Osmotic medicament releasing system

• US 6,294,201 B1
• Filed: 04/25/2000
• Issued: 09/25/2001
• Est. Priority Date: 10/25/1997
• Status: Expired due to Term

• Current Assignee: Bayer Intellectual Property GmbH (Bayer AG)
• Original Assignee: Bayer AG
• Inventors: Chantraine, Ernst, Kanikanti, Ranga-Rao, Bosché, Patrick, Weisemann, Claus, Eisele, Michael, Brendel, Erich, Kettelhoit, Stefan
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): TRAN, SUSAN T
• Application Number:
  US09/530,158
• Time in Patent Office: 518 Days
• Field of Search: 424/464, 424/473, 424/484, 424/486, 424/488, 424/469
• US Class Current: 424/473
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 Antihypertensives

Abstract

This invention relates to an orally administered osmotic drug release system that consists of a shell and a core containing a pharmaceutically active substance, as well as a process for its production. The invention relates further to an osmotic drug release system for use as a drug in human beings and animals, as well as the use of the osmotic drug release system in the production of a drug for the treatment and/or prevention of illnesses in human beings and animals.

Claims

1. Osmotic drug release system comprising:

(a) a shell comprising a material that is water-permeable but inpermeable to the components of the core, with at least one opening, and

(b) a core, comprising

15 to 35% in weight of a pharmaceutically active substance

20 to 50% in weight of xanthan

10 to 30% in weight of a vinyl pyrrolidone—

vinyl acetate copolymer

wherein additional components selected from a group consisting of other hydrophilic expandable polymers, osmotically active additives and pharmaceutically acceptable additive materials may also be contained in said core so that the sum of the core components totals 100% in weight, wherein the percent in weight figures refer to the total weight of the core components.

2. Osmotic drug release system according to claim 1, which includes a core comprising:

(a) 20 to 30% in weight of a pharmaceutically active substance

(b) 25 to 40% in weight xanthan

(c) 10 to 20% in weight of a vinyl pyrrolidone—

vinyl acetate copolymer

wherein additional components selected from a group consisting of other hydrophilic expandable polymers, osmotically active additives and pharmaceutically acceptable additive materials may also be contained in said core so that the sum of the core components totals 100% in weight, wherein the percent in weight figures refer to the total weight of the core components.

3. Osmotic drug release system according to claim 1 characterized in that the core contains at least one osmotically active additive.

4. Osmotic drug release system according to claim 1 characterized in that the core contains at least one osmotically active additive, as well as at least one pharmaceutically acceptable additive material.

5. Osmotic drug release system according to claim 1 which includes a core comprising:

20 to 30% in weight of a pharmaceutically active substance

25 to 40% in weight of xanthan

10 to 20% in weight of a vinyl pyrrolidone—

vinyl acetate copolymer

10 to 30% in weight of an osmotically active substance

8 to 20% in weight of at least one pharmaceutically acceptable additive material with the percent in weight figures referring to the total weight of the core components, and the sum of the core components totaling 100%.

6. Osmotic drug release system according to claim 1 characterized in that the active ingredient is a sparingly soluble active substance.

7. Osmotic drug release system according to claim 1 characterized in that the active ingredient is an active substance which is still absorbed in the colon.

8. Osmotic drug release system according to claim 1 characterized in that the active ingredient is a dihydropyridine.

9. Osmotic drug release system according to claim 1 characterized in that the active ingredient is nifedipine.

10. Osmotic drug release system according to claim 1 characterized in that the osmotically active additive is sodium chloride.

11. Osmotic drug release system according to claim 1 characterized in that the pharmaceutically acceptable additive material is selected from the group consisting of pharmaceutically acceptable buffer materials, pharmaceutically acceptable lubricants, pharmaceutically acceptable disintegrants, and pharmaceutically acceptable tablet-making process materials.

12. Osmotic drug release system according to claim 11, characterized in that the pharmaceutically acceptable buffer material is sodium bicarbonate, the pharmaceutically acceptable lubricant is magnesium stearate, the pharmaceutically acceptable disintegrant agent is sodium carboxy methyl starch, and a pharmaceutically acceptable tablet-making process material.

13. Osmotic drug release system according to claim 1 which includes a core comprising:

19 to 23% in weight of a pharmaceutically active substance

28 to 32% in weight of xanthan

15 to 20% in weight of a vinyl pyrrolidone—

vinyl acetate copolymer

15 to 20% in weight of sodium chloride

5 to 7% in weight of sodium bicarbonate

6 to 9% in weight of sodium carboxy methyl starch

<

1% in weight of magnesium stearate

with the percent in weight figures referring to the total weight of the core components, and the sum of the core, components totaling 100%.

14. Osmotic drug release system according to claim 1 characterized in that it is present in tablet form.

15. Procedure for the production of the osmotic drug release system according to claim 1 characterized in that the components of the core are mixed together, possible wet-granulated or dry-granulated, and made into tablets, and that the resulting core is coated with the shell.

16. Osmotic drug release system according to claim 1 for use as a drug in human beings and animals.

17. A method of treating high blood pressure, coronary heart disease, or cerebral performance disorders, and for therapy of neurological deficits following subarachnoid hemorrhage, comprising administering to a patient in need thereof an osmotic drug release system according to claim 1.