Thermoplastic material for drug coatings which dissolve in intestinal juices

• US 5,705,189 A
• Filed: 08/31/1995
• Issued: 01/06/1998
• Est. Priority Date: 08/31/1994
• Status: Expired due to Fees

• Current Assignee: Roehm GmbH Chemische Fabrik
• Original Assignee: Roehm GmbH Chemische Fabrik
• Inventors: Lehmann, Klaus, Hoess, Werner
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Spear, James M.
• Application Number:
  US08/521,738
• Time in Patent Office: 859 Days
• Field of Search: 424/462, 424/463, 424/482, 424/497, 424/451
• US Class Current: 424/451
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates
• CPC Class Codes: A61K 9/4816 Wall or shell material

Abstract

Thermoplastic materials which comprise a copolymer of

(A) 16 to 40 wt % of acrylic and/or methacrylic acid;

(B) 30 to 80 wt % of methyl acrylate; and

(C) 0 to 40 wt % of another alkyl ester of acrylic and/or methacrylic acid and perhaps conventional auxiliaries for drug coatings are suitable for the production of drug coatings which are soluble in intestinal juices, such as tablet coatings, dies, films, capsules, or multipart dosage units.

Claims

1. A thermoplastic material for the production of drug coatings, which are soluble in intestinal juices, comprising a copolymer of:

(A) 16 to 40 wt % of acrylic and/or methacrylic acid;

(B) 30 to 80 wt % of methyl acrylate; and

(C) 0 to 40 wt % of another alkyl ester of acrylic and/or methacrylic acid;

wherein said copolymer has a melt viscosity in the range of 1000 to 100,000 Pa.sec at 120°

to 145°

C. and a weight average molecular weight of 50,000 to 1,500,000 d.

2. A method for the production of a drug capsule, comprising melting a thermoplastic material which comprises a copolymer of:

(A) 16 to 40 wt % of acrylic and/or methacrylic acid;

(B) 30 to 80 wt % of methyl acrylate; and

(C) 0 to 40 wt % of another alkyl ester of acrylic and/or methacrylic acid,

to obtain a melt;

forming a film from said melt by extrusion; and

thermally shaping said film to form a capsule.

3. A method of delivering an active agent to the intestines, comprising administering to a patient in need thereof a pharmaceutical composition in which said active agent is coated with a thermoplastic material which comprises a copolymer of:

(A) 16 to 40 wt % of acrylic and/or methacrylic acid;

(B) 30 to 80 wt % of methyl acrylate; and

(C) 0 to 40 wt % of another alkyl ester of acrylic and/or methacrylic acid.

4. A weldable plastic film, comprising a thermoplastic material comprising a copolymer of:

(A) 16 to 40 wt % of acrylic and/or methacrylic acid;

(B) 30 to 80 wt % of methyl acrylate; and

(C) 0 to 40 wt % of another alkyl ester of acrylic and/or methacrylic acid;

wherein said copolymer has a melt viscosity in the range of 1000 to 100,000 Pa.sec at 120°

to 145°

C. and a weight average molecular weight of 50,000 to 1,500,000 d.

5. The weldable plastic film of claim 4, which is stretched in one or two dimensions.

6. A pharmaceutical composition, comprising an active agent coated with a thermoplastic material, wherein said thermoplastic material comprises a copolymer of:

(A) 16 to 40 wt % of acrylic and/or methacrylic acid;

(B) 30 to 80 wt % of methyl acrylate; and

(C) 0 to 40 wt % of another alkyl ester of acrylic and/or methacrylic acid;

wherein said copolymer has a melt viscosity in the range of 1000 to 100,000 Pa.sec at 120°

to 145°

C. and a weight average molecular weight of 50,000 to 1,500,000 d.

7. A drug capsule, comprising a thermoplastic material, said thermoplastic material comprising a copolymer of:

(A) 16 to 40 wt % of acrylic and/or methacrylic acid;

(B) 30 to 80 wt % of methyl acrylate; and

(C) 0 to 40 wt % of another alkyl ester of acrylic and/or methacrylic acid;

wherein said copolymer has a melt viscosity in the range of 1000 to 100,000 Pa.sec at 120°

to 145°

C. and a weight average molecular weight of 50,000 to 1,500,000 d.

8. A drug dosage unit, comprising one or more active substance dosages and at least one molded part comprising thermoplastic material, said thermoplastic material comprising a copolymer of:

(A) 16 to 40 wt % of acrylic and/or methacrylic acid;

(B) 30 to 80 wt % of methyl acrylate; and

(C) 0 to 40 wt % of another alkyl ester of acrylic and/or methacrylic acid;

wherein said copolymer has a melt viscosity in the range of 1000 to 100,000 Pa.sec at 120°

to 145°

C. and a weight average molecular weight of 50,000 to 1,500,000 d.

9. A method for coating a drug, wherein a thermoplastic material comprising a copolymer of:

(A) 16 to 40 wt % of acrylic and/or methacrylic acid;

(B) 30 to 80 wt % of methyl acrylate; and

(C) 0 to 40 wt % of another alkyl ester of acrylic and/or methacrylic acid

is melted to obtain a melt and a drug coating is molded from said melt.

10. The method of claim 9, wherein said drug coating is molded from said melt by injection molding.