Cholesterol matrix delivery system for sustained release of macromolecules
AssigneeSyntex (U.S.A.) Inc.
InventorJohn S. Kent
Life of this patent
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Abstract
Delivery systems for releasing macromolecular active agents to a body site at a controlled rate for a prolonged period of time, comprising a cholesteric matrix permeable to passage of the macromolecular active agent by diffusion, are disclosed. The cholesteric matrix comprises cholesterol powder and cholesterol prills optionally in combination with a binding agent and a lubricating agent. The macromolecular active agent is dispersed throughout the matrix; macromolecules suitable for release from this delivery system have molecular weights of about 1300 to about 75,000 and are at least very slightly soluble in water.
Claims21
A diffusional matrix delivery system for administering a macromolecular active agent at a controlled rate for a prolonged period of time to an animal body site capable of making available its intracellular and/or extracellular fluid for transfer into the system, said system comprising 90.0-99.9%, by weight, of a matrix composed of, by weight:
- (a) 20-80% cholesterol powder;
- (b) 20-80% cholesterol prills having diameters of 100-1200 microns;
- (c) 0.1-5.0% biocompatible binding agent;
- and
- (d) 0.1-5.0% biocompatible lubricating agent, in which is dispersed, by weight,
- (e) 0.1-10.0% macromolecular active agent,
- wherein the matrix contains a plurality of micropores which are substantially permeable to the passage by diffusion of the macromolecular active agent, and said macromolecular active agent has a molecular weight between 10,000 and 400,000 and is at least ery slightly water soluble.
A method of administering a pharmaceutically acceptable macromolecular active agent to an animal at a controlled rate for a prolonged period of time which method comprises placing a delivery system shaped, sized and adapted for placement in an animal body site capable of making available its intracellular and/or extracellular fluid for transfer into the system, wherein said delivery system is a matrix which comprises, by weight:
- (a) 20-80% cholesterol powder;
- (b) 20-80% cholesterol prills having diameters of 100-1200 microns;
- (c) 0.1-5.0% biocompatible binding agent;
- and
- (d) 0.1-5.0% biocompatible lubricating agent, in which is dispersed, by weight:
- (e) 0.1-10.0% macromolecular active agent,
- wherein said matrix contains a plurality of micropores which are substantially permeable to the passage by diffusion of the macromolecular active agent, and said macromolecular active agent has a molecular weight between 10,000 and 400,000 and is at least very slightly water soluble.
Dependencies are inferred from the claim text.