MXPA05001004A - Formulacion farmaceutica. - Google Patents
Formulacion farmaceutica.Info
- Publication number
- MXPA05001004A MXPA05001004A MXPA05001004A MXPA05001004A MXPA05001004A MX PA05001004 A MXPA05001004 A MX PA05001004A MX PA05001004 A MXPA05001004 A MX PA05001004A MX PA05001004 A MXPA05001004 A MX PA05001004A MX PA05001004 A MXPA05001004 A MX PA05001004A
- Authority
- MX
- Mexico
- Prior art keywords
- further characterized
- weight
- composition according
- composition
- simvastatin
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 122
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 title claims abstract description 21
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 title claims abstract description 14
- 229940122502 Cholesterol absorption inhibitor Drugs 0.000 title claims abstract description 8
- 239000003381 stabilizer Substances 0.000 title claims description 18
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 51
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 26
- 235000010323 ascorbic acid Nutrition 0.000 claims abstract description 25
- 239000011668 ascorbic acid Substances 0.000 claims abstract description 25
- 229960005070 ascorbic acid Drugs 0.000 claims abstract description 25
- 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 abstract description 19
- 239000008101 lactose Substances 0.000 claims abstract description 19
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 18
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 18
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 18
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 18
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract description 13
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 13
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 13
- 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 abstract description 13
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 13
- 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 abstract description 6
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 6
- 235000006708 antioxidants Nutrition 0.000 claims abstract description 5
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 50
- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims description 49
- RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims description 48
- 229960002855 simvastatin Drugs 0.000 claims description 48
- OLNTVTPDXPETLC-XPWALMASSA-N ezetimibe Chemical compound N1([C@@H]([C@H](C1=O)CC[C@H](O)C=1C=CC(F)=CC=1)C=1C=CC(O)=CC=1)C1=CC=C(F)C=C1 OLNTVTPDXPETLC-XPWALMASSA-N 0.000 claims description 37
- 229960000815 ezetimibe Drugs 0.000 claims description 35
- ZTHYODDOHIVTJV-UHFFFAOYSA-N Propyl gallate Chemical compound CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 claims description 34
- 235000019282 butylated hydroxyanisole Nutrition 0.000 claims description 25
- 239000004255 Butylated hydroxyanisole Substances 0.000 claims description 24
- 229940043253 butylated hydroxyanisole Drugs 0.000 claims description 20
- CZBZUDVBLSSABA-UHFFFAOYSA-N butylated hydroxyanisole Chemical compound COC1=CC=C(O)C(C(C)(C)C)=C1.COC1=CC=C(O)C=C1C(C)(C)C CZBZUDVBLSSABA-UHFFFAOYSA-N 0.000 claims description 20
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 19
- 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 19
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 19
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 19
- 229960001375 lactose Drugs 0.000 claims description 18
- 239000000473 propyl gallate Substances 0.000 claims description 17
- 235000010388 propyl gallate Nutrition 0.000 claims description 17
- 229940075579 propyl gallate Drugs 0.000 claims description 17
- 238000011282 treatment Methods 0.000 claims description 14
