CA2524091A1 - Pharmaceutical formulation of the telmisartan sodium salt - Google Patents
Pharmaceutical formulation of the telmisartan sodium salt Download PDFInfo
- Publication number
- CA2524091A1 CA2524091A1 CA002524091A CA2524091A CA2524091A1 CA 2524091 A1 CA2524091 A1 CA 2524091A1 CA 002524091 A CA002524091 A CA 002524091A CA 2524091 A CA2524091 A CA 2524091A CA 2524091 A1 CA2524091 A1 CA 2524091A1
- Authority
- CA
- Canada
- Prior art keywords
- composition according
- sodium salt
- water
- telmisartan
- present
- 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.)
- Granted
Links
- RSGAIWOEJXRYRV-UHFFFAOYSA-M sodium;2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoate Chemical compound [Na+].CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C([O-])=O RSGAIWOEJXRYRV-UHFFFAOYSA-M 0.000 title claims 5
- 239000008194 pharmaceutical composition Substances 0.000 title claims 4
- 239000000203 mixture Substances 0.000 claims abstract 17
- RMMXLENWKUUMAY-UHFFFAOYSA-N telmisartan Chemical compound CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(O)=O RMMXLENWKUUMAY-UHFFFAOYSA-N 0.000 claims abstract 11
- 239000005537 C09CA07 - Telmisartan Substances 0.000 claims abstract 5
- 159000000000 sodium salts Chemical class 0.000 claims abstract 5
- 229960005187 telmisartan Drugs 0.000 claims abstract 5
- 238000009472 formulation Methods 0.000 claims abstract 3
- 238000004519 manufacturing process Methods 0.000 claims abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 10
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 6
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 6
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims 5
- 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 5
- 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 5
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 5
- 229960002003 hydrochlorothiazide Drugs 0.000 claims 5
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 5
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims 5
- 239000000600 sorbitol Substances 0.000 claims 5
- 235000010356 sorbitol Nutrition 0.000 claims 5
- 229960002920 sorbitol Drugs 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 4
- 239000013543 active substance Substances 0.000 claims 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 4
- 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 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 4
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 3
- 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 3
- 229930195725 Mannitol Natural products 0.000 claims 3
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 3
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 3
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 3
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims 3
- 239000002934 diuretic Substances 0.000 claims 3
- 230000001882 diuretic effect Effects 0.000 claims 3
- 235000019359 magnesium stearate Nutrition 0.000 claims 3
- 239000000594 mannitol Substances 0.000 claims 3
- 235000010355 mannitol Nutrition 0.000 claims 3
- 229960001855 mannitol Drugs 0.000 claims 3
- 239000008108 microcrystalline cellulose Substances 0.000 claims 3
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 3
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 3
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 229920002472 Starch Polymers 0.000 claims 2
- 229930006000 Sucrose Natural products 0.000 claims 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical class [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 2
- 229920001577 copolymer Polymers 0.000 claims 2
- 229920001531 copovidone Polymers 0.000 claims 2
- 229960000913 crospovidone Drugs 0.000 claims 2
- 235000013681 dietary sucrose Nutrition 0.000 claims 2
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 2
- 229940116364 hard fat Drugs 0.000 claims 2
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 2
- 229960004063 propylene glycol Drugs 0.000 claims 2
- 235000013772 propylene glycol Nutrition 0.000 claims 2
- 239000008109 sodium starch glycolate Substances 0.000 claims 2
- 229920003109 sodium starch glycolate Polymers 0.000 claims 2
- 229940079832 sodium starch glycolate Drugs 0.000 claims 2
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- 229940032147 starch Drugs 0.000 claims 2
- 235000019698 starch Nutrition 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 229960004793 sucrose Drugs 0.000 claims 2
- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 claims 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 2
- 239000000811 xylitol Substances 0.000 claims 2
- 235000010447 xylitol Nutrition 0.000 claims 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims 2
- 229960002675 xylitol Drugs 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
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims 1
- 229920002261 Corn starch Polymers 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 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 1
- 235000019759 Maize starch Nutrition 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 229960003563 calcium carbonate Drugs 0.000 claims 1
- 235000010216 calcium carbonate Nutrition 0.000 claims 1
- 239000001506 calcium phosphate Substances 0.000 claims 1
- 229910000389 calcium phosphate Inorganic materials 0.000 claims 1
- 229960001714 calcium phosphate Drugs 0.000 claims 1
- 235000011010 calcium phosphates Nutrition 0.000 claims 1
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims 1
- 239000008187 granular material Substances 0.000 claims 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 229960001375 lactose Drugs 0.000 claims 1
- 229940057948 magnesium stearate Drugs 0.000 claims 1
- 229920002689 polyvinyl acetate Polymers 0.000 claims 1
- 239000011118 polyvinyl acetate Substances 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229940083542 sodium Drugs 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 235000015424 sodium Nutrition 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- 229940033134 talc Drugs 0.000 claims 1
- 235000012222 talc Nutrition 0.000 claims 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
Classifications
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/39—Heterocyclic compounds having sulfur as a ring hetero atom having oxygen in the same ring
-
- 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P7/10—Antioedematous agents; Diuretics
-
- A—HUMAN NECESSITIES
- 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
-
- A—HUMAN NECESSITIES
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- 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
-
- A—HUMAN NECESSITIES
- 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
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
The invention relates to a medicament formulation of the crystalline sodium salt of 4'-[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (Telmisartan) and methods for production thereof.
