US4990337A
Expired / Lapsed
US
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Cyclosporin formulations of mono or diglyceride fatty acid
Assignee: Novartis AG
•
Filing: 1990-04-12
•
Granted: 1991-02-05
•
Expires: 2010-04-12
Abstract
Abstract Cyclosporins are useful immunosuppressive, anti-fungal and antiphlogistic agents which are relatively insoluble in water and aqueous fluids (including body fluids). They may be rendered more soluble or dispersible in aqueous media by first dissolving them in at least one mono- or di- glyceride of a C 6 -C 10 fatty acid, and the resulting solution can then easily be emulsified in water or an aqueous fluid.
Inventors
- 👤 Kozo Kurihara
- 👤 Masaru Murano
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 12:02
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K38/00; A61K38/04; A61K38/12; A61K38/13; A61K9/00; A61K9/10; A61K9/107; A61K9/1075
Claims Analysis
Total Claims: 66
Claim 1
Independent Claim
34 words
A pharmaceutical composition comprising at least one cyclosporin in admixture with an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin.
Claim 2
Dependent Claim
34 words
A pharmaceutical composition comprising at least one cyclosporin in admixture with an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin.
Claim 3
Dependent Claim
16 words
The composition of claim 1, wherein said fatty acid has from 8 to 10 carbon atoms.
Claim 4
Dependent Claim
13 words
The composition of claim 1, wherein said fatty acid has 8 carbon atoms.
Claim 5
Dependent Claim
41 words
The composition of claim 1, wherein said fatty acid is at least one acid selected from the group consisting of caproic acid, 4-methylpentanoic acid, enanthic acid, 5-methylhexanoic acid, 2-ethylhexanoic acid, caprylic acid, 6-methylheptanoic acid, pelargonic acid, capric acid and 8-methylnonanoic acid.
Claim 6
Dependent Claim
27 words
The composition of claim 1, wherein said fatty acid is at least one acid selected from the group consisting of caproic acid, caprylic acid and capric acid.
Claim 7
Dependent Claim
11 words
The composition of claim 1, wherein said glyceride is a diglyceride.
Claim 8
Dependent Claim
11 words
The composition of claim 2, wherein said glyceride is a diglyceride.
Claim 9
Dependent Claim
11 words
The composition of claim 3, wherein said glyceride is a diglyceride.
Claim 10
Dependent Claim
11 words
The composition of claim 4, wherein said glyceride is a diglyceride.
Claim 11
Dependent Claim
20 words
The composition of claim 1, wherein the weight ratio of the glyceride to the cyclosporin is from 1:0.1 to 1:1.
Claim 12
Dependent Claim
20 words
The composition of claim 1, wherein the weight ratio of the glyceride to the cyclosporin is from 1:0.1 to 1:0.5.
Claim 13
Dependent Claim
20 words
The composition of claim 1, wherein the weight ratio of the glyceride to the cyclosporin is from 1:0.25 to 1:0.5.
Claim 14
Dependent Claim
41 words
A pharmaceutical composition comprising an oily solution or aqueous emulsion of at least one cyclosporin in admixture with an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin.
Claim 15
Dependent Claim
41 words
A pharmaceutical composition comprising an oily solution or aqueous emulsion of at least one cyclosporin in admixture with an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin.
Claim 16
Dependent Claim
16 words
The composition of claim 13, wherein said fatty acid has from 8 to 10 carbon atoms.
Claim 17
Dependent Claim
13 words
The composition of claim 13, wherein said fatty acid has 8 carbon atoms.
Claim 18
Dependent Claim
41 words
The composition of claim 13, wherein said fatty acid is at least one acid selected from the group consisting of caproic acid, 4-methylpentanoic acid, enanthic acid, 5-methylhexanoic acid, 2-ethylhexanoic acid, caprylic acid, 6-methylheptanoic acid pelargonic acid, capric acid and 8-methylnonanoic acid.
Claim 19
Dependent Claim
27 words
The composition of claim 13, wherein said fatty acid is at least one acid selected from the group consisting of caproic acid, caprylic acid and capric acid.
