Chewable drug-delivery compositions and methods for preparing the same

• US 5,380,535 A
• Filed: 11/25/1992
• Issued: 01/10/1995
• Est. Priority Date: 05/28/1991
• Status: Expired due to Term

• Current Assignee: McNeil-PPC Incorporated (Johnson & Johnson)
• Original Assignee: IBAH, Inc. (Laboratory Corporation Of America Holdings)
• Inventors: Tuliani, Vinod V., Geyer, Robert P.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): BENSTON JR, WILLIAM E
• Application Number:
  US07/981,369
• Time in Patent Office: 776 Days
• Field of Search: 424/484, 424/487, 424/489, 424/440
• US Class Current: 424/484
• 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 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules

Abstract

A non-aqueous, chewable composition for oral delivery of unpalatable drugs is provided along with preparative methods therefor. The composition contains the drug intimately dispersed or dissolved in a pharmaceutically-acceptable lipid that is solid at room temperatures. The composition also has a matrix that contains a granulating agent for the total composition and a rapid dispersal agent and optionally additives such as buffering agents, flavoring agents, surfactants, and the like.

Claims

1. A non-aqueous process for preparing non-aqueous, chewable composition for oral delivery of unpalatable drugs, comprising a therapeutically-effective amount of one or more unpalatable drugs intimately dispersed or dissolved in a pharmaceutically-acceptable lipid which is a solid at ambient temperature, or a mixture of said lipids, the method comprising:

(a) providing a therapeutically-effective amount of one or more unpalatable drugs and a pharmaceutically-acceptable molten lipid;

(b) feeding said drug and molten lipid into a fluidized bed apparatus comprising means for fluidizing said drug and lipid; and

(c) fluidizing said drug and lipid in said fluidized bed apparatus in the absence of a solvent for a time sufficient to solidify the molten lipid and drug into particles comprising said drug and lipid, wherein said particles have a number average particle size of from 10-150 microns,

wherein said drug is present in an amount of from about 0.1-75 weight percent of said composition and said lipid is present in an amount of from about 5-50 weight percent of said composition.

2. The process of claim 1 wherein the drug is fed into the fluidized bed apparatus in the molten state.

3. The process of claim 2 wherein the drug comprises ibuprofen.

4. The process of claim 3 further comprising blending a granulating agent with the solidified drug and lipid particles., wherein said granulating agent is present in an amount of from about 25-75 weight percent of said composition.

9. The process of claim 4 further comprising blending a rapid dispersal agent with the drug and lipid particles, wherein said rapid dispersal agent is present in an amount of from about 1-30 weight percent of said composition.

10. The process of claim 9 further comprising compressing the drug and lipid particles into a tablet.

11. The process of claim 3 further comprising mixing said molten drug and said molten lipid prior to the fluidization step.

12. The process of claim 3 wherein the mass ratio of the drug to the lipid is 1:

2 to 2;

1.

13. The process of claim 12 wherein the size of said drug and lipid particles is from about 20-80 microns.

5. A non-aqueous process for preparing a non-aqueous, chewable composition for oral delivery of unpalatable drugs, comprising a therapeutically-effective amount of one or more unpalatable drugs dissolved in a pharmaceutically-acceptable lipid which is a solid at ambient temperature, or a mixture of said lipids, the method comprising:

(a) providing a molten mixture of a therapeutically-effective amount of one or more unpalatable drugs in its molten state with a pharmaceutically-acceptable lipid in its molten state in the absence of a solvent; and

(b) solidifying the molten drug and lipid mixture by contacting the molten mixture with air into particles comprising said drug and lipid,

wherein said drug is present in an amount of from about 0.1-75 weight percent of said composition and said lipid is present in an amount of from about 5-50 weight percent of said composition.

6. The method of claim 5 wherein the solidification step comprises spray congealing the molten drug and molten lipid mixture.

7. The process of claim 6 wherein the drug comprises ibuprofen and wherein the number average particle size of the drug and lipid particles is from about 10-150 microns.

8. The process of claim 7 further comprising blending a granulating agent. with the solidified drug and lipid particles, wherein said granulating agent is present in an amount of from about 25-75 weight percent of said composition.

14. The process of claim 7 wherein the mass ratio of the drug to the lipid is 1:

2 to 2;

1.

15. The process of claim 14 wherein the number average particle size of said drug and lipid particles is from about 40-140 microns.

16. The process of claim 8 further comprising blending a rapid dispersal agent with the solidified drug and lipid particles and wherein the number average particle size of said drug and lipid particles is from about 40-140 microns and wherein said rapid dispersal agent is present in an amount of from about 1-30 weight percent of said composition.

17. The process of claim 16 further comprising compressing the particles into a tablet.