- 229920000881 Modified starch Polymers 0.000 claims description 13
- 235000015165 citric acid Nutrition 0.000 claims description 13
- 229960004106 citric acid Drugs 0.000 claims description 13
- 239000003112 inhibitor Substances 0.000 claims description 12
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 10
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 10
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 10
- 239000011248 coating agent Substances 0.000 claims description 9
- 238000000576 coating method Methods 0.000 claims description 9
- 201000010099 disease Diseases 0.000 claims description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 9
- 229940069328 povidone Drugs 0.000 claims description 7
- 150000001875 compounds Chemical class 0.000 claims description 6
- 201000001320 Atherosclerosis Diseases 0.000 claims description 5
- PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 claims description 5
- 230000001906 cholesterol absorption Effects 0.000 claims description 5
- 229960004844 lovastatin Drugs 0.000 claims description 5
- PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 claims description 5
- QLJODMDSTUBWDW-UHFFFAOYSA-N lovastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(C)C=C21 QLJODMDSTUBWDW-UHFFFAOYSA-N 0.000 claims description 5
- 230000002265 prevention Effects 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- 230000001225 therapeutic effect Effects 0.000 claims description 5
- 230000002792 vascular Effects 0.000 claims description 5
- TUZYXOIXSAXUGO-UHFFFAOYSA-N Pravastatin Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(O)C=C21 TUZYXOIXSAXUGO-UHFFFAOYSA-N 0.000 claims description 4
- 238000010521 absorption reaction Methods 0.000 claims description 4
- 230000003078 antioxidant effect Effects 0.000 claims description 4
- 229960002965 pravastatin Drugs 0.000 claims description 4
- TUZYXOIXSAXUGO-PZAWKZKUSA-N pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 claims description 4
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims description 3
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims description 3
- 229960005370 atorvastatin Drugs 0.000 claims description 3
- 239000012453 solvate Substances 0.000 claims description 3
- ZGGHKIMDNBDHJB-NRFPMOEYSA-M (3R,5S)-fluvastatin sodium Chemical compound [Na+].C12=CC=CC=C2N(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC([O-])=O)=C1C1=CC=C(F)C=C1 ZGGHKIMDNBDHJB-NRFPMOEYSA-M 0.000 claims description 2
- 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 2
- 229960005110 cerivastatin Drugs 0.000 claims description 2
- SEERZIQQUAZTOL-ANMDKAQQSA-N cerivastatin Chemical compound COCC1=C(C(C)C)N=C(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC(O)=O)=C1C1=CC=C(F)C=C1 SEERZIQQUAZTOL-ANMDKAQQSA-N 0.000 claims description 2
- 229960003765 fluvastatin Drugs 0.000 claims description 2
- 229960001021 lactose monohydrate Drugs 0.000 claims description 2
- 229960002797 pitavastatin Drugs 0.000 claims description 2
- VGYFMXBACGZSIL-MCBHFWOFSA-N pitavastatin Chemical compound OC(=O)C[C@H](O)C[C@H](O)\C=C\C1=C(C2CC2)N=C2C=CC=CC2=C1C1=CC=C(F)C=C1 VGYFMXBACGZSIL-MCBHFWOFSA-N 0.000 claims description 2
- 229960000672 rosuvastatin Drugs 0.000 claims description 2
- BPRHUIZQVSMCRT-VEUZHWNKSA-N rosuvastatin Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O BPRHUIZQVSMCRT-VEUZHWNKSA-N 0.000 claims description 2
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims 1
- 229940123934 Reductase inhibitor Drugs 0.000 claims 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
- 229930182558 Sterol Natural products 0.000 claims 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 1
- 235000003702 sterols Nutrition 0.000 claims 1
- 150000003432 sterols Chemical class 0.000 claims 1
