HRP20120072T1 - Farmaceutske formulacije koje sadrže klopidogrel - Google Patents
Farmaceutske formulacije koje sadrže klopidogrel Download PDFInfo
- Publication number
- HRP20120072T1 HRP20120072T1 HR20120072T HRP20120072T HRP20120072T1 HR P20120072 T1 HRP20120072 T1 HR P20120072T1 HR 20120072 T HR20120072 T HR 20120072T HR P20120072 T HRP20120072 T HR P20120072T HR P20120072 T1 HRP20120072 T1 HR P20120072T1
- Authority
- HR
- Croatia
- Prior art keywords
- clopidogrel
- preparation according
- weight
- preparation
- pharmaceutically acceptable
- Prior art date
Links
- GKTWGGQPFAXNFI-HNNXBMFYSA-N clopidogrel Chemical compound C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl GKTWGGQPFAXNFI-HNNXBMFYSA-N 0.000 title claims 9
- 239000005552 B01AC04 - Clopidogrel Substances 0.000 title claims 7
- 229960003009 clopidogrel Drugs 0.000 title claims 7
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 7
- 239000000203 mixture Substances 0.000 claims abstract 5
- 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 abstract 2
- 239000000314 lubricant Substances 0.000 claims 5
- 229950010562 clopidogrel hydrobromide Drugs 0.000 claims 4
- 229950010477 clopidogrel hydrogen sulphate Drugs 0.000 claims 4
- FDEODCTUSIWGLK-UHFFFAOYSA-N hydrogen sulfate;hydron;methyl 2-(2-chlorophenyl)-2-(6,7-dihydro-4h-thieno[3,2-c]pyridin-5-yl)acetate Chemical compound OS(O)(=O)=O.C1CC=2SC=CC=2CN1C(C(=O)OC)C1=CC=CC=C1Cl FDEODCTUSIWGLK-UHFFFAOYSA-N 0.000 claims 4
- QKLHYWAZTQRTBR-RSAXXLAASA-N methyl (2s)-2-(2-chlorophenyl)-2-(6,7-dihydro-4h-thieno[3,2-c]pyridin-5-yl)acetate;hydrobromide Chemical compound Br.C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl QKLHYWAZTQRTBR-RSAXXLAASA-N 0.000 claims 4
- 239000007884 disintegrant Substances 0.000 claims 3
- 229920002472 Starch Polymers 0.000 claims 2
- 229950010557 clopidogrel besilate Drugs 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- GNWCZBXSKIIURR-UHFFFAOYSA-N (2-docosanoyloxy-3-hydroxypropyl) docosanoate Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(CO)OC(=O)CCCCCCCCCCCCCCCCCCCCC GNWCZBXSKIIURR-UHFFFAOYSA-N 0.000 claims 1
- SERLAGPUMNYUCK-YJOKQAJESA-N 6-O-alpha-D-glucopyranosyl-D-glucitol 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-YJOKQAJESA-N 0.000 claims 1
- 229920002261 Corn starch Polymers 0.000 claims 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- SZYSLWCAWVWFLT-UTGHZIEOSA-N [(2s,3s,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)-2-[(2r,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxolan-2-yl]methyl octadecanoate Chemical group O([C@@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@]1(COC(=O)CCCCCCCCCCCCCCCCC)O[C@H](CO)[C@@H](O)[C@@H]1O SZYSLWCAWVWFLT-UTGHZIEOSA-N 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229950010560 clopidogrel hydrochloride Drugs 0.000 claims 1
- 239000008120 corn starch Substances 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 238000007907 direct compression Methods 0.000 claims 1
- 238000007908 dry granulation Methods 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- XLYOFNOQVPJJNP-ZSJDYOACSA-N heavy water Substances [2H]O[2H] XLYOFNOQVPJJNP-ZSJDYOACSA-N 0.000 claims 1
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims 1
- 239000001341 hydroxy propyl starch Substances 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 235000013828 hydroxypropyl starch Nutrition 0.000 claims 1
- 229960003511 macrogol Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- XIHVAFJSGWDBGA-RSAXXLAASA-N methyl (2s)-2-(2-chlorophenyl)-2-(6,7-dihydro-4h-thieno[3,2-c]pyridin-5-yl)acetate;hydrochloride Chemical compound Cl.C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl XIHVAFJSGWDBGA-RSAXXLAASA-N 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 229960000502 poloxamer Drugs 0.000 claims 1
- 229920001983 poloxamer Polymers 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 229920001592 potato starch Polymers 0.000 claims 1
- 229940069328 povidone Drugs 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- -1 sucrose ester Chemical class 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- VOCBWIIFXDYGNZ-IXKNJLPQSA-N testosterone enanthate Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCC)[C@@]1(C)CC2 VOCBWIIFXDYGNZ-IXKNJLPQSA-N 0.000 claims 1
- 238000005550 wet granulation Methods 0.000 claims 1
- 239000008203 oral pharmaceutical composition Substances 0.000 abstract 2
- 239000003085 diluting agent Substances 0.000 abstract 1
- 235000010439 isomalt Nutrition 0.000 abstract 1
- 239000000905 isomalt Substances 0.000 abstract 1
- HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K31/4353—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
- A61K31/4365—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 having sulfur as a ring hetero atom, e.g. ticlopidine
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
Abstract
Pripravak u obliku tablete, naznačen time što navedena tableta sadrži farmaceutski prihvatljivu sol klopidogrela i izomaltit. Patent sadrži još 18 patentnih zahtjeva.
