WO2004039360B1 - Compositions pharmaceutiques aqueuses 2,6-diisopropylphenol - Google Patents
Compositions pharmaceutiques aqueuses 2,6-diisopropylphenolInfo
- Publication number
- WO2004039360B1 WO2004039360B1 PCT/US2003/031086 US0331086W WO2004039360B1 WO 2004039360 B1 WO2004039360 B1 WO 2004039360B1 US 0331086 W US0331086 W US 0331086W WO 2004039360 B1 WO2004039360 B1 WO 2004039360B1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- formulation
- amount
- formulation according
- antimicrobial agent
- peg
- Prior art date
Links
- OLBCVFGFOZPWHH-UHFFFAOYSA-N propofol Chemical compound CC(C)C1=CC=CC(C(C)C)=C1O OLBCVFGFOZPWHH-UHFFFAOYSA-N 0.000 title claims abstract 21
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 claims abstract 159
- 229960004134 propofol Drugs 0.000 claims abstract 7
- 238000009472 formulation Methods 0.000 claims 155
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 51
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 48
- 239000004599 antimicrobial Substances 0.000 claims 46
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 claims 45
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims 34
- 239000002202 Polyethylene glycol Substances 0.000 claims 23
- 229920001223 polyethylene glycol Polymers 0.000 claims 23
- 239000013011 aqueous formulation Substances 0.000 claims 18
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims 17
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims 17
- 229960002216 methylparaben Drugs 0.000 claims 17
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 16
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims 15
- 235000019445 benzyl alcohol Nutrition 0.000 claims 15
- 229920001993 poloxamer 188 Polymers 0.000 claims 14
- 229940044519 poloxamer 188 Drugs 0.000 claims 14
- 238000000034 method Methods 0.000 claims 8
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 5
- 229920001400 block copolymer Polymers 0.000 claims 5
- 206010002091 Anaesthesia Diseases 0.000 claims 4
- 230000037005 anaesthesia Effects 0.000 claims 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 230000000845 anti-microbial effect Effects 0.000 claims 3
- 239000008181 tonicity modifier Substances 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 2
- 229920001983 poloxamer Polymers 0.000 claims 2
- 229960000502 poloxamer Drugs 0.000 claims 2
- 235000002639 sodium chloride Nutrition 0.000 claims 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 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 claims 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 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 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 229920002511 Poloxamer 237 Polymers 0.000 claims 1
- 229920002556 Polyethylene Glycol 300 Polymers 0.000 claims 1
- GZCGUPFRVQAUEE-SLPGGIOYSA-N aldehydo-D-glucose Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O GZCGUPFRVQAUEE-SLPGGIOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
- 235000018417 cysteine Nutrition 0.000 claims 1
- 239000008121 dextrose Substances 0.000 claims 1
- 235000011187 glycerol Nutrition 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- -1 metabisulfate Chemical compound 0.000 claims 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims 1
- 229920002523 polyethylene Glycol 1000 Polymers 0.000 claims 1
- 239000001103 potassium chloride Substances 0.000 claims 1
- 235000011164 potassium chloride Nutrition 0.000 claims 1
- 235000013772 propylene glycol Nutrition 0.000 claims 1
- 102200110015 rs3087373 Human genes 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 230000007613 environmental effect Effects 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 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
- A61K9/08—Solutions
-
- 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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- 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
