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Method and system for the controlled release of biologically active substances to a body fluid

Assignee: Rockefeller University
•
Filing: 1979-07-31
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Granted: 1982-09-07
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Expires: 1999-07-31
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Abstract

Abstract A process and system for controlled delivery of a biologically active substance to an animal body fluid which comprises contacting fluid with a reversible complex of a conjugate (1) and a binding macromolecule (2), wherein the conjugate (1) comprises a biologically active portion which is intended to be proportionately released into a body fluid stream in response to varying concentration levels of a component of the body fluid stream, and a complexing substrate portion which conjugates with the biologically active portion and which is characterized by affinity to the binding macromolecule (2), competitively or non-competitively with the variable component of the body fluid; thereby causing the component present in the body fluid to complex to the binding macromolecule and thus releasing the conjugate (1) therefrom into the fluid. The process and system are particularly applicable for the glucose-controlled release of insulin and other hypoglycemic agents in the treatment of diabetes.

Inventors

  • 👤 Michael Brownlee
  • 👤 Anthony Cerami

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-24 10:02
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/16; A61K38/17; A61K38/22; A61K38/28; A61K47/00; A61K47/50; A61K47/51; A61K47/62; A61K47/64; A61K47/6415; A61M; A61M31/00; A61M31/002; A61P; A61P3/00; A61P3/08

Claims Analysis

Total Claims: 17
Claim 1
Independent Claim 73 words
A process of treating hyperglycemia which comprises: delivering to a glucose containing human body fluid a reversible complex of (1) a hypoglycemically active insulin analogue which is a conjugate between a carbohydrate and an insulin and (2) a lectin having affinity for glucose and for the carbohydrate portion of said conjugate (1); thereby causing the glucose present in said fluid to complex to said lectin and to release said conjugate into said fluid.
Claim 2
Dependent Claim 73 words
A process of treating hyperglycemia which comprises: delivering to a glucose containing human body fluid a reversible complex of (1) a hypoglycemically active insulin analogue which is a conjugate between a carbohydrate and an insulin and (2) a lectin having affinity for glucose and for the carbohydrate portion of said conjugate (1); thereby causing the glucose present in said fluid to complex to said lectin and to release said conjugate into said fluid.
Claim 3
Dependent Claim 11 words
The process of claim 1 wherein said lectin is Concanavalin A.
Claim 4
Dependent Claim 10 words
The process of claim 1 wherein said carbohydrate is maltose.
Claim 5
Dependent Claim 21 words
The process of claim 1 wherein said reversible complex comprises at least two conjugates of different affinity towards said lectin (2).
Claim 6
Dependent Claim 19 words
The process of claim 1 wherein said reversible complex comprises at least two conjugates with different hypoglycemically active portions.
Claim 7
Dependent Claim 16 words
The process of claim 5 wherein said two different hypoglycemically active portions are guanosine and insulin.
Claim 8
Dependent Claim 19 words
The process of claim 1 wherein said carbohydrate is a manno-oligosaccharide containing from 2 to 7 (1→2) α-D-mannopyranosyl residues.
Claim 9
Dependent Claim 47 words
A controlled release medication which comprises: a hypoglycemically active amount of a reversible complex of (1) a hypoglycemically active insulin analogue which is a conjugate between a carbohydrate and an insulin and (2) a lectin having affinity for glucose and for the carbohydrate portion of said conjugate.
Claim 10
Dependent Claim 47 words
A controlled release medication which comprises: a hypoglycemically active amount of a reversible complex of (1) a hypoglycemically active insulin analogue which is a conjugate between a carbohydrate and an insulin and (2) a lectin having affinity for glucose and for the carbohydrate portion of said conjugate.
Claim 11
Dependent Claim 12 words
The medication system of claim 8 wherein said lectin is Concanavalin A.
Claim 12
Dependent Claim 11 words
The medication system of claim 8 wherein said carbohydrate is maltose.
Claim 13
Dependent Claim 22 words
The medication system of claim 8 wherein said reversible complex comprises at least two conjugates (1) having different affinity towards said lectin.
Claim 14
Dependent Claim 20 words
The medication system of claim 8 wherein said reversible complex comprises at least two conjugates with different hypoglycemically active portions.
Claim 15
Dependent Claim 20 words
The medication system of claim 8 wherein said carbohydrate is a manno-oligosaccharide containing from 2 to 7 (1→2) α-D-mannopyranosyl residues.
Claim 16
Dependent Claim 25 words
The process of claim 1 wherein said insulin/carbohydrate conjugate is such that not all three primary amino groups of insulin are substituted by said carbohydrate.
Claim 17
Dependent Claim 25 words
The medication of claim 8 wherein said insulin/carbohydrate conjugate is such that not all three primary amino groups of insulin are substituted by said carbohydrate.

References Cited (Backward Citations)

US4003792A Cited
US3847890A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1985-09-06 1986-03-08 1986-09-07 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1989-09-06 1990-03-08 1990-09-07 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1993-09-06 1994-03-08 1994-09-07 $7700.00 Window Closed / Lapsed

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