NO320366B1 - Vandige risperidonformuleringer - Google Patents
Vandige risperidonformuleringer Download PDFInfo
- Publication number
- NO320366B1 NO320366B1 NO19970051A NO970051A NO320366B1 NO 320366 B1 NO320366 B1 NO 320366B1 NO 19970051 A NO19970051 A NO 19970051A NO 970051 A NO970051 A NO 970051A NO 320366 B1 NO320366 B1 NO 320366B1
- Authority
- NO
- Norway
- Prior art keywords
- solution
- risperidone
- range
- water
- solution according
- Prior art date
Links
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 title claims abstract description 35
- 229960001534 risperidone Drugs 0.000 title claims abstract description 34
- 239000000203 mixture Substances 0.000 title claims abstract description 30
- 238000009472 formulation Methods 0.000 title description 6
- 238000000034 method Methods 0.000 claims abstract description 9
- 238000002360 preparation method Methods 0.000 claims abstract description 6
- 238000007911 parenteral administration Methods 0.000 claims abstract description 5
- 239000007864 aqueous solution Substances 0.000 claims abstract description 4
- 239000000243 solution Substances 0.000 claims description 39
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 24
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 22
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 14
- 239000000872 buffer Substances 0.000 claims description 13
- 239000003755 preservative agent Substances 0.000 claims description 13
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 10
- 239000002253 acid Substances 0.000 claims description 10
- 229940100688 oral solution Drugs 0.000 claims description 9
- 239000011975 tartaric acid Substances 0.000 claims description 9
- 235000002906 tartaric acid Nutrition 0.000 claims description 9
- 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 description 8
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 8
- 239000000600 sorbitol Substances 0.000 claims description 8
- 239000005711 Benzoic acid Substances 0.000 claims description 7
- 235000010233 benzoic acid Nutrition 0.000 claims description 7
- 239000003795 chemical substances by application Substances 0.000 claims description 7
- 239000003182 parenteral nutrition solution Substances 0.000 claims description 7
- 230000002335 preservative effect Effects 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 7
- 238000003756 stirring Methods 0.000 claims description 7
- 239000000796 flavoring agent Substances 0.000 claims description 6
- 239000004480 active ingredient Substances 0.000 claims description 5
- 235000003599 food sweetener Nutrition 0.000 claims description 5
- 239000003765 sweetening agent Substances 0.000 claims description 5
- 239000011780 sodium chloride Substances 0.000 claims description 4
- 238000007865 diluting Methods 0.000 claims description 3
- 238000004090 dissolution Methods 0.000 claims description 3
- 238000001816 cooling Methods 0.000 claims description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 6
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 6
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 6
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 5
- 229960001367 tartaric acid Drugs 0.000 description 5
- -1 1,2-benzisoxazol-3-yl Chemical class 0.000 description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 4
- WINXNKPZLFISPD-UHFFFAOYSA-M Saccharin sodium Chemical compound [Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 WINXNKPZLFISPD-UHFFFAOYSA-M 0.000 description 4
- 239000002585 base Substances 0.000 description 4
- 235000019634 flavors Nutrition 0.000 description 4
- 239000000825 pharmaceutical preparation Substances 0.000 description 4
- 150000005846 sugar alcohols Polymers 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 239000007958 cherry flavor Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 238000010790 dilution Methods 0.000 description 3
- 239000012895 dilution Substances 0.000 description 3
- ZCTXEAQXZGPWFG-UHFFFAOYSA-N imidurea Chemical compound O=C1NC(=O)N(CO)C1NC(=O)NCNC(=O)NC1C(=O)NC(=O)N1CO ZCTXEAQXZGPWFG-UHFFFAOYSA-N 0.000 description 3
- 239000004310 lactic acid Substances 0.000 description 3
