EP0215313A2
Expired / Lapsed
EP
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Emulsion compositions for the parenteral and/or oral administration of sparingly water soluble ionizable hydrophobic drugs
Assignee: Wyeth Holdings LLC
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Filing: 1986-08-19
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Granted: —
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Expires: 2006-08-19
Abstract
Abstract This disclosure describes quick breaking, in vivo , intravenous, intramuscular, intraarticular and/or oral fat emulsion compositions which incorporate the use of benzyl alcohol as a cosurfactant and/or a cosolvent in combination with materials such as synthetic surfactants, e.g. sorbitan triisostearate, triglycerol diisostearate or triglycerol pentaoleate; naturally occurring vegetable oils, e.g. sesame oil, and soybean oil; natural lecithins such as egg lecithin or soy lecithin; saturated or unsaturated aliphatic acids, e.g. oleic acid, hexanoic acid and linolenic acid; and other excipients such as glycerine, polyvinylpyrrolidone, Pluronic® F-68 dl-α-tocopherol.
Inventors
- 👤 Narendra Raghunathji Desai
- 👤 Eugene Albert Carpentier
- 👤 Madurai Ganesan
- 👤 Edward Charles Shinal
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 17:46
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/0012; A61K9/0019; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/44; A61K9/107
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
90 words
A composition of matter for delivery of hydrophobic drugs comprising: (a) a hydrophobic drug; (b) an oleaginous vehicle or oil phase (c) a surfactant or emulsifier (d) a co-surfactant or auxiliary emulsifier and (e) benzyl alcohol as a co-solvent. wherein the hydrophobic drug may be a sparingly water soluble ionizable solid or a water insoluble viscous oily liquid and may be a basic drug which has an ionization constant lower or nearer the physiological pH or an acid drug which has an ionization constant higher or nearer the physiological pH.
Claim 2
Dependent Claim
90 words
A composition of matter for delivery of hydrophobic drugs comprising: (a) a hydrophobic drug; (b) an oleaginous vehicle or oil phase (c) a surfactant or emulsifier (d) a co-surfactant or auxiliary emulsifier and (e) benzyl alcohol as a co-solvent. wherein the hydrophobic drug may be a sparingly water soluble ionizable solid or a water insoluble viscous oily liquid and may be a basic drug which has an ionization constant lower or nearer the physiological pH or an acid drug which has an ionization constant higher or nearer the physiological pH.
Claim 3
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 4
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 5
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 6
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 7
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 8
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 9
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 10
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 11
Dependent Claim
16 words
The composition of matter as recited in Claim 5, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.
Claim 12
Dependent Claim
16 words
A composition in accordance with Claim 4, in which the hydrophobic drug is 3-[4,6-bis[(1,1-2,2-tetramethylpropyl)amino]- s -triazin-2-yl]-3-azabicyclo[3·2·2]nonane.
Claim 13
Dependent Claim
18 words
The composition of matter as recited in Claim 6, in which the hydrophobic drug is 3-[4,6-bis[(1,1-2,2-tetramethylpropyl)amino]- s -triazin-2-yl]-3-azabicyclo[3·2·2]nonane.
Claim 14
Dependent Claim
16 words
The composition of matter as recited in Claim 7, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.
Claim 15
Dependent Claim
16 words
The composition of matter as recited in Claim 8, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.
Claim 16
Dependent Claim
16 words
The composition of matter as recited in Claim 9, in which the hydrophobic drug is bis(2-imidazolin-2-ylhydrazone)-9,10-anthracenedicarboxaldehyde.
Claim 17
Dependent Claim
104 words
A process for the formation of a pharmaceutical composition of a hydrophobic drug characterized by the steps of combining said hydrophobic drug with a pharmaceutically acceptable oleaginous vehicle or oil; a surfactant or emulsifier; a co-surfactant or auxiliary emulsifier and sufficient benzyl alcohol to act as a co-solvent for the drug in question wherein the hydrophobic drug may be a sparingly water soluble ionizable solid or a water insoluble viscous oily liquid and may be a basic drug which has an ionization constant lower or nearer the physiological pH or an acid drug which has an ionization constant higher or nearer the physiological pH.
Claim 18
Dependent Claim
104 words
A process for the formation of a pharmaceutical composition of a hydrophobic drug characterized by the steps of combining said hydrophobic drug with a pharmaceutically acceptable oleaginous vehicle or oil; a surfactant or emulsifier; a co-surfactant or auxiliary emulsifier and sufficient benzyl alcohol to act as a co-solvent for the drug in question wherein the hydrophobic drug may be a sparingly water soluble ionizable solid or a water insoluble viscous oily liquid and may be a basic drug which has an ionization constant lower or nearer the physiological pH or an acid drug which has an ionization constant higher or nearer the physiological pH.
References Cited (Backward Citations)
No citation records indexed.
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