ITMI20070720A1 - Composizioni orali contenenti tacrolimus in forma amorfa - Google Patents

Composizioni orali contenenti tacrolimus in forma amorfa Download PDF

Info

Publication number: ITMI20070720A1
Authority: IT; Italy
Prior art keywords: tacrolimus; gelatin capsules; compositions according; capsule; diluent
Prior art date: 2007-04-06

Application number

Other languages

English (en)

Italian (it)

Inventor

Manuela Astulfoni

Giancarlo Ceschel

Luca Rampoldi

Celestino Ronchi

Original Assignee

Monteresearch Srl

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.)

2007-04-06

Filing date

2007-04-06

Publication date

2008-10-07

2007-04-06 Application filed by Monteresearch Srl filed Critical Monteresearch Srl

2007-04-06 Priority to ITMI20070720 priority Critical patent/ITMI20070720A1/it

2008-04-04 Priority to PCT/EP2008/002716 priority patent/WO2008122425A2/fr

2008-10-07 Publication of ITMI20070720A1 publication Critical patent/ITMI20070720A1/it

Links

239000000203 mixture Substances 0.000 title claims description 103
QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 title claims description 82
229960001967 tacrolimus Drugs 0.000 title claims description 73
QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 title claims description 73
239000007903 gelatin capsule Substances 0.000 claims description 63
XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 claims description 27
238000009472 formulation Methods 0.000 claims description 27
150000002632 lipids Chemical class 0.000 claims description 27
239000003795 chemical substances by application Substances 0.000 claims description 24
238000004090 dissolution Methods 0.000 claims description 21
239000002904 solvent Substances 0.000 claims description 21
239000004480 active ingredient Substances 0.000 claims description 20
239000003085 diluting agent Substances 0.000 claims description 20
239000008187 granular material Substances 0.000 claims description 14
238000000034 method Methods 0.000 claims description 11
239000007787 solid Substances 0.000 claims description 10
239000006057 Non-nutritive feed additive Substances 0.000 claims description 9
230000008569 process Effects 0.000 claims description 9
239000000126 substance Substances 0.000 claims description 9
235000014113 dietary fatty acids Nutrition 0.000 claims description 7
239000000194 fatty acid Substances 0.000 claims description 7
229930195729 fatty acid Natural products 0.000 claims description 7
238000004519 manufacturing process Methods 0.000 claims description 7
238000003756 stirring Methods 0.000 claims description 7
PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 6
150000004665 fatty acids Chemical class 0.000 claims description 6
239000000843 powder Substances 0.000 claims description 5
239000000725 suspension Substances 0.000 claims description 5
150000002148 esters Chemical class 0.000 claims description 4
239000007788 liquid Substances 0.000 claims description 4
238000000265 homogenisation Methods 0.000 claims description 3
239000000155 melt Substances 0.000 claims description 3
230000003381 solubilizing effect Effects 0.000 claims description 3
238000001179 sorption measurement Methods 0.000 claims description 3
230000000087 stabilizing effect Effects 0.000 claims description 3
229940075557 diethylene glycol monoethyl ether Drugs 0.000 claims description 2
229920001223 polyethylene glycol Polymers 0.000 claims description 2
239000002202 Polyethylene glycol Substances 0.000 claims 1
238000013270 controlled release Methods 0.000 claims 1
239000002775 capsule Substances 0.000 description 87
NWJQLQGQZSIBAF-MSLXHMNKSA-N (1R,9S,12S,13R,14S,17R,18Z,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone hydrate Chemical compound O.C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)\C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 NWJQLQGQZSIBAF-MSLXHMNKSA-N 0.000 description 26
229960001569 tacrolimus monohydrate Drugs 0.000 description 26
239000000546 pharmaceutical excipient Substances 0.000 description 20
239000006072 paste Substances 0.000 description 19
238000000113 differential scanning calorimetry Methods 0.000 description 14
FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 description 13
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 description 12
229930195725 Mannitol Natural products 0.000 description 11
239000000594 mannitol Substances 0.000 description 11
235000010355 mannitol Nutrition 0.000 description 11
238000002360 preparation method Methods 0.000 description 10
238000013019 agitation Methods 0.000 description 9
FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 9
235000019700 dicalcium phosphate Nutrition 0.000 description 9
229940095079 dicalcium phosphate anhydrous Drugs 0.000 description 9
239000003960 organic solvent Substances 0.000 description 9
229940072288 prograf Drugs 0.000 description 9
239000000454 talc Substances 0.000 description 9
229910052623 talc Inorganic materials 0.000 description 9
