Dosage form for delivering drug in short-time period

• US 5,178,867 A
• Filed: 08/19/1991
• Issued: 01/12/1993
• Est. Priority Date: 08/19/1991
• Status: Expired due to Term

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Hamel, Lawrence G., Quan, Ernest S., Guittard, George V., Carpenter, Howard A., Wong, Patrick S.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Bawa, Raj
• Application Number:
  US07/747,899
• Time in Patent Office: 512 Days
• Field of Search: 424/473
• 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 invention pertains to a dosage form for orally administering a drug in eight hours or less to the stomach and small intestine for a therapeutic result.

Claims

1. An improvement in a method for administering a drug to a patient in need of gastrointestinal therapy, wherein the method comprises:

(a) admitting orally into the gastrointestinal tract of the patient a dosage form comprising;

(1) a semipermeable wall permeable to fluid, which wall surrounds;

(2) a compartment;

(3) means in the wall for increasing fluid-passage into the dosage form, said means comprising 40 to 55% of the wall;

(4) a drug in the compartment for gastrointestinal therapy;

(5) a passageway in the wall for delivering the drug from the dosage form;

(b) letting gastrointestinal fluid enter the dosage form by (1) passing fluid through the semipermeable wall and (3) passing fluid through the means; and

wherein the improvement comprises;

(c) delivering the drug from the compartment by the combined operations of (1) and (3) in up to 8 hours to the gastrointestinal tract for the gastrointestinal therapy.

2. The improvement in a method for administering the drug to the patient in need of gastrointestinal therapy according to claim 1, wherein the method comprises administering a drug possessing histamine receptor antagonist therapy.

3. The improvement in a method for administering the drug to the patient in need of gastrointestinal therapy according to claim 1, wherein the method comprises administering a drug possessing hydrogen ion suppression therapy.

4. The improvement in a method for administering the drug to the patient in need of gastrointestinal therapy according to claim 1, wherein the method comprises administering a drug possessing anti-ulcer therapy.

5. The improvement in a method for administering the drug to the patient in need of gastrointestinal therapy according to claim 1, wherein an instant release coat comprising a gastrointestinal drug is present on the semipermeable wall.

6. The improvement in a method for administering the drug to the patient in need of gastrointestinal therapy according to claim 1, wherein the drug is cimetidine.

7. An improvement in a dosage form for delivering a drug, wherein the dosage form comprises:

(1) a semipermeable wall permeable to the passage of fluid, which wall surrounds;

(2) a compartment;

(3) a drug in the compartment;

(4) a passageway in the wall for delivering the drug form the dosage form; and

wherein the improvement comprises;

(5) means in the wall for increasing fluid-flux into the dosage form, said means comprising 40 to 55% of the wall; and

which dosage form;

(6) delivers the drug from the compartment by the combined operations of (1) the semipermeable wall permitting fluid to pass through the wall into the compartment and by (5) the means in the wall permitting fluid to pass into the compartment, whereby the drug in the compartment is delivered in up to 8 hours from the dosage form.

8. The improvement in the dosage form for delivering the drug according to claim 7, wherein the dosage form comprises 100 ng to 1500 mg of drug.

9. The improvement in the dosage form for delivering the drug according to claim 7, wherein the dosage form comprises 100 ng to 1500 mg of cimetidine.

10. The improvement in the dosage form for delivering the drug according to claim 7, wherein the dosage form comprises 100 ng to 1500 mg of a drug selected from the group consisting of ranitidine, famotidine, nizatidine, bifentidine, erbrotidine, nifentidine, roxatidine, omeprazole, and lansoprazole.

11. An improvement in a dosage form for delivering a drug, wherein the dosage form comprises:

(1) a semipermeable wall permeable to the passage of fluid that surrounds;

(2) a compartment;

(3) 100 ng to 1550 mg of a drug comprising a member selected from the group consisting of quinapril, indolapril, olindapril, rentiapril, spirapril, cilazaprilat, lisinopril, imidapril, benazeprilat, cilazapril, alacepril, captopril, delapril, fosinopril, libenzapril, pentopril, perindopril, altiopril, quinaprilat, ramipril, spiraprilat, teprotide, zofenopril, enalapril, benazepril, enalaprilat, antipain and cilastatin;

(4) an exit port in the wall for delivering the drug from the dosage form, and wherein the improvement comprises;

(5) means in the wall for increasing fluid-passage into the dosage form, said means comprising 40 to 55% of the wall; and

which dosage form;

(6) delivers the drug from the compartment by the combined operations of (1) letting fluid pass through the semipermeable wall into the compartment and by (2) the means in the wall permitting an increase of fluid passage into the compartment, whereby the drug is delivered in up to 8 hours form the dosage form.

