JP2019533008A5 - - Google Patents
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- JP2019533008A5 JP2019533008A5 JP2019535991A JP2019535991A JP2019533008A5 JP 2019533008 A5 JP2019533008 A5 JP 2019533008A5 JP 2019535991 A JP2019535991 A JP 2019535991A JP 2019535991 A JP2019535991 A JP 2019535991A JP 2019533008 A5 JP2019533008 A5 JP 2019533008A5
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- 239000000203 mixture Substances 0.000 claims description 115
- 239000013078 crystal Substances 0.000 claims description 39
- 239000007788 liquid Substances 0.000 claims description 31
- 239000000725 suspension Substances 0.000 claims description 27
- 239000004067 bulking agent Substances 0.000 claims description 21
- 239000008194 pharmaceutical composition Substances 0.000 claims description 21
- -1 alkenyl ether Chemical compound 0.000 claims description 17
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 14
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 12
- 229920000053 polysorbate 80 Polymers 0.000 claims description 12
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 10
- 229920001577 copolymer Polymers 0.000 claims description 10
- 239000000654 additive Substances 0.000 claims description 9
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims description 8
- 229910019142 PO4 Inorganic materials 0.000 claims description 8
- 230000000996 additive effect Effects 0.000 claims description 8
- 229920001531 copovidone Polymers 0.000 claims description 8
- LYCAIKOWRPUZTN-UHFFFAOYSA-N ethylene glycol Natural products OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 8
- 239000000796 flavoring agent Substances 0.000 claims description 8
- 235000019634 flavors Nutrition 0.000 claims description 8
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 8
- 239000010452 phosphate Substances 0.000 claims description 8
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 7
- 229920000642 polymer Polymers 0.000 claims description 7
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 7
- 239000003381 stabilizer Substances 0.000 claims description 7
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 6
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 6
- 235000003599 food sweetener Nutrition 0.000 claims description 5
- 239000003765 sweetening agent Substances 0.000 claims description 5
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims description 4
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 4
- 235000006679 Mentha X verticillata Nutrition 0.000 claims description 4
- 235000002899 Mentha suaveolens Nutrition 0.000 claims description 4
- 235000001636 Mentha x rotundifolia Nutrition 0.000 claims description 4
- 229920002675 Polyoxyl Polymers 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- SYELZBGXAIXKHU-UHFFFAOYSA-N dodecyldimethylamine N-oxide Chemical compound CCCCCCCCCCCC[N+](C)(C)[O-] SYELZBGXAIXKHU-UHFFFAOYSA-N 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims description 4
- 229940041616 menthol Drugs 0.000 claims description 4
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 claims description 3
- 229920001214 Polysorbate 60 Polymers 0.000 claims description 3
- 239000003125 aqueous solvent Substances 0.000 claims description 3
- 239000008369 fruit flavor Substances 0.000 claims description 3
- 229920000136 polysorbate Polymers 0.000 claims description 3
- 229950008882 polysorbate Drugs 0.000 claims description 3
- CMCBDXRRFKYBDG-UHFFFAOYSA-N 1-dodecoxydodecane Chemical compound CCCCCCCCCCCCOCCCCCCCCCCCC CMCBDXRRFKYBDG-UHFFFAOYSA-N 0.000 claims description 2
- HBXWUCXDUUJDRB-UHFFFAOYSA-N 1-octadecoxyoctadecane Chemical compound CCCCCCCCCCCCCCCCCCOCCCCCCCCCCCCCCCCCC HBXWUCXDUUJDRB-UHFFFAOYSA-N 0.000 claims description 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 2
- IEORSVTYLWZQJQ-UHFFFAOYSA-N 2-(2-nonylphenoxy)ethanol Chemical compound CCCCCCCCCC1=CC=CC=C1OCCO IEORSVTYLWZQJQ-UHFFFAOYSA-N 0.000 claims description 2
- NLMKTBGFQGKQEV-UHFFFAOYSA-N 2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2-hexadecoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol Chemical compound CCCCCCCCCCCCCCCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO NLMKTBGFQGKQEV-UHFFFAOYSA-N 0.000 claims description 2
- AMRBZKOCOOPYNY-QXMHVHEDSA-N 2-[dimethyl-[(z)-octadec-9-enyl]azaniumyl]acetate Chemical compound CCCCCCCC\C=C/CCCCCCCC[N+](C)(C)CC([O-])=O AMRBZKOCOOPYNY-QXMHVHEDSA-N 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 2
- 229920000858 Cyclodextrin Polymers 0.000 claims description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 2
