UA79984C2 - Preparation on the basis of aripiprazole complex and use thereof - Google Patents
Preparation on the basis of aripiprazole complex and use thereof Download PDFInfo
- Publication number
- UA79984C2 UA79984C2 UAA200502492A UA2005002492A UA79984C2 UA 79984 C2 UA79984 C2 UA 79984C2 UA A200502492 A UAA200502492 A UA A200502492A UA 2005002492 A UA2005002492 A UA 2005002492A UA 79984 C2 UA79984 C2 UA 79984C2
- Authority
- UA
- Ukraine
- Prior art keywords
- aripiprazole
- cyclodextrin
- acid
- preparation
- salt
- Prior art date
Links
- CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 title claims abstract description 68
- 229960004372 aripiprazole Drugs 0.000 title claims abstract description 68
- 238000002360 preparation method Methods 0.000 title claims abstract description 42
- 238000002347 injection Methods 0.000 claims abstract description 47
- 239000007924 injection Substances 0.000 claims abstract description 47
- 230000007794 irritation Effects 0.000 claims abstract description 18
- -1 preferably Chemical compound 0.000 claims abstract description 12
- 238000000034 method Methods 0.000 claims abstract description 9
- NZAQRZWBQUIBSF-UHFFFAOYSA-N 4-(4-sulfobutoxy)butane-1-sulfonic acid Chemical compound OS(=O)(=O)CCCCOCCCCS(O)(=O)=O NZAQRZWBQUIBSF-UHFFFAOYSA-N 0.000 claims abstract description 8
- 238000011282 treatment Methods 0.000 claims abstract description 7
- 201000000980 schizophrenia Diseases 0.000 claims abstract description 6
- 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 abstract 13
- 229940079593 drug Drugs 0.000 claims description 34
- 239000003814 drug Substances 0.000 claims description 34
- 229920000858 Cyclodextrin Polymers 0.000 claims description 31
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 16
- 150000003839 salts Chemical class 0.000 claims description 13
- 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 13
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 12
- 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
- 239000000203 mixture Substances 0.000 claims description 10
- 235000002906 tartaric acid Nutrition 0.000 claims description 10
- 239000011975 tartaric acid Substances 0.000 claims description 10
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 9
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 8
- 239000007853 buffer solution Substances 0.000 claims description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 6
- 238000007918 intramuscular administration Methods 0.000 claims description 5
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 4
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 3
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- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 claims description 2
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- ODLHGICHYURWBS-FOSILIAISA-N molport-023-220-444 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-FOSILIAISA-N 0.000 claims 2
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- UYXTWWCETRIEDR-UHFFFAOYSA-N Tributyrin Chemical compound CCCC(=O)OCC(OC(=O)CCC)COC(=O)CCC UYXTWWCETRIEDR-UHFFFAOYSA-N 0.000 description 2
- 230000002378 acidificating effect Effects 0.000 description 2
- 150000008044 alkali metal hydroxides Chemical class 0.000 description 2
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- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 description 2
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
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- 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
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- A61K47/6949—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
- A61K47/6951—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
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Landscapes
- Health & Medical Sciences (AREA)
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Applications Claiming Priority (2)
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US40471302P | 2002-08-20 | 2002-08-20 | |
PCT/US2003/025573 WO2004017897A2 (en) | 2002-08-20 | 2003-08-14 | Aripiprazole complex formulation and method |
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UA79984C2 true UA79984C2 (en) | 2007-08-10 |
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UAA200502492A UA79984C2 (en) | 2002-08-20 | 2003-08-14 | Preparation on the basis of aripiprazole complex and use thereof |
Country Status (32)
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US (8) | US7115587B2 (pl) |
EP (1) | EP1542668B1 (pl) |
JP (1) | JP4729306B2 (pl) |
KR (1) | KR101043866B1 (pl) |
CN (1) | CN100335047C (pl) |
AR (2) | AR040887A1 (pl) |
AT (1) | ATE428423T1 (pl) |
AU (1) | AU2003269965B2 (pl) |
BR (1) | BR0313602A (pl) |
CA (1) | CA2495864C (pl) |
CY (1) | CY1110331T1 (pl) |
DE (1) | DE60327225D1 (pl) |
DK (1) | DK1542668T3 (pl) |
ES (1) | ES2322953T3 (pl) |
GE (1) | GEP20063996B (pl) |
HR (1) | HRP20050149B1 (pl) |
IL (1) | IL166623A (pl) |
IS (1) | IS2878B (pl) |
MX (1) | MXPA05001865A (pl) |
MY (1) | MY140793A (pl) |
NO (1) | NO333458B1 (pl) |
NZ (1) | NZ537995A (pl) |
PE (1) | PE20040895A1 (pl) |
PL (1) | PL212428B1 (pl) |
PT (1) | PT1542668E (pl) |
RS (1) | RS51903B (pl) |
RU (1) | RU2342931C2 (pl) |
SI (1) | SI1542668T1 (pl) |
TW (1) | TWI307626B (pl) |
UA (1) | UA79984C2 (pl) |
WO (1) | WO2004017897A2 (pl) |
ZA (1) | ZA200501064B (pl) |
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US20040170705A1 (en) * | 2001-03-08 | 2004-09-02 | Dusan Miljkovic | Compositions and methods for non-insulin glucose uptake |
RU2342931C2 (ru) * | 2002-08-20 | 2009-01-10 | Бристол-Маерс Сквибб Компани | Состав на основе комплекса арипипразола |
CN1870980B (zh) * | 2003-10-23 | 2010-06-23 | 大冢制药株式会社 | 控释无菌阿立哌唑注射剂和方法 |
US7714129B2 (en) | 2003-12-16 | 2010-05-11 | Teva Pharmaceutical Industries Ltd. | Methods of preparing anhydrous aripiprazole form II |
TW200529850A (en) * | 2003-12-16 | 2005-09-16 | Teva Pharma | Methods of preparing aripiprazole crystalline forms |
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