CA2675538C - Oral pharmaceutical compositions comprising unmicronized nebivolol or a nebivolol analogue as active ingredient, and a decreased ratio of wetting agent to active ingredient - Google Patents
Oral pharmaceutical compositions comprising unmicronized nebivolol or a nebivolol analogue as active ingredient, and a decreased ratio of wetting agent to active ingredient Download PDFInfo
- Publication number
- CA2675538C CA2675538C CA2675538A CA2675538A CA2675538C CA 2675538 C CA2675538 C CA 2675538C CA 2675538 A CA2675538 A CA 2675538A CA 2675538 A CA2675538 A CA 2675538A CA 2675538 C CA2675538 C CA 2675538C
- Authority
- CA
- Canada
- Prior art keywords
- nebivolol
- wetting agent
- active ingredient
- pharmaceutical composition
- polysorbate
- 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.)
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Links
- KOHIRBRYDXPAMZ-YHBROIRLSA-N (S,R,R,R)-nebivolol Chemical compound C1CC2=CC(F)=CC=C2O[C@H]1[C@H](O)CNC[C@@H](O)[C@H]1OC2=CC=C(F)C=C2CC1 KOHIRBRYDXPAMZ-YHBROIRLSA-N 0.000 title claims abstract description 65
- 239000000080 wetting agent Substances 0.000 title claims abstract description 52
- 229960000619 nebivolol Drugs 0.000 title claims abstract description 51
- 239000004480 active ingredient Substances 0.000 title claims abstract description 44
- 230000003247 decreasing effect Effects 0.000 title description 2
- 239000008203 oral pharmaceutical composition Substances 0.000 title description 2
- 239000000203 mixture Substances 0.000 claims abstract description 46
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 39
- 238000000034 method Methods 0.000 claims abstract description 28
- 150000003839 salts Chemical class 0.000 claims abstract description 27
- 208000019553 vascular disease Diseases 0.000 claims abstract description 5
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 22
- JWEXHQAEWHKGCW-VCVZPGOSSA-N (S,R,R,R)-nebivolol hydrochloride Chemical compound [Cl-].C1CC2=CC(F)=CC=C2O[C@H]1[C@H](O)C[NH2+]C[C@@H](O)[C@H]1OC2=CC=C(F)C=C2CC1 JWEXHQAEWHKGCW-VCVZPGOSSA-N 0.000 claims description 21
- 229940068174 nebivolol hydrochloride Drugs 0.000 claims description 21
- 238000004090 dissolution Methods 0.000 claims description 18
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 17
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims description 17
- 239000000945 filler Substances 0.000 claims description 17
- 239000011230 binding agent Substances 0.000 claims description 16
- 239000007884 disintegrant Substances 0.000 claims description 14
- 239000000314 lubricant Substances 0.000 claims description 13
- 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 description 12
- 239000002245 particle Substances 0.000 claims description 12
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 12
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 12
- 229940068968 polysorbate 80 Drugs 0.000 claims description 12
- 229920000053 polysorbate 80 Polymers 0.000 claims description 12
- 229920002261 Corn starch Polymers 0.000 claims description 11
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 11
- 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 claims description 11
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 11
- 239000008120 corn starch Substances 0.000 claims description 11
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 11
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 11
- 229960001375 lactose Drugs 0.000 claims description 11
- 239000008101 lactose Substances 0.000 claims description 11
- 235000019359 magnesium stearate Nutrition 0.000 claims description 11
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 11
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- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 10
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 10
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 10
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group 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 description 10
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- 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 description 9
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- 229950008882 polysorbate Drugs 0.000 claims description 8
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims description 7
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- SHFJWMWCIHQNCP-UHFFFAOYSA-M hydron;tetrabutylazanium;sulfate Chemical compound OS([O-])(=O)=O.CCCC[N+](CCCC)(CCCC)CCCC SHFJWMWCIHQNCP-UHFFFAOYSA-M 0.000 description 4
- 238000011835 investigation Methods 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
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- 150000007513 acids Chemical class 0.000 description 3
- 239000000674 adrenergic antagonist Substances 0.000 description 3
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- 229940088679 drug related substance Drugs 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 239000006186 oral dosage form Substances 0.000 description 3
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- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 3
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- METKIMKYRPQLGS-GFCCVEGCSA-N (R)-atenolol Chemical compound CC(C)NC[C@@H](O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-GFCCVEGCSA-N 0.000 description 2
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- 241000416162 Astragalus gummifer Species 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- RPTUSVTUFVMDQK-UHFFFAOYSA-N Hidralazin Chemical compound C1=CC=C2C(NN)=NN=CC2=C1 RPTUSVTUFVMDQK-UHFFFAOYSA-N 0.000 description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 2
- 239000004698 Polyethylene Substances 0.000 description 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
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- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 229920001615 Tragacanth Polymers 0.000 description 2
- 239000008186 active pharmaceutical agent Substances 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 229960002274 atenolol Drugs 0.000 description 2
- 235000012216 bentonite Nutrition 0.000 description 2
- 230000000903 blocking effect Effects 0.000 description 2
