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 14
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 14
- 239000008108 microcrystalline cellulose Substances 0.000 claims 14
- 235000019359 magnesium stearate Nutrition 0.000 claims 13
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 12
- 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 claims 12
- 239000011230 binding agent Substances 0.000 claims 12
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- 229960001681 croscarmellose sodium Drugs 0.000 claims 12
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- 229940123208 Biguanide Drugs 0.000 claims 7
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 7
- 239000003472 antidiabetic agent Substances 0.000 claims 7
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- 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 claims 4
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 4
- 239000008103 glucose Substances 0.000 claims 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 4
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 4
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- 229940069328 povidone Drugs 0.000 claims 3
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 claims 2
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 claims 2
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 claims 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
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- 210000004369 blood Anatomy 0.000 claims 2
- 239000003086 colorant Substances 0.000 claims 2
- 239000006185 dispersion Substances 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
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- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 229960003105 metformin Drugs 0.000 claims 2
- 229920003145 methacrylic acid copolymer Polymers 0.000 claims 2
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- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 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 claims 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.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 WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 1
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- 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 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 229920003134 Eudragit® polymer Polymers 0.000 claims 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 102000017011 Glycated Hemoglobin A Human genes 0.000 claims 1
- 108010014663 Glycated Hemoglobin A Proteins 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
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- 229930195725 Mannitol Natural products 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 229920000881 Modified starch Polymers 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
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- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 125000000129 anionic group Chemical group 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 235000006708 antioxidants Nutrition 0.000 claims 1
- 229960004111 buformin Drugs 0.000 claims 1
- XSEUMFJMFFMCIU-UHFFFAOYSA-N buformin Chemical compound CCCC\N=C(/N)N=C(N)N XSEUMFJMFFMCIU-UHFFFAOYSA-N 0.000 claims 1
- YYRMJZQKEFZXMX-UHFFFAOYSA-L calcium bis(dihydrogenphosphate) Chemical compound [Ca+2].OP(O)([O-])=O.OP(O)([O-])=O YYRMJZQKEFZXMX-UHFFFAOYSA-L 0.000 claims 1
- 229940062672 calcium dihydrogen phosphate Drugs 0.000 claims 1
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- LDHBWEYLDHLIBQ-UHFFFAOYSA-M iron(3+);oxygen(2-);hydroxide;hydrate Chemical compound O.[OH-].[O-2].[Fe+3] LDHBWEYLDHLIBQ-UHFFFAOYSA-M 0.000 claims 1
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- ICFJFFQQTFMIBG-UHFFFAOYSA-N phenformin Chemical compound NC(=N)NC(=N)NCCC1=CC=CC=C1 ICFJFFQQTFMIBG-UHFFFAOYSA-N 0.000 claims 1
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- 230000000291 postprandial effect Effects 0.000 claims 1
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- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
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Classifications
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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
- A61K31/13—Amines
- A61K31/133—Amines having hydroxy groups, e.g. sphingosine
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- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
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- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
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- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810556685 | 2018-05-31 | ||
| EP19810783.1A EP3804714B1 (en) | 2018-05-31 | 2019-05-28 | Pharmaceutical combination and composition, and combination preparation containing glucokinase activator and biguanide hypoglycemic drug as well as preparation method and use thereof |
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| US11813274B2 (en) * | 2020-04-22 | 2023-11-14 | Hua Medicine (Shanghai) Ltd. | Treating untreated or treatment-resistant diabetes with glucokinase activator and sodium-glucose cotransporter-2 inhibitor |
| WO2021212360A1 (en) * | 2020-04-22 | 2021-10-28 | Hua Medicine (Shanghai) Ltd. | Treating untreated or treatment-resistant diabetes with glucokinase activator and sodium-glucose cotransporter-2 inhibitor |
| CA3185831A1 (en) * | 2020-06-04 | 2021-12-09 | Hua Medicine (Shanghai) Ltd. | Glucokinase activator for treating diabetes with renal impairment |
| WO2021243646A1 (en) * | 2020-06-04 | 2021-12-09 | Hua Medicine (Shanghai) Ltd. | Glucokinase activator for treating diabetes with hepatic impairment |
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2020
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2022
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2023
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2024
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