Oral delivery of pharmaceuticals via encapsulation

• US 20020022057A1
• Filed: 08/17/2001
• Published: 02/21/2002
• Est. Priority Date: 08/17/2000
• Status: Abandoned Application

• Current Assignee: Alyce S. Battey, Jacob Battey
• Original Assignee: Alyce S. Battey, Jacob Battey
• Inventors: Battey, Alyce S., Battey, Jacob
• Application Number:
  US09/931,793
• Publication Number:
  US 20020022057A1
• Time in Patent Office: Days
• US Class Current: 424/490
• 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 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/5015 Organic compounds, e.g. fats, sugars
• CPC Class Codes: A61K 9/5042 Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose

Abstract

An alternate drug delivery system for dissolution of pharmaceuticals in the mouth wherein a therapeutically effective amount of a drug is encapsulated using an encapsulation method. Encapsulation reduces the perceived off flavors of drugs, allowing the active components to dissolve pleasantly in the mouth. This allows more rapid absorption of the active compounds through the oral cavity compared to traditional tablets, which require breakdown and absorption in the gastrointestinal tract. The delivery system can be incorporated into a variety of applications, such as breath mint tablets or chewing gum. Benefits of this invention include portability and the ability to take pharmaceuticals without water and without the off taste of chewable tablets, thereby leading to increased patient compliance.

Claims

1. A dry particulate drug delivery system for dissolution of pharmaceutical compounds in the mouth, comprising:

a therapeutically-effective amount of at least one drug, and an encapsulant, wherein said at least one drug is encapsulated by said encapsulant.

2. The dry particulate drug delivery system of claim 1, further comprising at least one volatile flavorant.

3. The dry particulate drug delivery system of claim 1, further comprising at least one sweetener.

4. The dry particulate drug delivery system of claim 3, further comprising at least one volatile flavorant.

5. The dry particulate drug delivery system of claim 1, wherein said encapsulant is a sucrose-based matrix.

6. The dry particulate drug delivery system of claim 1, wherein said therapeutically effective amount of said at least one drug is dependent on the desired dosage, method of encapsulation, absorption characteristics, and desired tablet size.

7. The dry particulate drug delivery system of claim 1, wherein said drug is a therapeutic agent selected from the group consisting essentially of anesthetics, decongestants, antihistamines, antitussives, antibotics, analgesics, alkaloids, amphetamines, hormones, barbiturates, analeptics and mixtures thereof.

8. The dry particulate drug delivery system of claim 7, wherein said alkaloids are selected from the group consisting essentially of morphine, codeine, caffeine, and cocaine.

9. The dry particulate drug delivery system of claim 7, wherein said hormones are selected from the group consisting essentially of adrenaline and epinephrine.

10. The dry particulate drug delivery system of claim 3, wherein said at least one sweetener is selected from the group consisting essentially of sucrose, fructose, dextrose, lactose, mannitol, sorbitol, maltose, xylitol, saccharin and saccharin sodium, cyclamates, neotame, aspartame, sucralose, acesulfame potassium and mixtures thereof.

11. The dry particulate drug delivery system of claim 1, further comprising at least one of natural and artificial sweeteners, colors, preservatives, fillers, binders, lubricants, suspending agents, acids, buffers, and stabilizing agents.

12. The dry particulate drug delivery system of claim 1, wherein said system is a compressed tablet.

13. The dry particulate drug delivery system of claim 1, wherein said system is a chewing gum.

14. The dry particulate drug delivery system of claim 1, wherein said drug is encapsulated by a method selected from the group consisting essentially of spray drying, air suspension coating, extrusion, spray cooling and chilling, emulsion, microemulsion, adsorption, centrifugal extrusion, rotational suspension separation, rotogranulation, coacervation, continuous crystallization, cocrystallization, inclusion, and liposome formation.

15. The dry particulate drug delivery system of claim 14, wherein aspirin is encapsulated by said cocrystallization method.

16. The dry particulate drug delivery system of claim 14, wherein caffeine is encapsulated by said cocrystallization method.

17. The dry particulate drug delivery system of claim 14, wherein estradiol is encapsulated by said cocrystallization method.

18. The dry particulate drug delivery system of claim 14, wherein estradiol is encapsulated by said extrusion method.

19. The dry particulate drug delivery system of claim 14, wherein ibuprofen is encapsulated by said cocrystallization method.

20. The dry particulate drug delivery system of claim 14, wherein progesterone is encapsulated by said cocrystallization method.

21. The dry particulate drug delivery system of claim 14, wherein warfarin is encapsulated by said cocrystallization method.

22. The dry particulate drug delivery system of claim 14, wherein nicotine is encapsulated by said cocrystallization method.

23. The dry particulate drug delivery system of claim 14, wherein diphenhydramine is encapsulated by said spray drying method.

24. The dry particulate drug delivery system of claim 14, wherein acetaminophen is encapsulated by said rotogranulating method.

25. The dry particulate drug delivery system of claim 14, wherein phenmetrazine is encapsulated by said cocrystallization method.

26. The dry particulate drug delivery system of claim 14, wherein benzocaine is encapsulated by said cocrystallization method.

27. The dry particulate drug delivery system of claim 14, wherein phenylephrine hydrochloride is encapsulated by said cocrystallization method.

28. The dry particulate drug delivery system of claim 14, wherein amobarbital is encapsulated by said cocrystallization method.

29. The dry particulate drug delivery system of claim 14, wherein phenylpropanolamine hydrochloride is encapsulated by said cocrystallization method.

30. The dry particulate drug delivery system of claim 14, wherein dimenhydrinate is encapsulated by said cocrystallization method.

31. The dry particulate drug delivery system of claim 14, wherein pesudoephedrine hydrochloride is encapsulated by said cocrystallization method.

32. The dry particulate drug delivery system of claim 14, wherein meclizine is encapsulated by said cocrystallization method.

33. The dry particulate drug delivery system of claim 14, wherein Phenobarbital sodium is encapsulated by said cocrystallization method.

34. The dry particulate drug delivery system of claim 14, wherein testosterone is encapsulated by said cocrystallization method.

35. The dry particulate drug delivery system of claim 14, wherein prednisolone is encapsulated by said cocrystallization method.

36. The dry particulate drug delivery system of claim 14, wherein diazepam is encapsulated by said cocrystallization method.

37. The dry particulate drug delivery system of claim 14, wherein dyclonine hydrochloride is encapsulated by said cocrystallization method.

38. The dry particulate drug delivery system of claim 14, wherein chlorpheniramine is encapsulated by said coacervation method.

39. The dry particulate drug delivery system of claim 14, wherein cyclizine hydrochloride is encapsulated by said cocrystallization method.

40. The method of dissolving a pharmaceutical compound in the mouth of a user, comprising the steps of:

encapsulating a therapeutically-effective amount of at least one drug within an encapsulant and forming an encapsulated drug,

inserting said encapsulated drug into the mouth of the user,

subjecting said encapsulated drug to fluids secreted within the mouth of said user,

dissolving said encapsulant and releasing said drug in said mouth,

dissolving said drug within said mouth of said user.