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/186—Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- 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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61K9/10—Dispersions; Emulsions
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Inorganic Chemistry (AREA)
- Dispersion Chemistry (AREA)
- Dermatology (AREA)
- Medicinal Preparation (AREA)
Abstract
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP03759636A EP1556022A4 (fr) | 2002-10-29 | 2003-10-02 | Compositions pharmaceutiques aqueuses 2,6-diisopropylphenol |
AU2003275360A AU2003275360A1 (en) | 2002-10-29 | 2003-10-02 | Aqueous 2,6-diisopropylphenol pharmaceutical compositions |
US10/766,631 US7550155B2 (en) | 2002-07-29 | 2004-01-28 | Aqueous pharmaceutical compositions of 2,6-diisopropylphenol (propofol) and their uses |
US12/333,887 US8133918B2 (en) | 2002-07-29 | 2008-12-12 | Aqueous pharmaceutical compositions of 2,6-diisopropylphenol (propofol) and their uses |
Applications Claiming Priority (16)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US42219502P | 2002-10-29 | 2002-10-29 | |
US60/422,195 | 2002-10-29 | ||
US43697902P | 2002-12-30 | 2002-12-30 | |
US60/436,979 | 2002-12-30 | ||
US44349003P | 2003-01-29 | 2003-01-29 | |
US60/443,490 | 2003-01-29 | ||
US46245003P | 2003-04-11 | 2003-04-11 | |
US60/462,450 | 2003-04-11 | ||
US46431403P | 2003-04-21 | 2003-04-21 | |
US60/464,314 | 2003-04-21 | ||
US47040303P | 2003-05-14 | 2003-05-14 | |
US60/470,403 | 2003-05-14 | ||
US48535403P | 2003-07-07 | 2003-07-07 | |
US60/485,354 | 2003-07-07 | ||
US10/629,308 US7915317B2 (en) | 2002-07-29 | 2003-07-29 | Aqueous 2,6-diisopropylphenol pharmaceutical compositions |
US10/629,308 | 2003-07-29 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2004039360A1 WO2004039360A1 (fr) | 2004-05-13 |
WO2004039360B1 true WO2004039360B1 (fr) | 2004-06-17 |
Family
ID=32234547
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US2003/031086 WO2004039360A1 (fr) | 2002-07-29 | 2003-10-02 | Compositions pharmaceutiques aqueuses 2,6-diisopropylphenol |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP1556022A4 (fr) |
AU (1) | AU2003275360A1 (fr) |
WO (1) | WO2004039360A1 (fr) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7550155B2 (en) * | 2002-07-29 | 2009-06-23 | Transform Pharmaceuticals Inc. | Aqueous pharmaceutical compositions of 2,6-diisopropylphenol (propofol) and their uses |
US20220183999A1 (en) * | 2019-04-05 | 2022-06-16 | Sorrento Therapeutics, Inc. | Cannabidiol Pharmaceutical Compositions |
CN114601800B (zh) * | 2021-09-28 | 2023-07-28 | 天津瑞普生物技术股份有限公司 | 一种甲磷丙泊酚钠无菌粉针剂及其制备方法 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1472793A (en) * | 1974-03-28 | 1977-05-04 | Ici Ltd | Pharmaceutical compositions |
ES2211151T3 (es) * | 1998-08-19 | 2004-07-01 | Skyepharma Canada Inc. | Dispersiones acuosas inyectables de propofol. |
AU5574200A (en) * | 1999-06-21 | 2001-01-09 | Kuhnil Pharm. Co., Ltd. | Anesthetic composition for intravenous injection comprising propofol |
US6623765B1 (en) * | 2000-08-01 | 2003-09-23 | University Of Florida, Research Foundation, Incorporated | Microemulsion and micelle systems for solubilizing drugs |
GB0124071D0 (en) * | 2001-10-08 | 2001-11-28 | Kbig Ltd | Improvement in the administration of high boiling point aneasthetics |
-
2003
- 2003-10-02 EP EP03759636A patent/EP1556022A4/fr not_active Withdrawn
- 2003-10-02 AU AU2003275360A patent/AU2003275360A1/en not_active Abandoned
- 2003-10-02 WO PCT/US2003/031086 patent/WO2004039360A1/fr not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
EP1556022A4 (fr) | 2010-03-10 |
WO2004039360A1 (fr) | 2004-05-13 |
AU2003275360A8 (en) | 2004-05-25 |
AU2003275360A1 (en) | 2004-05-25 |
EP1556022A1 (fr) | 2005-07-27 |
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