US4680309A
Expired / Lapsed
US
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Methods and compositions for treating inflammation or arthritis
Assignee: National Research Laboratories
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Filing: 1986-02-03
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Granted: 1987-07-14
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Expires: 2006-02-03
Abstract
Abstract A method of treating inflammation or arthritis with metal complexes that can traverse skin and animal cell membranes intact and effectively deliver and release metal ions in a controlled manner upon demand at the targeted inflammatory or arthritic areas containing endogenous reacting moieties which demand the metal ions. The metal complexes have an aqueous proton induced dissociation property represented by a sigmoidally-shaped curve on a cartesian coordinate plot of the negative log of the metal ion concentration versus the negative log of hydrogen ion concentration. This dissociation property enables the metal complexes to release metal ions in a controlled manner upon demand at the targeted inflammatory or arthritic areas containing endogenous reacting moieties which demand the metal ions. The metal complexes can be effectively administered either topically or subcutaneously. Upon topical application, the metal complexes are dispersed in a vehicle to provide a buffered composition to neutralize the initial acidic layer of the skin. These unique and advantageous properties permit the metal complexes to be incorporated into vehicles with an adjusted pH minimizing premature release of the metal ions prior to reaching the targeted inflammatory or arthritic areas. Further, the metal complexes can be dispersed in a greaseless cold cream vehicle formulated to avoid or minimize undesirable chemical incompatibilities. An example of a topical composition employed is disodiummonocopper(II) citrate in an amount of about 10% w/w in a water-dispersible cream base vehicle comprising an oil-in-water emulsion having a pH of about 7.0.
Inventors
- 👤 Gerald L. Maurer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 14:33
CPC Classifications
C; C07; C07C; C07C59/00; C07C59/235; C07C59/245; A; A61; A61K; A61K31/00; A61K31/28; A61K31/30; A61K31/315; C07C59/255; C07C59/265
Claims Analysis
Total Claims: 40
Claim 1
Independent Claim
43 words
A method of alleviating an inflammatory disorder in an animal which comprises delivering to the site of the inflammation of said disorder an effective anti-inflammatory amount of a metal complex consisting of dialkali metal monoheavymetal chelate of an alpha or beta-hydroxy polycarboxylic acid.
Claim 2
Independent Claim
43 words
A method of alleviating an inflammatory disorder in an animal which comprises delivering to the site of the inflammation of said disorder an effective anti-inflammatory amount of a metal complex consisting of dialkali metal monoheavymetal chelate of an alpha or beta-hydroxy polycarboxylic acid.
Claim 3
Dependent Claim
23 words
The method of claim 1 wherein said metal complex is topically administered to the skin of the body portion afflicted with said disorder.
Claim 4
Dependent Claim
24 words
The method of claim 2 wherein said metal complex is dispersed in a vehicle to provide a composition having a pH above about 7.
Claim 5
Dependent Claim
22 words
The method of claim 2 wherein said metal complex diffuses through the skin intact to facilitate subcutaneous release of said metal ion.
Claim 6
Dependent Claim
18 words
The method of claim 1 wherein said metal complex is introduced subcutaneously at the location of said disorder.
Claim 7
Dependent Claim
26 words
The method of claim 1 wherein said complex is dispersed in a vehicle to provide a composition having a pH of about 6.5 to about 9.
Claim 8
Dependent Claim
13 words
The method of claim 1 wherein said complex is dialkalimetal monocopper (II) citrate.
Claim 9
Dependent Claim
12 words
The method of claim 7 wherein said complex is in aqueous admixture.
Claim 10
Dependent Claim
17 words
The method of claim 8 wherein the admixture has a pH of about 7 to about 9.
Claim 11
Dependent Claim
11 words
The method of claim 1 wherein said metal ion is copper.
Claim 12
Dependent Claim
19 words
The method of claim 1 wherein said disorder is a tissue response to injury or destruction of animal cells.
Claim 13
Dependent Claim
10 words
The method of claim 11 wherein said disorder is arthritis.
Claim 14
Dependent Claim
13 words
The method of claim 12 wherein said arthritis is osteoarthritis or rheumatoid arthritis.
Claim 15
Dependent Claim
10 words
The method of claim 11 wherein said disorder is arthralgia.
Claim 16
Dependent Claim
11 words
The method of claim 11 wherein said disorder is microbially infected.
