TWI700100B - 用於口服投藥之包含依澤替米貝（ｅｚｅｔｉｍｉｂｅ）及羅舒伐他汀（ｒｏｓｕｖａｓｔａｔｉｎ）的複合調配物及其製備方法 - Google Patents

用於口服投藥之包含依澤替米貝（ｅｚｅｔｉｍｉｂｅ）及羅舒伐他汀（ｒｏｓｕｖａｓｔａｔｉｎ）的複合調配物及其製備方法 Download PDF

Info

Publication number: TWI700100B
Authority: TW; Taiwan
Prior art keywords: ezetimibe; rosuvastatin; wet; fluid bed; mixture
Prior art date: 2014-06-25

Application number

TW104119406A

Other languages

English (en)

Chinese (zh)

Other versions

TW201625223A (zh

Inventor

金用鎰

鄭夏瑩

金京洙

李承俊

朴宰賢

禹鍾守

Original Assignee

南韓商韓美藥品股份有限公司

Priority date (The priority date 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 date listed.)

2014-06-25

Filing date

2015-06-16

Publication date

2020-08-01

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54938391&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI700100(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2015-06-16 Application filed by 南韓商韓美藥品股份有限公司 filed Critical 南韓商韓美藥品股份有限公司

2016-07-16 Publication of TW201625223A publication Critical patent/TW201625223A/zh

