PE20060291A1 - POSACONAZOLE INJECTABLE PHARMACEUTICAL COMPOSITIONS WITH STABILIZED PARTICLES - Google Patents
POSACONAZOLE INJECTABLE PHARMACEUTICAL COMPOSITIONS WITH STABILIZED PARTICLESInfo
- Publication number
- PE20060291A1 PE20060291A1 PE2005000599A PE2005000599A PE20060291A1 PE 20060291 A1 PE20060291 A1 PE 20060291A1 PE 2005000599 A PE2005000599 A PE 2005000599A PE 2005000599 A PE2005000599 A PE 2005000599A PE 20060291 A1 PE20060291 A1 PE 20060291A1
- Authority
- PE
- Peru
- Prior art keywords
- posaconazole
- microns
- particles
- infections
- moldes
- Prior art date
Links
- 239000002245 particle Substances 0.000 title abstract 3
- RAGOYPUPXAKGKH-XAKZXMRKSA-N posaconazole Chemical compound O=C1N([C@H]([C@H](C)O)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@H]3C[C@@](CN4N=CN=C4)(OC3)C=3C(=CC(F)=CC=3)F)=CC=2)C=C1 RAGOYPUPXAKGKH-XAKZXMRKSA-N 0.000 title abstract 3
- 229960001589 posaconazole Drugs 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 abstract 3
- 208000015181 infectious disease Diseases 0.000 abstract 3
- 239000007853 buffer solution Substances 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 230000001012 protector Effects 0.000 abstract 2
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 abstract 1
- DHMQDGOQFOQNFH-CNRUNOGKSA-N 2-amino-2-tritioacetic acid Chemical compound [3H]C(N)C(O)=O DHMQDGOQFOQNFH-CNRUNOGKSA-N 0.000 abstract 1
- 241000233866 Fungi Species 0.000 abstract 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 abstract 1
- 206010030154 Oesophageal candidiasis Diseases 0.000 abstract 1
- 206010050346 Oropharyngeal candidiasis Diseases 0.000 abstract 1
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 abstract 1
- 206010061418 Zygomycosis Diseases 0.000 abstract 1
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 abstract 1
- 239000007900 aqueous suspension Substances 0.000 abstract 1
- 239000000872 buffer Substances 0.000 abstract 1
- 201000005655 esophageal candidiasis Diseases 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 abstract 1
- 239000007972 injectable composition Substances 0.000 abstract 1
- 201000009085 invasive aspergillosis Diseases 0.000 abstract 1
- 201000007524 mucormycosis Diseases 0.000 abstract 1
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 abstract 1
- 150000003904 phospholipids Chemical class 0.000 abstract 1
- 239000001509 sodium citrate Substances 0.000 abstract 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 abstract 1
Classifications
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- 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
- A61K47/02—Inorganic compounds
-
- 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
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biochemistry (AREA)
- Inorganic Chemistry (AREA)
- Biophysics (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
REFERIDA A UNA FORMULACION INYECTABLE ESTERILIZADA POR AUTOCLAVE, QUE COMPRENDE UNA SUSPENSION ACUOSA DE POSACONAZOL, ESTABILIZADA POR UN FOSFOLIPIDO, EN UNA MEZCLA QUE CONTIENE UN PROTECTOR TERMICO Y UN SISTEMA TAMPON. EL SISTEMA TAMPON CONTIENE UN TAMPON ORGANICO TAL COMO HISTIDINA, ACIDO CITRICO, GLICINA, CITRATO DE SODIO, ENTRE OTROS, EL CUAL PERMITE MANTENER UN PH DE ENTRE 3 A 9; EL FOSOFOLIPIDO PUEDE SER NATURAL Y/O SINTETICO TAL COMO 1-PALMITOIL-2-OLEOIL-SN-GLICERO-3-FOSFOCOLINA (POPC); Y EL PROTECTOR TERMICO CONTIENE TREHALOSA. EL POSACONAZOL TIENE UNA DISTRIBUCION GRANULOMETRICA CUYA MEDIANA ESTA ENTRE 1,0 Y 8,0 MICRONES, CON NO MAS DE 3000 PARTICULAS DE 10 MICRONES O DE MAYOR TAMANO, NI MAS DE 300 PARTICULAS DE 25 