DK2482806T3 - Farmaceutisk sammensætning, farmaceutisk doseringsform, fremgangsmåde til fremstilling deraf, fremgangsmåder til behandling og anvendelser deraf - Google Patents
Farmaceutisk sammensætning, farmaceutisk doseringsform, fremgangsmåde til fremstilling deraf, fremgangsmåder til behandling og anvendelser deraf Download PDFInfo
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- DK2482806T3 DK2482806T3 DK10759923.5T DK10759923T DK2482806T3 DK 2482806 T3 DK2482806 T3 DK 2482806T3 DK 10759923 T DK10759923 T DK 10759923T DK 2482806 T3 DK2482806 T3 DK 2482806T3
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- pharmaceutical composition
- inhibitor
- sglt
- metformin
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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- A—HUMAN NECESSITIES
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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Claims (13)
1. Fast farmaceutisk sammensætning omfattende SGLT-2-hæmmeren l-chlor-4-(p-D-glukopyranos-l-yl)-2-[4-(('S/)-tetrahydrofuran-3-yloxy)-benzyl]-benzen, metforminhydro-chlorid og en eller flere farmaceutiske excipienser, hvor SGLT-2-hæmmeren er til stede i en doseringsstyrke på 5 mg eller 12,5 mg, og hvor metforminhydrochlorid er til stede i en doseringsstyrke på 500 mg, 850 mg eller 1000 mg, og hvor den faste farmaceutiske sammensætning omfatter copovidon som bindemiddel.
2. Farmaceutisk sammensætning ifølge krav 1, hvor excipienserne er udvalgt fra gruppen bestående af et eller fyldstoffer indbefattende mikrokrystallinsk cellulose; D-mannitol, majsstivelse og prægelatineret stivelse; et bindemiddel indbefattende copovidon; et smøremiddel indbefattende magnesiumstearat eller natriumstearylfumarat; og et glidemiddel indbefattende kolloid vandfri siliciumdioxid.
3. Farmaceutisk sammensætning ifølge krav 2, yderligere omfattende en eller flere blandt følgende: fyldstoffet majsstivelse, smøremidlet magnesiumstearat eller natriumstearylfumarat og glidemidlet kolloid vandfri siliciumdioxid.
4. Farmaceutisk sammensætning ifølge krav 2, yderligere omfattende en eller flere blandt følgende: fyldstoffet mikrokrystallinsk cellulose, smøremidlet magnesiumstearat eller natriumstearylfumarat og glidemidlet kolloid vandfri siliciumdioxid.
5. Fast farmaceutisk sammensætning ifølge et eller flere af de foregående krav, omfattende en eller flere af følgende mængder (% efter vægt af samlet overtrukket tabletmasse): 0,1-2,11 % SGLT-2-hæmmer, 47-88 % metformin HCI, 3.9- 8,3 % bindemiddel (f.eks. copovidon), 2.3- 8,0 % fyldstof 1 (f.eks. majsstivelse), 0-4,4 % fyldstof 2 (f.eks. prægelatiniseret stivelse), 0-33 % fyldstof 3 (f.eks. D-mannitol), 0,7-1,5 % smøremiddel (f.eks. magnesiumstearat), 0,05-0,5 % glidemiddel (f.eks. kolloid vandfri siliciumdioxid), 0,00-3,0 % desintegrationsmiddel (f.eks. crospovidon eller croscarmello- senatrium)
6. Fast farmaceutisk sammensætning ifølge et eller flere af de foregående krav, omfattende en eller flere af følgende mængder (% efter vægt af samlet overtrukket tabletmasse): 0,1-2,11 % SGLT-2-hæmmer, 47-88 % metformin HCI, 3.9- 8,3 % copovidon som bindemiddel, 2.3- 8,0 % majsstivelse som fyldstof, 0-4,4 % prægelatiniseret stivelse som fyldstof, 0-33 % D-mannitol som fyldstof, 0,7-1,5 % magnesiumstearat som smøremiddel, 0,05-0,5 % kolloid vandfri siliciumdioxid som glidemiddel, 0,00-3,0 % crospovidon eller croscarmellosenatrium som desintegrations middel.
