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EP0190969A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Lipid osmotic pump

Assignee: Merck and Co Inc
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Filing: 1986-01-29
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Granted: —
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Expires: 2006-01-29
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Abstract

Abstract The instant invention is directed to a lipid osmotic pump, comprising: (A) a core, comprising: (i) a beneficial amount of at least one substantially water insoluble active agent which is lipid soluble and/or lipid wettable; (ii) a sufficient amount of at least one water immiscible lipid carrier, which is liquid at the temperature of intended use, to dissolve and/or suspend said active agent; and (iii) a sufficient amount of at least one osmotic agent to ensure release of said lipid carrier from the pump; and (B) surrounded by a water insoluble wall: (i) having a thickness of about 1 to 1000 microns; (ii) which is preferentially wetted by said lipid carrier over an aqueous solution of said osmotic agent; (iii) having a water permeability of about 1 x 10 -18 to 4 x 10 -15 cm 3 sec/g; (iv) prepared from at least one polymer permeable to water but substantially impermeable to said osmotic agent; and (v) having a means for said active agent and lipid carrier to be released through said water insoluble wall.

Inventors

  • 👤 Gordon L. Amidon
  • 👤 Jennifer B. Dressman
  • 👤 Takeru Higuchi

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-23 12:12
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5036; A61K9/5042; A61K9/0002; A61K9/0004

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 168 words
A lipid osmotic pump, comprising: (A) a core, comprising: (i) a beneficial amount of at least one substantially water insoluble active agent which is lipid soluble and/or lipid wettable; (ii) a sufficient amount of at least one water immiscible lipid carrier, which is liquid at the temperature of intended use, to dissolve and/or suspend said active agent; and (iii) a sufficient amount of at least one osmotic agent to ensure release of said lipid carrier from the pump; and (B) surrounded by a water insoluble wall: (i) having a thickness of about 1 to 1000 microns; (ii) which is preferentially wetted by said lipid carrier over an aqueous solution of said osmotic agent; (iii) having a water permeability of about 1 x 10 -18 to 4 x 10 -15 cm 3 sec/ g ; (iv) prepared from at least one polymer permeable to water but substantially impermeable to said osmotic agent; and (v) having a means for said active agent to be released through said water insoluble wall.
Claim 2
Dependent Claim 168 words
A lipid osmotic pump, comprising: (A) a core, comprising: (i) a beneficial amount of at least one substantially water insoluble active agent which is lipid soluble and/or lipid wettable; (ii) a sufficient amount of at least one water immiscible lipid carrier, which is liquid at the temperature of intended use, to dissolve and/or suspend said active agent; and (iii) a sufficient amount of at least one osmotic agent to ensure release of said lipid carrier from the pump; and (B) surrounded by a water insoluble wall: (i) having a thickness of about 1 to 1000 microns; (ii) which is preferentially wetted by said lipid carrier over an aqueous solution of said osmotic agent; (iii) having a water permeability of about 1 x 10 -18 to 4 x 10 -15 cm 3 sec/ g ; (iv) prepared from at least one polymer permeable to water but substantially impermeable to said osmotic agent; and (v) having a means for said active agent to be released through said water insoluble wall.
Claim 3
Dependent Claim 36 words
The lipid osmotic pump of Claim 1, wherein said means for said active agent to be released through said water insoluble wall is a hole connecting said core with the exterior of said water insoluble wall.
Claim 4
Dependent Claim 31 words
The lipid osmotic pump of Claim 1, wherein said water insoluble wall is microporous and, thus, provides a means for said active agent to be released through said water insoluble wall.
Claim 5
Dependent Claim 33 words
The lipid osmotic pump of Claim 1, wherein said microporous, water impermeable, wall is made by dispersing throughout said wall 5 to 100 parts of pore forming additive per 150 parts wall polymer.
Claim 6
Dependent Claim 35 words
The lipid osmotic pump of Claim 4, wherein said pore forming additive is selected from the group consisting of alkali metal salts, alkaline earth metal salts, transition metal salts, organic acids, saccharides, and organic polyols.
Claim 7
Dependent Claim 43 words
The lipid osmotic pump of Claim 3, wherein said microporous, water insoluble, wall is made by a process selected from the group consisting of etched nuclear tracking, solvent evaporation gas formation, cold stretching, hot stretching, solvent leaching, ion exchange reaction, and polyelectrolyte processes.
Claim 8
Dependent Claim 43 words
The lipid osmotic pump of Claim 1, wherein said water insoluble wall is comprised of at least two different polymer layers with the polymer closest to the core being preferentially wetted by said lipid carrier over an aqueous solution of said osmotic agent.
Claim 9
Dependent Claim 16 words
The lipid osmotic pump of Claim 1, wherein said lipid carrier is a liquid at 37°C.
Claim 10
Dependent Claim 37 words
The lipid osmotic pump of Claim 1, wherein said lipid carrier is selected from the group consisting of triglycerides, cocoa butter, hard butter, mineral oil, petrolatum-mineral oil mixtures, saqualine, fluorocarbons, fatty acids, their esters and mixtures thereof.
Claim 11
Dependent Claim 37 words
The lipid osmotic pump of Claim 1, wherein said polymer used to prepare said water insoluble wall is selected from the group consisting of cellulose acetate, cellulose diacetate, cellulose triacetate, cellulose acetate propionate, and cellulose acetate butyrate.

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