Claim 17
Dependent Claim
21 words
The method of claim 11 wherein said disorder is synovitis, gonococcal arthritis, gout, spondylitis, or arthrosis deformans or any combination thereof.
Claim 18
Dependent Claim
14 words
The method of claim 8 wherein said admixture is an oil and water dispersion.
Claim 19
Dependent Claim
15 words
The method of claim 8 wherein said admixture further contains a vehicle for said complex.
Claim 20
Dependent Claim
19 words
The method of claim 18 wherein said vehicle comprises an emulsifier, a hydrocarbon wax, a polyhydric alcohol and water.
Claim 21
Dependent Claim
44 words
The method of claim 19 wherein said vehicle is a cream base comprising in an amount of about 11% w/w glyceryl monostearate, about 2% w/w white wax, about 3% w/w ceresin, about 4% w/w petrolatum, about 6% w/w glycerin, and about 74% w/w water.
Claim 22
Dependent Claim
10 words
The method of claim 8 wherein said admixture is oleophilic.
Claim 23
Dependent Claim
12 words
The method of claim 8 wherein said complex is disodium monocopper(II) citrate.
Claim 24
Dependent Claim
42 words
An anti-inflammatory composition containing as the active anti-inflammatory ingredient a monometal complex consisting of dialkali metal monoheavymetal chelate of an alpha or beta-hydroxy polycarboxylic acid and an acceptable vehicle wherein said composition has a pH which will not deleteriously dissociate said complex.
Claim 25
Dependent Claim
42 words
An anti-inflammatory composition containing as the active anti-inflammatory ingredient a monometal complex consisting of dialkali metal monoheavymetal chelate of an alpha or beta-hydroxy polycarboxylic acid and an acceptable vehicle wherein said composition has a pH which will not deleteriously dissociate said complex.
Claim 26
Dependent Claim
16 words
The composition of claim 23 wherein said composition has a pH in excess of about 7.
Claim 27
Dependent Claim
26 words
The composition of claim 23 wherein said complex is dispersed in a vehicle having a pH within the physiological range of about 7 to about 9.
Claim 28
Dependent Claim
13 words
The composition of claim 25 wherein said complex is dialkalimetal monocopper (II) citrate.
Claim 29
Dependent Claim
12 words
The composition of claim 26 wherein said complex is in aqueous admixture.
Claim 30
Dependent Claim
19 words
The composition of claim 27 wherein the pH range of the composition is from about 7 to about 9.
Claim 31
Dependent Claim
11 words
The composition of claim 23 wherein said metal ion is copper.
Claim 32
Dependent Claim
14 words
The oomposition of claim 27 wherein said admixture is an oil and water dispersion.
Claim 33
Dependent Claim
15 words
The composition of claim 27 wherein said admixture further contains a vehicle for said complex.
Claim 34
Dependent Claim
18 words
The composition of claim 31 wherein said vehicle comprises an emulsifier, a hydrocarbon wax, polyhydric alcohol and water.
Claim 35
Dependent Claim
18 words
The composition of claim 32 wherein said vehicle is a cream base comprising glyceryl monostearate as the emulsifier.
Claim 36
Dependent Claim
18 words
The composition of claim 32 wherein said vehicle comprises glyceryl monostearate, white wax, ceresin, petrolatum, glycerin and water.
Claim 37
Dependent Claim
10 words
The composition of claim 27 wherein said admixture is oleophilic.
Claim 38
Dependent Claim
55 words
The composition of claim 23 wherein said metal complex is contained in a dispersion of oil and water with an emulsifier agent selected from the group of anionic and nonanionic agents by providing in the aqueous phase a dialkalimetal monocopper(II) citrate in an effective anti-inflammatory amount at a pH of about 7 to about 9.
Claim 39
Dependent Claim
20 words
The composition of claim 36 wherein said dialkalimetal monocopper(II) citrate is about 5% to about 15% w/w of said composition.
Claim 40
Dependent Claim
35 words
The composition of claim 36 wherein said composition comprises disodium monocopper(II) citrate in an amount of about 10% w/w in a water-dispersable cream base vehicle comprising an oil-in-water emulsion having a pH of about 7.0.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1990-07-13 | 1991-01-12 | 1991-07-14 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-07-13 | 1995-01-12 | 1995-07-14 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-07-13 | 1999-01-12 | 1999-07-14 | $7700.00 | Window Closed / Lapsed |