Novel drug delivery system for antitussives

• US 4,929,508 A
• Filed: 07/26/1988
• Issued: 05/29/1990
• Est. Priority Date: 10/05/1984
• Status: Expired due to Term

• Current Assignee: Cadbury Adams USA LLC (Mondelez International, Inc.)
• Original Assignee: Warner-Lambert Company (Pfizer Inc.)
• Inventors: Yang, Robert K., Sharma, Shri C., Shaw, James J.
• Primary Examiner(s): Page, Thurman K.
• Application Number:
  US07/224,601
• Time in Patent Office: 672 Days
• Field of Search: 424/439, 424/440, 424/441, 424/450, 424/498, 514/850
• US Class Current: 424/439
• CPC Class Codes: A23G 4/02 Apparatus specially adapted for manufacture or treatment of chewing gum
• CPC Class Codes: A23G 4/06 characterised by the composition containing organic or inorganic compounds
• CPC Class Codes: A23G 4/10 characterised by the carbohydrates used, e.g. polysaccharides containing dairy products A23G4/16
• CPC Class Codes: A23G 4/20 Composite products, e.g. centre-filled , multi-layer, laminated
• CPC Class Codes: A23L 27/70 Fixation, conservation, or encapsulation of flavouring agents
• CPC Class Codes: A23V 2002/00 Food compositions, function of food ingredients or processes for food or foodstuffs
• CPC Class Codes: A23V 2200/202 Agglomerating agent
• CPC Class Codes: A23V 2200/22 Coating agent
• CPC Class Codes: A23V 2250/1582 Chlorine
• CPC Class Codes: A23V 2250/16 Potassium
• CPC Class Codes: A23V 2250/18 Lipids
• CPC Class Codes: A23V 2250/1842 Lecithin
• CPC Class Codes: A23V 2250/192 Monoglycerides
• CPC Class Codes: A23V 2250/2482 Aspartam
• CPC Class Codes: A23V 2250/26 Saccharin
• CPC Class Codes: A23V 2250/30 Other Organic compounds
• CPC Class Codes: A23V 2250/51088 Other cellulose derivatives
• CPC Class Codes: A23V 2250/6406 Glycerol
• CPC Class Codes: A23V 2250/6418 Mannitol
• CPC Class Codes: A23V 2250/642 Sorbitol
• CPC Class Codes: A61K 9/1617 : Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/5015 : Organic compounds, e.g. fats, sugars

Abstract

A drug delivery system comprising a core material comprising a drug, and a hydrophobic matrix coating the core. The coating delays hydration of the drug and masks the taste of the drug. The coating comprises an emulsifier, an edible fatty acid or wax and a glyceride. The delivery system can be incorporated into various food products, pharmaceutical preparations and proprietary products.

Claims

1. A dry particulate drug delivery system designed to be chewed or swallowed whole comprising:

(A) an antitussive in an amount of about 1% to about 75%; and

(B) a hydrophobic matrix comprising

(i) about 0.5% to about 20% by weight of an emulsifier; and

(ii) about 61% to about 95% by weight of an edible material having a melting point in the range of about 25°

C. to about 100°

C. selected from the group consisting of (a) fatty acids having an iodine value of about 1 to about 10, (b) natural waxes, (c) synthetic waxes and (d) mixtures thereof; and

(iii) at least one glyceride, wherein the antitussive and hydrophobic matrix form an agglomerate, and

(C) a coating surrounding said agglomerate effective to delay hydration until ingested comprising about 200% to about 400% by weight of the agglomerate an edible material having a melting point in the range of about 25°

C. to about 100°

C. selected from the group consisting of (a) fatty acids having an iodine value of about 1 to about 10, (b) natural waxes, (c) synthetic waxes and (d) mixtures thereof;

wherein the coating forms a protective barrier effective to prevent unpleasant taste perception for the antitussive agglomerate.

2. The delivery system of claim 1 wherein the emulsifier is lecithin.

3. The delivery system of claim 1 wherein the fatty acid is selected from the group consisting of hydrogenated palm oil, hydrogenated palm kernel oil, hydrogenated peanut oil, hydrogenated rapeseed oil, hydrogenated rice bran oil, hydrogenated soybean oil, hydrogenated cottonseed oil, hydrogenated sunflower oil and mixtures thereof.

4. The delivery system of claim 3 wherein the fatty acid is present in amounts of about 61% to about 95% by weight of the delivery system.

5. The delivery system of claim 3 wherein the fatty acid is refined hydrogenated palm oil present in amounts of about 63% to about 90% by weight of the delivery system.

6. The delivery system of claim 1 wherein the glyceride is present in amounts of about 0.5% to about 20% by weight of the delivery system.

7. The delivery system of claim 6 wherein the glyceride is a distilled monoglyceride present in amounts of about 1% to about 3% by weight of the delivery system.

8. The delivery system of claim 6 wherein the emulsifier is lecithin, present in amounts of about 0.5% to about 9%.

9. The delivery system of claim 3 having a melting point in the range of about 25°

C. to about 90°

C.

10. The delivery system of claim 1 having a particle size of about 200 to about 30 U.S. Standard mesh size.

15. The delivery system of claim 1 wherein the antitussive is selected from the group consisting of dextromethorphan, dextromethorphan hydrobromide, noscapine, carbetapentane citrate and chlophedianol hydrochloride.

16. The delivery system of claim 1 wherein the antitussive is dextromethorphan.

19. A method of preparing the dry particulate drug delivery system of claim 1 comprising:

A. Formation of an agglomerate of the antitussive and the hydrophobic matrix comprising the steps of melting the hydrophobic matrix and dispersing the antitussive uniformly therein;

feeding the dispersion under controlled pressure to maintain the particle size between about 200 to about 30 mesh, collecting the agglomerate; and

B. Coating the agglomerate by conducting the agglomerate through a stream of air passing through a zone of atomized droplets of a second hydrophobic material.

20. The method of claim 19 wherein said antitussive is selected from the group consisting of dextromethorphan, dextromethorphan hydrobromide, noscopine, carbetapentane citrate and chlophedianal hydrochloride.

21. The method of claim 20 wherein the antitussive is dextromethorphan.

11. A dry particulate composite having a substantially hydrophobic exterior designed to be chewed or swallowed whole comprising

(A) an agglomerated mixture of about 1% to about 75% of an antitussive and a matrix wherein the matrix comprises:

(i) about 0.5% to about 20% fat soluble lecithin;

(ii) about 61% to about 90% of an edible material having a melting point in the range of about 25°

C. to about 100°

C. selected from the group consisting of (a) a fatty acid having an iodine value of about 1 to about 10;

(b) natural waxes;

(c) synthetic waxes;

(d) and mixtures thereof;

(iii) about 0.5% to about 30% of a glyceride;

said composite having a melting point in the range of about 20°

C. to about 90°

C.

12. The composite of claim 11 contained in a confectionary product.

13. The composite of claim 11 contained in a chewing gum product.

14. The composite of claim 11 contained in a pharmaceutical preparation.

17. The composite of claim 11 wherein the antitussive is selected from the group consisting of dextromethorphan, dextromethorphan hydrobromide, noscapine, carbetapentane citrate and chlophedianol hydrochloride.

18. The composite of claim 11 wherein the antitussive is dextromethorphan.