Gastric remaining preparation, swollen molding, and production process

• US 6,312,726 B1
• Filed: 02/20/1996
• Issued: 11/06/2001
• Est. Priority Date: 08/20/1993
• Status: Expired due to Fees

• Current Assignee: Nippon Shinyaku Company Limited
• Original Assignee: Nippon Shinyaku Company Limited
• Inventors: Izumi, Shougo, Nakamichi, Kouichi, Yasuura, Hiroyuki
• Primary Examiner(s): Kulkosky, Peter F.
• Application Number:
  US08/591,682
• Time in Patent Office: 2,086 Days
• Field of Search: 424/484, 424/487, 424/488
• US Class Current: 424/487
• CPC Class Codes: A61K 9/0065 Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus

Abstract

A gastric remaining preparation having a configuration entirely different from that of the conventional ones. It comprises a swollen molding having a mesh-like cross-section and an apparent density of less than 1, containing an acid-resistant polymer compound as a predominant component as well as at least an auxiliary blowing agent and a drug substance. The molding can be produced by using a multi-screw extruder.

Claims

1. An extruded expanded gastric molding for a sustained release preparation comprising an extruded pharmaceutically acceptable acid resistant polymer or co-polymer which is capable of being expanded into a microfine porous structure, as a predominant component comprising at least 25% by weight of the molding, and a pharmaceutical drug substance, with said polymer compound having been physically reacted with sufficient auxiliary blowing agent, during extrusion of the polymer compound and the drug substance;

to provide said microfine porous structure with a mesh-like cross section in the extruded molding and an apparent density of less than 1, whereby the microfine porous molding is capable of floating on gastric fluids for sustained release of the pharmaceutical drug substance.

2. A swollen molding according to claim 1 wherein said acid-resistant polymer or co-polymer is a pH-dependent coating agent polymer or a pH-independent coating agent polymer.

3. A swollen molding according to claim 1 wherein said acid-resistant polymer is selected from the group consisting of hydroxypropylmethylcellulose acetate succinate, hydroxypropylmethyl cellulose phthalate, methacrylic copolymer, carboxymethylethylcellulose, cellulose acetate phthalate, ethylcellulose, and aminoalkyl methacrylate copolymer.

4. A swollen molding according to claim 1 wherein said acid-resistant polymer is selected from the group consisting of hydroxypropylmethylcellulose acetate succinate, hydroxypropylmethyl cellulose phthalate, methacrylic copolymer, carboxymethylethylcellulose, cellulose acetate phthalate, ethylcellulose, and aminoalkyl methacrylate copolymer and said auxilary blowing agent is selected from the group consisting of dried aluminum hydroxide gel, synthetic aluminosilicate, calcium hydrogen phosphate, calcium carbonate, precipitated calcium carbonate, calcium hydrogen carbonate, and talc.

5. A method of producing the swollen molding of claim 1 characterized in that all the components thereof and water are processed in a lump using a multi-screw extruder.

6. A method according to claim 5 wherein said multi-screw extruder is a twin-screw extruder.

7. A sustained release preparation comprising the swollen molding of claim 1.

8. The gastric molding of claim 1 wherein the microfine porous structure comprises a porosity of from about 61.2% to about 88.8% a mean pore diameter of from about 10 μ

m to about 20 μ

m.