Patent US6615165B2 successfully refreshed from Google Patents.
US5284645A
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US
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Fluorocarbon emulsions containing amino acid based anti-inflamatory agents and buffer systems
Assignee: PFC Therapeutics LLC
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Filing: 1989-10-04
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Granted: 1994-02-08
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Expires: 2009-10-04
Abstract
Abstract Disclosed are fluorocarbon emulsions comprising amino acids and substances related to amino acids, such as substituted amino acids or amphoteric groups of amino acid side chains, for example, the imidazolyl group of histidine. Emulsion formulations comprising imidazole and imidazole based drugs possess anti-inflammatory and antipyretic properties which counteract transient inflammatory responses which occur when these emulsions are administered in vivo. Lipid constituents of histidine-containing emulsions are protected against oxidation caused by free radical formation. Disclosed also are emulsion formulations buffered with amino acids comprising histidine, imidazole, and related compounds that have a buffering capacity sufficient to maintain the emulsion pH within a specified range under storage conditions and protect these emulsions from the endogenous production of acid. Disclosed also is a method of calculation which assists in the selection of an optimum buffer composition and concentration to preserve physiological compatibility and stability of the emulsions within selected pH limits.
Inventors
- 👤 David M. Long, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 23:34
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0026; A61K31/00; A61K31/02; A61K31/33; A61K31/395; A61K31/41; A61K31/415; A61K31/435; A61K31/44; A61K31/60; A61K47/00; A61K47/06; A61K47/16; A61K47/18; A61K47/183; A61P; A61P29/00; A61P43/00
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
51 words
A fluorocarbon emulsion suitable for use in the tissues, organs and cavities of the body, comprising: an aqueous phase; a effective amount of a fluorocarbon; an emulsifying agent; and at least one anti-inflammatory agent which is imidazole, a drug having a chemical structure which includes an imidazolyl group, or combinations thereof.
Claim 2
Dependent Claim
51 words
A fluorocarbon emulsion suitable for use in the tissues, organs and cavities of the body, comprising: an aqueous phase; a effective amount of a fluorocarbon; an emulsifying agent; and at least one anti-inflammatory agent which is imidazole, a drug having a chemical structure which includes an imidazolyl group, or combinations thereof.
Claim 3
Dependent Claim
17 words
The emulsion of claim 1, further comprising an oligopeptide, an amino acid, or a substituted amino acid.
Claim 4
Dependent Claim
48 words
A fluorocarbon suitable for use in the tissues, organs and cavities of the body, comprising: an aqueous phase; an effective amount of a fluorocarbon; an emulsifying agent; and at least one anti-inflammatory agent selected from the group consisting of N(7-carboxyheptyl)imidazole, 4-(2-(1-H-imidazol-1-yl)ethoxy)benzoic acid (dazoxiben), or imidazo(1,5-α-pyridine-5-hexanoic acid (CGS 13080).
Claim 5
Dependent Claim
48 words
A fluorocarbon suitable for use in the tissues, organs and cavities of the body, comprising: an aqueous phase; an effective amount of a fluorocarbon; an emulsifying agent; and at least one anti-inflammatory agent selected from the group consisting of N(7-carboxyheptyl)imidazole, 4-(2-(1-H-imidazol-1-yl)ethoxy)benzoic acid (dazoxiben), or imidazo(1,5-α-pyridine-5-hexanoic acid (CGS 13080).
Claim 6
Dependent Claim
16 words
The emulsion of claim 1, wherein the emulsion is capable of carrying oxygen to the tissues.
Claim 7
Dependent Claim
64 words
A fluorocarbon emulsion suitable for use in the tissues, organs and cavities of an animal body, comprising A continuous aqueous phase; an effective amount of fluorocarbon; an effective amount of an emulsifying agent; and a buffering agent selected from the group consisting of histidine, imidazole, substituted histidine or imidazole compounds retaining the amphoteric site of the imidazole ring, oligopeptides containing histidine, and mixtures thereof.
Claim 8
Dependent Claim
64 words
A fluorocarbon emulsion suitable for use in the tissues, organs and cavities of an animal body, comprising A continuous aqueous phase; an effective amount of fluorocarbon; an effective amount of an emulsifying agent; and a buffering agent selected from the group consisting of histidine, imidazole, substituted histidine or imidazole compounds retaining the amphoteric site of the imidazole ring, oligopeptides containing histidine, and mixtures thereof.
Claim 9
Dependent Claim
16 words
The emulsion of claim 5, wherein said buffering agent comprises a mixture of histidine and imidazole.
Claim 10
Dependent Claim
30 words
The emulsion of claim 6, wherein the concentration of imidazole is between about 0.01 and 0.2 molar, and wherein the concentration of histidine is between about 0.01 and 0.2 molar.
Claim 11
Dependent Claim
17 words
The emulsion of claim 5, wherein the pH of the emulsion is maintained between 5.3 and 8.9.
Claim 12
Dependent Claim
18 words
The emulsion of claim 8, wherein the pH of the emulsion is maintained between about 7.3 and 7.9.
Claim 13
Dependent Claim
19 words
The emulsion of claim 8, wherein said buffer maintains said pH at a physiological temperature of about 37° C.
Claim 14
Dependent Claim
20 words
The emulsion of claim 8 or 9, wherein said buffer maintains said pH at a temperature below about 30° C.
Claim 15
Dependent Claim
32 words
The emulsion of claim 5, wherein the concentration of said buffer is sufficient to provide buffering capacity of at least 20 mmol/L/pH unit between pH values of from about 5.3 to 8.9.
Claim 16
Dependent Claim
14 words
The emulsion of claim 1 or 5, wherein said fluorocarbon is a brominated perfluorocarbon.
Claim 17
Dependent Claim
14 words
The emulsion of claim 1 or 5, wherein said fluorocarbon is a perfluorocarbon hydride.
Claim 18
Dependent Claim
22 words
The emulsion of claim 1 or 5 wherein said fluorocarbon is present in an amount of from about 40% to 125% weight/volume.
Claim 19
Dependent Claim
18 words
The emulsion of claim 15, wherein said fluorocarbon is present in an amount greater than about 75% weight/volume.
Claim 20
Dependent Claim
14 words
The emulsion of claim 1 or 5 wherein said emulsifying agent is a phospholipid.
Claim 21
Dependent Claim
16 words
An emulsion, according to claim 1 or 5 wherein said emulsifying agent is a nonionic surfactant.
Claim 22
Dependent Claim
15 words
The emulsion of claim 1 or 5 wherein said emulsifying agent comprises a fluorinated surfactant.
Claim 23
Dependent Claim
13 words
An emulsion, according to claim 1 or 5 further comprising an antioxidant agent.
Claim 24
Dependent Claim
12 words
An emulsion, according to claim 20, wherein the antioxidant is a tocopherol.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-02-07 | 1997-08-09 | 1998-02-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-02-07 | 2001-08-09 | 2002-02-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-02-07 | 2005-08-09 | 2006-02-08 | $7700.00 | Window Closed / Lapsed |