- 235000014655 lactic acid Nutrition 0.000 description 3
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 3
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 3
- 229960002216 methylparaben Drugs 0.000 description 3
- 229940127557 pharmaceutical product Drugs 0.000 description 3
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 3
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 3
- 229960003415 propylparaben Drugs 0.000 description 3
- 230000001105 regulatory effect Effects 0.000 description 3
- KSWIOGDSXUFKOC-LREBCSMRSA-N (2r,3r)-2,3-dihydroxybutanedioic acid;3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 KSWIOGDSXUFKOC-LREBCSMRSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 2
- 235000011034 Rubus glaucus Nutrition 0.000 description 2
- 244000235659 Rubus idaeus Species 0.000 description 2
- 235000009122 Rubus idaeus Nutrition 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 235000013361 beverage Nutrition 0.000 description 2
- 239000008366 buffered solution Substances 0.000 description 2
- SOROIESOUPGGFO-UHFFFAOYSA-N diazolidinylurea Chemical compound OCNC(=O)N(CO)C1N(CO)C(=O)N(CO)C1=O SOROIESOUPGGFO-UHFFFAOYSA-N 0.000 description 2
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 229960000448 lactic acid Drugs 0.000 description 2
- 235000019629 palatability Nutrition 0.000 description 2
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 2
- 239000012453 solvate Substances 0.000 description 2
- 235000010199 sorbic acid Nutrition 0.000 description 2
- 239000004334 sorbic acid Substances 0.000 description 2
- 229940075582 sorbic acid Drugs 0.000 description 2
- 235000019640 taste Nutrition 0.000 description 2
- HFVMEOPYDLEHBR-UHFFFAOYSA-N (2-fluorophenyl)-phenylmethanol Chemical compound C=1C=CC=C(F)C=1C(O)C1=CC=CC=C1 HFVMEOPYDLEHBR-UHFFFAOYSA-N 0.000 description 1
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 description 1
- MIDXCONKKJTLDX-UHFFFAOYSA-N 3,5-dimethylcyclopentane-1,2-dione Chemical compound CC1CC(C)C(=O)C1=O MIDXCONKKJTLDX-UHFFFAOYSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-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
- 241000894006 Bacteria Species 0.000 description 1
- 241000167854 Bourreria succulenta Species 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- UDIPTWFVPPPURJ-UHFFFAOYSA-M Cyclamate Chemical compound [Na+].[O-]S(=O)(=O)NC1CCCCC1 UDIPTWFVPPPURJ-UHFFFAOYSA-M 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- 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 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 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
- 239000005715 Fructose Substances 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- 241000233866 Fungi Species 0.000 description 1
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 244000171263 Ribes grossularia Species 0.000 description 1
- 235000002357 Ribes grossularia Nutrition 0.000 description 1
- 240000001890 Ribes hudsonianum Species 0.000 description 1
- 235000016954 Ribes hudsonianum Nutrition 0.000 description 1
- 235000001466 Ribes nigrum Nutrition 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 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
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 244000269722 Thea sinensis Species 0.000 description 1
- 244000299461 Theobroma cacao Species 0.000 description 1
- 235000009470 Theobroma cacao Nutrition 0.000 description 1
- 235000010358 acesulfame potassium Nutrition 0.000 description 1
- 229960004998 acesulfame potassium Drugs 0.000 description 1
- 239000000619 acesulfame-K Substances 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 230000000561 anti-psychotic effect Effects 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 1
- 150000008316 benzisoxazoles Chemical class 0.000 description 1
- 229960004365 benzoic acid Drugs 0.000 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 210000001124 body fluid Anatomy 0.000 description 1
- 239000010839 body fluid Substances 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- ZCCIPPOKBCJFDN-UHFFFAOYSA-N calcium nitrate Chemical compound [Ca+2].[O-][N+]([O-])=O.[O-][N+]([O-])=O ZCCIPPOKBCJFDN-UHFFFAOYSA-N 0.000 description 1
