HRP20151321T1 - Epalrestat ili njegov derivat u oblicima s prilagođenim otpuštanjem te postupci uporabe istih - Google Patents
Epalrestat ili njegov derivat u oblicima s prilagođenim otpuštanjem te postupci uporabe istih Download PDFInfo
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- HRP20151321T1 HRP20151321T1 HRP20151321TT HRP20151321T HRP20151321T1 HR P20151321 T1 HRP20151321 T1 HR P20151321T1 HR P20151321T T HRP20151321T T HR P20151321TT HR P20151321 T HRP20151321 T HR P20151321T HR P20151321 T1 HRP20151321 T1 HR P20151321T1
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- Croatia
- Prior art keywords
- pharmaceutical form
- epalrestat
- modified
- diabetic
- release pharmaceutical
- Prior art date
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- CHNUOJQWGUIOLD-NFZZJPOKSA-N epalrestat Chemical group C=1C=CC=CC=1\C=C(/C)\C=C1/SC(=S)N(CC(O)=O)C1=O CHNUOJQWGUIOLD-NFZZJPOKSA-N 0.000 title claims 10
- 229950010170 epalrestat Drugs 0.000 title claims 10
- CHNUOJQWGUIOLD-UHFFFAOYSA-N epalrestate Natural products C=1C=CC=CC=1C=C(C)C=C1SC(=S)N(CC(O)=O)C1=O CHNUOJQWGUIOLD-UHFFFAOYSA-N 0.000 title claims 10
- 238000000034 method Methods 0.000 title claims 3
- 239000000203 mixture Substances 0.000 title 1
- 125000000129 anionic group Chemical group 0.000 claims 10
- -1 hydroxypropyl ethyl Chemical group 0.000 claims 6
- 229920000642 polymer Polymers 0.000 claims 6
- 230000036470 plasma concentration Effects 0.000 claims 4
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims 3
- 230000001225 therapeutic effect Effects 0.000 claims 3
- 208000002249 Diabetes Complications Diseases 0.000 claims 2
- 206010012655 Diabetic complications Diseases 0.000 claims 2
- 150000001720 carbohydrates Chemical class 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 229920005862 polyol Polymers 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- SERLAGPUMNYUCK-DCUALPFSSA-N 1-O-alpha-D-glucopyranosyl-D-mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-DCUALPFSSA-N 0.000 claims 1
- 229920001817 Agar Polymers 0.000 claims 1
- 102000016912 Aldehyde Reductase Human genes 0.000 claims 1
- 108010053754 Aldehyde reductase Proteins 0.000 claims 1
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 229920001661 Chitosan Polymers 0.000 claims 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 claims 1
- 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
- HEBKCHPVOIAQTA-QWWZWVQMSA-N D-arabinitol Chemical compound OC[C@@H](O)C(O)[C@H](O)CO HEBKCHPVOIAQTA-QWWZWVQMSA-N 0.000 claims 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 claims 1
- FBPFZTCFMRRESA-ZXXMMSQZSA-N D-iditol Chemical compound OC[C@@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-ZXXMMSQZSA-N 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 208000032781 Diabetic cardiomyopathy Diseases 0.000 claims 1
- 206010051153 Diabetic gastroparesis Diseases 0.000 claims 1
- 206010063547 Diabetic macroangiopathy Diseases 0.000 claims 1
- 206010054044 Diabetic microangiopathy Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 239000001856 Ethyl cellulose Substances 0.000 claims 1
- 208000003790 Foot Ulcer Diseases 0.000 claims 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 claims 1
- 229920002907 Guar gum Polymers 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 1
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- SKCKOFZKJLZSFA-UHFFFAOYSA-N L-Gulomethylit Natural products CC(O)C(O)C(O)C(O)CO SKCKOFZKJLZSFA-UHFFFAOYSA-N 0.000 claims 1
- 229920000161 Locust bean gum Polymers 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 229920000881 Modified starch Polymers 0.000 claims 1
- 239000004368 Modified starch Substances 0.000 claims 1
- JVWLUVNSQYXYBE-UHFFFAOYSA-N Ribitol Natural products OCC(C)C(O)C(O)CO JVWLUVNSQYXYBE-UHFFFAOYSA-N 0.000 claims 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims 1
- 239000008272 agar Substances 0.000 claims 1