Claim 20
Dependent Claim
11 words
The composition of claim 13, wherein said glyceride is a diglyceride.
Claim 21
Dependent Claim
11 words
The composition of claim 14, wherein said glyceride is a diglyceride.
Claim 22
Dependent Claim
11 words
The composition of claim 15, wherein said glyceride is a diglyceride.
Claim 23
Dependent Claim
11 words
The composition of claim 16, wherein said glyceride is a diglyceride.
Claim 24
Dependent Claim
20 words
The composition of claim 13, wherein the weight ratio of the glyceride to the cyclosporin is from 1:0.1 to 1:1.
Claim 25
Dependent Claim
20 words
The composition of claim 13, wherein the weight ratio of the glyceride to the cyclosporin is from 1:0.1 to 1:0.5.
Claim 26
Dependent Claim
20 words
The composition of claim 13, wherein the weight ratio of the glyceride to the cyclosporin is from 1:0.25 to 1:0.5.
Claim 27
Dependent Claim
16 words
The composition of claim 13, wherein the concentration of cyclosporin is from 0.1 to 500 mg/ml.
Claim 28
Dependent Claim
14 words
The composition of claim 25, wherein said concentration is from 0.2 to 200 mg/ml.
Claim 29
Dependent Claim
23 words
The composition of claim 13, wherein non-aqueous components are present in amounts of about 50% by weight or less of the whole composition.
Claim 30
Dependent Claim
21 words
The composition of claim 13, wherein non-aqueous components are present in amounts of about 25% or less of the whole composition.
Claim 31
Independent Claim
52 words
A method of suppressing the mammalian immune system by administering to a mammal an oily solution or aqueous emulsion comprising an effective amount of at least one cyclosporin in association with sufficient of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid to dissolve said cyclosporin.
Claim 32
Independent Claim
52 words
A method of suppressing the mammalian immune system by administering to a mammal an oily solution or aqueous emulsion comprising an effective amount of at least one cyclosporin in association with sufficient of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid to dissolve said cyclosporin.
Claim 33
Dependent Claim
13 words
The method of claim 29, wherein said fatty acid has 8 carbon atoms.
Claim 34
Dependent Claim
27 words
The method of claim 29, wherein said fatty acid is at least one acid selected from the group consisting of caproic acid, caprylic acid and capric acid.
Claim 35
Dependent Claim
11 words
The method of claim 31, wherein said glyceride is a diglyceride.
Claim 36
Dependent Claim
20 words
The method of claim 29, wherein the weight ratio of the glyceride to the cyclosporin is from 1:0.1 to 1:1.
Claim 37
Dependent Claim
21 words
The method of claim 29, wherein the pharmaceutical composition is employed in the form of an oily solution or aqueous emulsion.
Claim 38
Dependent Claim
16 words
The method of claim 34, wherein the concentration of cyclosporin is from 0.1 to 500 mg/ml.
Claim 39
Dependent Claim
23 words
The method of claim 34, wherein non-aqueous components are present in amounts of about 50% by weight or less of the whole composition.
Claim 40
Independent Claim
53 words
A method of treating the ocular symptoms of Behcet's Syndrome by administering to the eye of a mammal a composition comprising an effective amount of at least one cyclosporin in association with sufficient of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid to dissolve said cyclosporin.
Claim 41
Independent Claim
53 words
A method of treating the ocular symptoms of Behcet's Syndrome by administering to the eye of a mammal a composition comprising an effective amount of at least one cyclosporin in association with sufficient of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid to dissolve said cyclosporin.
Claim 42
Dependent Claim
27 words
The method of claim 37, wherein said fatty acid is at least one acid selected from the group consisting of caproic acid, caprylic acid and capric acid.
Claim 43
Dependent Claim
11 words
The method of claim 38, wherein said glyceride is a diglyceride.
Claim 44
Dependent Claim
20 words
The method of claim 37, wherein the weight ratio of the glyceride to the cyclosporin is from 1:0.1 to 1:1.