- NNOYLBKZPCUCQT-UHFFFAOYSA-L calcium;1,1-dioxo-1,2-benzothiazol-3-olate;heptahydrate Chemical compound O.O.O.O.O.O.O.[Ca+2].C1=CC=C2C([O-])=NS(=O)(=O)C2=C1.C1=CC=C2C([O-])=NS(=O)(=O)C2=C1 NNOYLBKZPCUCQT-UHFFFAOYSA-L 0.000 description 1
- 235000013736 caramel Nutrition 0.000 description 1
- 239000004202 carbamide Substances 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 235000019693 cherries Nutrition 0.000 description 1
- 239000008370 chocolate flavor Substances 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000006184 cosolvent Substances 0.000 description 1
- 239000000625 cyclamic acid and its Na and Ca salt Substances 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- 239000008369 fruit flavor Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 229940093915 gynecological organic acid Drugs 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 229940102223 injectable solution Drugs 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000000845 maltitol Substances 0.000 description 1
- 235000010449 maltitol Nutrition 0.000 description 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
- 229940035436 maltitol Drugs 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- NJTGANWAUPEOAX-UHFFFAOYSA-N molport-023-220-454 Chemical compound OCC(O)CO.OCC(O)CO NJTGANWAUPEOAX-UHFFFAOYSA-N 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 235000013615 non-nutritive sweetener Nutrition 0.000 description 1
- 229940098462 oral drops Drugs 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- WLJNZVDCPSBLRP-UHFFFAOYSA-N pamoic acid Chemical compound C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1 WLJNZVDCPSBLRP-UHFFFAOYSA-N 0.000 description 1
- 239000007967 peppermint flavor Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920002981 polyvinylidene fluoride Polymers 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 235000010333 potassium nitrate Nutrition 0.000 description 1
- FGIUAXJPYTZDNR-UHFFFAOYSA-N potassium nitrate Inorganic materials [K+].[O-][N+]([O-])=O FGIUAXJPYTZDNR-UHFFFAOYSA-N 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 239000001294 propane Substances 0.000 description 1
- 229960004063 propylene glycol Drugs 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- 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 description 1
- 229960001462 sodium cyclamate Drugs 0.000 description 1
- 235000014214 soft drink Nutrition 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pain & Pain Management (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/272,462 US5453425A (en) | 1994-07-11 | 1994-07-11 | Risperidone oral formulation |
| US08/429,435 US5616587A (en) | 1994-07-11 | 1995-04-26 | Aqueous risperidone formulations |
| PCT/EP1995/002615 WO1996001652A1 (en) | 1994-07-11 | 1995-07-04 | Aqueous risperidone formulations |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| NO970051L NO970051L (no) | 1997-01-07 |
| NO970051D0 NO970051D0 (no) | 1997-01-07 |
| NO320366B1 true NO320366B1 (no) | 2005-11-28 |
Family
ID=26955530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO19970051A NO320366B1 (no) | 1994-07-11 | 1997-01-07 | Vandige risperidonformuleringer |
Country Status (37)
| Country | Link |
|---|---|
| US (3) | US5453425A (da) |
| EP (1) | EP0769965B1 (da) |
| JP (1) | JP2872412B2 (da) |
| KR (1) | KR100212942B1 (da) |
| CN (1) | CN1148226C (da) |
| AP (1) | AP774A (da) |
| AT (1) | ATE206931T1 (da) |
| AU (1) | AU684193B2 (da) |
| BG (1) | BG63070B1 (da) |
| BR (1) | BR9508253A (da) |
| CA (1) | CA2194564C (da) |
| CY (1) | CY2268B1 (da) |
| CZ (1) | CZ285204B6 (da) |
| DE (1) | DE69523313T2 (da) |
| DK (1) | DK0769965T3 (da) |
| EE (1) | EE03426B1 (da) |
| ES (1) | ES2165918T3 (da) |
| FI (1) | FI116510B (da) |
| HK (1) | HK1010691A1 (da) |
| HR (1) | HRP950397B1 (da) |
| HU (1) | HU222352B1 (da) |
| IL (1) | IL114525A (da) |
| MX (1) | MX9700374A (da) |
| MY (1) | MY114389A (da) |
| NO (1) | NO320366B1 (da) |
| NZ (1) | NZ289432A (da) |
| PH (1) | PH31626A (da) |
| PL (1) | PL179972B1 (da) |
| PT (1) | PT769965E (da) |
| RO (1) | RO116778B1 (da) |
