Therapeutic system for sparingly soluble active ingredients

• US 4,992,278 A
• Filed: 08/03/1989
• Issued: 02/12/1991
• Est. Priority Date: 01/14/1987
• Status: Expired due to Fees

• Current Assignee: ADD Advanced Drug Delivery Technologies AG
• Original Assignee: Ciba-Geigy Corporation (Novartis Ag)
• Inventors: Khanna, Satish C.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Horne, Leon R.
• Application Number:
  US07/390,435
• Time in Patent Office: 558 Days
• Field of Search: 424/464, 424/468, 424/472, 424/473, 424/467, 424/470
• US Class Current: 424/473
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

Abstract

The present invention relates to a therapeutic system with systemic action for peroral administration, having a compartment for active ingredients, which system contains in that compartment sparingly soluble active ingredients, swelling agents and, optionally, water-soluble substances for producing an osmotic pressure.

Claims

1. Peroral therapeutic system in tablet form for continuous and controlled administration of active ingredients that are sparingly soluble in water, consisting of

(a) a casing made of a material that is permeable to water and impermeable to the components of the core containing the active ingredient,

(b) a compressed core from a granular powder of an active ingredient that is sparingly soluble in water or a mixture of such active ingredients, a hydrophilic, polymeric swelling agent consisting of a mixture of a vinylpyrrolidone/vinyl acetate copolymer with an ethylene oxide homopolymer, optionally a water-soluble substance for inducing osmosis and optionally other pharmaceutically acceptable adjuncts and

(c) a passage through the casing (a) for the transport of the constituents contained in the core into the surrounding aqueous body fluid.

2. Peroral therapeutic system in tablet form according to claim 1, consisting of

(a) a casing made of acylated cellulose, that is permeable to water and impermeable to the components of the core containing the active ingredient and to the ions contained in body fluids,

(b) a compressed core from a granular powder of an active ingredient that is sparingly soluble in water or a mixture of such active ingredients, a 1:

1 mixture (by weight) of a vinyl-pyrrolidone/vinyl acetate copolymer with an ethylene oxide homopolymer, sodium or potassium chloride for inducing osmosis and optionally other pharmaceutically acceptable adjuncts and

(c) a passage through the casing (a) for the transport of the constituents contained in the core into the surrounding aqueous body fluid.

3. Peroral therapeutic system in tablet form according to claim 1, consisting of

(a) a casing made of acylated cellulose, that is permeable to water and impermeable to the components of the core containing the active ingredient and to the ions contained in body fluids,

(b) a compressed core from a granular powder of an active ingredient that is sparingly soluble in water or a mixture of such active ingredients, a 1:

1 mixture (by weight) of a vinyl-pyrrolidone/vinyl acetate copolymer having a molecular weight of 60,000±

15,000 and a monomer ratio of approximately 60;

40 (% by weight) and an ethylene oxide homopolymer having a degree of polymerisation of from 2,000 to 100,000 and

(c) a passage through the casing (a) for the transport of the constituents contained in the core into the surrounding aqueous body fluid.

4. Peroral therapeutic system in tablet form according to claim 2 wherein said acylated cellulose is cellulose acetate.

5. Peroral therapeutic system in tablet form according to claim 2 wherein said body fluids are gastric or intestinal juices.

6. Peroral therapeutic system in tablet form according to claim 3 wherein said acylated cellulose is cellulose acetate.

7. Peroral therapeutic system in tablet form according to claim 3 wherein said body fluids are gastric or intestinal juices.