Claim 45
Dependent Claim
21 words
The method of claim 37, wherein the pharmaceutical composition is employed in the form of an oily solution or aqueous emulsion.
Claim 46
Dependent Claim
16 words
The method of claim 41, wherein the concentration of cyclosporin is from 0.1 to 500 mg/ml.
Claim 47
Dependent Claim
23 words
The method of claim 41, wherein non-aqueous components are present in amounts of about 50% by weight or less of the whole composition.
Claim 48
Dependent Claim
46 words
A pharmaceutical composition in the form of a non-irritating oily solution or aqueous emulsion and comprising at least one cyclosporin in admixture with an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin.
Claim 49
Dependent Claim
46 words
A pharmaceutical composition in the form of a non-irritating oily solution or aqueous emulsion and comprising at least one cyclosporin in admixture with an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin.
Claim 50
Dependent Claim
27 words
The composition of claim 44, wherein said fatty acid is at least one acid selected from the group consisting of caproic acid, caprylic acid and capric acid.
Claim 51
Dependent Claim
11 words
The composition of claim 44, wherein said glyceride is a diglyceride.
Claim 52
Dependent Claim
54 words
A pharmaceutical composition in the form of a non-irritating oily solution or aqueous emulsion and comprising at least one cyclosporin of which a major proportion is cyclosporin A in admixture with an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin.
Claim 53
Dependent Claim
54 words
A pharmaceutical composition in the form of a non-irritating oily solution or aqueous emulsion and comprising at least one cyclosporin of which a major proportion is cyclosporin A in admixture with an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin.
Claim 54
Dependent Claim
27 words
The composition of claim 47, wherein said fatty acid is at least one acid selected from the group consisting of caproic acid, caprylic acid and capric acid.
Claim 55
Dependent Claim
11 words
The composition of claim 47, wherein said glyceride is a diglyceride.
Claim 56
Independent Claim
51 words
A method of suppressing the mammalian immune system by the oral administration to a mammal of a composition comprising an effective amount of at least one cyclosporin in association with sufficient of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid to dissolve said cyclosporin.
Claim 57
Independent Claim
51 words
A method of suppressing the mammalian immune system by the oral administration to a mammal of a composition comprising an effective amount of at least one cyclosporin in association with sufficient of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid to dissolve said cyclosporin.
Claim 58
Dependent Claim
13 words
The method of claim 50, wherein said fatty acid has 8 carbon atoms.
Claim 59
Dependent Claim
27 words
The method of claim 50, wherein said fatty acid is at least one acid selected from the group consisting of caproic acid, caprylic acid and capric acid.
Claim 60
Dependent Claim
11 words
The method of claim 52, wherein said glyceride is a diglyceride.
Claim 61
Dependent Claim
20 words
The method of claim 50, wherein the weight ratio of the glyceride to the cyclosporin is from 1:0.1 to 1:1.
Claim 62
Dependent Claim
21 words
The method of claim 50, wherein the pharmaceutical composition is employed in the form of an oily solution or aqueous emulsion.
Claim 63
Dependent Claim
16 words
The method of claim 55, wherein the concentration of cyclosporin is from 0.1 to 500 mg/ml.
Claim 64
Dependent Claim
23 words
The method of claim 55, wherein non-aqueous components are present in amounts of about 50% by weight or less of the whole composition.
Claim 65
Dependent Claim
42 words
A pharmaceutical composition in which a solution of at least one cyclosporin in an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin is emulsified in an aqueous medium.
Claim 66
Dependent Claim
42 words
A pharmaceutical composition in which a solution of at least one cyclosporin in an amount of at least one mono- or di- glyceride of a C 6 -C 10 fatty acid sufficient to dissolve the cyclosporin is emulsified in an aqueous medium.
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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) | 1994-02-04 | 1994-08-06 | 1995-02-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-02-04 | 1998-08-06 | 1999-02-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-02-04 | 2002-08-06 | 2003-02-05 | $7700.00 | Window Closed / Lapsed |