- 229960003237 betaine Drugs 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 230000005961 cardioprotection Effects 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 229920002678 cellulose Polymers 0.000 claims 1
- 229960001231 choline Drugs 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000009101 diabetic angiopathy Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 229920001249 ethyl cellulose Polymers 0.000 claims 1
- 235000019325 ethyl cellulose Nutrition 0.000 claims 1
- SKCKOFZKJLZSFA-FSIIMWSLSA-N fucitol Chemical compound C[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO SKCKOFZKJLZSFA-FSIIMWSLSA-N 0.000 claims 1
- FBPFZTCFMRRESA-GUCUJZIJSA-N galactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-GUCUJZIJSA-N 0.000 claims 1
- 229930182830 galactose Natural products 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 239000000665 guar gum Substances 0.000 claims 1
- 235000010417 guar gum Nutrition 0.000 claims 1
- 229960002154 guar gum Drugs 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229960003943 hypromellose Drugs 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000905 isomalt Substances 0.000 claims 1
- 235000010439 isomalt Nutrition 0.000 claims 1
- HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 claims 1
- 235000010420 locust bean gum Nutrition 0.000 claims 1
- 239000000711 locust bean gum Substances 0.000 claims 1
- 239000000845 maltitol Substances 0.000 claims 1
- 235000010449 maltitol Nutrition 0.000 claims 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 claims 1
- 229940035436 maltitol Drugs 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 239000011159 matrix material Substances 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000010981 methylcellulose Nutrition 0.000 claims 1
- 235000019426 modified starch Nutrition 0.000 claims 1
- 239000007935 oral tablet Substances 0.000 claims 1
- 229940096978 oral tablet Drugs 0.000 claims 1
- 229920001282 polysaccharide Polymers 0.000 claims 1
- 239000005017 polysaccharide Substances 0.000 claims 1
- HEBKCHPVOIAQTA-ZXFHETKHSA-N ribitol Chemical compound OC[C@H](O)[C@H](O)[C@H](O)CO HEBKCHPVOIAQTA-ZXFHETKHSA-N 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 239000000230 xanthan gum Substances 0.000 claims 1
- 229920001285 xanthan gum Polymers 0.000 claims 1
- 235000010493 xanthan gum Nutrition 0.000 claims 1
- 229940082509 xanthan gum Drugs 0.000 claims 1
- 239000000811 xylitol Substances 0.000 claims 1
- 235000010447 xylitol Nutrition 0.000 claims 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims 1
- 229960002675 xylitol Drugs 0.000 claims 1
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- 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
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
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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
- A61K9/20—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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- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
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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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
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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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2886—Dragees; Coated pills or tablets, e.g. with film or compression coating having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer
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- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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Claims (15)
1. Farmaceutski oblik s prilagođenim otpuštanjem, koji sadrži:
epalrestat ili njegov farmaceutski prikladan derivat;
polimer koji bubri u vodi i pH je neovisan;
anionski polimer koji nije na bazi celuloze i koji bubri u vodi;
i sredstvo na bazi saharida koje prilagođava brzinu otpuštanja.
2. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, koji,
(i) kada se daje bolesniku u redovnom režimu doziranja, daje relativno ravan profil koncentracije epalrestata u plazmi u stanju ravnoteže, pri čemu nema bitnih pikova ili valova u relativno ravnom profilu koncentracije u plazmi i minimalna koncentracija epalrestata u plazmi u relativno ravnom profilu koncentracije u plazmi jest dovoljna da omogući terapijski učinak u bolesnika; ili
(ii) kada se daje bolesniku u redovnom režimu doziranja, daje relativno ravan profil koncentracije epalrestata u plazmi u stanju ravnoteže tako da je srednji omjer Cmin/Cmax epalrestata tijekom intervala doziranja oko 0,55 do oko 1,0 i Cmin jest dovoljan da omogući terapijski učinak; ili
(iii) jest oblik za doziranje jednom ili dva puta dnevno, daje bolesniku terapijski učinak kroz oko 12 do oko 24 sata i relativno ravan profil koncentracije epalrestata u plazmi u stanju ravnoteže tako da minimalna koncentracija epalrestata u plazmi tijekom intervala doziranja iznosi oko 55% maksimalne koncentracije u plazmi tijekom intervala doziranja.
3. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje se polimer koji bubri u vodi i pH je neovisan izabire iz grupe koja obuhvaća hipromelozu, hidroksipropil etil celuloze, hidroksipropil celulozu, hidroksietil celulozu, metil celulozu i njihove kombinacije.
4. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje se anionski polimer koji nije na bazi celuloze i koji bubri u vodi izabire iz grupe koja obuhvaća anionske derivate agara; anionske derivate guar gume; anionske derivate karuba gume; anionske derivate ksantan gume; anionske derivate alginina; anionske derivate polisaharida manoze i galaktoze, ili kitosana; anionske derivate modificiranog škroba i njihove kombinacije.
5. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje je sredstvo na bazi saharida koje prilagođava brzinu otpuštanja poliolski spoj.
6. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 5, gdje se poliolski spoj izabire između arabitola, ksilitola, ribitola, manitola, sorbitola, dulcitola, fucitola, iditola, izomalta, maltitola i laktitiola.
7. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, koji je u matriksnoj formi, kao što je oralna tableta.
8. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje je težinski omjer polimera koji bubri u vodi i pH je neovisan prema anionskom polimeru koji nije na bazi celuloze i koji bubri u vodi od oko 2,5 : 1 do oko 1,5 : 1.
9. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje je epalrestat ili njegov farmaceutski prikladan derivat u količini od oko 30% do oko 45% težine.
10. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, gdje epalrestat ili njegov farmaceutski prikladan derivat jest kolin hidrogen diepalrestat ili betain hidrogen diepalrestat.
11. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, za uporabu u postupku koji obuhvaća primjenu bolesniku jednom ili dva puta dnevno.
12. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, za uporabu u postupku liječenja dijabetesa ili dijabetičke komplikacije kod subjekta kojem je to potrebno.
13. Farmaceutski oblik s prilagođenim otpuštanjem za uporabu prema zahtjevu 12, koja obuhvaća primjenu bolesniku jednom ili dva puta dnevno.
14. Farmaceutski oblik s prilagođenim otpuštanjem za uporabu prema zahtjevu 12, gdje se dijabetička komplikacija izabire iz grupe koju čine dijabetička neuropatija, dijabetička nefropatija, dijabetička kardiomiopatija, dijabetička retinopatija, dijabetička gastropareza, katarakte, čirevi stopala, dijabetička makroangiopatija, dijabetička mikroangiopatija, visoka razina glukoze u krvi, visoke razine HbA1c i njihove kombinacije.
