RU2016126430A - Пероральная фармацевтическая композиция - Google Patents
Пероральная фармацевтическая композиция Download PDFInfo
- Publication number
- RU2016126430A RU2016126430A RU2016126430A RU2016126430A RU2016126430A RU 2016126430 A RU2016126430 A RU 2016126430A RU 2016126430 A RU2016126430 A RU 2016126430A RU 2016126430 A RU2016126430 A RU 2016126430A RU 2016126430 A RU2016126430 A RU 2016126430A
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- Russia
- Prior art keywords
- poorly soluble
- soluble drug
- paragraphs
- pharmaceutical composition
- solid particle
- Prior art date
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- 239000008203 oral pharmaceutical composition Substances 0.000 title claims 8
- 239000002245 particle Substances 0.000 claims 20
- 239000007787 solid Substances 0.000 claims 16
- 239000003814 drug Substances 0.000 claims 12
- 229940079593 drug Drugs 0.000 claims 11
- -1 myristyl paraben Chemical compound 0.000 claims 6
- 239000002904 solvent Substances 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 3
- 229960003511 macrogol Drugs 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000004094 surface-active agent Substances 0.000 claims 3
- 239000003826 tablet Substances 0.000 claims 3
- 239000000263 2,3-dihydroxypropyl (Z)-octadec-9-enoate Substances 0.000 claims 2
- RZRNAYUHWVFMIP-GDCKJWNLSA-N 3-oleoyl-sn-glycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@H](O)CO RZRNAYUHWVFMIP-GDCKJWNLSA-N 0.000 claims 2
- QNZCBYKSOIHPEH-UHFFFAOYSA-N Apixaban Chemical compound C1=CC(OC)=CC=C1N1C(C(=O)N(CC2)C=3C=CC(=CC=3)N3C(CCCC3)=O)=C2C(C(N)=O)=N1 QNZCBYKSOIHPEH-UHFFFAOYSA-N 0.000 claims 2
- 229920001214 Polysorbate 60 Polymers 0.000 claims 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 2
- 239000003146 anticoagulant agent Substances 0.000 claims 2
- 229940127219 anticoagulant drug Drugs 0.000 claims 2
- 229960003886 apixaban Drugs 0.000 claims 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 claims 2
- 239000008387 emulsifying waxe Substances 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 229930195729 fatty acid Natural products 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims 2
- RZRNAYUHWVFMIP-UHFFFAOYSA-N monoelaidin Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-UHFFFAOYSA-N 0.000 claims 2
- 239000013618 particulate matter Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims 2
- 229960001148 rivaroxaban Drugs 0.000 claims 2
- KGFYHTZWPPHNLQ-AWEZNQCLSA-N rivaroxaban Chemical compound S1C(Cl)=CC=C1C(=O)NC[C@@H]1OC(=O)N(C=2C=CC(=CC=2)N2C(COCC2)=O)C1 KGFYHTZWPPHNLQ-AWEZNQCLSA-N 0.000 claims 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 2
- CUNWUEBNSZSNRX-RKGWDQTMSA-N (2r,3r,4r,5s)-hexane-1,2,3,4,5,6-hexol;(z)-octadec-9-enoic acid Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.CCCCCCCC\C=C/CCCCCCCC(O)=O.CCCCCCCC\C=C/CCCCCCCC(O)=O.CCCCCCCC\C=C/CCCCCCCC(O)=O CUNWUEBNSZSNRX-RKGWDQTMSA-N 0.000 claims 1
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical class OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims 1
- FFJCNSLCJOQHKM-CLFAGFIQSA-N (z)-1-[(z)-octadec-9-enoxy]octadec-9-ene Chemical compound CCCCCCCC\C=C/CCCCCCCCOCCCCCCCC\C=C/CCCCCCCC FFJCNSLCJOQHKM-CLFAGFIQSA-N 0.000 claims 1
- CMCBDXRRFKYBDG-UHFFFAOYSA-N 1-dodecoxydodecane Chemical compound CCCCCCCCCCCCOCCCCCCCCCCCC CMCBDXRRFKYBDG-UHFFFAOYSA-N 0.000 claims 1
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N 4-hydroxybenzoic acid Chemical compound OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims 1
- 244000215068 Acacia senegal Species 0.000 claims 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 1
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims 1
- 229920000858 Cyclodextrin Polymers 0.000 claims 1
- 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 1
- 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 1
- 229920001353 Dextrin Polymers 0.000 claims 1
- 239000004375 Dextrin Substances 0.000 claims 1
- 229940123583 Factor Xa inhibitor Drugs 0.000 claims 1
- 229920002907 Guar gum Polymers 0.000 claims 1
- 229920000084 Gum arabic Polymers 0.000 claims 1
- 229920000569 Gum karaya Polymers 0.000 claims 1
- 239000005639 Lauric acid Substances 0.000 claims 1
- 240000001090 Papaver somniferum Species 0.000 claims 1
- 235000008753 Papaver somniferum Nutrition 0.000 claims 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 1
- 229920001213 Polysorbate 20 Polymers 0.000 claims 1
- 229920001219 Polysorbate 40 Polymers 0.000 claims 1
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
- 229920002125 Sokalan® Polymers 0.000 claims 1
- NWGKJDSIEKMTRX-AAZCQSIUSA-N Sorbitan monooleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O NWGKJDSIEKMTRX-AAZCQSIUSA-N 0.000 claims 1
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims 1
- 239000004147 Sorbitan trioleate Substances 0.000 claims 1
- PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 claims 1
- 241000934878 Sterculia Species 0.000 claims 1
- 208000001435 Thromboembolism Diseases 0.000 claims 1
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims 1
- LWZFANDGMFTDAV-BURFUSLBSA-N [(2r)-2-[(2r,3r,4s)-3,4-dihydroxyoxolan-2-yl]-2-hydroxyethyl] dodecanoate Chemical compound CCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O LWZFANDGMFTDAV-BURFUSLBSA-N 0.000 claims 1
- 235000010489 acacia gum Nutrition 0.000 claims 1
- 239000000205 acacia gum Substances 0.000 claims 1
- 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 1
- 125000005907 alkyl ester group Chemical group 0.000 claims 1
- 239000000010 aprotic solvent Substances 0.000 claims 1
- UREZNYTWGJKWBI-UHFFFAOYSA-M benzethonium chloride Chemical compound [Cl-].C1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 UREZNYTWGJKWBI-UHFFFAOYSA-M 0.000 claims 1
- 229960001950 benzethonium chloride Drugs 0.000 claims 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 1
- 239000004359 castor oil Substances 0.000 claims 1
- 235000019438 castor oil Nutrition 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 229920002678 cellulose Polymers 0.000 claims 1
- 235000010980 cellulose Nutrition 0.000 claims 1
- 229960002798 cetrimide Drugs 0.000 claims 1
- 229960001927 cetylpyridinium chloride Drugs 0.000 claims 1
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims 1
- 229920001531 copovidone Polymers 0.000 claims 1
- 235000019425 dextrin Nutrition 0.000 claims 1
- 238000007907 direct compression Methods 0.000 claims 1
- 235000013399 edible fruits Nutrition 0.000 claims 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 125000005456 glyceride group Chemical group 0.000 claims 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims 1
- 239000000665 guar gum Substances 0.000 claims 1
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- 229920013821 hydroxy alkyl cellulose Polymers 0.000 claims 1
- 235000010494 karaya gum Nutrition 0.000 claims 1
- 239000000231 karaya gum Substances 0.000 claims 1
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- 229940033355 lauric acid Drugs 0.000 claims 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims 1
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims 1
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- 210000000214 mouth Anatomy 0.000 claims 1
- 229940124531 pharmaceutical excipient Drugs 0.000 claims 1
- 150000003904 phospholipids Chemical class 0.000 claims 1
- 229960000502 poloxamer Drugs 0.000 claims 1
- 229920001983 poloxamer Polymers 0.000 claims 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims 1
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 1
- 235000010483 polyoxyethylene sorbitan monopalmitate Nutrition 0.000 claims 1
- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 claims 1
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 claims 1
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 claims 1
- 229920000136 polysorbate Polymers 0.000 claims 1
- 229940068977 polysorbate 20 Drugs 0.000 claims 1
- 229940101027 polysorbate 40 Drugs 0.000 claims 1
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- 229940068968 polysorbate 80 Drugs 0.000 claims 1
- 229920000053 polysorbate 80 Polymers 0.000 claims 1
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
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- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
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- 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 1
- 235000010413 sodium alginate Nutrition 0.000 claims 1
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- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 claims 1
- 235000010199 sorbic acid Nutrition 0.000 claims 1
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- 125000004079 stearyl group Chemical group [H]C([*])([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])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
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- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims 1
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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Claims (26)
1. Твердая частица слаборастворимого лекарственного средства, имеющего средний размер частиц 100 мкм или менее, где на поверхности слаборастворимого лекарственного средства адсорбирован солюбилизатор.
2. Твердая частица по п. 1, где слаборастворимое лекарственное средство выбрано из антикоагулянта, выбранного из ингибиторов фактора Ха.
3. Твердая частица по п. 2, где слаборастворимое лекарственное средство представляет собой ривароксабан.
4. Твердая частица по п. 2, где слаборастворимое лекарственное средство представляет собой апиксабан.
5. Твердая частица по любому из пп. 1-4, где слаборастворимое лекарственное средство находится в микронизированной форме.
