Drug in combination with flavor masking agent and method for making same

• US 4,910,023 A
• Filed: 06/09/1988
• Issued: 03/20/1990
• Est. Priority Date: 06/09/1988
• Status: Expired due to Fees

• Current Assignee: Warner-Lambert Company (Pfizer Inc.)
• Original Assignee: Warner-Lambert Company (Pfizer Inc.)
• Inventors: Harris, Michael R., Botzolakis, John E., Nesbitt, Russell U.
• Primary Examiner(s): Robinson, Ellis P.
• Assistant Examiner(s): HORNE, LEON
• Application Number:
  US07/204,437
• Time in Patent Office: 649 Days
• Field of Search: 424/470, 424/464, 424/465
• US Class Current: 424/470
• CPC Class Codes: A61K 9/1611 Inorganic compounds
• CPC Class Codes: A61K 9/501 Inorganic compounds
• CPC Class Codes: A61K 9/5042 Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose

Abstract

According to this invention various hygroscopic malflavored drugs can be proceeded by a unique wet granulation process wherein a slurry of the drug in water is dried in combination with colloidal silicon dioxide and, in a particularly preferred embodiment microcrystalline cellulose with the colloidal silicon dioxide absorbing onto the drug particles.

The result is a protective coating of silicon dioxide which masks unpleasant taste and odor and also reduces the adhesive of the granulation onto the punch faces used in the manufacture of the granules. By adsorbing silicon dioxide on the particulate surface of the malflavored hygroscopic drug, the drug becomes not only easier to handle but the unpleasant tastes and/or odors are masked making the fiinal product more susceptible to proper patient compliance.

Claims

1. In combination, a particulate unpleasant flavored drug and at least 3% by weight of the combination of SiO₂ adsorbed on said drug particle, SiO₂ being present at a level sufficient to minimize the unpleasant flavor effects of the drug.

2. The combination of claim 1 wherein the SiO₂ is present at a level of not more than 30%.

3. The combination of claim 1 wherein SiO₂ is present at a level of 4-15%.

4. The combination of claims 1, 2 or 3 wherein the drug is present at a level of 30 to 70% by weight of the combination.

5. The combination of claim 1 wherein an adjunct is added to further dry the formulation.

6. The combination of claim 5 wherein the adjunct is microcrystalline cellulose.

7. A tablet formed from the combination of claim 1, 2, 3, 5 or 6 comprising at least one member selected from the group consisting of excipients, disintegrants and glidants.

8. 3-phenoxypyridine monosulfate in combination with SiO₂ at a level of between 3 and 20% by weight of the combination.

9. Pramiracetam in combination with SiO₂ at a level of between about 3 and 20% by weight of the combination.

10. Gemfibrozil in combination with SiO₂ at a level between about 3 and 20% by weight of the combination.

11. The combination of claims 8, 9, or 10 wherein microcrystalline cellulose is present at a level of about 5-45% by weight of the combination.