15. Farmaceutski oblik s prilagođenim otpuštanjem prema zahtjevu 1, za uporabu u postupku inhibicije aldoza reduktaze kod subjekta kojem je to potrebno; ili za uporabu kardiozaštite kod subjekta kojem je to potrebno.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161434637P | 2011-01-20 | 2011-01-20 | |
| PCT/US2012/022094 WO2012100208A1 (en) | 2011-01-20 | 2012-01-20 | Modified release compositions of epalrestat or a derivative thereof and methods for using the same |
| EP12736674.8A EP2665477B1 (en) | 2011-01-20 | 2012-01-20 | Modified release compositions of epalrestat or a derivative thereof and methods for using the same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20151321T1 true HRP20151321T1 (hr) | 2016-01-29 |
Family
ID=46516126
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20151321TT HRP20151321T1 (hr) | 2011-01-20 | 2015-12-03 | Epalrestat ili njegov derivat u oblicima s prilagođenim otpuštanjem te postupci uporabe istih |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9566269B2 (hr) |
| EP (2) | EP2665477B1 (hr) |
| CY (1) | CY1117483T1 (hr) |
| DK (1) | DK2665477T3 (hr) |
| ES (1) | ES2555927T3 (hr) |
| HK (1) | HK1191569A1 (hr) |
| HR (1) | HRP20151321T1 (hr) |
| HU (1) | HUE026715T2 (hr) |
| PL (1) | PL2665477T3 (hr) |
| PT (1) | PT2665477E (hr) |
| RS (1) | RS54447B1 (hr) |
| RU (2) | RU2013135224A (hr) |
| SI (1) | SI2665477T1 (hr) |
| SM (1) | SMT201500307B (hr) |
| WO (1) | WO2012100208A1 (hr) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US9550780B2 (en) * | 2012-09-18 | 2017-01-24 | Auspex Pharmaceuticals, Inc. | Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2 |
| CN114796209A (zh) | 2015-03-06 | 2022-07-29 | 奥斯拜客斯制药有限公司 | 氘代丁苯那嗪或包含氘代丁苯那嗪的组合物 |
| CN104922052A (zh) * | 2015-06-09 | 2015-09-23 | 扬子江药业集团南京海陵药业有限公司 | 一种依帕司他缓释制剂及其制备方法和应用 |
| CN110548014B (zh) * | 2019-09-06 | 2022-02-01 | 南京康川济医药科技有限公司 | 一种依帕司他双层渗透泵控释片及其制备方法 |
| CN115721621A (zh) * | 2022-12-16 | 2023-03-03 | 杭州剂泰医药科技有限责任公司 | 一种依帕司他缓释制剂 |
Family Cites Families (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2996431A (en) | 1953-12-16 | 1961-08-15 | Barry Richard Henry | Friable tablet and process for manufacturing same |
| US2990332A (en) | 1958-04-02 | 1961-06-27 | Wallace & Tiernan Inc | Pharmaceutical preparations comprising cation exchange resin adsorption compounds and treatment therewith |
| US3138525A (en) | 1961-06-16 | 1964-06-23 | Hoffmann La Roche | Castor wax-amprotropine-resin compositions |
| US3499960A (en) | 1965-01-25 | 1970-03-10 | Merck & Co Inc | Palatable coated particles of an anion exchange resin |
| US3492397A (en) | 1967-04-07 | 1970-01-27 | Warner Lambert Pharmaceutical | Sustained release dosage in the pellet form and process thereof |
| US3594470A (en) | 1968-02-19 | 1971-07-20 | Abbott Lab | Chewable tablets including coated particles of pseudoephedrine-weak cation exchange resin |
| US3536809A (en) | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
| US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
| US3870790A (en) | 1970-01-22 | 1975-03-11 | Forest Laboratories | Solid pharmaceutical formulations containing hydroxypropyl methyl cellulose |
| DE2010416B2 (de) | 1970-03-05 | 1979-03-29 | Hoechst Ag, 6000 Frankfurt | Oral anwendbare Arzneiform mit Retardwirkung |