MICRONES O DE MAYOR TAMANO. DICHA FORMULACION ES UTIL EN EL TRATAMIENTO DE INFECCIONES TALES COMO CANDIDIASIS OROFARINGEA O ESOFAGICA, ASPERGILOSIS INVASIVA, INFECCIONES CAUSADAS POR HONGOS DIMORFICOS, ZIGOMICOSIS E INFECCIONES INVASIVAS DEBIDAS A MOHOS Y LEVADURAS POCO FRECUENTES, ENFERMEDAD DE CHAGAS Y LEISHMANIASIS, ENTRE OTRASREFERRED TO AN INJECTABLE FORMULATION STERILIZED BY AUTOCLAVE, INCLUDING AN AQUEOUS SUSPENSION OF POSACONAZOLE, STABILIZED BY A PHOSPHOLIPID, IN A MIXTURE CONTAINING A THERMAL PROTECTOR AND A BUFFER SYSTEM. THE BUFFER SYSTEM CONTAINS AN ORGANIC BUFFER SUCH AS HISTIDINE, CITRIC ACID, GLYCINE, SODIUM CITRATE, AMONG OTHERS, WHICH ALLOWS TO MAINTAIN A PH OF BETWEEN 3 TO 9; THE PHOSOPHOLIPID MAY BE NATURAL AND / OR SYNTHETIC SUCH AS 1-PALMITOIL-2-OLEOIL-SN-GLYCERO-3-PHOSPHOCOLINE (POPC); AND THE THERMAL PROTECTOR CONTAINS TREHALOSE. POSACONAZOLE HAS A MEDIUM GRANULOMETRIC DISTRIBUTION WHICH IS BETWEEN 1.0 AND 8.0 MICRONS, WITH NO MORE THAN 3000 PARTICLES OF 10 MICRONS OR LARGER SIZE, NOR MORE THAN 300 PARTICLES OF 25 MICRONS OR LARGER SIZE. SUCH FORMULATION IS USEFUL IN THE TREATMENT OF INFECTIONS SUCH AS OROPHARYNGEAL OR ESOPHAGEAL CANDIDIASIS, INVASIVE ASPERGILLOSIS, INFECTIONS CAUSED BY DIMORPHIC FUNGI, ZYGOMYCOSIS AND INVASIVE INFECTIONS DUE TO MOLDES AND FRESH LEAVES, MOLDES AND LEAVES OF CHEMISTRY
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57512604P | 2004-05-28 | 2004-05-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20060291A1 true PE20060291A1 (en) | 2006-04-14 |
Family
ID=34971355
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2005000599A PE20060291A1 (en) | 2004-05-28 | 2005-05-27 | POSACONAZOLE INJECTABLE PHARMACEUTICAL COMPOSITIONS WITH STABILIZED PARTICLES |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP1761247A1 (en) |
| JP (1) | JP2008501034A (en) |
| KR (1) | KR20070027564A (en) |
| CN (1) | CN1988887A (en) |
| AR (1) | AR049063A1 (en) |
| AU (1) | AU2005249502A1 (en) |
| CA (1) | CA2567803A1 (en) |
| IL (1) | IL179627A0 (en) |
| MX (1) | MXPA06013886A (en) |
| NO (1) | NO20066005L (en) |
| PE (1) | PE20060291A1 (en) |
| RU (1) | RU2006146555A (en) |
| TW (1) | TWI290051B (en) |
| WO (1) | WO2005117831A1 (en) |
| ZA (1) | ZA200609890B (en) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060009469A1 (en) * | 2004-05-28 | 2006-01-12 | Leonore Witchey-Lakshmanan | Particulate-stabilized injectable pharmacutical compositions of posaconazole |
| RU2008148977A (en) | 2006-05-12 | 2010-06-20 | Фармакон-Форшунг Унд Бератунг Гмбх (At) | APPLICATION OF COMBINED DRUGS CONTAINING ANTIFUNGIC AGENTS |
| EP2130540A1 (en) * | 2008-06-02 | 2009-12-09 | Sandoz AG | Pharmaceutical compositions containing a crystalline form of posaconazole |
| EP2141159A1 (en) | 2008-07-03 | 2010-01-06 | Sandoz AG | A Crystalline form of posaconazole |
| WO2011003992A1 (en) | 2009-07-09 | 2011-01-13 | Sandoz Ag | A crystalline form of posaconazole |
| WO2011144655A1 (en) | 2010-05-19 | 2011-11-24 | Sandoz Ag | Process for the preparation of chiral hydrazides |
| AU2011254657B2 (en) | 2010-05-19 | 2016-02-04 | Sandoz Ag | Preparation of posaconazole intermediates |
| AU2011254658B2 (en) | 2010-05-19 | 2016-02-18 | Sandoz Ag | Purification of posaconazole and of posaconazole intermediates |
| MX342850B (en) | 2010-05-19 | 2016-10-14 | Sandoz Ag | Process for the preparation of chiral triazolones. |
| MX338685B (en) * | 2010-06-29 | 2016-04-26 | Merck Sharp & Dohme | Posaconazole intravenous solution formulations stabilized by substituted beta-cyclodextrin. |