2020-08-01 Application granted granted Critical

2020-08-01 Publication of TWI700100B publication Critical patent/TWI700100B/zh

Links

239000000203 mixture Substances 0.000 title claims abstract description 111
238000009472 formulation Methods 0.000 title claims abstract description 82
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 title claims abstract description 77
229960000815 ezetimibe Drugs 0.000 title claims abstract description 75
239000002131 composite material Substances 0.000 title claims abstract description 74
229960000672 rosuvastatin Drugs 0.000 title claims abstract description 57
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 title claims abstract description 57
238000000034 method Methods 0.000 title claims description 47
238000002360 preparation method Methods 0.000 title claims description 12
230000008569 process Effects 0.000 title description 4
239000007787 solid Substances 0.000 claims abstract description 58
239000008187 granular material Substances 0.000 claims abstract description 46
150000003839 salts Chemical class 0.000 claims abstract description 17
238000004090 dissolution Methods 0.000 claims description 47
239000012530 fluid Substances 0.000 claims description 44
239000003826 tablet Substances 0.000 claims description 24
239000000479 mixture part Substances 0.000 claims description 22
239000002904 solvent Substances 0.000 claims description 20
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical group O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 16
239000012153 distilled water Substances 0.000 claims description 14
239000007937 lozenge Substances 0.000 claims description 13
WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 12
235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 11
229920000168 Microcrystalline cellulose Polymers 0.000 claims description 10
239000011230 binding agent Substances 0.000 claims description 10
239000007884 disintegrant Substances 0.000 claims description 10
235000019813 microcrystalline cellulose Nutrition 0.000 claims description 10
239000008108 microcrystalline cellulose Substances 0.000 claims description 10
229940016286 microcrystalline cellulose Drugs 0.000 claims description 10
239000010410 layer Substances 0.000 claims description 9
229920002785 Croscarmellose sodium Polymers 0.000 claims description 8
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 8
229960001681 croscarmellose sodium Drugs 0.000 claims description 8
235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 8
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 8
229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 8
229940069328 povidone Drugs 0.000 claims description 8
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 6
DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 6
239000002775 capsule Substances 0.000 claims description 6
238000011978 dissolution method Methods 0.000 claims description 6
239000008101 lactose Substances 0.000 claims description 6
229960001375 lactose Drugs 0.000 claims description 6
235000019333 sodium laurylsulphate Nutrition 0.000 claims description 6
239000000654 additive Substances 0.000 claims description 5
239000000853 adhesive Substances 0.000 claims description 5
239000002552 dosage form Substances 0.000 claims description 5
239000000314 lubricant Substances 0.000 claims description 5
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 description 4
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 description 4
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 4
229930195725 Mannitol Natural products 0.000 claims description 4
229960000913 crospovidone Drugs 0.000 claims description 4
239000003085 diluting agent Substances 0.000 claims description 4
235000019359 magnesium stearate Nutrition 0.000 claims description 4
239000000594 mannitol Substances 0.000 claims description 4
235000010355 mannitol Nutrition 0.000 claims description 4
229960001855 mannitol Drugs 0.000 claims description 4
235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 4
229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 4
239000002356 single layer Substances 0.000 claims description 4
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 description 3
235000017858 Laurus nobilis Nutrition 0.000 claims description 3
QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 3
235000005212 Terminalia tomentosa Nutrition 0.000 claims description 3
244000125380 Terminalia tomentosa Species 0.000 claims description 3
230000000996 additive effect Effects 0.000 claims description 3
229920001531 copovidone Polymers 0.000 claims description 3
239000006187 pill Substances 0.000 claims description 3
239000000843 powder Substances 0.000 claims description 3
239000011734 sodium Substances 0.000 claims description 3
229910052708 sodium Inorganic materials 0.000 claims description 3
229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 2
229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 2
229920002472 Starch Polymers 0.000 claims description 2
239000007853 buffer solution Substances 0.000 claims description 2
239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 2
239000008112 carboxymethyl-cellulose Substances 0.000 claims description 2
229940105329 carboxymethylcellulose Drugs 0.000 claims description 2
MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 2
239000001863 hydroxypropyl cellulose Substances 0.000 claims description 2
235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 2
239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
229940071676 hydroxypropylcellulose Drugs 0.000 claims description 2
229960003943 hypromellose Drugs 0.000 claims description 2
229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 2
229940057948 magnesium stearate Drugs 0.000 claims description 2
RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 claims description 2
235000012239 silicon dioxide Nutrition 0.000 claims description 2
229940083542 sodium Drugs 0.000 claims description 2
239000008109 sodium starch glycolate Substances 0.000 claims description 2
229940079832 sodium starch glycolate Drugs 0.000 claims description 2
229920003109 sodium starch glycolate Polymers 0.000 claims description 2
229940045902 sodium stearyl fumarate Drugs 0.000 claims description 2
239000008107 starch Substances 0.000 claims description 2
229940032147 starch Drugs 0.000 claims description 2
235000019698 starch Nutrition 0.000 claims description 2
239000000454 talc Substances 0.000 claims description 2
229910052623 talc Inorganic materials 0.000 claims description 2
VILMUCRZVVVJCA-UHFFFAOYSA-M sodium glycolate Chemical compound [Na+].OCC([O-])=O VILMUCRZVVVJCA-UHFFFAOYSA-M 0.000 claims 1
229940071117 starch glycolate Drugs 0.000 claims 1
239000002245 particle Substances 0.000 description 16
