TH4209A - New pharmaceutical preparation - Google Patents

Abstract

Controlled-release drug formulations consist of numerous beads with metoprolol salt as the main soluble component; methods for their production and therapeutic use in cardiovascular disorders.

Claims (16)

1. A procedure for preparing a controlled-release drug of metoprolol that continuously releases the active ingredient for at least 15 hours, regardless of the pH of the gastrointestinal tract, is unique because numerous beads containing at least 95% w/w of metoprolol salt as the active ingredient, with a solubility of less than 600 mg/ml in water at 25°C, are spray-encapsulated with a membrane-forming solution. This creates a polymer membrane composed of a proton-depositing cellulose derivative. This method yields a drug that releases the active ingredient at a rate of 3-7% w/w/hour. 2. The process described in claim 1 is unique because the size of these beads is in the range of 0.25 - 2 mm. 3. The process under claim 2 is unique because the size of these beads is in the range of 0.35 - 1.0 mm. 4. The process under claim 1 is unique because the beads have a porosity of less than 15%. 5. The process under claim 1 is unique because the salt of mitoprolol has a solubility of 30 - 600 mg/ml. 6. The process under claim 5 is unique because this salt is formed from a carboxylic organic acid. 7. The process under claim 6 is unique because the salt of metoprolol is a succinate or fumarate of the resinous metoprolol. 8. The process under claim 6 is unique because this methoprolol sulfate is a benzoate or sorbate of the S-enantiomer of methoprolol. 9. The process under claim 1 is unique because this uncoated bead has a strong mitoprolol salt on an insoluble core. 10. The process under claim 9 is unique because the non-dissolving core, which has a size of 0.1 - 1.0 mm, should have a size of 0.15 - 0.3 mm. 11. The process under claim 9 is unique because the insoluble core has a size of 0.15 - 0.3 mm and is coated with a methoprolol salt, resulting in beads with a size of 0.35 - 1.0 mm which are coated with a polymer membrane. 12. The process under claim 1 is unique because the uncoated beads, with a size of 0.35 - 1.0 mm, consist of methoprolol salts and are coated with a polymer membrane. 13. The process under claim 1 is unique because this polymer membrane consists of ethyl cellulose. 14. The process under claim 1 is unique because the polymer membrane consists of ethyl cellulose combined with hydroxypropylmethyl cellulose. 15. A procedure for the manufacture of a finished pharmaceutical product consisting of a controlled-release drug under patent 1, which is unique because the coated beads are enclosed in a hard gelatin capsule. 16. A process for the manufacture of a finished pharmaceutical product consisting of a controlled-release drug in accordance with Patent 1, which is characterized by the moving beads combined with pharmaceutical fillers being compressed into flat, spherical tablets that disintegrate into coated beads upon initial contact with gastric and intestinal fluids (Patent 16, 3 pages, 3 figures).