JP2006514923A5 - - Google Patents

Info

Publication number

JP2006514923A5

JP2006514923A5 JP2004546264A JP2004546264A JP2006514923A5 JP 2006514923 A5 JP2006514923 A5 JP 2006514923A5 JP 2004546264 A JP2004546264 A JP 2004546264A JP 2004546264 A JP2004546264 A JP 2004546264A JP 2006514923 A5 JP2006514923 A5 JP 2006514923A5

Authority

JP

Japan

Prior art keywords

depot preparation

preparation according

injectable depot

ziprasidone

sbecd

Prior art date

2003-10-13

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.)

Abandoned

Links

• Espacenet
• Global Dossier
• Discuss

• 239000003405 delayed action preparation Substances 0.000 claims 13
• 229920000858 Cyclodextrin Polymers 0.000 claims 7
• -1 aryl heterocyclic compound Chemical class 0.000 claims 7
• VNDHXHMRJVTMTK-WZVRVNPQSA-H hexasodium 4-[[(1S,3R,5R,6S,8R,10R,11S,13R,15R,16S,18R,20R,21S,23R,25R,26S,28R,30R,31S,33R,35R,36R,37R,38R,39R,40R,41R,42R,43R,44R,45R,46R,47R,48R,49R)-36,37,38,39,40,41,42,43,44,45,46,47,48,49-tetradecahydroxy-10-(hydroxymethyl)-15,20,25,30,35-pentakis(4-sulfonatobutoxymethyl)-2,4,7,9,12,14,17,19,22,24,27,29,32,34-tetradecaoxaoctacyclo[31.2.2.23,6.28,11.213,16.218,21.223,26.228,31]nonatetracontan-5-yl]methoxy]butane-1-sulfonate Chemical compound [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].OC[C@H]1O[C@@H]2O[C@H]3[C@H](O)[C@@H](O)[C@H](O[C@@H]3COCCCCS([O-])(=O)=O)O[C@H]3[C@H](O)[C@@H](O)[C@H](O[C@@H]3COCCCCS([O-])(=O)=O)O[C@H]3[C@H](O)[C@@H](O)[C@H](O[C@@H]3COCCCCS([O-])(=O)=O)O[C@H]3[C@H](O)[C@@H](O)[C@H](O[C@@H]3COCCCCS([O-])(=O)=O)O[C@H]3[C@H](O)[C@@H](O)[C@H](O[C@@H]3COCCCCS([O-])(=O)=O)O[C@H]3[C@H](O)[C@@H](O)[C@H](O[C@@H]3COCCCCS([O-])(=O)=O)O[C@H]1[C@H](O)[C@H]2O VNDHXHMRJVTMTK-WZVRVNPQSA-H 0.000 claims 6
• 239000000203 mixture Substances 0.000 claims 5
• 239000011345 viscous material Substances 0.000 claims 5
• 229960000607 ziprasidone Drugs 0.000 claims 5
• MVWVFYHBGMAFLY-UHFFFAOYSA-N ziprasidone Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 MVWVFYHBGMAFLY-UHFFFAOYSA-N 0.000 claims 5
• 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 4
• 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 3
• 239000001768 carboxy methyl cellulose Substances 0.000 claims 3
• 238000010255 intramuscular injection Methods 0.000 claims 3
• 239000007927 intramuscular injection Substances 0.000 claims 3
• 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 3
• 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 3
• 229960004487 ziprasidone mesylate Drugs 0.000 claims 3
• WLQZEFFFIUHSJB-UHFFFAOYSA-N ziprasidone mesylate trihydrate Chemical compound O.O.O.CS(O)(=O)=O.C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 WLQZEFFFIUHSJB-UHFFFAOYSA-N 0.000 claims 3
• AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims 2
• 229920000954 Polyglycolide Polymers 0.000 claims 2
• 229920002678 cellulose Polymers 0.000 claims 2
• 239000001913 cellulose Substances 0.000 claims 2
• 229920001577 copolymer Polymers 0.000 claims 2
• 238000002425 crystallisation Methods 0.000 claims 2
• 238000009472 formulation Methods 0.000 claims 2
• 229920000747 poly(lactic acid) Polymers 0.000 claims 2
• 229920001897 terpolymer Polymers 0.000 claims 2
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
• LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims 1
• HIXDQWDOVZUNNA-UHFFFAOYSA-N 2-(3,4-dimethoxyphenyl)-5-hydroxy-7-methoxychromen-4-one Chemical compound C=1C(OC)=CC(O)=C(C(C=2)=O)C=1OC=2C1=CC=C(OC)C(OC)=C1 HIXDQWDOVZUNNA-UHFFFAOYSA-N 0.000 claims 1
• FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 claims 1
• QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
• FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 claims 1
• FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 1
• 229920002101 Chitin Polymers 0.000 claims 1
• 229920001661 Chitosan Polymers 0.000 claims 1
• 229920002307 Dextran Polymers 0.000 claims 1
• 239000001116 FEMA 4028 Substances 0.000 claims 1
