264 results about "Cyclosporins" patented technology

Stable solutions of lipophilic drugs, such as cyclosporin, forming a polar lipid self-emulsifying drug delivery system. The solutions can include lipophilic drugs, such as cyclosporin, dissolved in a polar lipid, such as having a C₆-C₁₂ fatty acid monoglyceride content of at least about 50%, surfactants and triglycerides. The composition forms a fine emulsion on exposure to water. The encapsulated dosage form of this composition needs neither a hydrophilic component nor air-tight blister packaging, and is particularly suitable for oral administration.

Drug eluting coating compositions are composed of at least one therapeutic agent dispersed in modified, biologically active binders. The therapeutic agents included in the coating composition are paclitaxel, sirolimus, tacrolimus, everolimus, actinomycin-D, dexamethasone, mycophenolic acid, cyclosporins, estradiol, and derivatives and analogs thereof. These therapeutic agents are applied to the surface of the medical device by a modified, biologically active binders. By using these biologically active binders, the therapeutic agents can be applied to at least one surface of a medical implant without using inert polymer carriers.

A pharmaceutical composition comprising a cyclosporin solid-state microemulsion is disclosed. In a preferred embodiment, the composition comprises a cyclosporin microemulsion dispersed in an enteric carrier. The composition does not dissolve in external phases such as artificial gastric fluid, but dissolves rapidly in artificial intestinal fluid, whereby it releases the cyclosporin microemulsion, providing rapid delivery of cyclosporin. The composition effectively maintains a therapeutic blood concentration of cyclosporin with once a day dosing, providing for convenience of administration and avoiding adverse effects induced by increasing peak blood cyclosporin concentrations associated with conventional cyclosporin formulations.

A topical ophthalmic formulation in the form of an aqueous solution comprising a cyclosporin, hyaluronic acid or one of its salts, and polysorbate 80 is described.

A composition is disclosed herein comprising from about 0.001% to about 0.4% cyclosporin A, castor oil, and a surfactant selected from the group consisting of alcohol ethoxylates, alcohols, alkyl glycosides, alkyl polyglycosides, alkylphenol ethoxylates, amine oxides, block polymers, carboxylated alcohol or alkylphenol ethoxylates, carboxylic acids/fatty acids, cellulose derivatives, ethoxylated alcohols, ethoxylated alkylphenols, ethoxylated aryl phenols, ethoxylated fatty acids, ethoxylated fatty acids, ethoxylated fatty esters and oils, fatty alcohols, fatty esters, glycol esters, lanolin-based derivatives, lecithin and lecithin derivatives, lignin and lignin derivatives, methyl esters, monoglycerides and derivatives , phosphalipids, polyacrylic acids, polyethylene glycols, polyethylene oxide-polypropylene oxide copolymers, polyethylene oxides, polymeric surfactants, polypropylene oxides, propoxylated alcohols, propoxylated alkyl phenols, propoxylated fatty acids, protein-based surfactants, sarcosine derivatives, silicone-based surfactants, sorbitan derivatives, stearates, sucrose and glucose esters and derivatives, and combinations thereof.

A liquid comprising a therapeutically effective concentration of a cyclosporin and a vitamin E tocopherol polyethylene glycol succinate, wherein said liquid is an aqueous solution, and wherein no hydrophilic organic solvent is present at a concentration greater than half of that of the cyclosporin is also disclosed herein. A composition comprising a therapeutically effective concentration of cyclosporin A and an effective amount of a vitamin E tocopherol polyethylene glycol succinate, wherein said composition is an aqueous liquid solution which is intended for ophthalmic use, and wherein no hydrophilic organic solvent is present at a mass concentration greater than or equal to that of the cyclosporin, is disclosed herein. A composition comprising a therapeutically effective concentration of cyclosporin A and an effective amount of a vitamin E tocopherol polyethylene glycol succinate, wherein said composition is an aqueous liquid solution which is intended for parenteral use, and wherein no hydrophilic organic solvent is present at a mass concentration greater than or equal to that of the cyclosporin, is disclosed herein. Methods of treating diseases or conditions using said compositions, and medicaments related thereto, are also disclosed herein.

Berberine or pharmaceutically acceptable salts thereof either alone or in combination with cyclosporin can be used to treat or prevent graft vs. host disease. Berberine or pharmaceutically acceptable salts thereof can also be used to treat or prevent septic shock syndrome.

The compounds of the present invention are represented by Formula I, as shown below:

or a pharmaceutically acceptable salt thereof,

• • with X, R₀, R₁, and R₂ defined herein.

A novel cyclosporine formulation, which is a pro-nanodispersion at room temperature, featuring solid particles of a relatively large particle size (at least about 150 nm) and yet which is a nanodispersion at body temperature.