| US9493428B2 (en) | 2011-06-16 | 2016-11-15 | Sandoz Ag | Process for the preparation of a chiral compound |
| CN103284959B (en) * | 2012-02-22 | 2015-06-03 | 重庆圣华曦药业股份有限公司 | Posaconazole freeze-dried powder injection and preparation method thereof |
| CN102755628B (en) * | 2012-07-16 | 2013-10-23 | 中国科学院微生物研究所 | Antifungal pharmaceutical composition |
| CN102805731B (en) * | 2012-08-22 | 2014-04-30 | 北京莱瑞森医药科技有限公司 | Posaconazole dry suspension and preparation method thereof |
| CN105030668B (en) * | 2015-06-26 | 2018-03-27 | 济川药业集团有限公司 | Oral posaconazole supensoid agent and preparation method thereof |
| CN106333925B (en) * | 2015-07-10 | 2019-06-18 | 上海美悦生物科技发展有限公司 | A kind of posaconazole liquid suspension and preparation method thereof |
| CN105997872B (en) * | 2016-07-08 | 2019-02-19 | 河南省立眼科医院 | An ophthalmic nanomicelle antifungal solution containing posaconazole |
| CA3056919A1 (en) * | 2017-03-26 | 2018-10-04 | Vivi Robyn Stafford | Method of treatment of skin conditions of eye lids |
| EP3609329A4 (en) * | 2017-04-12 | 2021-03-17 | Bhagwandin, Vikash J. | Compositions, packaged pharmaceuticals, and methods of using posaconazole for the sensitization of resistant tumors |
| CN110507609B (en) * | 2018-05-21 | 2021-09-17 | 上海医药工业研究院 | Preparation method of posaconazole oral suspension |
| CN111514146A (en) * | 2020-04-28 | 2020-08-11 | 山西振东泰盛制药有限公司 | Pharmaceutical composition containing posaconazole |
| CN113933131B (en) * | 2021-09-24 | 2024-01-26 | 合肥天一生物技术研究所有限责任公司 | Vaginal microorganism fluorescent staining solution |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5091188A (en) * | 1990-04-26 | 1992-02-25 | Haynes Duncan H | Phospholipid-coated microcrystals: injectable formulations of water-insoluble drugs |
| AU2002257104B2 (en) * | 2001-04-03 | 2006-02-09 | Merck Sharp & Dohme Corp. | Antifungal composition with enhanced bioavailability |
-
2005
- 2005-05-27 CA CA002567803A patent/CA2567803A1/en not_active Abandoned
- 2005-05-27 WO PCT/US2005/018945 patent/WO2005117831A1/en not_active Ceased
- 2005-05-27 PE PE2005000599A patent/PE20060291A1/en not_active Application Discontinuation
- 2005-05-27 JP JP2007515456A patent/JP2008501034A/en not_active Withdrawn
- 2005-05-27 KR KR1020067024996A patent/KR20070027564A/en not_active Withdrawn
- 2005-05-27 AU AU2005249502A patent/AU2005249502A1/en not_active Abandoned
- 2005-05-27 CN CNA2005800248542A patent/CN1988887A/en active Pending
- 2005-05-27 MX MXPA06013886A patent/MXPA06013886A/en unknown
- 2005-05-27 TW TW094117524A patent/TWI290051B/en not_active IP Right Cessation
- 2005-05-27 AR ARP050102203A patent/AR049063A1/en not_active Application Discontinuation
- 2005-05-27 EP EP05755118A patent/EP1761247A1/en not_active Withdrawn
- 2005-05-27 RU RU2006146555/15A patent/RU2006146555A/en not_active Application Discontinuation
-
2006
- 2006-11-27 IL IL179627A patent/IL179627A0/en unknown
- 2006-11-27 ZA ZA200609890A patent/ZA200609890B/en unknown
- 2006-12-22 NO NO20066005A patent/NO20066005L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2567803A1 (en) | 2005-12-15 |
| MXPA06013886A (en) | 2007-01-26 |
| JP2008501034A (en) | 2008-01-17 |
| AU2005249502A1 (en) | 2005-12-15 |
| IL179627A0 (en) | 2007-05-15 |
| KR20070027564A (en) | 2007-03-09 |
| AR049063A1 (en) | 2006-06-21 |
| TWI290051B (en) | 2007-11-21 |
| RU2006146555A (en) | 2008-07-20 |
| NO20066005L (en) | 2007-02-27 |
| EP1761247A1 (en) | 2007-03-14 |
| CN1988887A (en) | 2007-06-27 |
| TW200609001A (en) | 2006-03-16 |
| WO2005117831A1 (en) | 2005-12-15 |
| ZA200609890B (en) | 2008-09-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |