US4452775A
Expired / Lapsed
US
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Cholesterol matrix delivery system for sustained release of macromolecules
Assignee: Syntex USA LLC
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Filing: 1982-12-03
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Granted: 1984-06-05
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Expires: 2002-12-03
Abstract
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.
Inventors
- 👤 John S. Kent
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 13:41
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2013; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/12
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
131 words
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.
Claim 2
Dependent Claim
131 words
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.
Claim 3
Dependent Claim
38 words
The delivery system of claim 1 wherein the matrix is composed of, by weight: (a) 40-60% cholesterol powder; (b) 40-60% cholesterol prills having diameters of 200-800 microns; (c) 0.1-1.0% biocompatible binding agent; and (d) 0.5-1.5% biocompatible lubricating agent.
Claim 4
Dependent Claim
38 words
The delivery system of claim 1 wherein the matrix is composed of, by weight: (a) 48-52% cholesterol powder; (b) 48-52% cholesterol prills having diameters of 420-710 microns; (c) 0.4-0.6% biocompatible binding agent; and (d) 0.8-1.0% biocompatible lubricating agent.
Claim 5
Dependent Claim
13 words
The delivery system of claim 1 wherein the active agent is a protein.
Claim 6
Dependent Claim
13 words
The delivery system of claim 1 wherein the active agent is a polypeptide.
Claim 7
Dependent Claim
12 words
The delivery system of claim 5 wherein the polypeptide has hormonal activity.
Claim 8
Dependent Claim
15 words
The delivery system of claim 6 wherein the active agent is a mammalian growth hormone.
Claim 9
Dependent Claim
14 words
The delivery system of claim 7 wherein the active agent is bovine growth hormone.
Claim 10
Dependent Claim
14 words
The delivery system of claim 7 wherein the active agent is porcine growth hormone.
Claim 11
Dependent Claim
14 words
The delivery system of claim 8 wherein the active agent is human growth hormone.
Claim 12
Dependent Claim
12 words
The delivery system of claim 6 wherein the active agent is insulin.
Claim 13
Independent Claim
144 words
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.
Claim 14
Independent Claim
144 words
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.
Claim 15
Dependent Claim
28 words
The method of claim 12 wherein the delivery system is an implant which is sized, shaped and adapted for placement in the subcutaneous space of a warm-blooded animal.
Claim 16
Dependent Claim
29 words
The method of claim 13 wherein the active agent is a member selected from the group consisting of bovine growth hormone, porcine growth hormone, human growth hormone and insulin.
Claim 17
Dependent Claim
28 words
The method of claim 12 wherein the delivery system is an implant which is sized, shaped and adapted for placement in the intraperitoneal space of a warm-blooded animal.
Claim 18
Dependent Claim
23 words
The method of claim 12 wherein the delivery system is an implant which is sized, shaped and adapted for placement in the eye.
Claim 19
Dependent Claim
23 words
The method of claim 12 wherein the delivery system is an insert which is sized, shaped, and adapted for placement in the eye.
Claim 20
Dependent Claim
23 words
The method of claim 12 wherein the delivery system is an insert which is sized, shaped and adapted for placement in the vagina.
Claim 21
Dependent Claim
21 words
The method of claim 12 wherein the delivery system is an insert sized, shaped and adapted for placement in the uterus.
Claim 22
Dependent Claim
23 words
The method of claim 12 wherein the delivery system is an insert which is sized, shaped and adapted for placement in the anus.
Claim 23
Dependent Claim
22 words
The method of claim 12 wherein the delivery system is an insert sized, shaped and adapted for placement in the nasal passages.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-06-05 | 1987-12-05 | 1988-06-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-06-05 | 1991-12-05 | 1992-06-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-06-05 | 1995-12-05 | 1996-06-05 | $7700.00 | Window Closed / Lapsed |