235000012222 talc Nutrition 0.000 description 9
239000012736 aqueous medium Substances 0.000 description 7
239000004094 surface-active agent Substances 0.000 description 7
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
230000004927 fusion Effects 0.000 description 5
239000000243 solution Substances 0.000 description 5
239000006185 dispersion Substances 0.000 description 4
239000003814 drug Substances 0.000 description 4
-1 fatty acid esters Chemical class 0.000 description 4
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
230000000052 comparative effect Effects 0.000 description 3
229940079593 drug Drugs 0.000 description 3
150000007524 organic acids Chemical class 0.000 description 3
239000007962 solid dispersion Substances 0.000 description 3
PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 description 2
108010036949 Cyclosporine Proteins 0.000 description 2
GHVNFZFCNZKVNT-UHFFFAOYSA-N Decanoic acid Natural products CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 2
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
229960001265 ciclosporin Drugs 0.000 description 2
229930182912 cyclosporin Natural products 0.000 description 2
230000000694 effects Effects 0.000 description 2
239000003623 enhancer Substances 0.000 description 2
238000001704 evaporation Methods 0.000 description 2
230000008020 evaporation Effects 0.000 description 2
239000000314 lubricant Substances 0.000 description 2
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
239000002609 medium Substances 0.000 description 2
239000004530 micro-emulsion Substances 0.000 description 2
IPCSVZSSVZVIGE-UHFFFAOYSA-N n-hexadecanoic acid Natural products CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 description 2
210000000056 organ Anatomy 0.000 description 2
239000000047 product Substances 0.000 description 2
238000001757 thermogravimetry curve Methods 0.000 description 2
DCXXMTOCNZCJGO-UHFFFAOYSA-N tristearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 description 2
VPBYZLCHOKSGRX-UHFFFAOYSA-N 1-[2-chloro-4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-propylurea Chemical compound C1=C(Cl)C(NC(=O)NCCC)=CC=C1OC1=NC=NC2=CC(OC)=C(OC)C=C12 VPBYZLCHOKSGRX-UHFFFAOYSA-N 0.000 description 1
OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 description 1
239000005632 Capric acid (CAS 334-48-5) Substances 0.000 description 1
239000005635 Caprylic acid (CAS 124-07-2) Substances 0.000 description 1
229920002261 Corn starch Polymers 0.000 description 1
229920000858 Cyclodextrin Polymers 0.000 description 1
ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 description 1
201000004624 Dermatitis Diseases 0.000 description 1
PVNIQBQSYATKKL-UHFFFAOYSA-N Glycerol trihexadecanoate Natural products CCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCC PVNIQBQSYATKKL-UHFFFAOYSA-N 0.000 description 1
229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 description 1
239000011786 L-ascorbyl-6-palmitate Substances 0.000 description 1
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 description 1
229920000168 Microcrystalline cellulose Polymers 0.000 description 1
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235000021314 Palmitic acid Nutrition 0.000 description 1
102000045595 Phosphoprotein Phosphatases Human genes 0.000 description 1
108700019535 Phosphoprotein Phosphatases Proteins 0.000 description 1
102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 1
108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 1
229940124639 Selective inhibitor Drugs 0.000 description 1
MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
235000021355 Stearic acid Nutrition 0.000 description 1
241001647839 Streptomyces tsukubensis Species 0.000 description 1
229930006000 Sucrose Natural products 0.000 description 1
CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
210000001744 T-lymphocyte Anatomy 0.000 description 1
102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 1
108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 1
230000004913 activation Effects 0.000 description 1
239000013543 active substance Substances 0.000 description 1
239000002671 adjuvant Substances 0.000 description 1
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229910000147 aluminium phosphate Inorganic materials 0.000 description 1
239000012491 analyte Substances 0.000 description 1
238000004458 analytical method Methods 0.000 description 1
239000003963 antioxidant agent Substances 0.000 description 1
235000006708 antioxidants Nutrition 0.000 description 1
235000010385 ascorbyl palmitate Nutrition 0.000 description 1
239000000378 calcium silicate Substances 0.000 description 1
229910052918 calcium silicate Inorganic materials 0.000 description 1
OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 description 1
201000011510 cancer Diseases 0.000 description 1
230000015556 catabolic process Effects 0.000 description 1
238000006243 chemical reaction Methods 0.000 description 1
239000013065 commercial product Substances 0.000 description 1
