Taste masking microparticles for oral dosage forms

• US 5,607,697 A
• Filed: 06/07/1995
• Issued: 03/04/1997
• Est. Priority Date: 06/07/1995
• Status: Expired due to Term

• Current Assignee: Wells Fargo Business Credit, Inc. (Wells Fargo & Company)
• Original Assignee: Cima Labs Incorporated (Teva Pharmaceutical Industries Limited)
• Inventors: Schuehle, Steven S., Alkire, Todd G., Sanftleben, Ronald A.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Spear, James M.
• Application Number:
  US08/478,419
• Time in Patent Office: 636 Days
• Field of Search: 424/494, 424/495, 424/497, 424/490, 424/464, 424/466
• US Class Current: 424/495
• CPC Class Codes: A61K 9/0007 Effervescent A61K9/0065 takes precedence
• 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 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/5015 Organic compounds, e.g. fats, sugars
• CPC Class Codes: A61K 9/5026 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/5047 Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose

Abstract

The present invention relates to a solid dosage form including a new type of taste masking microparticle having an adsorbate of, for example, mannitol, in the core thereof.

Claims

1. A solid pharmaceutical dosage form adapted for direct oral administration, in solid form, to a mammal comprising:

a plurality of microparticles, each said microparticle having a core including at least one pharmaceutical ingredient and a compound which is sweet in taste and which has a negative heat of solution, said compound which is sweet in taste and which has a negative heat of solution being selected from the group consisting of mannitol, sorbitol, a mixture of an artificial sweetener and menthol, a mixture of a sugar and menthol, and methyl salicylate, said compound being present in said microparticles in an amount of between greater than 0 and about 80% by weight of the resulting microparticle, said core being coated with a coating material, which will retard dissolution of said pharmaceutical ingredient in the mouth, as well as the objectionable taste of said pharmaceutical ingredient, surrounding at least a portion of said core;

said solid dosage form being sized and shaped and having a composition and hardness which are adapted for direct oral administration, said dosage form being disintegratable in the mouth so as to release said microparticles.

2. The dosage form of claim 1 further comprising at least one saliva activated effervescent agent in an amount which is effective to provide disintegration of said dosage form in the mouth of a patient, without chewing, to thereby release said microparticles.

3. The pharmaceutical dosage form of claim 1 wherein said microparticles are discrete particulate at least partially coated with said coating material.

4. The pharmaceutical dosage form of claim 3 wherein said microparticles are coated with said coating material.

5. The pharmaceutical dosage form of claim 1 wherein said pharmaceutical ingredient is adsorbed on said compound which is sweet in taste and which has a negative heat of solution.

6. The pharmaceutical dosage form of claim 1 wherein said pharmaceutical ingredient is intimately mixed with said compound which is sweet in taste and which has a negative heat of solution.

7. The pharmaceutical dosage form of claim 1 wherein said microparticles comprise between about 1 and 80% of the dosage form by weight.

8. The pharmaceutical dosage form of claim 7 wherein said compound which is sweet in taste and which has a negative heat of solution is selected from a group consisting of mannitol and sorbitol.

9. The pharmaceutical dosage form of claim 1 further comprising at least one binder disposed within said core.

10. The pharmaceutical dosage form of claim 1 wherein said coating material is ethylcellulose.

11. The pharmaceutical dosage form of claim 1 wherein the balance of the weight of the dosage form is composed of one or more compounds of the group consisting of lubricants, fillers, disintegrants, binding agents, disintegration agents, sweeteners, flavors, colorants.

12. The pharmaceutical dosage form of claim 1 wherein said coating material is provided in an amount of at least about 5% by weight, based on the weight of the particle.

13. The pharmaceutical dosage form of claim 12 wherein said coating material is provided in an amount of at least about 10% by weight, based on the weight of the particle.

14. The pharmaceutical dosage form of claim 12 wherein said coating material is provided in an amount at between about 5% and about 75% by weight of the microparticles.

15. The pharmaceutical dosage form of claim 1 wherein said dosage form is a tablet having a hardness ranging from between about 5 to about 250 newtons.

16. The tablet of claim 15 having a hardness of between about 10 and about 50 newtons.

17. The pharmaceutical dosage form of claim 7 wherein said microparticles comprise between about 5 and about 50% of the dosage form by weight.