- QWZLBLDNRUUYQI-UHFFFAOYSA-M Methylbenzethonium chloride Chemical compound [Cl-].CC1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 QWZLBLDNRUUYQI-UHFFFAOYSA-M 0.000 claims description 2
- 206010028116 Mucosal inflammation Diseases 0.000 claims description 2
- 201000010927 Mucositis Diseases 0.000 claims description 2
- AOMUHOFOVNGZAN-UHFFFAOYSA-N N,N-bis(2-hydroxyethyl)dodecanamide Chemical compound CCCCCCCCCCCC(=O)N(CCO)CCO AOMUHOFOVNGZAN-UHFFFAOYSA-N 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 235000021028 berry Nutrition 0.000 claims description 2
- 229920003174 cellulose-based polymer Polymers 0.000 claims description 2
- 229940056318 ceteth-20 Drugs 0.000 claims description 2
- 229960000541 cetyl alcohol Drugs 0.000 claims description 2
- MRUAUOIMASANKQ-UHFFFAOYSA-N cocamidopropyl betaine Chemical compound CCCCCCCCCCCC(=O)NCCC[N+](C)(C)CC([O-])=O MRUAUOIMASANKQ-UHFFFAOYSA-N 0.000 claims description 2
- 229940073507 cocamidopropyl betaine Drugs 0.000 claims description 2
- 210000001072 colon Anatomy 0.000 claims description 2
- 239000002274 desiccant Substances 0.000 claims description 2
- RNPXCFINMKSQPQ-UHFFFAOYSA-N dicetyl hydrogen phosphate Chemical compound CCCCCCCCCCCCCCCCOP(O)(=O)OCCCCCCCCCCCCCCCC RNPXCFINMKSQPQ-UHFFFAOYSA-N 0.000 claims description 2
- 229940008099 dimethicone Drugs 0.000 claims description 2
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims description 2
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 235000010445 lecithin Nutrition 0.000 claims description 2
- 239000000787 lecithin Substances 0.000 claims description 2
- 229940067606 lecithin Drugs 0.000 claims description 2
- 239000008297 liquid dosage form Substances 0.000 claims description 2
- 239000000314 lubricant Substances 0.000 claims description 2
- 229960002285 methylbenzethonium chloride Drugs 0.000 claims description 2
- 229920000847 nonoxynol Polymers 0.000 claims description 2
- 229950004053 octoxinol Drugs 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 2
- 229920002401 polyacrylamide Polymers 0.000 claims description 2
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 238000001959 radiotherapy Methods 0.000 claims description 2
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 2
- FRHNXUKHAUWMOQ-UHFFFAOYSA-M sodium;16-methylheptadecanoate Chemical compound [Na+].CC(C)CCCCCCCCCCCCCCC([O-])=O FRHNXUKHAUWMOQ-UHFFFAOYSA-M 0.000 claims description 2
- 238000011200 topical administration Methods 0.000 claims description 2
- 239000007900 aqueous suspension Substances 0.000 claims 5
- 235000013355 food flavoring agent Nutrition 0.000 claims 5
- 235000019640 taste Nutrition 0.000 claims 4
- 239000005454 flavour additive Substances 0.000 claims 3
- 230000000873 masking effect Effects 0.000 claims 3
- HNLXNOZHXNSSPN-UHFFFAOYSA-N 2-[2-[2-[2-[2-[2-[2-[4-(2,4,4-trimethylpentan-2-yl)phenoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol Chemical compound CC(C)(C)CC(C)(C)C1=CC=C(OCCOCCOCCOCCOCCOCCOCCO)C=C1 HNLXNOZHXNSSPN-UHFFFAOYSA-N 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 230000002421 anti-septic effect Effects 0.000 claims 1
- 238000000149 argon plasma sintering Methods 0.000 claims 1
- 210000000941 bile Anatomy 0.000 claims 1
- 235000019658 bitter taste Nutrition 0.000 claims 1
- 230000035597 cooling sensation Effects 0.000 claims 1
- UUFFXMPIDQJWET-UHFFFAOYSA-N ethyl 2-methylprop-2-enoate;hydrochloride Chemical compound Cl.CCOC(=O)C(C)=C UUFFXMPIDQJWET-UHFFFAOYSA-N 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 230000005923 long-lasting effect Effects 0.000 claims 1
- 230000035807 sensation Effects 0.000 claims 1
- 235000019615 sensations Nutrition 0.000 claims 1
- 239000000375 suspending agent Substances 0.000 claims 1
- 229920003083 Kollidon® VA64 Polymers 0.000 description 14
- 239000007787 solid Substances 0.000 description 13
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 12
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 12
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 11
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- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 description 9
- 239000002904 solvent Substances 0.000 description 8
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- 229920002307 Dextran Polymers 0.000 description 6
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 229920000193 polymethacrylate Polymers 0.000 description 6
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 6
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 6