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 27
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 12
- 230000009467 reduction Effects 0.000 description 12
- 238000000034 method Methods 0.000 description 11
- 235000012000 cholesterol Nutrition 0.000 description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 9
- 239000013543 active substance Substances 0.000 description 8
- 230000003143 atherosclerotic effect Effects 0.000 description 7
- 239000012530 fluid Substances 0.000 description 7
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 6
- 239000008187 granular material Substances 0.000 description 6
- 238000005469 granulation Methods 0.000 description 6
- 230000003179 granulation Effects 0.000 description 6
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 6
- 229940124597 therapeutic agent Drugs 0.000 description 6
- 102000015779 HDL Lipoproteins Human genes 0.000 description 5
- 108010010234 HDL Lipoproteins Proteins 0.000 description 5
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 5
- 208000029078 coronary artery disease Diseases 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
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- PNAMDJVUJCJOIX-IUNFJCKHSA-N [(1s,3r,7s,8s,8ar)-8-[2-[(2r,4r)-4-hydroxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] 2,2-dimethylbutanoate;(3r,4s)-1-(4-fluorophenyl)-3-[(3s)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1.N1([C@@H]([C@H](C1=O)CC[C@H](O)C=1C=CC(F)=CC=1)C=1C=CC(O)=CC=1)C1=CC=C(F)C=C1 PNAMDJVUJCJOIX-IUNFJCKHSA-N 0.000 description 4
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- 229940074790 simvastatin and ezetimibe Drugs 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 3
- 102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 description 3
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- 230000015572 biosynthetic process Effects 0.000 description 3
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 3
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- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 2
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- WBZKQQHYRPRKNJ-UHFFFAOYSA-L disulfite Chemical compound [O-]S(=O)S([O-])(=O)=O WBZKQQHYRPRKNJ-UHFFFAOYSA-L 0.000 description 1
- 125000003438 dodecyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
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- IDGUHHHQCWSQLU-UHFFFAOYSA-N ethanol;hydrate Chemical compound O.CCO IDGUHHHQCWSQLU-UHFFFAOYSA-N 0.000 description 1
- -1 ezetimibe Chemical compound 0.000 description 1
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
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- 229940057948 magnesium stearate Drugs 0.000 description 1
- YDSWCNNOKPMOTP-UHFFFAOYSA-N mellitic acid Chemical compound OC(=O)C1=C(C(O)=O)C(C(O)=O)=C(C(O)=O)C(C(O)=O)=C1C(O)=O YDSWCNNOKPMOTP-UHFFFAOYSA-N 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 239000008203 oral pharmaceutical composition Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 238000012776 robust process Methods 0.000 description 1
- 235000021003 saturated fats Nutrition 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 238000009097 single-agent therapy Methods 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229940083542 sodium Drugs 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000010378 sodium ascorbate Nutrition 0.000 description 1
- PPASLZSBLFJQEF-RKJRWTFHSA-M sodium ascorbate Substances [Na+].OC[C@@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RKJRWTFHSA-M 0.000 description 1
- 229960005055 sodium ascorbate Drugs 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 238000009827 uniform distribution Methods 0.000 description 1
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- 239000001993 wax Substances 0.000 description 1