238000001816 cooling Methods 0.000 description 1
239000008120 corn starch Substances 0.000 description 1
239000004064 cosurfactant Substances 0.000 description 1
229940097362 cyclodextrins Drugs 0.000 description 1
ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 description 1
230000003247 decreasing effect Effects 0.000 description 1
238000010586 diagram Methods 0.000 description 1
238000007865 diluting Methods 0.000 description 1
238000001035 drying Methods 0.000 description 1
230000008030 elimination Effects 0.000 description 1
238000003379 elimination reaction Methods 0.000 description 1
238000000855 fermentation Methods 0.000 description 1
230000004151 fermentation Effects 0.000 description 1
239000013020 final formulation Substances 0.000 description 1
239000012530 fluid Substances 0.000 description 1
238000005469 granulation Methods 0.000 description 1
230000003179 granulation Effects 0.000 description 1
210000002216 heart Anatomy 0.000 description 1
238000010438 heat treatment Methods 0.000 description 1
238000004128 high performance liquid chromatography Methods 0.000 description 1
239000001863 hydroxypropyl cellulose Substances 0.000 description 1
235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
210000000987 immune system Anatomy 0.000 description 1
239000003018 immunosuppressive agent Substances 0.000 description 1
229940124589 immunosuppressive drug Drugs 0.000 description 1
230000006872 improvement Effects 0.000 description 1
238000000338 in vitro Methods 0.000 description 1
230000002401 inhibitory effect Effects 0.000 description 1
230000003993 interaction Effects 0.000 description 1
210000003734 kidney Anatomy 0.000 description 1
239000008101 lactose Substances 0.000 description 1
125000000400 lauroyl group Chemical group O=C([*])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 description 1
210000004185 liver Anatomy 0.000 description 1
210000004072 lung Anatomy 0.000 description 1
239000003120 macrolide antibiotic agent Substances 0.000 description 1
235000019359 magnesium stearate Nutrition 0.000 description 1
238000002844 melting Methods 0.000 description 1
230000008018 melting Effects 0.000 description 1
235000019813 microcrystalline cellulose Nutrition 0.000 description 1
239000008108 microcrystalline cellulose Substances 0.000 description 1
229940016286 microcrystalline cellulose Drugs 0.000 description 1
238000002156 mixing Methods 0.000 description 1
230000004048 modification Effects 0.000 description 1
238000012986 modification Methods 0.000 description 1
WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
231100000252 nontoxic Toxicity 0.000 description 1
230000003000 nontoxic effect Effects 0.000 description 1
QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
229960002446 octanoic acid Drugs 0.000 description 1
235000005985 organic acids Nutrition 0.000 description 1
210000000496 pancreas Anatomy 0.000 description 1
210000002381 plasma Anatomy 0.000 description 1
229920001983 poloxamer Polymers 0.000 description 1
230000003389 potentiating effect Effects 0.000 description 1
108090000623 proteins and genes Proteins 0.000 description 1
102000004169 proteins and genes Human genes 0.000 description 1
238000010298 pulverizing process Methods 0.000 description 1
239000008213 purified water Substances 0.000 description 1
238000011002 quantification Methods 0.000 description 1
238000011160 research Methods 0.000 description 1
238000007873 sieving Methods 0.000 description 1
HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
235000019333 sodium laurylsulphate Nutrition 0.000 description 1
235000010262 sodium metabisulphite Nutrition 0.000 description 1
239000004296 sodium metabisulphite Substances 0.000 description 1
230000007928 solubilization Effects 0.000 description 1
238000005063 solubilization Methods 0.000 description 1
239000007921 spray Substances 0.000 description 1
238000001694 spray drying Methods 0.000 description 1
239000008117 stearic acid Substances 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1
229940042585 tocopherol acetate Drugs 0.000 description 1
230000000699 topical effect Effects 0.000 description 1
231100000419 toxicity Toxicity 0.000 description 1
230000001988 toxicity Effects 0.000 description 1
230000007704 transition Effects 0.000 description 1
150000003626 triacylglycerols Chemical class 0.000 description 1
150000003712 vitamin E derivatives Chemical class 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
- A61K9/14—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
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
- A61K38/13—Cyclosporins
- 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
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1611—Inorganic compounds
- 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
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
- 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
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds

Landscapes

Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Epidemiology (AREA)
Animal Behavior & Ethology (AREA)
Biophysics (AREA)
Molecular Biology (AREA)
Inorganic Chemistry (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Immunology (AREA)
Gastroenterology & Hepatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)

ITMI20070720 2007-04-06 2007-04-06 Composizioni orali contenenti tacrolimus in forma amorfa ITMI20070720A1 (it)

Priority Applications (2)

Application Number	Priority Date	Filing Date	Title
ITMI20070720 ITMI20070720A1 (it)	2007-04-06	2007-04-06	Composizioni orali contenenti tacrolimus in forma amorfa
PCT/EP2008/002716 WO2008122425A2 (fr)	2007-04-06	2008-04-04	Compositions orales contenant du tacrolimus sous forme amorphe

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ITMI20070720 ITMI20070720A1 (it)	2007-04-06	2007-04-06	Composizioni orali contenenti tacrolimus in forma amorfa

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ITMI20070720A1 true ITMI20070720A1 (it)	2008-10-07

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IT (1)	ITMI20070720A1 (fr)
WO (1)	WO2008122425A2 (fr)

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MX2018001989A (es) *	2015-08-19	2018-06-19	Vivus Inc	Formulaciones farmaceuticas.
CN113577032A (zh) *	2021-08-27	2021-11-02	国药集团川抗制药有限公司	他克莫司固体分散体的制备方法、速释药物组合物和应用

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DE4322826A1 (de) *	1993-07-08	1995-01-12	Galenik Labor Freiburg Gmbh	Pharmazeutisches Präparat
ATE464900T1 (de) *	1998-03-26	2010-05-15	Astellas Pharma Inc	Retardpräparat mit makroliden wie tacrolimus
AU2004267909B2 (en) *	2003-08-29	2008-12-18	Veloxis Pharmaceuticals, Inc.	Modified release compositions comprising tacrolimus
KR100678829B1 (ko) *	2004-12-06	2007-02-05	한미약품 주식회사	타크로리무스의 경구용 마이크로에멀젼 조성물

2007
- 2007-04-06 IT ITMI20070720 patent/ITMI20070720A1/it unknown
2008
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Also Published As

Publication number	Publication date
WO2008122425A2 (fr)	2008-10-16
WO2008122425A3 (fr)	2009-01-08

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