| 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 |
| US4167588A (en) | 1974-04-10 | 1979-09-11 | Willard Miles J | Preparation of fabricated baked potato product |
| US4008719A (en) | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
| US4140755A (en) | 1976-02-13 | 1979-02-20 | Hoffmann-La Roche Inc. | Sustained release tablet formulations |
| US4111202A (en) | 1976-11-22 | 1978-09-05 | Alza Corporation | Osmotic system for the controlled and delivery of agent over time |
| GB1561204A (en) | 1977-06-01 | 1980-02-13 | Ici Ltd | Sustained release pharmaceutical composition |
| US4226849A (en) | 1979-06-14 | 1980-10-07 | Forest Laboratories Inc. | Sustained release therapeutic compositions |
| US4357469A (en) | 1979-06-14 | 1982-11-02 | Forest Laboratories, Inc. | Carrier base material for prolonged release therapeutic compositions |
| US4259314A (en) | 1979-12-10 | 1981-03-31 | Hans Lowey | Method and composition for the preparation of controlled long-acting pharmaceuticals |
| JPS5740478A (en) | 1980-08-22 | 1982-03-06 | Ono Pharmaceut Co Ltd | Rhodanine derivative, its preparation and aldose reductase inhibitor containing rhodanine derivative |
| US4327725A (en) | 1980-11-25 | 1982-05-04 | Alza Corporation | Osmotic device with hydrogel driving member |
| US4369172A (en) | 1981-12-18 | 1983-01-18 | Forest Laboratories Inc. | Prolonged release therapeutic compositions based on hydroxypropylmethylcellulose |
| US4389393A (en) | 1982-03-26 | 1983-06-21 | Forest Laboratories, Inc. | Sustained release therapeutic compositions based on high molecular weight hydroxypropylmethylcellulose |
| US4415547A (en) | 1982-06-14 | 1983-11-15 | Sterling Drug Inc. | Sustained-release pharmaceutical tablet and process for preparation thereof |
| US4783337A (en) | 1983-05-11 | 1988-11-08 | Alza Corporation | Osmotic system comprising plurality of members for dispensing drug |
| US5082668A (en) | 1983-05-11 | 1992-01-21 | Alza Corporation | Controlled-release system with constant pushing source |
| US4765989A (en) | 1983-05-11 | 1988-08-23 | Alza Corporation | Osmotic device for administering certain drugs |
| US4612008A (en) | 1983-05-11 | 1986-09-16 | Alza Corporation | Osmotic device with dual thermodynamic activity |
| US4894240A (en) | 1983-12-22 | 1990-01-16 | Elan Corporation Plc | Controlled absorption diltiazem formulation for once-daily administration |
| US4540566A (en) | 1984-04-02 | 1985-09-10 | Forest Laboratories, Inc. | Prolonged release drug dosage forms based on modified low viscosity grade hydroxypropylmethylcellulose |
| IE58110B1 (en) | 1984-10-30 | 1993-07-14 | Elan Corp Plc | Controlled release powder and process for its preparation |
| IT1188212B (it) | 1985-12-20 | 1988-01-07 | Paolo Colombo | Sistema per il rilascio a velocita' controllata di sostanze attive |
| US4786503A (en) | 1987-04-06 | 1988-11-22 | Alza Corporation | Dosage form comprising parallel lamine |
| US4894239A (en) | 1987-06-02 | 1990-01-16 | Takeda Chemical Industries, Ltd. | Sustained-release preparation and production thereof |
| US5073543A (en) | 1988-07-21 | 1991-12-17 | G. D. Searle & Co. | Controlled release formulations of trophic factors in ganglioside-lipsome vehicle |