Claims (14)
1. Pharmaceutical composition containing the telmisartan sodium salt and a diuretic.
2. The composition according to claim 1 containing one or more formulation excipients selected from among mannitol, sorbitol, xylitol, saccharose, calcium carbonate, calcium phosphate, lactose, croscarmellose sodium salt, crospovidone, sodium starch glycolate, hydroxypropylcellulose, maize starch, polyvinylpyrrolidone, copolymers of vinylpyrrolidone with other vinyl derivatives (copovidone), hydroxypropylcellulose, hydroxypropylmethylcellulose, microcrystalline cellulose or starch, magnesium stearate, sodium stearylfumarate, talc, hydroxypropylmethylcellulose, carboxymethylcellulose, cellulose acetate phthalate, polyvinyl acetate, water, water/ethanol, water/glycerol, water/sorbitol, water/polyethyleneglycol, propyleneglycol, cetylstearyl alcohol, carboxymethylcellulose or fatty substances such as hard fat or suitable mixtures thereof.
3. Pharmaceutical composition containing the telmisartan sodium salt, optionally a diuretic, and one or more formulation excipients selected from among sorbitol, xylitol, saccharose, croscarmellose sodium salt, crospovidone, sodium starch glycolate, hydroxypropylcellulose, polyvinylpyrrolidone, copolymers of vinylpyrrolidone with other vinyl derivatives (copovidone), hydroxypropylcellulose, hydroxypropylmethylcellulose, microcrystalline cellulose or sodium stearylfumarate, hydroxypropylmethylcellulose, water, water/ethanol, water/glycerol, water/sorbitol, water/polyethyleneglycol, propyleneglycol, cetylstearylalcohol, carboxymethylcellulose or fatty substances such as hard fat or suitable mixtures thereof.
4. The composition according to claims 1 to 3 containing the diuretic hydrochlorothiazide (HCTZ).
5. The composition according to claims 1 to 3, characterised in that the hydrochlorothiazide is present in an amount of 10-15 mg or 20-30 mg.
6. The composition according to claims 1 to 3, characterised in that the sodium salt of telmisartan is present in an amount of 60-90 mg.
7. The composition according to claim 8, characterised in that the sodium salt of telmisartan is present in an amount of 80-85 mg.
8. The composition according to claims 1 to 3, characterised in that the sodium salt of telmisartan is present in an amount of 30-60 mg.
9. The composition according to claim 8, characterised in that the sodium salt of telmisartan is present in an amount of 40-45 mg.
10. The composition according to claims 7 and 9, characterised in that hydrochlorothiazide is present in an amount of 12-13 mg or 24-26 mg.
11. The composition according to claim 1, characterised in that the active substances is present together with the excipients sorbitol and magnesium stearate, compressed directly into tablets.
12. The composition according to claim 1, characterised in that the active substances are present as compressed dry granules of the telmisartan sodium salt containing the excipients mannitol, magnesium stearate and hydroxypropylcellulose with a mixture of hydrochlorothiazide, mannitol, microcrystalline cellulose and sodium glycol starch.
13. The composition according to claim 1, characterised in that the telmisartan sodium salt is formulated with additional pharmaceutically active substances.