| RU (1) | RU2161965C2 (da) |
| SI (1) | SI9500220B (da) |
| SK (1) | SK282159B6 (da) |
| TR (1) | TR199500778A1 (da) |
| TW (1) | TW420615B (da) |
| WO (1) | WO1996001652A1 (da) |
| ZA (1) | ZA955720B (da) |
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| ES2236700T3 (es) * | 1993-11-19 | 2005-07-16 | Janssen Pharmaceutica N.V. | 1,2-benzazoles microencapsulados. |
| US5453425A (en) * | 1994-07-11 | 1995-09-26 | Janssen Pharmaceutica N.V. | Risperidone oral formulation |
| UA72189C2 (uk) | 1997-11-17 | 2005-02-15 | Янссен Фармацевтика Н.В. | Фармацевтична композиція, що містить водну суспензію субмікронних ефірів 9-гідроксирисперидон жирних кислот |
| US6682758B1 (en) | 1998-12-22 | 2004-01-27 | The United States Of America As Represented By The Department Of Health And Human Services | Water-insoluble drug delivery system |
| US6495164B1 (en) * | 2000-05-25 | 2002-12-17 | Alkermes Controlled Therapeutics, Inc. I | Preparation of injectable suspensions having improved injectability |
| US20050232995A1 (en) | 2002-07-29 | 2005-10-20 | Yam Nyomi V | Methods and dosage forms for controlled delivery of paliperidone and risperidone |
| EP1534288A1 (en) * | 2002-08-23 | 2005-06-01 | Ranbaxy Laboratories, Ltd. | Stable aqueous solutions of risperidone and methods for their preparation |
| WO2004094415A1 (en) * | 2003-04-22 | 2004-11-04 | Synthon B.V. | Risperidone monohydrochloride |
| AR044852A1 (es) | 2003-06-24 | 2005-10-05 | Novartis Ag | Una composicion farmaceutica para la administracion parenteral que comprende un analogo de somatostatina |
| US20050036977A1 (en) * | 2003-08-11 | 2005-02-17 | Dilip Gole | Taste-masked resinate and preparation thereof |
| ES2245252B1 (es) * | 2004-06-15 | 2007-03-01 | Farmalider, S.A. | Solucion acuosa de risperidona para administracion oral. |
| ES2245891B1 (es) * | 2004-07-09 | 2006-11-16 | Clinmet S.L. | "metodo para la obtencion de un excipiente universal para la administracion oral de principios activos farmaceuticos y composiciones de excipientes resultantes del metodo". |
| WO2006129160A2 (en) * | 2005-06-01 | 2006-12-07 | Aurobindo Pharma Limited | Stable aqueous oral solution of risperidone |
| ATE424399T1 (de) * | 2005-06-29 | 2009-03-15 | Verisfield Uk Ltd | Pharmazeutische zusammensetzungen von risperidon in wässriger lösung |
| US8852638B2 (en) | 2005-09-30 | 2014-10-07 | Durect Corporation | Sustained release small molecule drug formulation |
| JP4922657B2 (ja) * | 2006-05-09 | 2012-04-25 | 高田製薬株式会社 | リスペリドン経口用液剤 |
| WO2007138462A2 (en) * | 2006-06-01 | 2007-12-06 | Wockhardt Ltd | Aqueous oral formulations of risperidone |
| BRPI0811319A2 (pt) | 2007-05-25 | 2015-02-10 | Tolmar Therapeutics Inc | Composição fluida, método de formação de uma composição fluida, implante biodegrádavel formado in situ, método de formação de um implante biodegradável in situ, kit, implante e método de trataento |
| US7776866B2 (en) * | 2007-09-15 | 2010-08-17 | Protia, Llc | Deuterium-enriched risperidone |
| DK2234617T3 (da) * | 2007-12-19 | 2021-05-25 | Janssen Pharmaceutica Nv | Doseringsskema forbundet med langtidsvirkende injicerbare paliperidonestere |
| DK2389187T3 (da) | 2009-01-20 | 2017-02-20 | Los Angeles Biomedical Res Inst At Harbor-Ucla Medical Center | Sorbin- og benzoesyre og derivater deraf til forstærkning af aktiviteten af et neurofarmaceutisk middel |
| GB2513060B (en) | 2010-06-08 | 2015-01-07 | Rb Pharmaceuticals Ltd | Microparticle buprenorphine suspension |
| US9272044B2 (en) | 2010-06-08 | 2016-03-01 | Indivior Uk Limited | Injectable flowable composition buprenorphine |
| WO2013055386A2 (en) * | 2011-10-03 | 2013-04-18 | The University Of Utah Research Foundation | Application of 5-ht6 receptor antagonists for the alleviation of cognitive deficits of down syndrome |
| GB201404139D0 (en) | 2014-03-10 | 2014-04-23 | Rb Pharmaceuticals Ltd | Sustained release buprenorphine solution formulations |
| AU2015341490C1 (en) | 2014-11-07 | 2021-03-11 | Indivior Uk Limited | Buprenorphine dosing regimens |
| FI3468944T3 (fi) | 2016-06-13 | 2023-01-31 | Natriumbentsoaatin yhteiskiteitä ja niiden käyttöjä | |