| IT1229203B (it) | 1989-03-22 | 1991-07-25 | Bioresearch Spa | Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative. |
| US5120548A (en) | 1989-11-07 | 1992-06-09 | Merck & Co., Inc. | Swelling modulated polymeric drug delivery device |
| US5733566A (en) | 1990-05-15 | 1998-03-31 | Alkermes Controlled Therapeutics Inc. Ii | Controlled release of antiparasitic agents in animals |
| US5591767A (en) | 1993-01-25 | 1997-01-07 | Pharmetrix Corporation | Liquid reservoir transdermal patch for the administration of ketorolac |
| IT1270594B (it) | 1994-07-07 | 1997-05-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida |
| TWI238064B (en) | 1995-06-20 | 2005-08-21 | Takeda Chemical Industries Ltd | A pharmaceutical composition for prophylaxis and treatment of diabetes |
| US5811126A (en) | 1995-10-02 | 1998-09-22 | Euro-Celtique, S.A. | Controlled release matrix for pharmaceuticals |
| US6274171B1 (en) | 1996-03-25 | 2001-08-14 | American Home Products Corporation | Extended release formulation of venlafaxine hydrochloride |
| US6919373B1 (en) | 1996-11-12 | 2005-07-19 | Alza Corporation | Methods and devices for providing prolonged drug therapy |
| UA57811C2 (uk) | 1997-11-21 | 2003-07-15 | Пфайзер Продактс Інк. | Фармацевтична композиція, що містить інгібітор альдозоредуктази та інгібітор глікогенфосфорилази (варіанти), комплект, який її включає, та способи лікування ссавців зі станом інсулінорезистентності |
| EP1106210A3 (en) | 1999-12-07 | 2003-12-03 | Pfizer Products Inc. | Combination of aldose reductase inhibitors and antihypertensive agents for the treatment of diabetic complications |
| PL202623B1 (pl) | 2000-06-28 | 2009-07-31 | Smithkline Beecham Plc | Sposób wytwarzania drobno zmielonego preparatu substancji leczniczej, drobno zmielona substancja lecznicza wytworzona tym sposobem i zawierająca ją kompozycja farmaceutyczna |
| AU2002355686B2 (en) * | 2001-07-04 | 2007-11-29 | Sun Pharmaceutical Industries Limited | Gastric retention controlled drug delivery system |
| ATE415150T1 (de) | 2002-08-16 | 2008-12-15 | Orchid Chemicals & Pharm Ltd | Pharmazeutische zusammensetzung mit verzögerte freisetzung enthaltend einen cephalosporin- antibiotikum |
| JP4552189B2 (ja) * | 2002-11-14 | 2010-09-29 | 小野薬品工業株式会社 | 脊柱管狭窄症治療剤 |
| US7101912B2 (en) | 2002-12-06 | 2006-09-05 | Xenoport, Inc. | Carbidopa prodrugs and derivatives, and compositions and uses thereof |
| JP3547010B1 (ja) | 2002-12-27 | 2004-07-28 | 小野薬品工業株式会社 | ５−［（１ｚ，２ｅ）−２−メチル−３−フェニル−２−プロペニリデン］−４−オキソ−２−チオキソ−３−チアゾリジン酢酸の結晶の製造方法およびその製剤 |
| WO2004108067A2 (en) | 2003-04-03 | 2004-12-16 | Sun Pharmaceutical Industries Limited | Programmed drug delivery system |
| EP1642593A1 (en) * | 2003-06-06 | 2006-04-05 | Takeda Pharmaceutical Company Limited | Solid pharmaceutical preparation |
| JP2005139085A (ja) * | 2003-11-04 | 2005-06-02 | Ono Pharmaceut Co Ltd | 顆粒 |
| WO2005055983A2 (en) | 2003-12-09 | 2005-06-23 | Medcrystalforms, Llc | Method of preparation of mixed phase co-crystals with active agents |
| JP2005298424A (ja) | 2004-04-13 | 2005-10-27 | Sawai Pharmaceutical Co Ltd | エパルレスタット結晶の製造方法 |
| CA2566771A1 (en) * | 2004-06-07 | 2005-12-22 | Wyeth | Sugar coatings and methods therefor |