14. Process for preparing the pharmaceutical composition according to claims 1 to 3, characterised in that the active substances are compressed with the excipients to form tablets.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10319450A DE10319450A1 (en) | 2003-04-30 | 2003-04-30 | Pharmaceutical formulation of telmisartan sodium salt |
| DE10319450.9 | 2003-04-30 | ||
| PCT/EP2004/004425 WO2004096215A1 (en) | 2003-04-30 | 2004-04-27 | Pharmaceutical formulation of the sodium salt of telmisartan |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2524091A1 true CA2524091A1 (en) | 2004-11-11 |
| CA2524091C CA2524091C (en) | 2012-02-21 |
Family
ID=33305059
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2524091A Expired - Fee Related CA2524091C (en) | 2003-04-30 | 2004-04-27 | Pharmaceutical formulation of the telmisartan sodium salt |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP1622612B9 (en) |
| JP (2) | JP5156231B2 (en) |
| KR (1) | KR20060008943A (en) |
| CN (1) | CN100589802C (en) |
| AR (2) | AR044142A1 (en) |
| AT (1) | ATE388703T1 (en) |
| AU (1) | AU2004233581B2 (en) |
| BR (1) | BRPI0409809A (en) |
| CA (1) | CA2524091C (en) |
| CL (1) | CL2004000899A1 (en) |
| DE (2) | DE10319450A1 (en) |
| DK (1) | DK1622612T3 (en) |
| ES (1) | ES2303634T4 (en) |
| IL (1) | IL171465A (en) |
| MX (1) | MXPA05011647A (en) |
| NZ (1) | NZ543775A (en) |
| PE (1) | PE20050464A1 (en) |
| RU (1) | RU2372918C2 (en) |
| TW (1) | TWI364278B (en) |
| UY (1) | UY28293A1 (en) |
| WO (1) | WO2004096215A1 (en) |
| ZA (1) | ZA200507223B (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006044754A3 (en) * | 2004-10-18 | 2006-12-14 | Reddys Lab Ltd Dr | Process for preparing telmisartan |
| WO2011147026A2 (en) * | 2010-05-28 | 2011-12-01 | Pharmascience, Inc. | A stable pharmaceutical formulation comprising telmisartan and hydrochlorothiazide |
| US8637078B2 (en) | 2005-11-24 | 2014-01-28 | Boehringer Ingelheim International Gmbh | Bilayer tablet comprising telmisartan and diuretic |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10319450A1 (en) * | 2003-04-30 | 2004-11-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical formulation of telmisartan sodium salt |
| DE10319592A1 (en) * | 2003-05-02 | 2004-11-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Treatment of diabetic retinopathy with angiotensin II receptor blockers |
| SI2269583T1 (en) | 2006-06-16 | 2014-12-31 | Lek Pharmaceuticals D.D. | Pharmaceutical composition comprising hydrochlorothiazide and telmisartan |
| TWI482772B (en) | 2006-08-21 | 2015-05-01 | Astrazeneca Ab | Compositions, suitable for oral administration, comprising a triazolo(4,5-d)pyrimidin derivate |
| WO2009058950A2 (en) * | 2007-10-30 | 2009-05-07 | Dr. Reddy's Laboratories Ltd. | Pharmaceutical formulations comprising telmisartan and hydrochlorothiazide |
| DE102008047910A1 (en) | 2008-09-19 | 2010-03-25 | Molkerei Meggle Wasserburg Gmbh & Co. Kg | Tabletting excipient based on lactose and cellulose |
| CZ301299B6 (en) | 2008-11-24 | 2010-01-06 | Zentiva, A.S. | Solid pharmaceutical composition with atorvastatin and telmisartan active ingredients |
| SI2443094T1 (en) | 2009-06-19 | 2013-08-30 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Process for the preparation of telmisartan |
| EP2448575A2 (en) * | 2009-07-02 | 2012-05-09 | Bilgic Mahmut | Pharmaceutical composition increasing solubility and stability |
| JP2011136908A (en) * | 2009-12-25 | 2011-07-14 | Kyowa Yakuhin Kogyo Kk | Solid preparation including angiotensin ii receptor antagonist and method of improving storage stability of angiotensin ii receptor antagonist in the solid preparation |
| WO2011161123A2 (en) | 2010-06-21 | 2011-12-29 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Multilayer pharmaceutical tablet comprising telmisartan and a diuretic |
| PT2640371T (en) * | 2010-11-15 | 2020-04-17 | Boehringer Ingelheim Int | Vasoprotective and cardioprotective antidiabetic therapy |
