Buccal delivery system

• US 6,183,775 B1
• Filed: 01/25/1999
• Issued: 02/06/2001
• Est. Priority Date: 05/13/1996
• Status: Expired due to Term

• Current Assignee: Novartis Consumer Health S.A. (Glaxosmithkline Holdings Ltd.)
• Original Assignee: Novartis Consumer Health S.A. (Glaxosmithkline Holdings Ltd.)
• Inventors: Ventouras, Kimon
• Primary Examiner(s): Azpuru, Carlos A.
• Application Number:
  US09/180,242
• Time in Patent Office: 743 Days
• Field of Search: 424/434, 424/464, 424/465, 424/468
• US Class Current: 424/465
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 27/00 Drugs for disorders of the senses
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid
• CPC Class Codes: A61P 7/12 Antidiuretics, e.g. drugs for diabetes insipidus ADH A61P5/10
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/04 : Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• CPC Class Codes: A61P 9/06 : Antiarrhythmics

Abstract

A controlled release lozenge having pleasant organoleptic properties, said lozenge consisting essentially of (a) a soluble filler which is selected from the group consisting of maltitol, xylitol, sorbitol, mannitol, lactose, dextrose, saccharose, fructose, and mixtures thereof; (b) an insoluble film forming agent which is capable of forming an insoluble matrix, said insoluble film forming agent is selected from the group consisting of a polyacrylate, ethyl cellulose, polyvinylchloride, cellulose acetate, cellulose acetate phthalate, and shellac; (c) a swellable polymer which is selected from the group consisting of xanthan gum, guar gum, alginic acid or a salt thereof, pectin, polyvinyl alcohol, polysaccharide, and cellulose derivatives; and (d) at least one active substance.

Claims

1. A controlled release lozenge having pleasant organoleptic properties, said lozenge consisting essentially of

(a) 50 to 99 weight percent, based on the total weight of the lozenge, of a soluble filler which is selected from the group consisting of maltitol, xylitol, sorbitol, mannitol, lactose, dextrose, saccharose, fructose, and mixtures thereof;

(b) 0.5 to 30 weight percent, based on the total weight of the lozenge, of an insoluble film forming agent which is capable of forming an insoluble matrix, said insoluble film forming agent is selected from the group consisting of a polyacrylate, ethyl cellulose, polyvinylchloride, cellulose acetate, cellulose acetate phthalate, shellac, and mixtures thereof;

(c) 0.5 to 30 weight percent, based on the total weight of the lozenge, of a swellable polymer which is selected from the group consisting of xanthan gum, guar gum, alginic acid or a salt thereof, pectin, polyvinyl alcohol, polysaccharide, cellulose derivatives, and mixtures thereof; and

(d) at least one active substance.

3. The lozenge according to claim 1 wherein the active ingredient is nicotine or a salt or derivative of nicotine.

4. The lozenge according to claim 3 wherein the active ingredient is nicotine tartrate.

5. The lozenge according to claim 1 which additionally contains an auxiliary.

6. The lozenge according to claim 1 wherein the active substance is selected from the group consisting of a fluoride supplement, melatonin, a mixture of benzoxonium chloride and lidocaine, an antacid, an antiemetic, an analgesic agent, an agent against dental plaque, and combinations thereof.

7. The lozenge according to claim 1 wherein the release of the active substance is substantially in a constant manner.

2. A controlled release lozenge having pleasant organoleptic properties, said lozenge consisting essentially of

(a) 55 to 95 weight percent, based on the total weight of the lozenge, of a soluble filler which is selected from the group consisting of maltitol, xylitol, sorbitol, mannitol, lactose, dextrose, saccharose, fructose, and mixtures thereof;

(b) 0.5 to 24 weight percent, based on the total weight of the lozenge, of an insoluble film forming agent which is capable of forming an insoluble matrix, said insoluble film forming agent is selected from the group consisting of a polyacrylate, ethyl cellulose, polyvinylchloride, cellulose acetate, cellulose acetate phthalate, shellac, and mixtures thereof;

(c) 0.5 to 24 weight percent, based on the total weight of the lozenge, of a swellable polymer which is selected from the group consisting of xanthan gum, guar gum, alginic acid or a salt thereof, pectin, polyvinyl alcohol, polysaccharide, and cellulose derivatives; and

(d) at least one active substance.