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- 239000007853 buffer solution Substances 0.000 description 2
- 239000001506 calcium phosphate Substances 0.000 description 2
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 2
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- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 description 2
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- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical class OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 1
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Classifications
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- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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- A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
- A61J3/10—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
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- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
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- A—HUMAN NECESSITIES
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- 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
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
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- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- 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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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Biophysics (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA2675538A CA2675538C (en) | 2007-01-22 | 2008-01-22 | Oral pharmaceutical compositions comprising unmicronized nebivolol or a nebivolol analogue as active ingredient, and a decreased ratio of wetting agent to active ingredient |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA2575527 | 2007-01-22 | ||
| CA2,575,527 | 2007-01-22 | ||
| PCT/CA2008/000119 WO2008089549A1 (en) | 2007-01-22 | 2008-01-22 | Pharmaceutical compositions comprising nebivolol or a nebivolol analogue |
| CA2675538A CA2675538C (en) | 2007-01-22 | 2008-01-22 | Oral pharmaceutical compositions comprising unmicronized nebivolol or a nebivolol analogue as active ingredient, and a decreased ratio of wetting agent to active ingredient |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2675538A1 CA2675538A1 (en) | 2008-07-31 |
| CA2675538C true CA2675538C (en) | 2017-02-28 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2675538A Active CA2675538C (en) | 2007-01-22 | 2008-01-22 | Oral pharmaceutical compositions comprising unmicronized nebivolol or a nebivolol analogue as active ingredient, and a decreased ratio of wetting agent to active ingredient |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US20100137424A1 (enExample) |
| EP (1) | EP2124931A4 (enExample) |
| JP (1) | JP5448844B2 (enExample) |
| AU (1) | AU2008209264B2 (enExample) |
| CA (1) | CA2675538C (enExample) |
| WO (1) | WO2008089549A1 (enExample) |
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| WO2019183470A2 (en) | 2018-03-22 | 2019-09-26 | Incarda Therapeutics, Inc. | A novel method to slow ventricular rate |
| US20220016025A1 (en) * | 2020-07-08 | 2022-01-20 | Vinayak Dinesh DENDUKURI | Formulations of nebivolol |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1337429C (en) | 1983-12-05 | 1995-10-24 | Guy Rosalia Eugene Van Lommen | Derivatives of 2,2'-iminobisethanol |
| CA1337432C (en) | 1988-03-23 | 1995-10-24 | Raymond M. Xhonneux | Method of lowering the blood pressure |
| US5338732A (en) * | 1991-06-18 | 1994-08-16 | Bristol-Myers Squibb Company | Megestrol acetate formulation |
| TW355683B (en) * | 1994-02-17 | 1999-04-11 | Janssen Pharmaceutica Nv | Composition containing micronized nebivolol |
| JPH098913A (ja) | 1995-06-22 | 1997-01-10 | Hitachi Maxell Ltd | 情報通信システム |
| UA74141C2 (uk) * | 1998-12-09 | 2005-11-15 | Дж.Д. Сірл Енд Ко. | Фармацевтична композиція на основі тонкоподрібненого еплеренону (варіанти), спосіб її одержання та спосіб лікування розладів, опосередкованих альдостероном (варіанти) |
| FR2809731B1 (fr) * | 2000-05-31 | 2002-07-19 | Sanofi Synthelabo | Derives de 1,4-diazabicyclo-[3.2.2] nonane-pheylisoxazole, leur preparation et leur application en therapeutique |
| WO2005099699A1 (en) | 2004-04-07 | 2005-10-27 | Sepracor Inc. | Combination of (s)-amlodipine and a beta-blocker, and methods for reducing hypertension |
| WO2005117899A1 (en) * | 2004-06-02 | 2005-12-15 | Cipla Limited | Pharmaceutical composition comprising tibolone and process for procuding the same |
| EP1737847B1 (en) * | 2004-07-30 | 2008-06-04 | Torrent Pharmaceuticals Ltd | Nebivolol and its pharmaceutically acceptable salts, process for preparation and pharmaceutical compositions of nebivolol |
| EP1850842A1 (de) | 2005-02-11 | 2007-11-07 | Stada Arzneimittel Ag | Pharmazeutische zusammensetzungen nebivolo und ein hydrophiles polymer |
| CA2610694A1 (en) * | 2005-05-31 | 2006-12-07 | Mylan Laboratories, Inc. | Compositions comrising nebivolol |
| EP1839658A1 (en) * | 2006-03-30 | 2007-10-03 | Hexal A/S | Pharmaceutical composition comprising micronized nebivolol |
-
2008
- 2008-01-22 US US12/523,686 patent/US20100137424A1/en not_active Abandoned
- 2008-01-22 AU AU2008209264A patent/AU2008209264B2/en not_active Ceased
- 2008-01-22 EP EP08706266.7A patent/EP2124931A4/en not_active Withdrawn
- 2008-01-22 CA CA2675538A patent/CA2675538C/en active Active
- 2008-01-22 WO PCT/CA2008/000119 patent/WO2008089549A1/en not_active Ceased
- 2008-01-22 JP JP2009546620A patent/JP5448844B2/ja not_active Expired - Fee Related
-
2015
- 2015-05-05 US US14/704,375 patent/US10117939B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| AU2008209264B2 (en) | 2014-11-27 |
| EP2124931A4 (en) | 2013-08-28 |
| JP2010516712A (ja) | 2010-05-20 |
| WO2008089549A1 (en) | 2008-07-31 |
| JP5448844B2 (ja) | 2014-03-19 |
| CA2675538A1 (en) | 2008-07-31 |
| EP2124931A1 (en) | 2009-12-02 |
| US10117939B2 (en) | 2018-11-06 |
| AU2008209264A1 (en) | 2008-07-31 |
| US20100137424A1 (en) | 2010-06-03 |
| US20150231261A1 (en) | 2015-08-20 |
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| Date | Code | Title | Description |
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| EEER | Examination request |
Effective date: 20130122 |