| RU2022101542A (ru) | 2016-06-13 | 2022-02-03 | Сайньюрекс Интернэшнл (Тайвань) Корп. | Сокристаллы бензоата лития и их применения |
| KR20190066608A (ko) * | 2016-09-23 | 2019-06-13 | 델포어, 인코포레이티드 | 소분자 치료제 화합물 조성물 |
| RU2646812C1 (ru) * | 2016-10-24 | 2018-03-07 | Общество с ограниченной ответственностью "Трейдсервис" | Жидкая лекарственная форма рисперидона и способ ее получения |
| US11369579B2 (en) | 2016-10-24 | 2022-06-28 | Syneurx International (Taiwan) Corp. | Polymorphic forms of sodium benzoate and uses thereof |
| US10336679B2 (en) | 2016-10-24 | 2019-07-02 | Syneurx International (Taiwan) Corp. | Polymorphic forms of sodium benzoate and uses thereof |
| US10646484B2 (en) | 2017-06-16 | 2020-05-12 | Indivior Uk Limited | Methods to treat opioid use disorder |
| CN107260662A (zh) * | 2017-06-21 | 2017-10-20 | 南京正科医药股份有限公司 | 一种利培酮口服溶液及其制备方法 |
| CN107441037A (zh) * | 2017-08-16 | 2017-12-08 | 南京正科医药股份有限公司 | 一种利培酮口服溶液 |
| CN109589304A (zh) * | 2017-10-01 | 2019-04-09 | 万特制药(海南)有限公司 | 利培酮口服溶液及其制备方法 |
| US10098861B1 (en) | 2017-10-24 | 2018-10-16 | Syneurx International (Taiwan) Corp. | Pharmaceutical composition comprising sodium benzoate compound and clozapine, and uses thereof |
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| US4337261A (en) * | 1980-07-28 | 1982-06-29 | Hoechst-Roussel Pharmaceuticals Inc. | (1,2-Benzisoxazol)phenoxyacetic acids as diuretics |
| IL88233A (en) * | 1987-11-03 | 1993-08-18 | Genentech Inc | Gamma interferon formulation |
| FR2641278B1 (fr) * | 1989-01-05 | 1991-03-22 | Lipha | Piperidines, procedes de preparation et medicaments les contenant |
| DK203990D0 (da) * | 1990-08-24 | 1990-08-24 | Novo Nordisk As | Piperazinylderivater |
| TW376319B (en) * | 1993-04-28 | 1999-12-11 | Janssen Pharmaceutica Nv | Pharmaceutical composition containing risperidone pamoate and having a long acting activity for treating psychoses induced by the release of dopamine |
| US5453425A (en) * | 1994-07-11 | 1995-09-26 | Janssen Pharmaceutica N.V. | Risperidone oral formulation |
| FR2796273B1 (fr) * | 1999-07-15 | 2003-09-12 | Oreal | Composition a phase grasse liquide gelifiee par un polyamide a groupements ester terminaux |
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1994
- 1994-07-11 US US08/272,462 patent/US5453425A/en not_active Expired - Lifetime
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1995
- 1995-04-26 US US08/429,435 patent/US5616587A/en not_active Ceased
- 1995-05-19 TW TW084104959A patent/TW420615B/zh not_active IP Right Cessation
- 1995-05-31 PH PH50624A patent/PH31626A/en unknown
- 1995-06-29 TR TR95/00778A patent/TR199500778A1/xx unknown
- 1995-07-04 PL PL95318132A patent/PL179972B1/pl unknown
- 1995-07-04 DK DK95924978T patent/DK0769965T3/da active
- 1995-07-04 AU AU29275/95A patent/AU684193B2/en not_active Expired
- 1995-07-04 RO RO97-00032A patent/RO116778B1/ro unknown
- 1995-07-04 CA CA002194564A patent/CA2194564C/en not_active Expired - Lifetime
- 1995-07-04 CN CNB951940821A patent/CN1148226C/zh not_active Expired - Lifetime
- 1995-07-04 BR BR9508253A patent/BR9508253A/pt not_active IP Right Cessation
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- 1995-07-04 KR KR1019970700039A patent/KR100212942B1/ko not_active IP Right Cessation
- 1995-07-04 DE DE69523313T patent/DE69523313T2/de not_active Expired - Lifetime
- 1995-07-04 WO PCT/EP1995/002615 patent/WO1996001652A1/en active IP Right Grant
- 1995-07-04 CZ CZ9727A patent/CZ285204B6/cs not_active IP Right Cessation
- 1995-07-04 PT PT95924978T patent/PT769965E/pt unknown
- 1995-07-04 RU RU97102139/14A patent/RU2161965C2/ru active
- 1995-07-04 EP EP95924978A patent/EP0769965B1/en not_active Expired - Lifetime
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- 1995-07-04 SK SK22-97A patent/SK282159B6/sk not_active IP Right Cessation
- 1995-07-04 HU HU9700082A patent/HU222352B1/hu active IP Right Grant
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- 1995-07-04 AT AT95924978T patent/ATE206931T1/de active
- 1995-07-04 JP JP8504108A patent/JP2872412B2/ja not_active Expired - Lifetime
- 1995-07-04 EE EE9700009A patent/EE03426B1/xx unknown
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