Sustained delivery formulations of rapamycin compounds
First Claim
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1. An implant formed in situ comprising:
- (a) a biocompatible, biodegradable, substantially water insoluble thermoplastic polymer and(b) rapamycin or a rapamycin derivative;
wherein the implant has a solid monolithic structure, wherein the implant is located in the intravitreal region of a mammal, affixed to the sclera of the eye, wherein the implant has a microporous matrix, the matrix being a core surrounded by a skin, wherein the core and skin are composed of the biocompatible, biodegradable, substantially water insoluble thermoplastic polymer and wherein the implant is surrounded by body tissue.
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Abstract
The present invention relates to a rapamycin sustained release delivery system for treatment of diseases responsive to rapamycin. The sustained release delivery system of the invention includes a flowable composition containing rapamycin or a rapamycin derivative, which is capable of providing an implant containing the rapamycin or derivative thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid and rapamycin or a rapamycin derivative.
129 Citations
19 Claims
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1. An implant formed in situ comprising:
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(a) a biocompatible, biodegradable, substantially water insoluble thermoplastic polymer and (b) rapamycin or a rapamycin derivative; wherein the implant has a solid monolithic structure, wherein the implant is located in the intravitreal region of a mammal, affixed to the sclera of the eye, wherein the implant has a microporous matrix, the matrix being a core surrounded by a skin, wherein the core and skin are composed of the biocompatible, biodegradable, substantially water insoluble thermoplastic polymer and wherein the implant is surrounded by body tissue. - View Dependent Claims (3, 4, 5, 6, 7, 8, 9, 13, 15, 16, 17, 18, 19)
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2. An implant precursor formed in situ comprising:
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(a) a biodegradable, biocompatible thermoplastic polymer that is at least substantially insoluble in aqueous medium, water or body fluid; (b) a biocompatible organic liquid in which the thermoplastic polymer is soluble; and (c) rapamycin or a rapamycin derivative; wherein the biocompatible organic liquid is N-methyl-2-pyrrolidone, 2-pyrrolidone, N, N-dimethylformamide, dimethyl sulfoxide, propylene carbonate, caprolactam, triacetin, or any combination thereof;
wherein the implant precursor is located in the intravitreal region of a mammal, affixed to the sclera of the eye, and the implant precursor has a solid or gelatinous microporous matrix, the matrix being a core surrounded by a skin, wherein the core and skin are composed of the biodegradable, biocompatible thermoplastic polymer and wherein the implant precursor is surrounded by body tissue. - View Dependent Claims (10, 11, 12, 14)
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Specification