• 108010010803 Gelatin Proteins 0.000 claims 1
• 229930182556 Polyacetal Natural products 0.000 claims 1
• 229920002732 Polyanhydride Polymers 0.000 claims 1
• 239000002202 Polyethylene glycol Substances 0.000 claims 1
• 229920001710 Polyorthoester Polymers 0.000 claims 1
• 235000021355 Stearic acid Nutrition 0.000 claims 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 claims 1
• 229930006000 Sucrose Natural products 0.000 claims 1
• 229940072056 alginate Drugs 0.000 claims 1
• 235000010443 alginic acid Nutrition 0.000 claims 1
• 229920000615 alginic acid Polymers 0.000 claims 1
• 239000008135 aqueous vehicle Substances 0.000 claims 1
• WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 claims 1
• 235000011175 beta-cyclodextrine Nutrition 0.000 claims 1
• 229960004853 betadex Drugs 0.000 claims 1
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 239000006184 cosolvent Substances 0.000 claims 1
• 230000008025 crystallization Effects 0.000 claims 1
• RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 1
• GDSRMADSINPKSL-HSEONFRVSA-N gamma-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO GDSRMADSINPKSL-HSEONFRVSA-N 0.000 claims 1
• 229940080345 gamma-cyclodextrin Drugs 0.000 claims 1
• 229920000159 gelatin Polymers 0.000 claims 1
• 239000008273 gelatin Substances 0.000 claims 1
• 235000019322 gelatine Nutrition 0.000 claims 1
• 235000011852 gelatine desserts Nutrition 0.000 claims 1
• 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
• 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
• 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
• 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 claims 1
• 239000003112 inhibitor Substances 0.000 claims 1
• 229920000609 methyl cellulose Polymers 0.000 claims 1
• 239000001923 methylcellulose Substances 0.000 claims 1
• 235000010981 methylcellulose Nutrition 0.000 claims 1
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
• OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
• 239000008180 pharmaceutical surfactant Substances 0.000 claims 1
• 239000002798 polar solvent Substances 0.000 claims 1
• 229920001308 poly(aminoacid) Polymers 0.000 claims 1
• 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims 1
• 239000002745 poly(ortho ester) Substances 0.000 claims 1
• 229920002463 poly(p-dioxanone) polymer Polymers 0.000 claims 1
• 229920002627 poly(phosphazenes) Polymers 0.000 claims 1
• 229920000768 polyamine Polymers 0.000 claims 1
• 229920001610 polycaprolactone Polymers 0.000 claims 1
• 239000004632 polycaprolactone Substances 0.000 claims 1
• 229920000515 polycarbonate Polymers 0.000 claims 1
• 239000004417 polycarbonate Substances 0.000 claims 1
• 239000000622 polydioxanone Substances 0.000 claims 1
• 229920006149 polyester-amide block copolymer Polymers 0.000 claims 1
• 229920001223 polyethylene glycol Polymers 0.000 claims 1
• 229920001444 polymaleic acid Polymers 0.000 claims 1
• 229920000056 polyoxyethylene ether Polymers 0.000 claims 1
• 229940051841 polyoxyethylene ether Drugs 0.000 claims 1
• 229920006324 polyoxymethylene Polymers 0.000 claims 1
• 229920001451 polypropylene glycol Polymers 0.000 claims 1
• 229920002635 polyurethane Polymers 0.000 claims 1
• 239000004814 polyurethane Substances 0.000 claims 1
• 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
• 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
• 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
• 238000002360 preparation method Methods 0.000 claims 1
• 208000020016 psychiatric disease Diseases 0.000 claims 1
• HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 1
• 150000004040 pyrrolidinones Chemical class 0.000 claims 1
• 201000000980 schizophrenia Diseases 0.000 claims 1
• 239000008117 stearic acid Substances 0.000 claims 1
• KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
• 239000005720 sucrose Substances 0.000 claims 1
• ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 claims 1