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Classifications
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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
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
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- A—HUMAN NECESSITIES
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- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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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
- A61K9/2004—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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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- 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
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyrane Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39869102P | 2002-07-26 | 2002-07-26 | |
| PCT/US2003/022889 WO2004010993A1 (en) | 2002-07-26 | 2003-07-22 | Composition comprising a cholesterol absorption inhibitor, an hmg-coa reductase inhibitor and a stabilizing agent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA05001004A true MXPA05001004A (es) | 2005-05-16 |
Family
ID=31188454
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA05001004A MXPA05001004A (es) | 2002-07-26 | 2003-07-22 | Formulacion farmaceutica. |
Country Status (38)
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
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| GB0215579D0 (en) | 2002-07-05 | 2002-08-14 | Astrazeneca Ab | Chemical compounds |
| AR040588A1 (es) * | 2002-07-26 | 2005-04-13 | Schering Corp | Formulacion farmaceutica que comprende un inhibidor de la absorcion del colesterol y un inhibidor de una hmg- co a reductasa |
| PL1682499T3 (pl) * | 2003-11-10 | 2008-01-31 | Microbia Inc | 4-Biarylilo-1-fenyloazetydyn-2-ony |
| EP1699759B1 (en) | 2003-12-23 | 2010-10-20 | AstraZeneca AB | Diphenylazetidinone derivates possessing cholesterol absorption inhibitory activity |
| KR100598326B1 (ko) * | 2004-04-10 | 2006-07-10 | 한미약품 주식회사 | ＨＭＧ-ＣｏＡ 환원효소 억제제의 경구투여용 서방형 제제및 이의 제조방법 |
| US20060046996A1 (en) * | 2004-08-31 | 2006-03-02 | Kowa Co., Ltd. | Method for treating hyperlipidemia |
| SA06270191B1 (ar) | 2005-06-22 | 2010-03-29 | استرازينيكا ايه بي | مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم |
| EP1741427A1 (en) * | 2005-07-06 | 2007-01-10 | KRKA, D.D., Novo Mesto | Pharmaceutical composition comprising simvastatin and ezetimibe |
| EP1905424A3 (en) * | 2006-02-02 | 2008-04-30 | Ranbaxy Laboratories Limited | Process for the preparation of a pharmaceutical composition comprising stabilized statin particles |
| WO2007103453A1 (en) * | 2006-03-06 | 2007-09-13 | Teva Pharmaceutical Industries Ltd. | Ezetimibe compositions |
| AR060623A1 (es) | 2006-04-27 | 2008-07-02 | Astrazeneca Ab | Compuestos derivados de 2-azetidinona y un metodo de preparacion |
| KR20150029762A (ko) | 2006-06-19 | 2015-03-18 | 알파마 파머슈티컬스 엘엘씨 | 약제학적 조성물 |
| CN1994296B (zh) * | 2006-08-02 | 2010-06-16 | 浙江京新药业股份有限公司 | 一种含有辛伐他汀的药物制剂 |
| GB0713707D0 (en) | 2007-07-13 | 2007-08-22 | Generics Uk Ltd | Stable compositions |
| JP2010534644A (ja) * | 2007-07-27 | 2010-11-11 | シプラ・リミテッド | 医薬組成物およびその製造方法 |
| WO2009024889A2 (en) | 2007-08-21 | 2009-02-26 | Ranbaxy Laboratories Limited | Pharmaceutical composition comprising a hmg-coa reductase inhibitor and ezetimibe |
| AU2008337435A1 (en) * | 2007-12-17 | 2009-06-25 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Suspension comprising non-micronized ezetimibe micro-particles |
| US20090233898A1 (en) * | 2008-03-11 | 2009-09-17 | Glenmark Generics Ltd | Pharmaceutical Compositions Comprising Simvastatin and Ezetimibe |
| TR200806302A2 (tr) * | 2008-08-22 | 2010-03-22 | Bi̇lgi̇ç Mahmut | Çözünürlük ve stabilite artırıcı farmasötik formülasyon. |
