JP2017528516A5 - - Google Patents

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Publication number: JP2017528516A5
Authority: JP; Japan
Prior art keywords: weight; statin; particles; type; pharmaceutical formulation
Prior art date: 2015-08-13
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

Application number

JP2017528760A

Other languages

English (en)

Japanese (ja)

Other versions

JP2017528516A (ja

JP6667526B2 (ja

Filing date

2015-08-13

Publication date

2018-08-30

2015-08-13 Application filed filed Critical

2015-08-13 Priority claimed from PCT/US2015/045140 external-priority patent/WO2016025762A1/en

2017-09-28 Publication of JP2017528516A publication Critical patent/JP2017528516A/ja

2018-08-30 Publication of JP2017528516A5 publication Critical patent/JP2017528516A5/ja

2020-03-18 Application granted granted Critical

2020-03-18 Publication of JP6667526B2 publication Critical patent/JP6667526B2/ja

Status Active legal-status Critical Current

2035-08-13 Anticipated expiration legal-status Critical

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229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 56
238000009472 formulation Methods 0.000 claims description 48
239000000203 mixture Substances 0.000 claims description 48
239000002245 particle Substances 0.000 claims description 23
229920000642 polymer Polymers 0.000 claims description 18
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 16
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 16
238000002360 preparation method Methods 0.000 claims description 12
230000000968 intestinal effect Effects 0.000 claims description 10
229920000168 Microcrystalline cellulose Polymers 0.000 claims description 8
WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 8
229920001531 copovidone Polymers 0.000 claims description 8
229960000913 crospovidone Drugs 0.000 claims description 8
235000019359 magnesium stearate Nutrition 0.000 claims description 8
235000019813 microcrystalline cellulose Nutrition 0.000 claims description 8
239000008108 microcrystalline cellulose Substances 0.000 claims description 8
229940016286 microcrystalline cellulose Drugs 0.000 claims description 8
235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 8
229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 8
235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 8
239000000377 silicon dioxide Substances 0.000 claims description 8
235000012239 silicon dioxide Nutrition 0.000 claims description 8
206010010774 Constipation Diseases 0.000 claims description 7
150000002596 lactones Chemical class 0.000 claims description 6
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
238000013270 controlled release Methods 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
210000001198 duodenum Anatomy 0.000 claims description 4
239000002775 capsule Substances 0.000 claims description 3
239000003814 drug Substances 0.000 claims description 3
239000003826 tablet Substances 0.000 claims description 3
239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims description 2
230000002401 inhibitory effect Effects 0.000 claims description 2
239000011325 microbead Substances 0.000 claims description 2
239000008185 minitablet Substances 0.000 claims description 2
239000008194 pharmaceutical composition Substances 0.000 claims 14
239000000825 pharmaceutical preparation Substances 0.000 claims 5
125000005395 methacrylic acid group Chemical group 0.000 claims 1
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
238000000034 method Methods 0.000 description 13
239000011248 coating agent Substances 0.000 description 10
238000000576 coating method Methods 0.000 description 10
208000002551 irritable bowel syndrome Diseases 0.000 description 6
VNWKTOKETHGBQD-UHFFFAOYSA-N methane Chemical compound C VNWKTOKETHGBQD-UHFFFAOYSA-N 0.000 description 6
238000011282 treatment Methods 0.000 description 5
238000011283 initial treatment period Methods 0.000 description 4
229960002965 pravastatin Drugs 0.000 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 description 4
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 description 3
239000003112 inhibitor Substances 0.000 description 3
239000000651 prodrug Substances 0.000 description 3
229940002612 prodrug Drugs 0.000 description 3
150000003839 salts Chemical class 0.000 description 3
FJLGEFLZQAZZCD-JUFISIKESA-N (3S,5R)-fluvastatin Chemical compound 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 FJLGEFLZQAZZCD-JUFISIKESA-N 0.000 description 2
108010008184 Aryldialkylphosphatase Proteins 0.000 description 2
102000006996 Aryldialkylphosphatase Human genes 0.000 description 2
108090000790 Enzymes Proteins 0.000 description 2
102000004190 Enzymes Human genes 0.000 description 2
229940122601 Esterase inhibitor Drugs 0.000 description 2
239000003795 chemical substances by application Substances 0.000 description 2
238000003776 cleavage reaction Methods 0.000 description 2
210000001072 colon Anatomy 0.000 description 2
239000007771 core particle Substances 0.000 description 2
230000001419 dependent effect Effects 0.000 description 2
230000003628 erosive effect Effects 0.000 description 2
239000002329 esterase inhibitor Substances 0.000 description 2
210000004051 gastric juice Anatomy 0.000 description 2
210000003405 ileum Anatomy 0.000 description 2
210000002429 large intestine Anatomy 0.000 description 2
230000000813 microbial effect Effects 0.000 description 2
230000007017 scission Effects 0.000 description 2
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 2
210000000813 small intestine Anatomy 0.000 description 2
229940124597 therapeutic agent Drugs 0.000 description 2
230000036962 time dependent Effects 0.000 description 2
VDSBXXDKCUBMQC-HNGSOEQISA-N (4r,6s)-6-[(e)-2-[2-(4-fluoro-3-methylphenyl)-4,4,6,6-tetramethylcyclohexen-1-yl]ethenyl]-4-hydroxyoxan-2-one Chemical compound C1=C(F)C(C)=CC(C=2CC(C)(C)CC(C)(C)C=2\C=C\[C@H]2OC(=O)C[C@H](O)C2)=C1 VDSBXXDKCUBMQC-HNGSOEQISA-N 0.000 description 1
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
240000000560 Citrus x paradisi Species 0.000 description 1
235000016623 Fragaria vesca Nutrition 0.000 description 1
240000009088 Fragaria x ananassa Species 0.000 description 1
235000011363 Fragaria x ananassa Nutrition 0.000 description 1
102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 description 1
108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 description 1
208000008589 Obesity Diseases 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
AJLFOPYRIVGYMJ-UHFFFAOYSA-N SJ000287055 Natural products C12C(OC(=O)C(C)CC)CCC=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 AJLFOPYRIVGYMJ-UHFFFAOYSA-N 0.000 description 1
230000001174 ascending effect Effects 0.000 description 1
229960005370 atorvastatin Drugs 0.000 description 1
210000004534 cecum Anatomy 0.000 description 1
229960005110 cerivastatin Drugs 0.000 description 1
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 description 1
229950003040 dalvastatin Drugs 0.000 description 1
230000003247 decreasing effect Effects 0.000 description 1
206010012601 diabetes mellitus Diseases 0.000 description 1
229960003765 fluvastatin Drugs 0.000 description 1
230000005176 gastrointestinal motility Effects 0.000 description 1
210000001035 gastrointestinal tract Anatomy 0.000 description 1
230000005764 inhibitory process Effects 0.000 description 1
210000001630 jejunum Anatomy 0.000 description 1
229950009116 mevastatin Drugs 0.000 description 1
AJLFOPYRIVGYMJ-INTXDZFKSA-N mevastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=CCC[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 AJLFOPYRIVGYMJ-INTXDZFKSA-N 0.000 description 1
BOZILQFLQYBIIY-UHFFFAOYSA-N mevastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CCC=C21 BOZILQFLQYBIIY-UHFFFAOYSA-N 0.000 description 1
235000020824 obesity Nutrition 0.000 description 1
239000000546 pharmaceutical excipient Substances 0.000 description 1
229960002797 pitavastatin Drugs 0.000 description 1
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 description 1
210000000664 rectum Anatomy 0.000 description 1
229960000672 rosuvastatin Drugs 0.000 description 1
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 description 1
229960002855 simvastatin Drugs 0.000 description 1
210000002784 stomach Anatomy 0.000 description 1

JP2017528760A 2014-08-13 2015-08-13 抗メタン生成組成物及びその使用 Active JP6667526B2 (ja)

Applications Claiming Priority (9)

Application Number	Priority Date	Filing Date	Title
US201462036948P	2014-08-13	2014-08-13
US62/036,948		2014-08-13
US201462043649P	2014-08-29	2014-08-29
US201462043789P	2014-08-29	2014-08-29
US62/043,789		2014-08-29
US62/043,649		2014-08-29
US201562141355P	2015-04-01	2015-04-01
US62/141,355		2015-04-01
PCT/US2015/045140 WO2016025762A1 (en)	2014-08-13	2015-08-13	Anti-methanogenic compositions and uses thereof

Publications (3)

Publication Number	Publication Date
JP2017528516A JP2017528516A (ja)	2017-09-28
JP2017528516A5 true JP2017528516A5 (2)	2018-08-30
JP6667526B2 JP6667526B2 (ja)	2020-03-18

Family

ID=55301332

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2017528760A Active JP6667526B2 (ja)	2014-08-13	2015-08-13	抗メタン生成組成物及びその使用

Country Status (12)

Country	Link
US (5)	US9956292B2 (2)
EP (1)	EP3179983A4 (2)
JP (1)	JP6667526B2 (2)
KR (1)	KR102425303B1 (2)
CN (1)	CN106687107B (2)
AU (1)	AU2015301596B2 (2)
BR (1)	BR112017002761A2 (2)
CA (1)	CA2955666A1 (2)
IL (1)	IL250568B (2)
MX (1)	MX2017001971A (2)
RU (1)	RU2697851C2 (2)
WO (1)	WO2016025762A1 (2)

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2015
- 2015-08-13 KR KR1020177005268A patent/KR102425303B1/ko active Active
- 2015-08-13 JP JP2017528760A patent/JP6667526B2/ja active Active
- 2015-08-13 EP EP15831885.7A patent/EP3179983A4/en active Pending
- 2015-08-13 MX MX2017001971A patent/MX2017001971A/es active IP Right Grant
- 2015-08-13 WO PCT/US2015/045140 patent/WO2016025762A1/en not_active Ceased
- 2015-08-13 AU AU2015301596A patent/AU2015301596B2/en active Active
- 2015-08-13 CA CA2955666A patent/CA2955666A1/en not_active Abandoned
- 2015-08-13 BR BR112017002761A patent/BR112017002761A2/pt not_active Application Discontinuation
- 2015-08-13 RU RU2017106896A patent/RU2697851C2/ru active IP Right Revival
- 2015-08-13 US US14/826,115 patent/US9956292B2/en active Active
- 2015-08-13 CN CN201580050231.6A patent/CN106687107B/zh not_active Expired - Fee Related
2017
- 2017-02-12 IL IL250568A patent/IL250568B/en active IP Right Grant
2018
- 2018-03-29 US US15/940,063 patent/US10328151B2/en active Active
2019
- 2019-05-07 US US16/405,667 patent/US10668159B2/en active Active
2020
- 2020-04-27 US US16/859,082 patent/US11344501B2/en active Active
2022
- 2022-05-12 US US17/742,665 patent/US20230036151A1/en not_active Abandoned

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