| FR2891459B1 (fr) * | 2005-09-30 | 2007-12-28 | Flamel Technologies Sa | Microparticules a liberation modifiee d'au moins un principe actif et forme galenique orale en comprenant |
| JP4892915B2 (ja) | 2005-10-04 | 2012-03-07 | 大日本印刷株式会社 | エパルレスタット製造法 |
| WO2007090883A1 (en) | 2006-02-10 | 2007-08-16 | Boehringer Ingelheim International Gmbh | Extended release formulation |
| US20090270490A1 (en) | 2008-04-24 | 2009-10-29 | The Board Of Regents Of The University Of Texas System | Methods involving aldose reductase inhibition |
| WO2010011926A2 (en) | 2008-07-25 | 2010-01-28 | Bionevia Pharmaceuticals, Inc. | A novel betaine cocrystal of epalrestat |
| WO2010011922A2 (en) | 2008-07-25 | 2010-01-28 | Bionevia Pharmaceuticals, Inc. | Novel crystalline salts of epalrestat |
| ES2639019T3 (es) * | 2008-09-06 | 2017-10-25 | Bionevia Pharmaceuticals Inc. | Nuevo cocristal de colina de epalrestat |
| US20100203129A1 (en) * | 2009-01-26 | 2010-08-12 | Egalet A/S | Controlled release formulations with continuous efficacy |
| US8320844B2 (en) * | 2009-07-17 | 2012-11-27 | Broadcom Corporation | Configurable transceiver integrated circuit |
| JP5781062B2 (ja) * | 2010-03-03 | 2015-09-16 | 救急薬品工業株式会社 | 不快な味を有する薬物を含有するフィルム製剤 |
-
2012
- 2012-01-20 PT PT127366748T patent/PT2665477E/pt unknown
- 2012-01-20 PL PL12736674T patent/PL2665477T3/pl unknown
- 2012-01-20 WO PCT/US2012/022094 patent/WO2012100208A1/en active Application Filing
- 2012-01-20 RU RU2013135224/15A patent/RU2013135224A/ru unknown
- 2012-01-20 EP EP12736674.8A patent/EP2665477B1/en active Active
- 2012-01-20 SI SI201230394T patent/SI2665477T1/sl unknown
- 2012-01-20 US US13/980,744 patent/US9566269B2/en active Active
- 2012-01-20 HU HUE12736674A patent/HUE026715T2/en unknown
- 2012-01-20 ES ES12736674.8T patent/ES2555927T3/es active Active
- 2012-01-20 RS RS20150823A patent/RS54447B1/en unknown
- 2012-01-20 EP EP15184332.3A patent/EP3042654A1/en not_active Withdrawn
- 2012-01-20 RU RU2017124629A patent/RU2017124629A/ru not_active Application Discontinuation
- 2012-01-20 DK DK12736674.8T patent/DK2665477T3/en active
-
2014
- 2014-05-26 HK HK14104930.9A patent/HK1191569A1/zh not_active IP Right Cessation
-
2015
- 2015-12-03 HR HRP20151321TT patent/HRP20151321T1/hr unknown
- 2015-12-08 CY CY20151101111T patent/CY1117483T1/el unknown
- 2015-12-09 SM SM201500307T patent/SMT201500307B/it unknown
-
2017
- 2017-02-13 US US15/431,204 patent/US20180000792A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| RS54447B1 (en) | 2016-06-30 |
| PT2665477E (pt) | 2016-01-12 |
| RU2017124629A3 (hr) | 2019-01-30 |
| EP2665477A4 (en) | 2014-07-09 |
| HK1191569A1 (zh) | 2014-08-01 |
| SMT201500307B (it) | 2016-02-25 |
| ES2555927T3 (es) | 2016-01-11 |
| EP2665477A1 (en) | 2013-11-27 |
| RU2013135224A (ru) | 2015-03-10 |
| US20180000792A1 (en) | 2018-01-04 |
| SI2665477T1 (sl) | 2016-02-29 |
| EP3042654A1 (en) | 2016-07-13 |
| EP2665477B1 (en) | 2015-09-09 |
| WO2012100208A1 (en) | 2012-07-26 |
| RU2017124629A (ru) | 2019-01-30 |
| US20140296309A1 (en) | 2014-10-02 |
| CY1117483T1 (el) | 2017-04-26 |
| DK2665477T3 (en) | 2015-12-14 |
| HUE026715T2 (en) | 2016-07-28 |
| US9566269B2 (en) | 2017-02-14 |
| PL2665477T3 (pl) | 2016-05-31 |
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