6. Твердая частица по любому из пп. 1-4, где слаборастворимое лекарственное средство находится в микронизированной форме и имеет средний размер частиц менее 50 мкм.
7. Твердая частица по любому из пп. 1-4, где слаборастворимое лекарственное средство находится в микронизированной форме и имеет средний размер частиц менее 30 мкм.
8. Твердая частица по любому из пп. 1-4, где слаборастворимое лекарственное средство находится в микронизированной форме и имеет средний размер частиц менее 20 мкм.
9. Твердая частица по любому из пп. 1-4, где слаборастворимое лекарственное средство находится в микронизированной форме и имеет средний размер частиц менее 10 мкм.
10. Твердая частица по п. 1, где солюбилизатор выбран из полиэтиленоксида, гидроксиалкилцеллюлозы, гидроксипропилалкилцеллюлозы, поливинилового спирта, поливинилпирролидона, коповидона, карбоксиметилцеллюлозы натрия, карбопола, альгината натрия, ксантановой камеди, смолы плодов рожкового дерева, целлюлозной камеди, геллановой камеди, трагакантовой камеди, камеди карайи, гуаровой камеди, аравийской камеди, полоксамера, циклодекстрина, производных декстрина, поверхностно-активных веществ и их смесей.
11. Твердая частица по п. 1, где солюбилизатор представляет собой поверхностно-активное вещество, выбранное из самоэмульгирующегося глицерилмоноолеата, докузата натрия, эмульгирующего воска BP, лаурилсульфата натрия, хлорида бензэтония, цетримида, хлорида цетилпиридиния, лауриновой кислоты, миристилового спирта, бутилпарабена, этилпарабена, метилпарабена, пропилпарабена, сорбиновой кислоты, эмульгирующего воска, глицерилмоноолеата, фосфолипидов, алкиловых эфиров полиоксиэтилена (цетостеарилового эфира макрогола, лаурилового эфира макрогола, олеилового эфира макрогола, стеарилового эфира макрогола), производных полиоксиэтилена с касторовым маслом (макроголглицеринрицинолеата, макроголглицерингидроксистеарата), сложных эфиров полиоксиэтиленсорбитана с жирными кислотами (полисорбата 20, 40, 60 и 80), полиоксиэтиленстеаратов, полиоксилглицеридов (каприлокапроилполиоксилглицеридов, лауроилполиоксилглицеридов, линолеоилполиоксилглицеридов, олеоилполиоксилглицеридов и стеароилполиоксилглицеридов), сорбитановых сложных эфиров (сорбитанлаурата, сорбитанолеата, сорбитанпальмитата, сорбитансесквиолеата, сорбитанстеарата, сорбитантриолеата), триэтилцитрата и их смесей.
12. Твердая частица по п. 1, где солюбилизатор представляет собой поверхностно-активное вещество, выбранное из твердого лаурилсульфата натрия, сложных эфиров полиоксиэтиленсорбитана с жирными кислотами и полиоксилглицеридов.
13. Способ получения твердых частиц по п. 1, характеризующийся тем, что он включает следующие стадии:
а) солюбилизатор растворяют или суспендируют в полярном или неполярном протонном или апротонном растворителе или их смесях;
б) раствор, полученный на стадии (а), выливают или распыляют на поверхность слаборастворимого лекарственного средства.
14. Способ по п. 13, где растворитель представляет собой воду.
15. Пероральная фармацевтическая композиция, содержащая твердые частицы по п. 1 с по меньшей мере одним фармацевтически приемлемым эксципиентом.
16. Пероральная фармацевтическая композиция по п. 15, где твердые частицы содержат антикоагулянт.
17. Пероральная фармацевтическая композиция по п. 15, где твердые частицы содержат ривароксабан или апиксабан.
18. Пероральная фармацевтическая композиция по любому из пп. 15-17, представляющая собой таблетку, минитаблетку или таблетку, диспергируемую в полости рта.
19. Пероральная фармацевтическая композиция по п. 18, изготовленная путем прямого прессования.
20. Способ изготовления пероральной фармацевтической композиции по любому из пп. 15-17, включающий:
а) получение твердых частиц по п. 1;
б) смешивание частиц со стадии (а) с по меньшей мере одним фармацевтическим эксципиентом.
21. Способ по п. 20, дополнительно включающий прессование смеси, полученной на стадии (б), в таблетку.
22. Применение пероральной фармацевтической композиции по любому из пп. 15-17 в изготовлении лекарственного средства для профилактики и/или лечения тромбоэмболических заболеваний.