12. An improvement in a dosage form for delivering a drug, wherein the dosage form comprises:

(1) a semipermeable wall permeable to the passage of fluid that surrounds;

(2) a compartment;

(3) 100 ng to 1500 mg of a drug in the compartment, said drug a member selected from the group consisting of amrinone, bepridil, diltiazem, felodipine, fendiline, flunarizine, nicardipine, isradipine, nifedipine, nimodipine, nisoldipine, perhexiline, amlodipine, nilvadipine, prenylamine, verapamil, nitredipine, cinnarizine, gallopamil, belfosdil, and fostedil;

(4) an exit port in the wall for delivering the drug from the dosage form, and wherein the improvement comprises;

(5) chemical means in the wall for increasing fluid-passage into the compartment, said means comprising 40 to 55% of the wall; and

which dosage form;

(6) delivers the drug (3) by the combined operation of (1) the semipermeable wall letting fluid pass through the wall into the compartment and by (5) the means in the wall permitting an increase in fluid passage into the compartment in up to 8 hours from the dosage form.

13. An improvement in a dosage form for orally delivering an anti-ulcer drug to the stomach and the small intestine to a patient, wherein the dosage form comprises:

(1) a semipermeable wall permeable to the passage of fluid which wall comprises an exterior surface;

(2) a dose of an anti-ulcer drug on the exterior surface of the wall;

(3) a compartment formed by the wall;

(4) 100 ng to 1500 mg of an anti-ulcer drug in the compartment;

(5) an exit port in the wall for delivering the drug from the dosage form, and wherein the improvement comprises;

(6) fluid-flux increasing means in the wall for increasing the volume of fluid into the dosage form, said means comprising 40 to 55% of the wall; and

which dosage form;

(7) delivers the anti-ulcer drug form the exterior wall and delivers the anti-ulcer drug from the compartment by the combined operations of (1) the semipermeable wall letting fluid pass through the wall into the compartment and by (6) the means in the wall increasing fluid flux into the compartment, in up to 8 hours to the stomach and the small intestine.

14. The improvement in a dosage form for orally administering the drug according to claim 13, wherein the anti-ulcer drug in the compartment is a histamine antagonist.

15. The improvement in a dosage form for orally administering the drug according to claim 13, wherein the dosage form comprises multiple exit ports.

16. The improvement in the dosage form for orally administering the drug according to claim 13, wherein the exterior surface comprises 10 mg to 150 mg of anti-ulcer drug.

17. The improvement in the dosage form for orally administering the drug according to claim 13, wherein the small intestine consists of a member selected from the group consisting of the duodenum, the jejunum and the ileum.

18. The improvement in the dosage form for orally administering the drug according to claim 13, wherein the quick release dose is administered in one second to one hour.

19. The improvement in the dosage form for orally administering the drug according to claim 13, wherein the drug is delivered from the compartment in thirty minutes to six hours.

20. A composition comprising:

40 to 60 wt % cellulose acylate, 40 to 55% polyvinylpyrrolidone comprising a 38,000 to 45,000 molecular weight, and 0 to 5 wt % plasticizer, which composition equals 100 wt % and is useful for manufacturing an orally administerable dosage form.

21. The composition according to claim 20, wherein the cellulose acylate is cellulose acetate.

22. A method for delivering a histamine receptor antagonist drug to an animal, wherein the method comprises:

(a) admitting into the gastrointestinal tract of the animal a dosage form comprising;

(1) a semipermeable wall permeable to the passage of fluid comprising an exterior surface;

(2) a dose of a histamine receptor antagonist drug on the exterior surface of the wall;

(3) a compartment formed by the wall;

(4) 100 ng to 1,500 mg of a histamine receptor antagonist drug in the compartment;

(5) an exit port in the wall for delivering the drug from the dosage form;

(6) fluid-flux increasing means in the wall for increasing the volume of fluid passing into the dosage form;

(b) imbibing fluid into the dosage form; and

,

(c) delivering the histamine receptor antagonist drug from the exterior surface of the wall and from the compartment in less than 8 hours to the gastrointestinal tract.

23. A method for delivering a calcium influx inhibitor drug that inhibits a transmembrane influx of calcium ions into cardiac muscles and smooth muscles, wherein the method comprises:

(a) admitting into the gastrointestinal tract of the animal a dosage form comprising;

(1) a wall comprising an exterior surface;

(2) a dose of a calcium influx inhibitor drug, in contact with the exterior surface of the wall;

(3) a compartment defined by the wall;

(4) fluid-flux increasing means in the wall for increasing the volume of fluid passing through the wall into the dosage form;

(5) 100 ng to 1,500 mg of a calcium influx inhibitor drug in the dosage form;

(6) an exit passageway in the wall for delivering the drug from the dosage form;

(b) imbibing fluid into the dosage form; and

,

(c) delivering the calcium influx inhibitor drug form the dosage form in less than 8 hours to the animal.

24. A method for delivering an angiotensin converting enzyme inhibitor to the gastrointestinal tact of an animal, wherein the method comprises:

(a) admitting into the gastrointestinal tract of the animal a dosage form comprising;

(1) a wall comprising an exterior surface;

(2) a dose of an angiotensin converting enzyme inhibitor in contact with the exterior surface of the wall;

(3) a compartment defined by the wall;

(4) fluid-flux increasing means in the wall for increasing the volume of fluid passing into the dosage form;

(5) 100 ng to 1,500 mg of an angiotensin converting enzyme inhibitor in the compartment;

(6) a passageway in the wall for delivering the drug from the dosage form;

(b) imbibing fluid into the dosage form; and

,

(c) delivering 100 ng to 1,500 mg of the angiotensin converting enzyme inhibitor in less than 8 hours form the dosage form to the animal.