Ex vivo modifiable particle or polymeric based final dosage form

• US 20100068152A1
• Filed: 02/05/2009
• Published: 03/18/2010
• Est. Priority Date: 09/16/2008
• Status: Abandoned Application

• Current Assignee: Searete LLC (Intellectual Ventures LLC)
• Original Assignee: Searete LLC (Intellectual Ventures LLC)
• Inventors: Ishikawa, Muriel Y., Boyden, Edward S., Wood, Lowell L. JR., Rivet, Dennis J., Hyde, Roderick A., Sweeney, Elizabeth A., Wood, Victoria Y.H., Bangera, Mahalaxmi Gita
• Application Number:
  US12/322,877
• Publication Number:
  US 20100068152A1
• Time in Patent Office: Days
• US Class Current: 424/10.100
• CPC Class Codes: A61K 9/127 Liposomes
• CPC Class Codes: A61K 9/1629 Organic macromolecular compounds

Abstract

Provided embodiments include a final dosage form, an article of manufacture, and method. A final dosage form for administering a medicament to an animal is provided. The final dosage form includes the medicament, and a particle or polymeric material. The particle or polymeric material carries the medicament and is configured in a medicament-retention state. In medicament-retention state, the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal. The particle or polymeric material is modifiable ex vivo by an exposure to a stimulus to a medicament-release state. In the medicament-release state, the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

Claims

1. A final dosage form for administering a medicament to an animal, the final dosage form comprising:

the medicament; and

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal,

the particle or polymeric material being modifiable ex vivo by an exposure to a stimulus to carry the medicament in a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

2. The final dosage form of claim 1, wherein the medicament comprises a pharmacologically-active agent.

3. The final dosage form of claim 1, wherein the medicament comprises at least one of an agent, treatment agent, drug, prodrug, therapeutic, nutraceutical, medication, vitamin, nutritional supplement, medicine, remedy, medicinal substance, or cosmetic.

4. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament comprises:

a particle or polymeric material conjugated with the medicament.

5. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament comprises:

a particle or polymeric material containing, intertwined, or bound with the medicament.

6. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament comprises:

a particle or polymeric material encapsulating the medicament.

7. The final dosage form of claim 1, wherein the stimulus includes at least one of light, radio, or electromagnetic wave stimulus.

8. The final dosage form of claim 1, wherein the stimulus includes at least one of a thermal, acoustic or ultrasound stimulus.

9. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-withholding state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-supplying state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

10. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by at least one of a post-manufacture or a field exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

11. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-holding state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable to a in vivo release-facilitation state by an ex vivo exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

12. The final dosage form of claim 1, wherein the particle or polymeric material comprises:

a particle or polymeric material having a premodification characteristic that results in an insignificant uptake of the particle or polymeric material in the gastrointestinal tract of the animal.

13. The final dosage form of claim 1, wherein the polymeric material comprises an intelligent polymer.

14. The final dosage form of claim 1, wherein the particle or polymeric material comprises a polymer matrix structure.

15. The final dosage form of claim 1, wherein the particle or polymeric material comprises at least one of a microparticle, a gel or a dendrimer based microparticle.

16. The final dosage form of claim 1, wherein the particle or polymeric material comprises:

at least one of a noisome, fibrin, polymeric micelle, microsome, cyclodextrin, polymer-medicament conjugate, or cellulose responsive to the ex vivo exposure to a stimulus.

17. The final dosage form of claim 1, wherein the particle or polymeric material includes at least one of a gel, a gel matrix, a natural gel, a synthetic gel, a colloid gel, or a hydrogel structure covalently bonded to the medicament using a photo labile bond and responsive to the ex vivo exposure to a stimulus.

18. The final dosage form of claim 1, wherein the particle or polymeric material includes at least one of a dendrimer, dendrimsome, dendromsome, dendron, or dendriplex material.

19. The final dosage form of claim 1, wherein the particle or polymeric material includes at least one of an emulsion, nano-emulsion, or double emulsion.

20. The final dosage form of claim 1, wherein the particle or polymeric material includes at least one of a lipid, cationic lipid, lipid micelle, liposome, lipospheres, acoustically active lipospheres, acoustically-active microbubbles conjugated to liposomes, lipid-coated microbubbles, cerasomes, magnetic liposomes, metallosomes, or a mimetic.