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| PCT/EP2014/078783 WO2015097090A1 (en) | 2013-12-23 | 2014-12-19 | Oral pharmaceutical composition |
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| JP6585193B2 (ja) * | 2015-12-28 | 2019-10-02 | 沢井製薬株式会社 | ゲフィチニブ含有錠剤 |
| WO2017146709A1 (en) * | 2016-02-25 | 2017-08-31 | Mylan Inc. | A unique high-shear granulation process for improved bioavailability of rivaroxaban |
| CN105943508A (zh) * | 2016-05-27 | 2016-09-21 | 扬子江药业集团广州海瑞药业有限公司 | 一种利伐沙班药物组合物及其制备方法 |
| WO2018150286A1 (en) | 2017-02-17 | 2018-08-23 | Unichem Laboratories Ltd | Pharmaceutical composition of apixaban |
| US11510877B2 (en) | 2017-10-10 | 2022-11-29 | Capsugel Belgium Nv | Gelling multiparticulates |
| CN108743556A (zh) * | 2018-02-02 | 2018-11-06 | 重庆植恩药业有限公司 | 一种依度沙班片剂及其制备方法 |
| KR102128321B1 (ko) * | 2018-03-13 | 2020-06-30 | 주식회사 종근당 | 아픽사반을 포함하는 가용화를 위한 약제학적 제제 및 이의 제조 방법 |
| GR1009619B (el) * | 2018-05-09 | 2019-10-23 | Φαρμαζακ Α.Φ.Ε.Β.Ε. | Φαρμακευτικη συνθεση που περιεχει ριβαροξαβανη και μεθοδος για την παρασκευη αυτης |
| KR20190130411A (ko) | 2018-05-14 | 2019-11-22 | 신일제약주식회사 | 아픽사반 약제학적 제제 및 그의 제조방법 |
| KR102222774B1 (ko) * | 2018-07-27 | 2021-03-04 | 보령제약 주식회사 | 에독사반을 포함하는 약학적 제제 및 이의 제조방법 |
| WO2020060336A1 (ko) * | 2018-09-21 | 2020-03-26 | 동아에스티 주식회사 | 리바록사반을 포함하는 가용화 조성물 |
| EP3669866A1 (en) | 2018-12-19 | 2020-06-24 | KRKA, d.d., Novo mesto | Pharmaceutical composition comprising apixaban |
| WO2021006267A1 (ja) * | 2019-07-08 | 2021-01-14 | グリーン・テック株式会社 | ピラゾール誘導体の塩及びピラゾール誘導体の製剤 |
| KR102290670B1 (ko) * | 2019-12-30 | 2021-08-18 | 단국대학교 천안캠퍼스 산학협력단 | 자가나노유화 약물전달시스템을 이용한 리바록사반의 경구용 고형제 조성물 및 이의 제조방법 |
| JP7465157B2 (ja) * | 2020-06-15 | 2024-04-10 | 沢井製薬株式会社 | リバーロキサバン含有口腔内崩壊錠の製造方法 |
| CN112494489B (zh) * | 2020-12-18 | 2021-09-03 | 浙江诺得药业有限公司 | 一种含有阿哌沙班的复方缓释制剂及其制备方法 |
| CN114767647B (zh) * | 2022-03-22 | 2024-04-16 | 新发药业有限公司 | 一种利伐沙班口服固体制剂的制备方法 |
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| WO1994008709A1 (en) * | 1992-10-09 | 1994-04-28 | Kanegafuchi Kagaku Kogyo Kabushiki Kaisha | Production method for fine granulate |
| WO2010017948A2 (en) * | 2008-08-11 | 2010-02-18 | Ratiopharm Gmbh | Pharmaceutical compositions with modified release properties comprising 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl)-methyl)-2-thiophencarboxamid |
| US20100159001A1 (en) * | 2008-12-19 | 2010-06-24 | Cardinal John R | Extended-Release Pharmaceutical Formulations |
| MX2011013080A (es) * | 2009-06-16 | 2012-01-20 | Pfizer | Formas de dosis de apixaban. |
| HUE031177T2 (hu) * | 2009-06-18 | 2017-07-28 | Krka Tovarna Zdravil D D Novo Mesto | Rivaroxabant tartalmazó szilárd gyógyszerkészítmény |
| US20120189670A1 (en) * | 2009-09-14 | 2012-07-26 | Kirkpatrick D Lynn | Pharmaceutical compositions and formulations including inhibitors of the pleckstrin homology domain and methods for using same |
| WO2011042156A1 (en) * | 2009-10-06 | 2011-04-14 | Ratiopharm Gmbh | Pharmaceutical compositions comprising rivaroxaban |
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| CA2934120A1 (en) | 2015-07-02 |
| US20170000799A1 (en) | 2017-01-05 |
| AU2014372692A1 (en) | 2016-07-14 |
| WO2015097090A1 (en) | 2015-07-02 |
| IL246377A0 (en) | 2016-08-31 |
| CN105848644A (zh) | 2016-08-10 |
| EP3086778A1 (en) | 2016-11-02 |
| KR20160098508A (ko) | 2016-08-18 |
| JP2017500332A (ja) | 2017-01-05 |
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