EP0214501A2
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Emulsion compositions for administration of sparingly water soluble ionizable basic hydrophobic drugs
Assignee: Wyeth Holdings LLC
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Filing: 1986-08-16
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Granted: —
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Expires: 2006-08-16
Abstract
Abstract Lipid emulsion form compositions have been formulated and presented to eliminate adverse injection site reactions associated with the intravenous administration of certain sparingly water soluble, hydrophobic, ionizable drugs in mammals and to provide a solubilized drug form for oral, parenteral or intraarticular administration which enhances drug absorption and the therapeutic efficacy of the drug.
Inventors
- 👤 Narendra Raghunthji Desai
- 👤 Eugene Albert Carpentier
- 👤 Madurai Ganesan
- 👤 Edward Charles Shinal
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 15:01
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/0012; A61K9/0019; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/541; A61K9/107; A61K9/1075
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
117 words
A composition of matter for delivery of hydrophobic drugs comprising: (a) a hydrophobic drug; (b) a pharmaceutically acceptable oleaginous vehicle or oil selected from the group consisting of (i) naturally occurring vegetable oils and (ii) semisynthetic mono, di or triglycerides; (c) a surfactant or emulsifier; (d) a co-surfactant or auxiliary emulsifier; (e) an ion-pair former selected from C 6 -C 20 saturated or unsaturated aliphatic or aromatic acids when the hydrophobic drug is basic and a pharmaceutically acceptable aliphatic or aromatic amine such as glucamine and homologs thereof of the formula R-NH-CH 2 (CHOH) 4 CH 2 0H where R is H or C l -C 6 alkyl when the hydrophobic drug is acidic; and (f) water.
Claim 2
Dependent Claim
117 words
A composition of matter for delivery of hydrophobic drugs comprising: (a) a hydrophobic drug; (b) a pharmaceutically acceptable oleaginous vehicle or oil selected from the group consisting of (i) naturally occurring vegetable oils and (ii) semisynthetic mono, di or triglycerides; (c) a surfactant or emulsifier; (d) a co-surfactant or auxiliary emulsifier; (e) an ion-pair former selected from C 6 -C 20 saturated or unsaturated aliphatic or aromatic acids when the hydrophobic drug is basic and a pharmaceutically acceptable aliphatic or aromatic amine such as glucamine and homologs thereof of the formula R-NH-CH 2 (CHOH) 4 CH 2 0H where R is H or C l -C 6 alkyl when the hydrophobic drug is acidic; and (f) water.
Claim 3
Dependent Claim
61 words
The composition of matter as recited in Claim 1 comprising: wherein the hydrophobic drug may be a sparingly water soluble ionizable solid or a water insoluble viscous oily liquid and/or may be a basic drug which has an ionization constant lower or nearer the physiological pH or an acidic drug which has an ionization constant higher or nearer the physiological pH.
Claim 4
Dependent Claim
46 words
The composition of matter as recited in Claim 1 comprising: wherein the hydrophobic drug may be a sparingly water soluble ionizable solid or a water insoluble viscous oily liquid and/or may be an acidic drug which has an ionization constant higher or nearer the physiological pH.
Claim 5
Dependent Claim
16 words
The composition of matter as recited in Claim 2 where the hydrophobic drug is bis(2-imidazolin-2-ylhydra- zone)-9,10-anthracenedicarboxaldehyde.
Claim 6
Dependent Claim
16 words
The composition of matter as recited in Claim 2 where the hydrophobic drug is 3-[4,6-bis[(1,1-2,2-tetra- methylpropyl)amino]-s-triazin-2-yl]-3-azabicyclo[3·2·2]-nonane.
Claim 7
Dependent Claim
17 words
The composition of matter as recited in Claim 3 where the hydrophobic drug is 4-biphenyl acetic acid.
Claim 8
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 11
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 12
Dependent Claim
10 words
The composition of matter as recited in Claim 1 comprising:
Claim 13
Dependent Claim
16 words
The composition of matter as recited in Claim 7 where the hydrophobic drug is bis(2-imidazolin-2-ylhydra- zone)-9,10-anthracenedicarboxaldehyde.
Claim 14
Dependent Claim
16 words
The composition of matter as recited in Claim 8 where the hydrophobic drug is bis(2-imidazolin-2-ylhy- drazone)-9,10-anthracenedicarboxaldehyde.
Claim 15
Dependent Claim
17 words
The composition of matter as recited in Claim 9 where the hydrophobic drug is 4-biphenyl acetic acid.
Claim 16
Dependent Claim
11 words
'13. The composition of matter as recited in Claim 1 comprising:
Claim 19
Dependent Claim
16 words
The composition of matter as recited in Claim 3 where the hydrophobic drug is 3-[4,6-bis[(1,1-2,2-tetra- methylpropyl)amino]-s-triazin-2-yl]-3-azabicyclo[3·2·2]-nonane.
Claim 20
Dependent Claim
129 words
A process for the formation of a homogenized pharmaceutical composition characterized by the steps of: (a) Forming an ion-pair by reacting a hydrophobic drug with an ion-pair former selected from a C 6 -C 20 saturated or unsaturated aliphatic or aromatic acids when the hydrophobic drug is basic and a pharmaceutically acceptable aliphatic or aromatic amine when the hydrophobic drug is acidic; (b) forming an oil in water emulsion of said ion-pair by combining water; a pharmaceutically acceptable oleaginous vehicle or oil selected from (i) naturally occurring vegetable oils and (ii) semisynthetic mono, di or triglycerides; a surfactant or emulsifier; and, a co- surfactant or auxiliary emulsifier homogenizing said emulsion at pressures of from 8,000 to 15,000 p.s.i. to reduce the particle size to between 0.170 and 0.5 microns.
Claim 21
Dependent Claim
129 words
A process for the formation of a homogenized pharmaceutical composition characterized by the steps of: (a) Forming an ion-pair by reacting a hydrophobic drug with an ion-pair former selected from a C 6 -C 20 saturated or unsaturated aliphatic or aromatic acids when the hydrophobic drug is basic and a pharmaceutically acceptable aliphatic or aromatic amine when the hydrophobic drug is acidic; (b) forming an oil in water emulsion of said ion-pair by combining water; a pharmaceutically acceptable oleaginous vehicle or oil selected from (i) naturally occurring vegetable oils and (ii) semisynthetic mono, di or triglycerides; a surfactant or emulsifier; and, a co- surfactant or auxiliary emulsifier homogenizing said emulsion at pressures of from 8,000 to 15,000 p.s.i. to reduce the particle size to between 0.170 and 0.5 microns.
Claim 22
Dependent Claim
34 words
A process according to claim 15 characterized by the further step of homogenizing said emulsion at pressures of from 8,000 to 15,000 p.s.i. to reduce the particle size to between 0.170 and 0.5 microns.
References Cited (Backward Citations)
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