Sustained Release Dosage Forms For Delivery of Agents to an Oral Cavity of a User

• US 20090081291A1
• Filed: 09/26/2007
• Published: 03/26/2009
• Est. Priority Date: 09/26/2007
• Status: Abandoned Application

• Current Assignee: Bennes Incorporated
• Original Assignee: Bennes Incorporated
• Inventors: Ross, Benjamin F., Gin, Jerry B.
• Application Number:
  US11/904,420
• Publication Number:
  US 20090081291A1
• Time in Patent Office: Days
• US Class Current: 424/468
• CPC Class Codes: A61K 2800/5422 nonionic
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/185 Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids hydroxamic acids A61K31/16; peroxy acids A61K31/327
• CPC Class Codes: A61K 31/34 having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
• CPC Class Codes: A61K 31/40 having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/555 containing heavy metals, e.g. hemin, hematin, melarsoprol
• CPC Class Codes: A61K 31/60 Salicylic acid; Derivatives thereof
• CPC Class Codes: A61K 33/30 Zinc; Compounds thereof
• CPC Class Codes: A61K 36/534 Mentha (mint)
• CPC Class Codes: A61K 36/54 Lauraceae (Laurel family), e.g. cinnamon or sassafras
• CPC Class Codes: A61K 36/61 Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
• CPC Class Codes: A61K 36/752 Citrus, e.g. lime, orange or lemon
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 8/02 characterised by special physical form
• CPC Class Codes: A61K 8/731 Cellulose; Quaternized cellulose derivatives
• CPC Class Codes: A61K 8/922 of vegetable origin
• 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: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61Q 11/00 : Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Abstract

Aspects of the invention include a sustained release dosage form that can be administered to an oral cavity, e.g., the mouth. In certain embodiments, the sustained release dosage form is formulated as a lozenge or gum that may be administered to an oral cavity of a user for the purpose of dissolving over a prolonged period of time and thereby delivering an essential oil component therein. In certain embodiments, the sustained release dosage form includes a beneficial agent and, therefore, not only provides for the prolonged delivery of an essential oil component to an oral cavity, but also provides for the sustained release of a beneficial agent thereto. In certain embodiments, the sustained release dosage form includes a biocompatible, water-insoluble polymer, e.g., ethylcellulose and an essential oil component, which are combined in such a manner so as to produce a dosage form that substantially dissolves over a prolonged period of time when positioned within an aqueous environment, such as an oral cavity of a user. In certain embodiments, the sustained release dosage form may include an additional water soluble agent, such as gum arabic, which may be included so as to further provide the dosage form with a desired dissolution characteristic. In certain embodiments, the dosage form may also include a beneficial agent to be delivered to the mouth. Methods of formulating such dosage forms and administering them to an oral cavity for the treatment of an adverse condition are also provided herein.

Claims

1. A sustained release lozenge, comprising a gradually dissolving matrix, wherein the matrix comprises:

(a) an essential oil component, and

(b) a water-insoluble polymer;

wherein, in an aqueous environment, the matrix substantially dissolves, over a prolonged period of time.

2. The sustained release lozenge according to claim 1, wherein the essential oil component comprises an essential oil, a constituent of an essential oil, or a mixture thereof.

3. The sustained release lozenge of claim 2, wherein the lozenge comprises an essential oil comprising an oil selected from the group consisting of:

a citrus oil, lemon oil, lime oil, neroli oil, orange oil, a mint oil, peppermint oil, spearmint oil, anise oil, cardamom oil, cinnamon oil, clove oil, coriander oil, eucalyptus oil, fennel oil, lemongrass oil, nutmeg oil, eriodictyon fluid extract, glycyrrhiza extract, and combinations thereof.

4. The sustained release lozenge of claim 2, wherein the lozenge comprises a constituent of an essential oil comprising a terpene, a sesquiterpene, or combinations thereof.

5. The sustained release lozenge of claim 1, wherein the water-insoluble polymer comprises ethylcellulose.

6. The sustained release lozenge according to claim 5, wherein the ethylcellulose comprises a solution viscosity in the range of about 41 cP to 110 cP.

7. The sustained release lozenge according to claim 6, wherein the ethylcellulose comprises a solution viscosity in the range of about 90 cP to 110 cP.

8. The sustained release lozenge of claim 1, wherein the water-insoluble polymer comprises a substantially uniform particle size.

9. The sustained release lozenge of claim 1, wherein the water-insoluble polymer comprises an average particle size diameter in the range of about 1 micron to about 250 microns.

10. The sustained release lozenge of claim 1, wherein the water-insoluble polymer dissolves entirely over a prolonged period of time.

11. The sustained release lozenge of claim 1, wherein the water-insoluble polymer dissolves without breaking down into pieces.

12. The sustained release lozenge of claim 1, wherein the water-insoluble polymer comprises a solubility in water of less than 5 weight %.

13. The sustained release lozenge of claim 1, wherein the weight ratio of the water-insoluble polymer to essential oil component is in the range of about 2:

1 to 4;

1.

14. The sustained release lozenge of claim 1, wherein the combined weight % of the water-insoluble polymer and the essential oil component comprises from about 25 to about 100% weight % of the lozenge.

15. The sustained release lozenge of claim 1, wherein the dissolution of the lozenge occurs over a period of about 15 minutes to about 6 hours.

16. The sustained release lozenge of claim 1, wherein the dissolution of the lozenge results in the gradual release of the essential oil component.

17. The sustained release lozenge of claim 1, further comprising a water-soluble agent.

18. The sustained release lozenge of claim 17, wherein the water-soluble agent comprises a solubility in water that is greater than or equal to 5 weight %.

19. The sustained release lozenge of claim 17, wherein the water-soluble agent comprises a substantially uniform particle size.

20. The sustained release lozenge of claim 17, wherein the weight ratio of the water-insoluble polymer to water-soluble agent is in the range of about 2:

1 to 5;

1.

21. The sustained release lozenge of claim 17, wherein the water-soluble agent comprises gum arabic.

22. The sustained release lozenge of claim 21, wherein the gum arabic comprises an average particle size diameter in the range of about 1 micron to about 250 microns.

23. The sustained release lozenge of claim 1, further comprising an effective sweetening amount of a sweetener selected from a sugar, a non-sugar sweetening agent, and a mixture thereof.

24. The sustained release lozenge of claim 1, further comprising an effective amount of a beneficial agent.

25. The sustained release lozenge of claim 21, wherein the beneficial agent is a member of the group consisting of:

a saliva substitute, an agent for treating the common cold, a local antibiotic, a local anesthetic agent, pilocarpine, vitamin C, a source of Zn2+, chloride, propionate, butyrate, n-butyrate, β

-hydroxybutyrate, benzoate, formate, sulfate, a diet aid, 5-hydroxytryptophan, tyrosine, phenylalanine, pseudoephedrine, ephedrine, phenylpropanolamine, chromium picolinate, aspirin, caffeine, nicotine, a herbal mixture or extract thereof, guarana and ma huang, a source of fluoride ion, and combinations thereof.