7. Farmaceutisk sammensætning ifølge et hvilket som helst af kravene 1 til 6 på tabletdoseringsform.
8. Farmaceutisk doseringsform omfattende en farmaceutisk sammensætning ifølge et eller flere af kravene 1 til 7, kendetegnet ved, at der er tale om en fast farmaceutisk doseringsform, og at doseringsformen er en kapsel eller en tablet.
9. Farmaceutisk doseringsform ifølge et af kravene 1 til 7 til anvendelse i - forebyggelse, hæmning, forsinkelse eller behandling af en stofskifteforstyrrelse udvalgt fra gruppen bestående af type 1-diabetes mellitus, type 2-diabetes mellitus, nedsat glukosetolerance, nedsat fasteblodsukker, hyperglykæmi, postprandial hyperglyk-æmi, overvægt, svær overvægt og metabolisk syndrom; eller - forbedring af glykæmisk styring og/eller reduktion af fasteplasmaglukose, af postprandial plasmaglukose og/eller glykosyleret hæmoglobin HbAlc; eller - forebyggelse, hæmning, forsinkelse eller tilbagerulning af fremadskriden fra nedsat glukosetolerance, insulinresistens og/eller metabolisk syndrom til type 2-diabetes mellitus; eller - forebyggelse, hæmning, forsinkelse eller behandling af en tilstand eller lidelse udvalgt fra gruppen bestående af komplikationer til diabetes mellitus så som grå stær og mikro- og makrovaskulære sygdomme, såsom nefropati, retinopati, neuropati, vævsiskæmi, arteriosklerose, myokardinfarkt, slagtilfælde og perifer arterieokklusi-onssygdom; eller - forebyggelse, hæmning, forsinkelse eller behandling af degeneration af bugspytkir-tel-betaceller og/eller faldende funktionalitet af bugspytkirtel-betaceller og/eller til forbedring og/eller genoprettelse af funktionaliteten af bugspytkirtel-betaceller og/eller genoprettelse af funktionaliteten af bugspytkirtelinsulinsekretion; eller - til forebyggelse, hæmning, forsinkelse eller behandling af sygdomme eller tilstande, der tilskrives en abnorm ophobning af leverfedt; eller - opretholdelse og/eller forbedring af insulinsensitivitet og/eller til behandling eller forebyggelse af hyperinsulinæmi og/eller insulinresistens; hos en patient med behov derfor.
10. Farmaceutisk sammensætning til anvendelse ifølge krav 9, hvor patienten er et individ, der er diagnosticeret med en eller flere tilstande udvalgt fra gruppen bestående af overvægt, svær overvægt, indvoldsfedme og bugfedme.
11. Farmaceutisk sammensætning til anvendelse ifølge krav 9, hvor patienten er et individ, som udviser en, to eller flere af følgende tilstande: (a) et fasteblodsukker eller serumglukosekoncentration på over 110 mg/dl, navnlig over 125 mg/dl; (b) postprandial plasmaglukose lig med eller større end 140 mg/dl; (c) en HbAlc-værdi lig med eller større end 6,5 %, navnlig lig med eller større end 7,0%.
12. Farmaceutisk sammensætning til anvendelse ifølge krav 9, hvor patienten er et individ, hvorhos en, to, tre eller flere af de følgende tilstande gør sig gældende: (a) svær overvægt, indvoldsfedme og/eller bugfedme, (b) triglyceridblodindhold >150 mg/dl, (c) HDL-kolesterolblodindhold < 40 mg/dl hos kvindelige patienter og < 50 mg/dl hos mandlige patienter, (d) et systolisk blodtryk >130 mm Hg og et diastolisk blodtryk >85 mm Hg, (e) et fasteblodsukkerindhold >110 mg/dl.
13. Farmaceutisk sammensætning til anvendelse ifølge krav 9, hvor patienten har utilstrækkelig glykæmisk styring på trods af kost og motion eller på trods af monoterapi med et middel mod sukkersyge, navnlig metformin.
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PCT/EP2010/064619 WO2011039337A1 (en) | 2009-10-02 | 2010-10-01 | Pharmaceutical composition, pharmaceutical dosage form, process for their preparation, methods for treating and uses thereof |
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DK16195805.3T DK3150200T3 (da) | 2009-10-02 | 2010-10-01 | Fremgangsmåde til fremstilling af en tablet som består af en sglt-2-hæmmer og metformin |
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