Polymer-based, sustained release drug delivery system
First Claim
Patent Images
1. A sustained-release formulation comprising:
- at least one granule comprising a therapeutically effective amount of at least one agent, anda polymer matrix coating the at least one agent, wherein the at least one agent has a rate of release from the formulation that is limited primarily by the rate at which the at least one agent dissolves into the matrix.
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Abstract
Disclosed is a sustained release system that includes a polymer and a pharmaceutically active agent dispersed in the polymer. The agent is in granular or particulate form, and has a rate of release from the system that is limited primarily by the rate at which the agent dissolves from the granules into the polymer matrix. Advantageously, the polymer is permeable to the agent and is non-release-rate-limiting with respect to the rate of release of the agent from the polymer.
62 Citations
62 Claims
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1. A sustained-release formulation comprising:
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at least one granule comprising a therapeutically effective amount of at least one agent, and a polymer matrix coating the at least one agent, wherein the at least one agent has a rate of release from the formulation that is limited primarily by the rate at which the at least one agent dissolves into the matrix. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 60, 61, 62)
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22-55. -55. (canceled)
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56. A sustained-release formulation comprising:
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a plurality of granules comprising a therapeutically effective amount of a codrug, and a polymer matrix, wherein the polymer matrix is essentially non-release rate limiting with respect to the rate of release of the codrug from the matrix. - View Dependent Claims (59)
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57. A sustained-release formulation comprising:
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a polymer matrix surrounded by physiological tissue, and a plurality of granules comprising a therapeutically effective amount of a codrug dispersed in said matrix, wherein the granules have a surface area that is at least partially exposed to the surrounding tissue, and wherein the release rate of the codrug from the formulation is proportional to the exposed surface area of the granules.
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58. A sustained-release formulation comprising:
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a plurality of granules comprising a therapeutically effective amount of a codrug having a form selected from I, Ia, II, IIa, III, and IIIa, below,
A1*(-L-A2*)n
(I)
A1*(-A2*)n
(Ia)
A1-L-A2*
(II)
A1*-A2*
(IIa)
A2*-L-A1*-L-A2*
(III)
A2*-A1*-A2*
(IIIa),Wherein A1* is a residue of a first biologically active compound A1, A2* is a residue of a second biologically active compound A2, L is a linking group selected from a direct bond and a divalent organic linking group, and n is an integer having a value of from 1 to 4; and a polymer matrix, coating the codrug, wherein at least one biologically active compound has a rate of release from the formulation that is limited primarily by the rate at which that biologically active compound dissolves into the matrix.
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Specification