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Claims for Patent: 4,863,737

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Claims for Patent: 4,863,737

Title: Compositions and methods of manufacture of compressed powder medicaments
Abstract:Compositions and methods of manufacture for producing a medicament composition capable of absorption through the mucosal tissues of the mouth, pharynx, and esophagus. The present invention relates to such compositions and methods which are useful in administering drugs in a dose-to-effect manner such that sufficient drug is administered to produce precisely a desired effect. The invention also relates to a manufacturing technique that enables a therapeutic agent or drug to be incorporated into a flavored confectionary base and to compress or otherwise attach the solid confectionary mixture onto an appliance or holder. Employing the present invention, the drug may be introduced into the patient's bloodstream almost as fast as through injection, and much faster than using the oral administration route, while avoiding the negative aspects of both of these methods. The present invention achieves these advantages by incorporating the drug into a compressed powder "candy " matrix. The pH and pKa of the powder matrix can be modified to increase the absorption of the drug through the mucosal tissues.
Inventor(s): Stanley; Theodore H. (Salt Lake City, UT), Hague; Brian (West Valley, UT)
Assignee: University of Utah (Salt Lake City, UT)
Application Number:07/060,045
Patent Claims: 1. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient, the method comprising the steps of:

(a) obtaining a pharmacologically effective dose of the drug in a substantially powdered form, the drug being capable of absorption through mucosal tissues of the mouth, pharynx, and esophagus;

(b) obtaining a soluble carbohydrate material capable of forming a compressible confectionary matrix and capable of dissolving in the mouth of the patient;

(c) mixing the drug and the carbohydrate material at a temperature below the melting points of the drug and the carbohydrate material to form a drug-containing matrix such that the drug is dispersed substantially throughout the matrix, the drug-containing matrix being capable of releasing the drug for absorption through the mucosal tissues upon dissolution of the matrix in the mouth of the patient;

(d) compressing the drug-containing matrix in a mold to form an integral mass such that, when the integral mass dissolves in the mouth of the patient, the drug is released for absorption through the mucosal tissues; and

(e) incorporating a holder as part of the integral mass in order to form the drug-containing lollipop.

2. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein a buffer is added to the drug-containing matrix.

3. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 2 wherein the buffer modifies the pKa of the drug such that, when the integral mass is dissolved, a majority of the drug remains non-ionized in order to facilitate transmucosal absorption of the drug.

4. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 3 wherein the buffer is citric acid/sodium citrate.

5. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the drug has sufficient lipophilic properties such that the drug can be absorbed through the mucosal tissue.

6. A drug-containing lollipop for use in transmucosal delivery of the drug to a patient comprising:

a soluble, compressible carbohydrate material;

a pharmacologically effective dose of a drug in a substantially powdered form, the drug being capable of absorption through mucosal tissues of the mouth, pharnyx, and esophagus and being dispersed substantially uniformly throughout the carbohydrate material at a temperature below the melting points of the drug and the carbohydrate material and compressed with the carbohydrate material into a solid integral mass which is capable of dissolving in the mouth of the patient so that the drug is released for absorption through mucosal tissues of the mouth, pharnyx, and esophagus upon dissolution of the integral mass in the mouth of the patient;

holder means secured to the integral mass so as to form a drug-containing lollipop, the holder means being configured so as to permit convenient insertion and removal of the drug-containing integral mass into and out of the mouth of a patient.

7. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the holder is incorporated into the integral mass by compression of the drug-containing matrix around the holder during compressing step (d).

8. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the holder is incorporated as part of the integral mass by affixing the holder to the integral mass after compressing step (d).

9. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the soluble carbohydrate material in the drug-containing matrix includes compressible confectionary sugar.

10. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 9 wherein the drug-containing matrix includes a lubricating agent such that the integral mass can be released from the mold after compressing step (d).

11. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the drug-containing matrix includes at least one flavor enhancer.

12. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the drug-containing matrix includes maltodextrin in order to aid in dissipating any unpleasant flavors of the drug.

13. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein a substantially water-insoluble component is added to the drug-containing matrix such that the dissolution of the integral mass in the mouth of the patient is made slower by the substantially water-insoluble component in the drug-containing matrix.

14. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the confectionary mixture is compressed with forces in the range of from about 2000 newtons to about 5000 newtons.

15. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the drug is methohexital.

16. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the drug is selected from the group consisting of triazolan, oxazepam, lorazepam, etomidate, and thiamylal.

17. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 1 wherein the drug is nitroglycerin.

18. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient in a dose-to-effect manner, the method comprising the steps of:

(a) obtaining a pharmacologically effective dose of the drug in a substantially powdered lipophilic form capable of absorption through mucosal tissues of the mouth, pharnyx, and esophagus;

(b) obtaining a soluble carbohydrate material capable of forming a compressible confectionary matrix and capable of dissolving in the mouth of the patient;

(c) obtaining a buffer capable of modifying the pKa of the drug such that a majority of the drug remains non-ionized in order to facilitate transmucosal absorption of the drug;

(d) mixing the drug, the soluble carbohydrate material, and the buffer at a temperature below the melting points of the drug and the carbohydrate material to form a solid drug-containing matrix such that the drug is dispersed substantially throughout the matrix, the drug-containing matrix being capable of releasing the drug for absorption through the mucosal tissues upon dissolution of the matrix in the mouth of the patient;

(e) compressing the drug-containing matrix in a mold to form an integral mass such that when the integral mass dissolves in the mouth of the patient, the drug is released for absorption through the mucosal tissues such that the drug is administered in a dose-to-effect manner; and

(f) incorporating a holder as part of the integral mass in order to form the drug-containing lollipop.

19. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the holder is incorporated into the integral mass by compression of the drug-containing matrix around the holder during compressing step (e).

20. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the holder is incorporated as part of the integral mass by affixing the holder to the integral mass after compressing step (e).

21. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the drug-containing mixture includes maltodextrin in order to aid in dissipating any unpleasant flavors of the drug.

22. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the buffer comprises citric acid/sodium citrate.

23. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the drug-containing matrix includes compressible sugar.

24. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the drug-containing matrix includes a flavoring ingredient.

25. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the confectionary mixture is compressed with forces in the range of from about 2000 newtons to about 5000 newtons.

26. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the drug is methohexital.

27. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the drug is selected from the group consisting of triazolan, oxazepam, lorazepam, etomidate and thiamylal.

28. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the drug is selected from the group consisting of isosorbide dinitrate, captopril, nifedipine, clonidine, and esimolol.

29. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the drug is nitroglycerin.

30. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 18 wherein the drug is a potent, fast-acting drug.

31. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 30 wherein the drug has effects on the central nervous system of the patient.

32. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 30 wherein the drug has effects on the cardiovascular system of the patient.

33. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 30 wherein the drug has effects in the renal vascular system of the patient.

34. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 20 wherein the materials in the drug-containing matrix includes a lubricating agent such that the integral mass can be released from the mold after compressing step (d).

35. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 34 wherein the lubricating agent comprises glyceryl behenate.

36. A method for producing a drug-containing matrix for use in transmucosal delivery of the drug to a patient as defined in claim 34 wherein the releasing agent is a substantially water-insoluble component such that the dissolution of the integral mass in the mouth of the patient is made slower by the substantially water-insoluble component in the drug-containing matrix.

37. A drug-containing lollipop for use in transmucosal delivery of the drug to a patient, said composition comprising:

a soluble, compressible, substantially powdered carbohydrate material;

a pharmacologically effective dose of a lipophilic drug in a substantially powdered form, the drug being capable of absorption through mucosal tissues of the mouth, pharnyx, and esophagus and being dispersed substantially uniformly throughout the carbohydrate material at a temperature below the melting points of the drug and the carbohydrate material and compressed with the carbohydrate material into a solid integral mass which is capable of dissolving in the mouth of the patient so that the drug is released for absorption through mucosal tissues of the mouth, pharnyx, and esophagus upon dissolution of the integral mass in the mouth of the patient;

a buffer which is also dispersed substantially uniformly throughout the integral mass, the buffer being capable of modifying the pKa of the drug such that a majority of the drug remains non-ionized in order to facilitate transmucosal absorption of the drug; and

holder means secured to the integral mass so as to form a drug-containing lollipop, the holder means being configured so as to permit convenient insertion and removal of the drug-containing integral mass into and out of the mouth of a patient.

38. A drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 37, wherein the buffer is citric acid/sodium citrate.

39. A drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 37, wherein the soluble carbohydrate material in the drug-containing integral mass includes compressible confectionary sugar.

40. A drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 39, wherein the drug-containing integral mass further includes a lubricating agent dispersed substantially uniformly throughout the integral mass in order to aid in the manufacture of the drug-containing lollipop.

41. A drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 39, wherein the drug-containing integral mass further includes maltodextrin dispersed substantially uniformly throughout the integral mass in order to aid in dissipating any unpleasant flavors of the drug in the integral mass.

42. A drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 41, wherein the drug-containing integral mass further comprises at least one flavor enhancer dispersed substantially uniformly throughout the integral mass.

43. A drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 37, wherein the drug-containing integral mass further comprises a substantially water-insoluble component dispersed substantially uniformly throughout the integral mass in order to slow the dissolution of the integral mass in the mouth of the patient.

44. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 18 further comprising the step of mixing at least one flavoring with the drug-containing matrix.

45. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 18 further comprising the step of mixing at least one flavor enhancer with the drug-containing matrix.

46. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 15 wherein the drug-containing matrix comprises from about 10 milligrams to about 500 milligrams of methohexital.

47. A method for producing a drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 26 wherein the drug-containing matrix comprises from about 10 milligrams to about 500 milligrams of methohexital.

48. A drug-containing lollipop for use in transmucosal delivery of the drug to a patient as defined in claim 37 further comprising at least one flavoring.

49. A drug-containing lollipop as defined in claim 6 further comprising at least one flavoring dispersed within said integral mass.

50. A drug-containing lollipop as defined in claim 3 further comprising at least one releasing agent dispersed within said integral mass.

51. A drug-containing lollipop as defined in claim 6 further comprising at least one flavor enhancer dispersed within said integral mass.

52. A drug-containing lollipop as defined in claim 6 further comprising at least one sweetener in addition to said carbohydrate material dispersed within said integral mass.
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