Claims (19)
1. Pripravak u obliku tablete, naznačen time što navedena tableta sadrži farmaceutski prihvatljivu sol klopidogrela i izomaltit.
2. Pripravak u skladu s patentnim zahtjevom 1, naznačen time što se farmaceutski prihvatljivu sol klopidogrela bira iz skupine koju čine klopidogrela-hidrogensulfat, klopidogrel-hidrobromid, klopidogrel hidroklorid, klopidogrel-besilat, te klopidogrel-mesilat.
3. Pripravak u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je farmaceutski prihvatljiva sol klopidogrela klopidogrel-hidrobromid.
4. Pripravak u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je farmaceutski prihvatljiva sol klopidogrela klopidogrel-hidrogensulfat.
5. Pripravak u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je farmaceutski prihvatljiva sol klopidogrela klopidogrel-besilat.
6. Pripravak u skladu s patentnim zahtjevom 3, naznačen time što je Oblik A klopidogrel-hidrobromida klopidogrel-hidrobromida.
7. Pripravak u skladu s patentnim zahtjevom 4, naznačen time što je klopidogrel-hidrogensulfat Oblik 1 klopidogrel-hidrogensulfata.
8. Pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što je količina izomaltita između 30 i 65%, težinski, poželjnije između 39 i 50%, težinski, u odnosu na ukupnu težinu pripravka.
9. Pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time što se izomaltit tako bira da ima težinski odnos između 1,1-GPM·2H2O i 1,6-GPS između 1:6 i 4:1, poželjnije između 1:4 i 2:1.
10. Pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što dodatno sadrži mazivo, izborno pomiješano s talkom.
11. Pripravak u skladu s patentnim zahtjevom 10, naznačen time što se mazivo bira između jednog ili više od sljedećeg: glicerol-dibehenata, hidrogeniranih biljnih ulja, glicerol-mono/di/tripalmitatnih/stearatnih estera, makrogol 3000-6000, stearinske kiseline, poloksamera, te estera saharoze s masnim kiselinama.
12. Pripravak u skladu s patentnim zahtjevom 11, naznačen time što je mazivo saharozni stearat.
13. Pripravak u skladu s bilo kojim od patentnih zahtjeva 10 do 12, naznačen time što količina maziva je 0,5-7%, težinski, poželjnije 1-5%, težinski, u odnosu na ukupnu težinu pripravka.
14. Pripravak u skladu s bilo kojim od patentnih zahtjeva 1 do 13, naznačen time što dodatno sadrži sredstvo za raspadanje.
15. Pripravak u skladu s patentnim zahtjevom 14, naznačen time što sredstvo za raspadanje se bira između jednog ili više od sljedećeg: umreženog povidona, hidroksipropilceluloze i drugih vrsta škroba, koje se bira između kukuruznog škroba, krumpirovog škroba, djelomičnog alfa-škroba i hidroksipropilškroba.
16. Pripravak u skladu s patentnim zahtjevom 14 ili 15, naznačen time što je količina sredstva za raspadanje 1 do 20%, težinski, a poželjnije 2 do 15%, težinski, u odnosu na ukupnu težinu pripravka.
17. Pripravak u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što sadrži sljedeću kvantitativnu formulaciju:
– farmaceutski prihvatljiva sol klopidogrela: 25-50%, težinski
– izomaltit: 30-65%, težinski
– sredstvo za raspadanje: 1-20%, težinski
– mazivo: 0,5-7%, težinski.