This invention pertains to the formulation of small-particle suspensions of anticonvulsants and antidementia, particularly carbamazepine, for pharmaceutical use. This invention also pertains to the formulation of small-particle suspensions of immunosuppressive agents, particularly cyclosporin, for pharmaceutical use.

This invention relates to combinations comprising 3-[(R)-2-(N,N-dimethylamino)ethylthio-Sar]-4-(gammahydroxymethylleucine)cyclosporine, or a pharmaceutically acceptable salt, solvate or hydrate thereof; and certain nucleoside analogues, and their use in the treatment of hepatitis C virus.

The present invention discloses a topical scalp and transdermal preparation with excellent penetration to the skin and follicle, containing a [γ-hydroxy-N-methyl-L-leucine⁴] cylosporin derivative which is a non-immunosuppressive component with hair growth stimulating ability. The topical scalp and transdermal preparation is prepared by incorporating the cyclosporin derivative into a liposome, microcapsule, micro-sphere, composite particle or emulsion, capable of being employed as a hair growth stimulating agent and applied for the prevention of hair loss.

The present invention relates to methods of treating or preventing an inflammatory or immune disorder in a subject while eliminating or reducing the toxicity associated with the administration of cyclosporin A, comprising systemically administering to said subject a pharmaceutical composition comprising a therapeutically effective amount of at least one compound of Formula (I) or a pharmaceutically acceptable salt, ester or prodrug thereof, in combination with a pharmaceutically acceptable carrier or excipient:

in Formula (I), the formula for residue A is:

The present invention relates to a cyclosporin analog of the following formula (I) or its pro-drug or pharmaceutically acceptable salt:

In formula I, the formula for residue A is:

where X and Y are defined according to the claimed invention the present invention also relates to pharmaceutical compositions comprising pro-drugs or pharmaceutically acceptable salts of the compounds of the present invention and the use thereof for treating an inflammatory or immune disorder in a subject need of such treatment.

An oral cyclosporin composition comprises minicapsules having a core containing a cyclosporin, especially cyclosporin A in a solubilised liquid form. The minicapsules have a release profile to release the pre-solubilised cyclosporin, at least in the colon. The composition may be used for treating a range of intestinal diseases [FIG. 10].

Pharmaceutical compositions, which enable high absorption when administered orally, and which comprise a cyclosporin or cyclosporin derivative dissolved in a solvent-surfactant system further comprising a hydrophilic surfactant and a lipophilic surfactant, with minimal quantities of solvents.

A formulation for the administration of a cyclosporin. This formulation features a hydrophilic solvent which is characterized by being a lower alkyl ester of hydroxyalkanoic acid; and a surfactant, preferably a combination of a surfactant with a high HLB (hydrophilic/lipophilic balance) of at least about 8 and a surfactant with a low HLB of less than about 5. Other ingredients are optional, such as a fatty acid ester such as tricaprin, a phospholipid, and an ethoxylated fat such as Cremophor or another similar substance. Optionally, the ethoxylated fat is substituted for the surfactant. The preferred particle size of the resultant formulation is less than about 100 nm, more preferably less than about 60 nm, and most preferably from about 5 nm to about 50 nm. The formulation of the present invention is characterized by having high bioavailability.

A composition is disclosed herein comprising from about 0.001% to about 0.4% cyclosporin A, castor oil, and a surfactant selected from the group consisting of alcohol ethoxylates, alcohols, alkyl glycosides, alkyl polyglycosides, alkylphenol ethoxylates, amine oxides, block polymers, carboxylated alcohol or alkylphenol ethoxylates, carboxylic adds/fatty acids, cellulose derivatives, ethoxylated alcohols, ethoxylated alkylphenols, ethoxylated aryl phenols, ethoxylated fatty acids, ethoxylated fatty acids, ethoxylated fatty esters and oils, fatty alcohols, fatty esters, glycol esters, lanolin-based derivatives, lecithin and lecithin derivatives, lignin and lignin derivatives, methyl esters, monoglycerides and derivatives, phosphalipids, polyacrylic acids, polyethylene glycols, polyethylene oxide-polypropylene oxide copolymers, polyethylene oxides, polymeric surfactants, polypropylene oxides, propoxylated alcohols, propoxylated alkyl phenols, propoxylated fatty acids, protein-based surfactants, sarcosine derivatives, silicone-based surfactants, sorbitan derivatives, stearates, sucrose and glucose esters and derivatives, and combinations thereof.

A liquid comprising a therapeutically effective concentration of a cyclosporin and a vitamin E tocopherol polyethylene glycol succinate, wherein said liquid is an emulsion. is disclosed herein. Methods of treating diseases or conditions using said compositions, and medicaments related thereto, are also disclosed herein.