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Last Updated: March 18, 2024

Claims for Patent: 4,892,739


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Summary for Patent: 4,892,739
Title: Osmotic continuous dispensing oral delivery system containing a pharmaceutically acceptable active agent having a improved core membrane adhesion properties
Abstract:An osmotic dispensing delivery system suitable for oral administration, containing a pharmaceutically acceptable active agent for the controlled continuous release of about 50 to about 90 percent by weight of said active agent into the gastrointestinal tract at a rate of about 5 to about 12 percent by weight of said agent per hour consisting essentially of: (a) a shaped solid core containing an osmotically active composition comprising an effective amount of a pharmaceutically acceptable active agent, alone or in combination with a pharmaceutically acceptable binder, an osmotically active driving agent, or tabletting lubricant, or mixtures thereof; (b) said core being substantially evenly coated with a discrete layer of a water-soluble, or water-dispersible, and water permeable substantially non-osmotically active solid polymeric binder, said binder layer being present in an amount between about 0.3 percent and about 10 percent of the weight of the core; (c) a semi-permeable shaped wall member impermeable to said active composition and permeable to gastrointestinal fluid, surrounding and adhesively bonded to the binding layer; and (d) at least one passageway in the wall, for dispensing the active agent, in communication with said core and the external environment.
Inventor(s): Shah; Shailesh B. (Union, NJ), Koparkar; Arun D. (Westfield, NJ)
Assignee: Ciba-Geigy Corporation (Ardsley, NY)
Application Number:07/185,564
Patent Claims: 1. An osmotic dispensing oral delivery system containing a moderately water-soluble pharmaceutically active agent a B -blocker wherein upon activation in the gastrointestinal tract of the host, from about 60 up to about 90 percent of said active agent is delivered at a substantially continuous rate of about 5 to about 12 percent by weight of the total weight of said active agent, per hour, comprising:

(a) a semipermeable shaped wall membrane substantially impermeable to said pharmaceutically active agent and permeable to gastrointestinal fluid;

(b) a discrete layer within said wall membrane of a water-soluble or water dispersible but water permeable substantially non-osmotically active solid polymeric binder in an amount of from 0.3 to 10% by weight based on a core;

(c) said core within and defined by said discrete binder layer, said core being in the form of a solid osmotically active composition comprising about 5 to about 20 percent by weight of a tableting binder; 0 up to about 10 percent by weight of a tableting lubricant; 0 up to 80% by weight of an osmotically active driving agent; and the remainder said pharmaceutically active agent all based upon the total core composition weight; and

(d) at least one passageway in said wall in communication with said core and the external environment for dispensing said active agent into said gastrointestinal tract.

2. The system of claim 1 wherein the .beta.-blocker is metoprolol or a salt thereof.

3. The system of claim 2, wherein the .beta.-blocker is a metoprolol salt.

4. The system of claim 3 wherein the metoprolol salt is metoprolol fumarate.

5. A system according to claim 1, wherein the wall membrane consists essentially of cellulose acetate.

6. A system according to claim 1, wherein the core contains between about 25 and about 500 mg of metoprolol base as a salt.

7. The system of claim 6 wherein the core contains 30 to 400 mg of metoprolol base as a salt.

8. A system according to claim 1, wherein the core contains between about 1 and about 5 weight percent of tableting lubricant.

9. A system according to claim 8, wherein the tabletting lubricant is magnesium stcarate.

10. The system of claim 1 wherein the tabletting binder is hydroxypropyl methylcellulose or polyvinylpyrrolidone or mixtures thereof.

11. The system of claim 1 wherein the polymeric binder in the discrete layer of polymeric binder is hydroxypropylmethylcellulose, polyvinylpyrrolidone or mixtures thereof and 0% up to a total of 50% of polyethyleneglycol.

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