Osmotic caplet

• US 6,773,721 B1
• Filed: 05/16/1995
• Issued: 08/10/2004
• Est. Priority Date: 11/02/1992
• Status: Expired due to Fees

• Current Assignee: Encinal Pharmaceutical Investments, LLC
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Wong, Patrick S.-L., Ayer, Atul D., Guittard, George V., Theeuwes, Felix
• Primary Examiner(s): Webman, Edward J.
• Application Number:
  US08/442,210
• Time in Patent Office: 3,374 Days
• Field of Search: 424/451, 424/473, 424/469-70, 424/456
• 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: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61K 9/4816 Wall or shell material
• CPC Class Codes: A61K 9/4891 Coated capsules; Multilayered drug free capsule shells with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004

Abstract

An osmotic caplet is disclosed comprising an osmotic caplet exit for delivering a preselected dose of drug to a patient in need of therapy.

Claims

1. An osmotic caplet for delivering a maximum dose of a drug to a patient, the osmotic caplet comprising:

(1) a cylinder body;

(2) a dose of 300 ng to 1,200 mg of drug in the caplet;

(3) a semipermeable wall that defines the caplet; and

, wherein the osmotic caplet is characterized by;

(4) a lead end comprising a convex surface with a passageway for substantially eliminating residual drug inside the caplet, which convex surface possesses a radius of curvature equal to but not exceeding twice the radius of the cylinder body, for maximizing the dose of drug delivered from the osmotic caplet.

2. The osmotic caplet for delivering the maximum dose of drug according to claim 1, whereas the cylinder comprises a length greater that its width.

3. The osmotic caplet for delivering, the maximum dose of drug according to claim 1, wherein the osmotic caplet is an osmotic solid caplet.

4. The osmotic caplet for delivering the maximum dose of drug according to claim 1, wherein the drug exhibits an osmotic pressure gradient across the permeable wall.

6. The osmotic caplet for delivering the maximum dose of drug according to claim 4, wherein the drug is a member selected from the group consisting of cimetidine, ranitidine, famotidine, nizatidine, bifentidine, erbrotidine, nifentidine, roxatidine, omeprazole, and lansprazole.

8. The osmotic caplet for delivering a maximum dose of drug to a patient, according to claim 6, wherein the drug in the osmotic caplet is replaced by a drug comprising a member selected from the group consisting of amrinone, bencyclone, bepridil, diltiazem, felodipine, fendiline, flunarizine, nicardipine, isradipine, nifedipine, nimodipine, nisoldipine, nitredipine, perhexiline, amlodipine, nilvadipine, prenylamine, verapamil, cinnarizine, fendiline, gallopamil, belfosdil, and fostedil.

5. An osmotic caplet for delivering a maximum dose of a drug to a patient, the osmotic caplet comprising:

(1) a cylinder body;

(2) a dose of 300 ng to 1,200 mg of drug in the osmotic caplet;

(3) an osmagent in the osmotic caplet;

(4) a semipermeable wall that defines the caplet; and

wherein the osmotic caplet is characterized by;

(5) a convex end comprising a passageway with an inside surface possessing a radius of curvature r and not exceeding 2r of the cylinder body for delivering one-hundred percent of the drug from the osmotic caplet during the drug delivery period.

7. An osmotic caplet for delivering a maximum dose of drug to a patient, said osmotic caplet comprising:

(1) a body longer in proportion to its width;

(2) a dose of 300 ng to 1,200 mg of 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;

(3) a semipermeable wall that surrounds the body; and

wherein the osmotic caplet is characterized by;

(4) an end comprising a passageway for eliminating drug entrapment inside the caplet, said end comprising a convex surface with a radius of curvature r and not exceeding 2r of the caplet body width, thereby delivering the dose of drug from the osmotic caplet.

9. An osmotic solid caplet for delivering a dose of drug to a patient, said osmotic caplet comprising:

(1) a body possessing a length in millimeters greater than its width in millimeters;

(2) a dose of 300 ng to 1,200 mg of drug in the osmotic caplet;

(3) a gelatinous coat surrounding the body;

(4) a semipermeable wall surrounding the gelatinous coat;

(5) an end comprising an inside surface that eliminates residual drug retention in the osmotic caplet, said end comprising a radius of curvature r and not exceeding 2r of the width of the caplet body; and

,

(6) a passageway in the end for delivering the drug from the osmotic caplet over a prolonged period of time.

11. The osmotic caplet for delivering a drug according to claim 9, wherein the drug is a member selected from the group consisting of acetaminophen, aspirin, ibuprofen, acyclovir, gemfibrozil, selegiline, methyldopa, carbidopa, and levodopa.

12. The osmotic caplet for delivering a drug according to claim 9, wherein a composition comprising a drug and an immediate release pharmaceutically acceptable carrier is in contact with the exterior of the semipermeable wall.

14. The osmotic caplet for delivering an antiviral drug according to claim 12, wherein the antiviral drug is a member selected from the group consisting of zidovudine, didanosine, acyclovir, and dideoxycitidine.

15. The osmotic caplet for delivering an antiviral drug according to claim 12, wherein the antiviral drug is a member selected from the group consisting of zalcitabine, fluxuridine, ribavirin, cytarabine, vidarabine, azidouridine, gancidovir, deoxynojirmycin, fiacitabine, fialuridine, fluorothymidine, foscarnet, nevirapine, staviudine, dideoxyinosine, and isoprinosine.

10. An osmotic caplet for delivering a dose of drug to a drug receiving environment, said osmotic caplet comprising:

(1) a cylinder comprising a length greater than its width in millimeters;

(2) a dose of drug in a first layer in the osmotic caplet;

(3) a push composition in a second layer in the osmotic caplet;

(4) a wall surrounding the body;

(5) an end next to the first layer integral in the permeable wall; and

(6) a passageway for delivering the drug by hydro-osmotic energy from the osmotic caplet over a prolonged period of time, and wherein the osmotic caplet is characterized by the absence of a start-up time required for drug delivery and the end possessing a radius of curvature not exceeding the radius of the body width for reducing residual drug in the caplet as the end of delivering the dose of drug.

13. An osmotic caplet for delivering a drug to a patient, said osmotic caplet comprising:

(a) a cylinder;

(b) a dose of 300 ng to 1,200 mg of an antiviral drug in the oblong body;

(c) a semipermeable wall permeable to the passage of fluid and impermeable to the passage of drug that surrounds the oblong body;

(d) a convex end for delivering a one-hundred percent dose of antiviral drug, said convex end comprising a radius of curvature not exceeding twice the radius of the oblong body for obtaining the desired effect.