| US9446032B2 (en) * | 2011-08-26 | 2016-09-20 | Wockhardt Limited | Methods for treating cardiovascular disorders |
| CN102526037B (en) * | 2012-02-10 | 2014-08-27 | 重庆康刻尔制药有限公司 | Telmisartan medicinal composition, telmisartan medicinal composition tablets and preparation method for telmisartan medicinal composition tablets |
| EP2649996A1 (en) * | 2012-04-11 | 2013-10-16 | Laboratorios Del. Dr. Esteve, S.A. | Crystalline forms of sartans like telmisartan with beta blockers |
| JP6018420B2 (en) * | 2012-06-05 | 2016-11-02 | ニプロ株式会社 | Pharmaceutical composition comprising an angiotensin II receptor antagonist and thiazide diuretic |
| JP6428340B2 (en) * | 2014-05-23 | 2018-11-28 | ニプロ株式会社 | Method for granulating a pharmaceutical composition comprising telmisartan |
| JP5956034B1 (en) * | 2015-07-27 | 2016-07-20 | エルメッド エーザイ株式会社 | Telmisartan-containing pharmaceutical composition |
| CN107501192A (en) * | 2017-08-15 | 2017-12-22 | 中国科学院上海药物研究所 | The eutectic of Telmisartan and Hydrochioro |
| KR20200043618A (en) * | 2018-10-18 | 2020-04-28 | 주식회사유한양행 | Pharmaceutical composition for oral administration comprising an aminopyrimidine derivative or its salt |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI9210098B (en) * | 1991-02-06 | 2000-06-30 | Dr. Karl Thomae | Benzimidazoles, drugs with this compounds, and process for their preparation |
| JP4107831B2 (en) * | 2000-11-21 | 2008-06-25 | 第一三共株式会社 | Pharmaceutical composition |
| US20040242891A1 (en) * | 2001-10-26 | 2004-12-02 | Jonathan Campbell | Production of keto acids |
| DE10153737A1 (en) * | 2001-10-31 | 2003-05-28 | Boehringer Ingelheim Pharma | Crystalline sodium salt of telmisartan, process for its preparation and its use for the manufacture of a medicament |
| EA007614B1 (en) * | 2002-01-16 | 2006-12-29 | Бёрингер Ингельхайм Фарма Гмбх Унд Ко. Кг | Bilayer pharmaceutical tablet and method for producing thereof |
| DE10244681A1 (en) * | 2002-09-24 | 2004-04-08 | Boehringer Ingelheim International Gmbh | New solid telmisartan-containing pharmaceutical formulations and their preparation |
| DE10301371A1 (en) * | 2003-01-16 | 2004-08-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Treatment or prophylaxis of cardiovascular, cardiopulmonary or renal diseases, e.g. hypertension combined with hyperlipidemia or atherosclerosis, using combination of telmisartan and atorvastatin |
| DE10319450A1 (en) * | 2003-04-30 | 2004-11-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical formulation of telmisartan sodium salt |
-
2003
- 2003-04-30 DE DE10319450A patent/DE10319450A1/en not_active Withdrawn
-
2004
- 2004-04-27 AU AU2004233581A patent/AU2004233581B2/en not_active Ceased
- 2004-04-27 KR KR1020057020575A patent/KR20060008943A/en active Search and Examination
- 2004-04-27 JP JP2006500100A patent/JP5156231B2/en not_active Expired - Fee Related
- 2004-04-27 ES ES04729635T patent/ES2303634T4/en not_active Expired - Lifetime
- 2004-04-27 AT AT04729635T patent/ATE388703T1/en active
- 2004-04-27 RU RU2005137031/15A patent/RU2372918C2/en not_active IP Right Cessation
- 2004-04-27 EP EP04729635A patent/EP1622612B9/en not_active Expired - Lifetime
- 2004-04-27 DK DK04729635T patent/DK1622612T3/en active
- 2004-04-27 CN CN200480011725A patent/CN100589802C/en not_active Expired - Fee Related
- 2004-04-27 NZ NZ543775A patent/NZ543775A/en not_active IP Right Cessation
- 2004-04-27 WO PCT/EP2004/004425 patent/WO2004096215A1/en active IP Right Grant
- 2004-04-27 DE DE502004006500T patent/DE502004006500D1/en not_active Expired - Lifetime
- 2004-04-27 BR BRPI0409809-9A patent/BRPI0409809A/en not_active Application Discontinuation
- 2004-04-27 CA CA2524091A patent/CA2524091C/en not_active Expired - Fee Related
- 2004-04-27 MX MXPA05011647A patent/MXPA05011647A/en active IP Right Grant
- 2004-04-28 PE PE2004000417A patent/PE20050464A1/en not_active Application Discontinuation
- 2004-04-28 UY UY28293A patent/UY28293A1/en not_active Application Discontinuation
