US4647586A
Expired / Lapsed
US
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Pharmaceutical oil-in-water type micro-emulsion
Assignee: Pfizer Japan Inc
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Filing: 1985-08-08
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Granted: 1987-03-03
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Expires: 2005-08-08
Abstract
Abstract A pharmaceutical oil-in-water type micro-emulsion comprising fine particles of an oil or fat containing an effective amount of a 4-biphenylylacetic acid ester of the formula ##STR1## wherein R represents an alkyl group, an aqueous medium and a physiologically acceptable emulsifier for dispersing said fine particles in said aqueous medium. This micro-emulsion is useful for treating inflammation, pain and/or fever in a mammal.
Inventors
- 👤 Yutaka Mizushima
- 👤 Mitsuharu Fujii
- 👤 Hiroshi Takei
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 00:44
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/21; A61K31/215; A61K31/22; A61K9/00; A61K9/10; A61K9/107; A61K9/1075; A61P; A61P25/00; A61P25/04; A61P29/00
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
84 words
A method for treating inflammation, pain and/or fever in a mammal, which comprises parenterally administering to the mammal a pharmaceutical oil-in-water type micro-emulsion comprising fine particles of a vegetable oil or triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing an effective amount of a 4-biphenylylacetic acid ester of the formula ##STR4## wherein R represents an alkyl group, an aqueous medium and 0.05 to 25% (w/v) of a physiologically acceptable phospholipid for dispersing said fine particles in said aqueous medium.
Claim 2
Independent Claim
84 words
A method for treating inflammation, pain and/or fever in a mammal, which comprises parenterally administering to the mammal a pharmaceutical oil-in-water type micro-emulsion comprising fine particles of a vegetable oil or triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing an effective amount of a 4-biphenylylacetic acid ester of the formula ##STR4## wherein R represents an alkyl group, an aqueous medium and 0.05 to 25% (w/v) of a physiologically acceptable phospholipid for dispersing said fine particles in said aqueous medium.
Claim 3
Dependent Claim
13 words
The method of claim 1 wherein the 4-biphenylylacetic acid ester is ethyl 4-biphenylylacetate.
Claim 4
Dependent Claim
12 words
The method of claim 1 the micro-emulsion is administered intravenously or intra-articularly.
Claim 5
Dependent Claim
81 words
The method of claim 1 wherein the micro-emulsion consists essentially of 5 to 50% (w/v) of fine particles of a vegetable oil or triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing 0.01 to 10% (w/v) of the 4-biphenylylacetic acid ester, 0.05 to 25% (w/v) of the physiologically acceptable phospholipid, an isotonizing agent selected from the group consisting of glycerol, sugar alcohols, monosaccharides, disaccharides and amino acids in an amount sufficient to isotonize the emulsion, and water.
Claim 6
Dependent Claim
51 words
The method of claim 4 wherein the micro-emulsion consists essentially of 5 to 30% (w/v) of fine particles of soybean oil having dissolved therein 1 to 5% (w/v) of ethyl 4-biphenylylacetate, 0.5 to 25% (w/v) of purified soybean oil phospholipid, 1 to 5% (w/v) of glycerol, and the remainder being water.
Claim 7
Dependent Claim
28 words
The method of claim 5 wherein the purified soybean oil phospholipid has a phosphatidyl choline content of at least 80% and an iodine value of 35 to 45.
Claim 8
Dependent Claim
68 words
A pharmaceutical oil-in-water type micro-emulsion comprising fine particles of a vegetable oil or a triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing 0.01 to 10% (w/v) of a 4-biphenylylacetic acid ester of the formula ##STR5## wherein R represents an alkyl group, an aqueous medium, and 0.05 to 25% (w/v) of a physiologically acceptable phospholipid for dispersing said fine particles in said aqueous medium.
Claim 9
Dependent Claim
68 words
A pharmaceutical oil-in-water type micro-emulsion comprising fine particles of a vegetable oil or a triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing 0.01 to 10% (w/v) of a 4-biphenylylacetic acid ester of the formula ##STR5## wherein R represents an alkyl group, an aqueous medium, and 0.05 to 25% (w/v) of a physiologically acceptable phospholipid for dispersing said fine particles in said aqueous medium.
Claim 10
Dependent Claim
25 words
The micro-emulsion of claim 7 which further contains an isotonizing agent selected from the group consisting of glycerol, sugar alcohols, monosaccharides, disaccharides and amino acids.
Claim 11
Dependent Claim
13 words
The micro-emulsion of claim 8 wherein the 4-biphenylylacetic acid ester is ethyl 4-biphenylylacetate.
Claim 12
Dependent Claim
14 words
The micro-emulsion of claim 8 wherein the vegetable oil is pharmaceutically acceptable soybean oil.
Claim 13
Dependent Claim
16 words
The micro-emulsion of claim 5 wherein the physiologically acceptable phospholipid is a purified vegetable oil phospholipid.
Claim 14
Dependent Claim
16 words
The micro-emulsion of claim 6 wherein the purified vegetable oil phospholipid is purified soybean oil phospholipid.
Claim 15
Dependent Claim
79 words
The micro-emulsion of claim 7 which consists essentially of 5 to 50% (w/v) of fine particles of a vegetable oil or triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing 0.01 to 10% (w/v) of the 4-biphenylylacetic acid ester, 0.05 to 25% (w/v) of the physiologically acceptable phospholipid, an isotonizing agent selected from the group consisting of glycerol, sugar alcohols, monosaccharides, disaccharides and amino acids in an amount sufficient to isotonize the emulsion, and water.
Claim 16
Dependent Claim
13 words
The micro-emulsion of claim 13 wherein the 4-biphenylylacetic acid ester is ethyl 4-biphenylylacetate.
Claim 17
Dependent Claim
50 words
The micro-emulsion of claim 1 which consists essentially of 5 to 30% (w/v) of fine paritcles of soybean oil having dissolved therein 1 to 5% (w/v) of ethyl 4-biphenylylacetate, 0.5 to 25% (w/v) of a purified soybean oil phospholipid, 1 to 5% (w/v) of glycerol, and the remainder being water.
Claim 18
Dependent Claim
31 words
The micro-emulsion of claim 1 wherein the fine particles of the oil or fat have a mean particle diameter of not more than 1 micron, preferably not more than 0.3 micron.
Claim 19
Dependent Claim
28 words
The micro-emulsion of claim 12 wherein the purified soybean oil phospholipid has a phosphatidyl choline content of at least 80% and an iodine value of 35 to 45.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-03-02 | 1990-09-01 | 1991-03-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-03-02 | 1994-09-01 | 1995-03-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-03-02 | 1998-09-01 | 1999-03-03 | $7700.00 | Window Closed / Lapsed |