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 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 description 4
- 229920001993 poloxamer 188 Polymers 0.000 description 4
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 description 3
- 229920003081 Povidone K 30 Polymers 0.000 description 3
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 description 3
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 description 3
- 229940119744 dextran 40 Drugs 0.000 description 3
- AMTWCFIAVKBGOD-UHFFFAOYSA-N dioxosilane;methoxy-dimethyl-trimethylsilyloxysilane Chemical compound O=[Si]=O.CO[Si](C)(C)O[Si](C)(C)C AMTWCFIAVKBGOD-UHFFFAOYSA-N 0.000 description 3
- 229920001983 poloxamer Polymers 0.000 description 3
- 229940083037 simethicone Drugs 0.000 description 3
- CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 description 2
- SRBFZHDQGSBBOR-IOVATXLUSA-N D-xylopyranose Chemical compound O[C@@H]1COC(O)[C@H](O)[C@H]1O SRBFZHDQGSBBOR-IOVATXLUSA-N 0.000 description 2
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 2
- 239000004141 Sodium laurylsulphate Substances 0.000 description 2
- 239000004376 Sucralose Substances 0.000 description 2
- 238000001816 cooling Methods 0.000 description 2
- 238000002296 dynamic light scattering Methods 0.000 description 2
- 150000002170 ethers Chemical class 0.000 description 2
- CKNAQFVBEHDJQV-UHFFFAOYSA-N oltipraz Chemical compound S1SC(=S)C(C)=C1C1=CN=CC=N1 CKNAQFVBEHDJQV-UHFFFAOYSA-N 0.000 description 2
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- 239000004302 potassium sorbate Substances 0.000 description 2
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- WLAMNBDJUVNPJU-UHFFFAOYSA-N 2-methylbutyric acid Chemical compound CCC(C)C(O)=O WLAMNBDJUVNPJU-UHFFFAOYSA-N 0.000 description 1
- JYCQQPHGFMYQCF-UHFFFAOYSA-N 4-tert-Octylphenol monoethoxylate Chemical compound CC(C)(C)CC(C)(C)C1=CC=C(OCCO)C=C1 JYCQQPHGFMYQCF-UHFFFAOYSA-N 0.000 description 1
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 description 1
- 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 description 1
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- JDRSMPFHFNXQRB-CMTNHCDUSA-N Decyl beta-D-threo-hexopyranoside Chemical compound CCCCCCCCCCO[C@@H]1O[C@H](CO)C(O)[C@H](O)C1O JDRSMPFHFNXQRB-CMTNHCDUSA-N 0.000 description 1
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- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
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- 239000000619 acesulfame-K Substances 0.000 description 1
- IYKJEILNJZQJPU-UHFFFAOYSA-N acetic acid;butanedioic acid Chemical compound CC(O)=O.OC(=O)CCC(O)=O IYKJEILNJZQJPU-UHFFFAOYSA-N 0.000 description 1
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
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- PYMYPHUHKUWMLA-UHFFFAOYSA-N arabinose Natural products OCC(O)C(O)C(O)C=O PYMYPHUHKUWMLA-UHFFFAOYSA-N 0.000 description 1
- 239000000605 aspartame Substances 0.000 description 1
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| US8858995B2 (en) | 2008-03-10 | 2014-10-14 | University Of Louisville Research Foundation, Inc. | Methods and compositions for controlled delivery of phytochemical agents |
| US8142806B2 (en) | 2008-03-10 | 2012-03-27 | University Of Louisville Research Foundation, Inc. | Methods and compositions for controlled delivery of phytochemical agents |
| KR101057485B1 (ko) | 2008-08-04 | 2011-08-17 | 서울대학교산학협력단 | 1,2-디티올티온 유도체를 함유하는 엘엑스알-알파 과다발현으로 인한 질병의 예방 및 치료용 약학 조성물 |
| WO2010128026A2 (en) | 2009-05-05 | 2010-11-11 | Givaudan Sa | Organic compounds |
| US10463611B2 (en) * | 2011-06-08 | 2019-11-05 | Sti Pharma, Llc | Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration |
| ES2632443T3 (es) * | 2011-09-22 | 2017-09-13 | Viiv Healthcare Uk Limited | Compuestos de pirrolopiridinona y procedimientos de tratamiento del VIH |
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| CA2937766A1 (en) | 2014-02-27 | 2015-09-03 | The Procter & Gamble Company | Oral care compositions with a reduced bitter taste perception |
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| ITUB20159655A1 (it) | 2015-12-23 | 2017-06-23 | Bormioli Rocco Spa | Capsula di sicurezza di un contenitore. |
| ITUA20162141A1 (it) | 2016-03-31 | 2017-10-01 | Bormioli Pharma Spa | Capsula di chiusura |
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| KR20180123796A (ko) | 2017-05-10 | 2018-11-20 | 서울대학교산학협력단 | Nrf2-NEMO 경로 활성화를 통한 과중력으로 인한 세포괴사의 억제용 조성물 및 방법 |
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