- 2004-04-28 CL CL200400899A patent/CL2004000899A1/en unknown
- 2004-04-29 TW TW093112090A patent/TWI364278B/en not_active IP Right Cessation
- 2004-04-30 AR ARP040101480A patent/AR044142A1/en active Pending
-
2005
- 2005-09-08 ZA ZA200507223A patent/ZA200507223B/en unknown
- 2005-10-19 IL IL171465A patent/IL171465A/en not_active IP Right Cessation
-
2010
- 2010-03-16 JP JP2010059404A patent/JP5254268B2/en not_active Expired - Fee Related
-
2012
- 2012-07-17 AR ARP120102583A patent/AR087210A2/en not_active Application Discontinuation
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006044754A3 (en) * | 2004-10-18 | 2006-12-14 | Reddys Lab Ltd Dr | Process for preparing telmisartan |
| US7943781B2 (en) | 2004-10-18 | 2011-05-17 | Dr. Reddy's Laboratories Limited | Process for preparing telmisartan |
| US8637078B2 (en) | 2005-11-24 | 2014-01-28 | Boehringer Ingelheim International Gmbh | Bilayer tablet comprising telmisartan and diuretic |
| WO2011147026A2 (en) * | 2010-05-28 | 2011-12-01 | Pharmascience, Inc. | A stable pharmaceutical formulation comprising telmisartan and hydrochlorothiazide |
| WO2011147026A3 (en) * | 2010-05-28 | 2012-01-26 | Pharmascience, Inc. | A stable pharmaceutical formulation comprising telmisartan and hydrochlorothiazide |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2524091A1 (en) | Pharmaceutical formulation of the telmisartan sodium salt | |
| US6677342B2 (en) | Partial fatty acid oxidation inhibitors in the treatment of congestive heart failure | |
| US5948437A (en) | Pharmaceutical compositions using thiazepine | |
| CA2251944C (en) | Sustained release pharmaceutical compositions comprising a dibenzothiazepine derivative | |
| AU2007297333B2 (en) | Solid dosage form of olmesartan medoxomil and amlodipine | |
| US8785432B2 (en) | Pharmaceutical compositions of amlodipine and valsartan | |
| US11819577B2 (en) | Fixed dose pharmaceutical composition of valsartan and sacubitril | |
| EA021317B1 (en) | Monolayer tablets comprising irbesartan and amlodipine, their preparation and their therapeutic application | |
| WO2014030051A1 (en) | Stable pharmaceutical compositions comprising saxagliptin | |
| KR20190015329A (en) | A pharmaceutical composition of a dapagliflozin co-crystal | |
| US20080008751A1 (en) | Stable formulation comprising a combination of a moisture sensitive drug and a second drug and manufacturing procedure thereof | |
| US20080227836A1 (en) | Stable Solid Oral Dosage Forms of Valsartan | |
| WO2007049868A1 (en) | Stabilized pharmaceutical oral preparation containing clopidogrel bisulfate | |
| WO2007049291A1 (en) | Novel solid dosage forms of valsartan and rochlorothiazide | |
| WO2020106020A1 (en) | Bilayer tablet and preparation method therefor | |
| KR20090065510A (en) | Solid dosage form of olmesartan medoxomil and amlodipine | |
| EP1889629B1 (en) | Stable formulation comprising a combination of a moisture sensitive drug and a second drug and manufacturing procedure thereof | |
| JPH0820537A (en) | Solid preparation containing antiulcer agent | |
| KR100484994B1 (en) | Pharmacy Composition | |
| KR20120090401A (en) | Compositions for controlled release formulation containing zaltoprofen and process for the preparation thereof | |
| WO2017119629A1 (en) | Pharmaceutical composition comprising nebivolol with improved dissolution rate | |
| CN112263581A (en) | Double-layer tablet compound preparation for treating PE and ED and preparation method thereof | |
| CA2659814A1 (en) | Stable formulation comprising a combination of a moisture sensitive drug and a second drug and manufacturing procedure thereof | |
| GB2471970A (en) | Composition comprising olmesartan medoxomil, amlodipine and hydrochlorothiazide | |
| KR20090021222A (en) | Stable formulation comprising a combination of a moisture sensitive drug and a second drug and manufacturing procedure thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20160427 |