Patent US4996193A successfully refreshed from Google Patents.
US4996193A
Expired / Lapsed
US
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Combined topical and systemic method of administration of cyclosporine
Assignee: University of California
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Filing: 1989-03-03
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Granted: 1991-02-26
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Expires: 2009-03-03
Abstract
Abstract The present invention provides formulations for the topical application of cyclosporin to skin tissue for treatment of autoimmune, T-cell mediated immune disease, and inflammatory conditions, and for producing prolonged skin allograft survival and wound healing. In addition, methods for the use of said formulations--in tandem with systemic applications of cyclosporin or without same--are suggested. The present invention also suggests alternative formulations and delivery systems for the efficacious treatment of the aforementioned conditions, and further suggests a model with which formulations may be tested.
Inventors
- 👤 Charles W. Hewitt
- 👤 Kirby S. Black
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 05:13
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0014; A61K38/00; A61K38/04; A61K38/12; A61K38/13; A61P; A61P37/00; A61P37/02; A61P37/06
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
50 words
A method for treating T-cell mediated immune processes, allograft rejection, inflammations, autoimmune conditions or cyclosporin-responsive conditions in animals, comprising: topically applying a formulation containing cyclosporin in pharmaceutically effective amounts to the affected tissue; and systemically administering a formulation containing cyclosporin in pharmaceutically effective amounts in conjunction with said topical application.
Claim 2
Independent Claim
50 words
A method for treating T-cell mediated immune processes, allograft rejection, inflammations, autoimmune conditions or cyclosporin-responsive conditions in animals, comprising: topically applying a formulation containing cyclosporin in pharmaceutically effective amounts to the affected tissue; and systemically administering a formulation containing cyclosporin in pharmaceutically effective amounts in conjunction with said topical application.
Claim 3
Dependent Claim
30 words
A method according to claim 1, further comprising: initiating said systemic administration prior to said administration of topical cyclosporin, and discontinuing said systemic administration prior to discontinuing said topical administration.
Claim 4
Dependent Claim
36 words
A method according to claim 1, further comprising: initiating said systemic administration at a first dosage level prior to initiating said topical administration, and lowering said systemic dosage to a second level during said topical administration.
Claim 5
Dependent Claim
76 words
A method according to claim 2 or 3, wherein the topically-applied formulation comprises from about 0.2% to 25% cyclosporin by weight, and is applied to the tissue in such an amount that from about 0.5 mg/cm 2 to 5 mg/cm 2 of cyclosporin is applied per single dose, and further, wherein the systemically-applied cyclosporin-containing formulation is applied in such an amount that from about 1 mg/kg/day to 15 mg/kg/day of cyclosporin is applied per single dosage.
Claim 6
Dependent Claim
19 words
A method according to claim 4, wherein the topically-applied formulation contains from about 0.5% to 15% cyclosporin, by weight.
Claim 7
Dependent Claim
31 words
A method according to claim 5, wherein the topically-applied formulation containing cyclosporin further comprises one or more of the following: a pharmaceutical carrier; a co-solvent; a penetration enhancer; and an emulsifier.
Claim 8
Dependent Claim
75 words
A method according to claim 6, wherein the pharmaceutical carrier is a solvent, diluent, or carrier selected from the group consisting of waxes, cellulose derivatives, mineral oils, vegetable oils, petroleum derivatives, water, methylcellulose or paraffin, beeswax, glyceryl stearate, PEG-2 stearate, propylene glycol stearate, glycol stearate, cetyl alcohol, steryl alcohol and other similar agents, anhydrous lanolin, white petrolatum, liquid petrolatum, olive oil, ethanol, ethanolpolysorbate 80 solutions, propylene glycol-water solutions, and jojoba oils, and any mixture thereof.
Claim 9
Dependent Claim
47 words
A method according to claim 6, wherein the co-solvent is selected from the group consisting of ethanol; oleyl alcohol; alkylene polyols; glycerol; polyethylene glycol; oleic acids; vegetable oil PEG-6 complexes; caprylrc triglyceride; capric triglyceride; glyceryl caprylate; glyceryl caprate; PEG-8 caprylate; PEG-8 caprate; ethoxydiglycol; and any mixture thereof.