18. Pripravak u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je dodatno obložen filmom.
19. Postupak dobivanja pripravka u skladu s patentnim zahtjevima 1 do 17, naznačen time što ga se provodi izravnim komprimiranjem, vlažnim granuliranjem ili suhim granuliranjem njegovih komponenata.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP08380057A EP2095815B1 (en) | 2008-02-26 | 2008-02-26 | Pharmaceutical formulations containing clopidogrel |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20120072T1 true HRP20120072T1 (hr) | 2012-02-29 |
Family
ID=39561443
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20120072T HRP20120072T1 (hr) | 2008-02-26 | 2012-01-23 | Farmaceutske formulacije koje sadrže klopidogrel |
Country Status (6)
Country | Link |
---|---|
US (1) | US20090214646A1 (hr) |
EP (1) | EP2095815B1 (hr) |
AT (1) | ATE530172T1 (hr) |
ES (1) | ES2376057T3 (hr) |
HR (1) | HRP20120072T1 (hr) |
PT (1) | PT2095815E (hr) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102480987B (zh) * | 2009-08-18 | 2015-02-25 | 卡吉尔公司 | 压缩异麦芽糖酮醇的方法 |
CN103181885A (zh) * | 2011-12-30 | 2013-07-03 | 北京韩美药品有限公司 | 氯吡格雷的固体制剂及制备方法 |
HUP1400294A2 (hu) | 2014-06-13 | 2015-12-28 | Skillpharm Kft | Clopidogrel új alkalmazása |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2530247B1 (fr) | 1982-07-13 | 1986-05-16 | Sanofi Sa | Nouveaux derives de la thieno (3, 2-c) pyridine, leur procede de preparation et leur application therapeutique |
FR2623810B2 (fr) * | 1987-02-17 | 1992-01-24 | Sanofi Sa | Sels de l'alpha-(tetrahydro-4,5,6,7 thieno(3,2-c) pyridyl-5) (chloro-2 phenyl) -acetate de methyle dextrogyre et compositions pharmaceutiques en contenant |
FR2779726B1 (fr) | 1998-06-15 | 2001-05-18 | Sanofi Sa | Forme polymorphe de l'hydrogenosulfate de clopidogrel |
CN1343128B (zh) * | 1999-03-17 | 2010-04-21 | 第一制药株式会社 | 药物组合物 |
CA2363053C (en) * | 2001-11-09 | 2011-01-25 | Bernard Charles Sherman | Clopidogrel bisulfate tablet formulation |
GB2393181A (en) | 2002-09-19 | 2004-03-24 | Cipla Ltd | Amorphous clopidogrel |
GB0325603D0 (en) * | 2003-11-03 | 2003-12-10 | Sandoz Ag | Organic compounds |
WO2005070464A2 (en) | 2004-01-21 | 2005-08-04 | Biofarma Ilac Sanayi Ve Ticaret A.S. | A tablet formulation of clopidogrel bisulphate |
CN1997648A (zh) * | 2004-04-20 | 2007-07-11 | 赛诺菲-安万特 | (+)-(S)-α-(2-氯苯基)-6,7-二氢噻吩并[3,2-C]吡啶-5(4H)乙酸甲酯氢溴酸盐,即氯吡格雷氢溴酸盐的多晶型物 |
KR20070009851A (ko) | 2005-07-14 | 2007-01-19 | 씨제이 주식회사 | 클로피도그렐 황산수소염 함유 약학 조성물 |
KR20070044323A (ko) | 2005-10-24 | 2007-04-27 | 에스케이케미칼주식회사 | 보관안정성이 개선된 클로피도그렐 황산수소염 함유 경구용제제 |
IS2385B (is) | 2006-02-10 | 2008-07-15 | Actavis Group Hf. | Klópidógrel bísúlfat lyfjasamsetningar |
ATE464881T1 (de) | 2006-04-13 | 2010-05-15 | Riemser Specialty Production Gmbh | Partialglyceride als schmiermittel für pharmazeutische zusammensetzungen enthaltend thienoä3,2-cüpyridin-derivate |
-
2008
- 2008-02-26 AT AT08380057T patent/ATE530172T1/de not_active IP Right Cessation
- 2008-02-26 PT PT08380057T patent/PT2095815E/pt unknown
- 2008-02-26 ES ES08380057T patent/ES2376057T3/es active Active
- 2008-02-26 EP EP08380057A patent/EP2095815B1/en active Active
- 2008-04-28 US US12/110,555 patent/US20090214646A1/en not_active Abandoned
-
2012
- 2012-01-23 HR HR20120072T patent/HRP20120072T1/hr unknown
Also Published As
Publication number | Publication date |
---|---|
PT2095815E (pt) | 2012-02-03 |
EP2095815B1 (en) | 2011-10-26 |
US20090214646A1 (en) | 2009-08-27 |
EP2095815A1 (en) | 2009-09-02 |
ATE530172T1 (de) | 2011-11-15 |
ES2376057T3 (es) | 2012-03-08 |
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