21. The final dosage form of claim 1, wherein the particle or polymeric material comprises:

a liposome carrier entrapping the medicament and having an intact particle size resulting in an insignificant uptake in the gastrointestinal tract of the animal.

22. The final dosage form of claim 1, wherein the particle or polymeric material includes a liposome carrier having a particle size of at least approximately three microns.

23. The final dosage form of claim 1, wherein the particle or polymeric material includes a liposome having a particle size of at least approximately four microns.

24. The final dosage form of claim 1, wherein the particle or polymeric material includes a microparticle material.

25. The final dosage form of claim 1, wherein the particle material comprises:

at least one of a nanoparticle, a microsphere, or a polymeric microsphere responsive to the ex vivo exposure to a stimulus.

26. The final dosage form of claim 1, wherein the particle or polymeric material includes a pharmaceutically-acceptable inert particle or polymeric material.

27. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a non-ionizing radiation stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal

28. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to an electromagnetic radiation stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal

29. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to at least one of a light radiation, terahertz radiation, microwave radiation, and radio wave radiation stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

30. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a magnetic stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

31. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to an electric stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

32. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal after administration of the final dosage form and modifiable ex vivo to a medicament-release state by an exposure to a stimulus wherein the medicament is substantially bioavailable to the animal after administration of the final dosage form comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal after administration of the final dosage form and modifiable ex vivo to a medicament-release state wherein the medicament is substantially bioavailable to the animal after administration of the final dosage form by an exposure to an energetic stimulus.

33. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal after administration of the final dosage form and modifiable ex vivo to a medicament-release state by an exposure to a stimulus wherein the medicament is substantially bioavailable to the animal after administration of the final dosage form comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal after administration of the final dosage form and modifiable ex vivo to a medicament-release state wherein the medicament is substantially bioavailable to the animal after administration of the final dosage form by an exposure to a chemical stimulus.

34. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to at least one of a mechanical, heat, or pressure stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

35. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to at least one of an activation stimulus, or an actuation stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

36. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to at least one of at least one of a thermal, acoustic, or ultrasound stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal.

37. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal, the stimulus facilitating a release of the medicament by at least one of an expansion of a gel, gel matrix, or hydrogel carrier.

38. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal, the stimulus facilitating the release of the medicament from the particle or polymeric carrier by at least one of a bursting of a liposome material, formation of a pore in a liposome material, or an unpacking of the particle or polymeric material.

39. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state allowing an in vivo release of the medicament if the final dosage form is administered to the animal.

40. The final dosage form of claim 1, wherein the particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a medicament-release state wherein the medicament is substantially bioavailable to the animal if the final dosage form is administered to the animal comprises:

a first particle or polymeric material carrying the medicament; and

a second particle or polymeric material carrying the first particle or polymeric material, configured in a first particle or polymeric material-retention state wherein the first particle or polymeric material is substantially not bioavailable to the animal if the final dosage form is administered to the animal, and modifiable ex vivo by an exposure to a stimulus to a first particle or polymeric material-release state wherein the first particle or polymeric material is substantially bioavailable to the animal if the final dosage form is administered to the animal.

41. The final dosage form of claim 1, further comprising:

a transport medium suitable for delivering the particle or polymeric material carrying the medicament to the animal.

42. The final dosage form of claim 1, further comprising:

an indicator substance configured to indicate an exposure of the particle or polymeric substance to the stimulus.

43. A final dosage form for administering a medicament to an animal, the final dosage form comprising:

the medicament; and

a particle or polymeric material carrying the medicament in a medicament-retention state wherein the medicament is substantially not bioavailable to the animal if the final dosage form is administered to the animal,

the particle or polymeric material being modifiable ex vivo by an exposure to a first stimulus to carry the medicament in a first medicament-release state wherein the medicament has a first bioavailability to the animal if the final dosage form is administered to the animal, and

the particle or polymeric material being modifiable ex vivo by an exposure to a second stimulus to a second medicament-release state, wherein the medicament has a second bioavailability to the animal if the final dosage form is administered to the animal.