Claim 10
Dependent Claim
48 words
A method according to claim 6, wherein the penetration enhancer is selected from the group consisting of ethanol; oleyl alcohol; alkylene polyols; oleic acids; urea; pyrrolidones; surfactants; vegetable oil PEG-6 complexes; caprylic triglyceride; capric trrglyceride; glyceryl caprylate; glyceryl caprate; PEG-8 caprylate; PEG-8 caprate; ethoxydiglycol; and any mixture thereof.
Claim 11
Dependent Claim
51 words
A method according to claim 6, wherein the emulsifier is selected from a group consisting of PEG stearate and glycol stearate, PEG-6-32-stearate; PEG-6 stearate; polysorbate 80, sodium lauryl sulfate, potassium methyl sulfate, potassium butyl sulfate, sodium tetrapropylene benzene sulfonate, dodecyl trimethyl ammonium chloride, lauric diethanolamide, cetrimide, cetomacrogol, and any mixture thereof.
Claim 12
Dependent Claim
13 words
A method according to claim 6, wherein the topical formulation is an ointment.
Claim 13
Dependent Claim
13 words
A method according to claim 6, wherein the topical formulation is a paste.
Claim 14
Dependent Claim
13 words
A method according to claim 6, wherein the topical formulation is a gel.
Claim 15
Dependent Claim
13 words
A method according to claim 6, wherein the topical formulation is a cream.
Claim 16
Dependent Claim
13 words
A method according to claim 6, wherein the topical formulation is a liquid.
Claim 17
Dependent Claim
13 words
A method according to claim 15, wherein the topical formulation is a spray.
Claim 18
Dependent Claim
34 words
A method according to claim 6, wherein the topical formulation comprises, in approximate amounts by weight: a. 5-80% pharmaceutical carrier; b. 5-50% co-solvent; c. 1-5% penetration enhancer; d. 0.1-20% emulsifier; and e. 0.2-25% cyclosporin.
Claim 19
Dependent Claim
13 words
A method according to claim 17, wherein the cyclosporin is Cyclosporine A powder.
Claim 20
Independent Claim
72 words
A method for inducing acceptance of organ or tissue transplants by an animal host organism, comprising: a. systemically administering a formulation containing cyclosporin in pharmaceutically effective amounts, to the host organism; b. topically administering a formulation containing cyclosporin in pharmaceutically effective amounts to the transplanted or grafted tissue or organ, subsequent to said systemic treatment; and c. continuing the topical administration until the graft or transplant has been accepted by the host.
Claim 21
Independent Claim
72 words
A method for inducing acceptance of organ or tissue transplants by an animal host organism, comprising: a. systemically administering a formulation containing cyclosporin in pharmaceutically effective amounts, to the host organism; b. topically administering a formulation containing cyclosporin in pharmaceutically effective amounts to the transplanted or grafted tissue or organ, subsequent to said systemic treatment; and c. continuing the topical administration until the graft or transplant has been accepted by the host.
Claim 22
Dependent Claim
27 words
A method according to claim 19, further comprising: initiating said system administration at the time of allografting and discontinuing said systemic administration once wound healing has occurred.
Claim 23
Dependent Claim
15 words
A method according to claim 1 or claim 19, wherein said animal is a mammal.
Claim 24
Dependent Claim
12 words
A method according to claim 21, wherein said mammal is a human.
References Cited (Backward Citations)
US3288824A
Cited
US4108985A
Cited
US4210581A
Cited
US4117118A
Cited
US4289851A
Cited
US4220641A
Cited
US4388307A
Cited
US4288431A
Cited
US4396542A
Cited
US4554351A
Cited
US4384996A
Cited
US4857662A
Cited
US4639434A
Cited
US4553974A
Cited
US4681754A
Cited
US4703033A
Cited
US4771122A
Cited
US4649047A
Cited
US4677968A
Cited
US4764503A
Cited
GB2207678A
Cited
US4839342A
Cited
JPH0219513A
Cited
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