239000000243 solution Substances 0.000 description 13
239000004480 active ingredient Substances 0.000 description 12
230000000052 comparative effect Effects 0.000 description 12
238000005550 wet granulation Methods 0.000 description 12
238000012360 testing method Methods 0.000 description 11
239000003814 drug Substances 0.000 description 10
229940079593 drug Drugs 0.000 description 9
239000004615 ingredient Substances 0.000 description 9
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 8
229920006395 saturated elastomer Polymers 0.000 description 8
150000001875 compounds Chemical class 0.000 description 7
230000007423 decrease Effects 0.000 description 7
238000005469 granulation Methods 0.000 description 7
230000003179 granulation Effects 0.000 description 7
238000005070 sampling Methods 0.000 description 7
238000005507 spraying Methods 0.000 description 6
208000032928 Dyslipidaemia Diseases 0.000 description 5
208000017170 Lipid metabolism disease Diseases 0.000 description 5
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 description 4
229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 4
230000001070 adhesive effect Effects 0.000 description 4
235000012000 cholesterol Nutrition 0.000 description 4
238000011156 evaluation Methods 0.000 description 4
239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 4
229960001021 lactose monohydrate Drugs 0.000 description 4
HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
239000008280 blood Substances 0.000 description 3
210000004369 blood Anatomy 0.000 description 3
GWEJFLVSOGNLSS-WPFOTENUSA-N ethyl (2s)-2-amino-5-[[(2r)-3-benzylsulfanyl-1-[[(1r)-2-ethoxy-2-oxo-1-phenylethyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate Chemical compound C([C@H](NC(=O)CC[C@H](N)C(=O)OCC)C(=O)N[C@@H](C(=O)OCC)C=1C=CC=CC=1)SCC1=CC=CC=C1 GWEJFLVSOGNLSS-WPFOTENUSA-N 0.000 description 3
229950003030 ezatiostat Drugs 0.000 description 3
239000002609 medium Substances 0.000 description 3
229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 description 3
238000008214 LDL Cholesterol Methods 0.000 description 2
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
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 2
230000015572 biosynthetic process Effects 0.000 description 2
239000000872 buffer Substances 0.000 description 2
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
230000000694 effects Effects 0.000 description 2
238000012812 general test Methods 0.000 description 2
150000002632 lipids Chemical class 0.000 description 2
239000000463 material Substances 0.000 description 2
230000007246 mechanism Effects 0.000 description 2
229910000403 monosodium phosphate Inorganic materials 0.000 description 2
235000019799 monosodium phosphate Nutrition 0.000 description 2
230000000144 pharmacologic effect Effects 0.000 description 2
239000012925 reference material Substances 0.000 description 2
229940074795 rosuvastatin and ezetimibe Drugs 0.000 description 2
LALFOYNTGMUKGG-BGRFNVSISA-L rosuvastatin calcium Chemical compound [Ca+2].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.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 LALFOYNTGMUKGG-BGRFNVSISA-L 0.000 description 2
AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 2
238000003786 synthesis reaction Methods 0.000 description 2
238000009475 tablet pressing Methods 0.000 description 2
238000010998 test method Methods 0.000 description 2
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 description 1
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 description 1
OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
206010013710 Drug interaction Diseases 0.000 description 1
108010023302 HDL Cholesterol Proteins 0.000 description 1
108010010234 HDL Lipoproteins Proteins 0.000 description 1
102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 description 1
108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 description 1
108010028554 LDL Cholesterol Proteins 0.000 description 1
FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
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 description 1
230000002378 acidificating effect Effects 0.000 description 1
229910000147 aluminium phosphate Inorganic materials 0.000 description 1
229960005370 atorvastatin Drugs 0.000 description 1
230000009286 beneficial effect Effects 0.000 description 1
210000001124 body fluid Anatomy 0.000 description 1
239000010839 body fluid Substances 0.000 description 1
229910052791 calcium Inorganic materials 0.000 description 1
239000011575 calcium Substances 0.000 description 1
159000000007 calcium salts Chemical class 0.000 description 1
230000008859 change Effects 0.000 description 1
239000003795 chemical substances by application Substances 0.000 description 1
238000002648 combination therapy Methods 0.000 description 1
229940066901 crestor Drugs 0.000 description 1
230000007547 defect Effects 0.000 description 1
238000010790 dilution Methods 0.000 description 1
239000012895 dilution Substances 0.000 description 1
201000010099 disease Diseases 0.000 description 1
208000035475 disorder Diseases 0.000 description 1
239000012738 dissolution medium Substances 0.000 description 1
238000007922 dissolution test Methods 0.000 description 1
238000005538 encapsulation Methods 0.000 description 1
238000002474 experimental method Methods 0.000 description 1
239000012458 free base Substances 0.000 description 1
230000036541 health Effects 0.000 description 1
230000001788 irregular Effects 0.000 description 1
238000010030 laminating Methods 0.000 description 1
229910052749 magnesium Inorganic materials 0.000 description 1
239000011777 magnesium Substances 0.000 description 1
239000002075 main ingredient Substances 0.000 description 1
238000004519 manufacturing process Methods 0.000 description 1
238000010297 mechanical methods and process Methods 0.000 description 1
238000000465 moulding Methods 0.000 description 1
239000008188 pellet Substances 0.000 description 1
238000003825 pressing Methods 0.000 description 1
230000009103 reabsorption Effects 0.000 description 1
229960002855 simvastatin Drugs 0.000 description 1
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 description 1
229940074790 simvastatin and ezetimibe Drugs 0.000 description 1
210000000813 small intestine Anatomy 0.000 description 1
BHZOKUMUHVTPBX-UHFFFAOYSA-M sodium acetic acid acetate Chemical compound [Na+].CC(O)=O.CC([O-])=O BHZOKUMUHVTPBX-UHFFFAOYSA-M 0.000 description 1
159000000008 strontium salts Chemical class 0.000 description 1
239000006188 syrup Substances 0.000 description 1
235000020357 syrup Nutrition 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
229940009349 vytorin Drugs 0.000 description 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient

Landscapes

Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Chemical & Material Sciences (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Epidemiology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Obesity (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Hematology (AREA)
Diabetes (AREA)
Medicinal Preparation (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

TW104119406A 2014-06-25 2015-06-16 用於口服投藥之包含依澤替米貝（ｅｚｅｔｉｍｉｂｅ）及羅舒伐他汀（ｒｏｓｕｖａｓｔａｔｉｎ）的複合調配物及其製備方法 TWI700100B (zh)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
KR10-2014-0078388		2014-06-25
KR1020140078388A KR101977785B1 (ko)	2014-06-25	2014-06-25	에제티미브 및 로수바스타틴을 포함하는 경구용 복합제제 및 그 제조방법

Publications (2)

Publication Number	Publication Date
TW201625223A TW201625223A (zh)	2016-07-16
TWI700100B true TWI700100B (zh)	2020-08-01

Family

ID=54938391

Family Applications (1)

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TW104119406A TWI700100B (zh)	2014-06-25	2015-06-16	用於口服投藥之包含依澤替米貝（ｅｚｅｔｉｍｉｂｅ）及羅舒伐他汀（ｒｏｓｕｖａｓｔａｔｉｎ）的複合調配物及其製備方法

Country Status (10)

Country	Link
KR (1)	KR101977785B1 (es)
AR (1)	AR100977A1 (es)
BR (1)	BR112016030111A2 (es)
CL (1)	CL2016003283A1 (es)
EC (1)	ECSP16096477A (es)
JO (1)	JOP20150154B1 (es)
SG (2)	SG10201811586YA (es)
TW (1)	TWI700100B (es)
UY (1)	UY36190A (es)
WO (1)	WO2015199356A1 (es)

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CZ2016539A3 (cs) *	2016-09-05	2018-03-14	Zentiva, K.S.	Farmaceutická kompozice obsahující dvě rozdílné účinné látky a způsob její přípravy
CZ2016538A3 (cs)	2016-09-05	2018-03-14	Zentiva, K.S.	Farmaceutická kompozice obsahující dvě rozdílné účinné látky
KR102206535B1 (ko) *	2016-11-29	2021-01-22	한미약품 주식회사	에제티미브 및 로수바스타틴을 포함하는 경구용 복합정제
EP3437636A1 (en) *	2017-08-02	2019-02-06	Adamed sp. z o.o.	Pharmaceutical composition comprising ezetimibe
KR102500643B1 (ko) *	2019-04-18	2023-02-16	한미약품 주식회사	에제티미브 및 로사르탄을 포함하는 약제학적 복합제제
KR20200137243A (ko)	2019-05-29	2020-12-09	콜마파마(주)	로수바스타틴 및 에제티미브를 포함하는 복합제의 제조방법
BR112022001783A2 (pt)	2019-07-31	2022-03-22	Tecnimede Sociedade Tecnico Medicinal Sa	Composições orais sólidas multiunitárias de liberação imediata, seus métodos e usos.
BR112023003323A2 (pt) *	2020-08-25	2023-03-21	Daewoong Pharmaceutical Co Ltd	Composição farmacêutica em forma de dosagem única
KR20250096941A (ko)	2023-12-20	2025-06-30	안국약품 주식회사	피타바스타틴 및 에제티미브를 포함하는 단일 정제 형태의 약학 조성물 및 이의 제조방법
KR20250161310A (ko) *	2024-05-08	2025-11-17	한미약품 주식회사	복약순응도가 개선된 에제티미브, 로수바스타틴 및 엠파글리플로진을 포함하는 복합제제

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KR100907144B1 (ko) *	2007-09-05	2009-07-09	박재섭	이동부재를 이용한 골프 클럽
WO2009024889A2 (en) *	2007-08-21	2009-02-26	Ranbaxy Laboratories Limited	Pharmaceutical composition comprising a hmg-coa reductase inhibitor and ezetimibe
WO2011019326A2 (en) *	2009-07-02	2011-02-17	Mahmut Bilgic	Solubility and stability enchancing pharmaceutical formulation
PT2459175T (pt) *	2009-07-28	2018-02-07	Egyt Gyogyszervegyeszeti Gyar	Novo processo de granulação e o granulado assim preparado
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
ES2802252T3 (es) *	2012-05-01	2021-01-18	Althera Life Sciences Llc	Formulación de comprimido oral que consiste en la combinación fija de rosuvastatina y ezetimiba para el tratamiento de hiperlipidemia y enfermedades cardiovasculares

2014
- 2014-06-25 KR KR1020140078388A patent/KR101977785B1/ko active Active
2015
- 2015-06-09 WO PCT/KR2015/005779 patent/WO2015199356A1/en not_active Ceased
- 2015-06-09 SG SG10201811586YA patent/SG10201811586YA/en unknown
- 2015-06-09 BR BR112016030111A patent/BR112016030111A2/pt not_active Application Discontinuation
- 2015-06-09 SG SG11201610748RA patent/SG11201610748RA/en unknown
- 2015-06-16 TW TW104119406A patent/TWI700100B/zh active
- 2015-06-24 UY UY0001036190A patent/UY36190A/es not_active Application Discontinuation
- 2015-06-24 AR ARP150102016A patent/AR100977A1/es not_active Application Discontinuation
- 2015-06-24 JO JOP/2015/0154A patent/JOP20150154B1/ar active
2016
- 2016-12-21 CL CL2016003283A patent/CL2016003283A1/es unknown
- 2016-12-23 EC ECIEPI201696477A patent/ECSP16096477A/es unknown

Also Published As

Publication number	Publication date
KR20160000762A (ko)	2016-01-05
CL2016003283A1 (es)	2017-07-28
TW201625223A (zh)	2016-07-16
AR100977A1 (es)	2016-11-16
JOP20150154B1 (ar)	2021-08-17
WO2015199356A1 (en)	2015-12-30
UY36190A (es)	2015-10-30
ECSP16096477A (es)	2017-01-31
SG11201610748RA (en)	2017-01-27
BR112016030111A2 (pt)	2017-08-22
KR101977785B1 (ko)	2019-05-14
SG10201811586YA (en)	2019-02-27

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