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EP0126580A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Vesicle formulations for the controlled release of therapeutic agents

Assignee: Nexstar Pharmaceuticals Inc
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Filing: 1984-05-08
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Granted: —
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Expires: 2004-05-08
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Abstract

Abstract Vesicle compositions provide controlled sustained release of an encapsulated therapeutic agent after parenteral administration, depending upon the difference in osmolarity between the suspending solution and the solution within the vesicles. By adjusting the concentration of the suspending sotution, the rate of release of the therapeutic agent after parenteral administration can be varied. The compositions can be effectively administered by intramuscular, subcutaneous injection or other means.

Inventors

  • 👤 Richard A. Callahan
  • 👤 George Wing-Yiu Tin

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-25 15:42
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 52 words
A composition comprising a solution of a therapeutic agent encapsulated in vesicles, the vesicles being suspended in a solution containing sufficient solute to provide an osmolarity which is at least substantially isotonic with respect to the osmolarity of the solution within the vesicles and which is of greater osmolarity than physiological saline.
Claim 2
Dependent Claim 52 words
A composition comprising a solution of a therapeutic agent encapsulated in vesicles, the vesicles being suspended in a solution containing sufficient solute to provide an osmolarity which is at least substantially isotonic with respect to the osmolarity of the solution within the vesicles and which is of greater osmolarity than physiological saline.
Claim 3
Dependent Claim 27 words
A composition according to Claim 1 wherein the osmolarity of said suspending solution is at least about 25% of the osmolarity of said solution within said vesicles.
Claim 4
Dependent Claim 23 words
A composition according to Claim 1 or Claim 2 wherein the suspending solution is hypertonic with respect to the solution within the vesicles.
Claim 5
Dependent Claim 27 words
A composition according to any one of Claims 1, 2 or 3 wherein the suspending solution is physiological saline to which has been added a second solute.
Claim 6
Dependent Claim 16 words
A composition according to Claim 4 wherein the second solute is selected from sugars and polypeptides.
Claim 7
Dependent Claim 16 words
A composition according to Claim 5 wherein the second solute is dextrose, glucose or another hexose.
Claim 8
Dependent Claim 20 words
A composition according to any one of Claims 1, 2, or 3 wherein the suspending solution is a glucose solution.
Claim 9
Dependent Claim 14 words
A composition according to any preceding claims wherein the vesicle is a phospholipid vesicle.
Claim 10
Dependent Claim 11 words
A composition according to Claim 8 wherein the vesicle is unilamellar.
Claim 11
Dependent Claim 11 words
A composition according to Claim 8 wherein the vesicle is multilamellar.
Claim 12
Dependent Claim 22 words
A composition according to any preceding claim wherein the therapeutic agent is selected from antibiotics, metabolic regulators, immune modulators and toxin antidotes.
Claim 13
Dependent Claim 17 words
A composition according to Claim 11 wherein the therapeutic agent is an antidote for a cholinesterase inhibitor.
Claim 14
Dependent Claim 11 words
A composition according to Claim 1 wherein the agent is 2-PAMCl.
Claim 15
Dependent Claim 56 words
A process for producing a composition according to any preceding claim, comprising encapsulating a solution of the agent in vesicles and suspending the vesicles in a solution containing sufficient solute to provide an osmolarity which is substantially isotonic with the solution of the therapeutic agent within the vesicles and being of greater osmolarity than physiological saline.
Claim 16
Dependent Claim 41 words
A composition as claimed in any one of Claims 1 to 14 for use in a method for treatment of the human or animal body by surgery or therapy or in a diagnostic method practised on the human or animal body.
Claim 17
Dependent Claim 41 words
Use of a composition as claimed in any one of claims 1 to 14 in a method for treatment of the human or animal body by surgery or therapy or in a diagnostic method practised on the human or animal body.
Claim 18
Dependent Claim 22 words
A composition as claimed in Claim 15 or use as claimed in Claim 16 wherein the treatment is administration of toxin antidote.

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