| EP2168573A1 (en) * | 2008-09-30 | 2010-03-31 | LEK Pharmaceuticals D.D. | Formulations comprising ezetimibe |
| MX344885B (es) * | 2008-11-10 | 2017-01-10 | Psicofarma S A De C V | Proceso para la obtencion de una composicion de rosuvastatina calcica y producto obtenido. |
| EP2204170A1 (en) * | 2008-12-01 | 2010-07-07 | LEK Pharmaceuticals D.D. | Pharmaceutical composition comprising ezetimibe and simvastatin |
| WO2010066687A2 (en) * | 2008-12-11 | 2010-06-17 | Dsm Ip Assets B.V. | Stabalized statin-comprising compositions |
| EP2216016A1 (en) | 2009-02-06 | 2010-08-11 | LEK Pharmaceuticals d.d. | Process for the preparation of a pharmaceutical composition comprising ezetimibe |
| WO2011002424A2 (en) | 2009-07-02 | 2011-01-06 | Bilgic Mahmut | Solubility and stability enchancing pharmaceutical formulation |
| WO2011019326A2 (en) * | 2009-07-02 | 2011-02-17 | Mahmut Bilgic | Solubility and stability enchancing pharmaceutical formulation |
| EP2448564A2 (en) * | 2009-07-02 | 2012-05-09 | Bilgic Mahmut | Solubility enhancing pharmaceutical formulation |
| EP2368543A1 (en) * | 2010-03-25 | 2011-09-28 | KRKA, tovarna zdravil, d.d., Novo mesto | Method of preparing a granulated pharmaceutical composition comprising simvastatin and/or ezetimibe |
| KR101302243B1 (ko) * | 2010-07-28 | 2013-09-02 | 씨제이제일제당 (주) | 로수바스타틴 또는 이의 약학적 허용염을 포함하는 약학 조성물 |
| CN101978953A (zh) * | 2010-10-11 | 2011-02-23 | 上海交通大学 | 基于易吸湿性辅料的固体制剂 |
| EP2468258A1 (en) | 2010-12-22 | 2012-06-27 | LEK Pharmaceuticals d.d. | Process for the preparation of a pharmaceutical composition comprising a low soluble pharmaceutically active ingredient |
| RU2013136350A (ru) | 2011-02-02 | 2015-03-27 | АЛФАРМА ФАРМАСЬЮТИКЭЛЗ, ЭлЭлСи | Фармацевтическая композиция, содержащая опиоидный агонист и секвестрированный антагонист |
| CN102266323B (zh) * | 2011-08-04 | 2013-03-27 | 海南锦瑞制药股份有限公司 | 依折麦布和辛伐他汀组合物及其制备方法 |
| RU2614728C2 (ru) * | 2011-09-08 | 2017-03-28 | Хексал Аг | Фармацевтическая композиция для перорального введения, содержащая статин |
| PL2844233T3 (pl) * | 2012-05-01 | 2020-09-07 | Althera Life Sciences, Llc | Preparat w postaci tabletki do stosowania doustnego składający się ze stałego połączenia rosuwastatyny i ezetymibu w leczeniu hiperlipidemii i chorób sercowo-naczyniowych |
| WO2013166114A1 (en) * | 2012-05-01 | 2013-11-07 | Althera Life Sciences, Llc | Oral tablet formulation consisting of fixed combination of atorvastatin and ezetimibe |
| RU2547574C2 (ru) * | 2013-07-09 | 2015-04-10 | Общество с ограниченной ответственностью "Трейдсервис" | Лекарственная форма гиполипидемического действия и способ ее изготовления |
| CN103585146B (zh) * | 2013-11-09 | 2015-04-01 | 北京中申专利科技有限公司 | 辛伐他汀的药物组合物 |
| TWI586380B (zh) * | 2013-12-18 | 2017-06-11 | 夢製藥公司 | 包含ＨＭＧ－ＣｏＡ還原酶抑制劑及膽固醇吸收抑制劑之醫藥組合製劑 |
| CN104306348B (zh) * | 2014-09-30 | 2017-05-31 | 地奥集团成都药业股份有限公司 | 一种辛伐他汀片及其制备方法 |
| SG10201912754UA (en) * | 2015-11-06 | 2020-02-27 | Gemphire Therapeutics Inc | Treatment of mixed dyslipidemia |
| CN106937952A (zh) * | 2016-01-04 | 2017-07-11 | 重庆华邦制药有限公司 | 依折麦布和辛伐他汀的制剂 |
| EP3281649A1 (en) * | 2016-08-09 | 2018-02-14 | Teleflex Lifesciences | Wetting agent formulation |
| JP6937195B2 (ja) * | 2017-09-01 | 2021-09-22 | 興和株式会社 | 医薬組成物 |
| WO2019101150A1 (zh) * | 2017-11-23 | 2019-05-31 | 浙江海正药业股份有限公司 | 一种海泽麦布片剂及其制备方法 |
| TWI760067B (zh) * | 2020-08-13 | 2022-04-01 | 友霖生技醫藥股份有限公司 | 固態口服醫藥組成物 |
| US11833133B2 (en) * | 2020-08-13 | 2023-12-05 | Orient Pharma Co., Ltd. | Solid oral pharmaceutical composition |
| CN112168801A (zh) * | 2020-10-22 | 2021-01-05 | 哈药集团技术中心 | 一种辛伐他汀片的制备方法 |
| CN115227659B (zh) * | 2022-08-19 | 2023-05-02 | 北京百奥药业有限责任公司 | 一种依折麦布辛伐他汀组合物及其制备方法 |
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