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Details for Patent: 6,433,040

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Details for Patent: 6,433,040

Title: Stabilized bioactive preparations and methods of use
Abstract:Stabilized dispersions are provided for the delivery of a bioactive agent. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a liquid fluorochemical. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments the stabilized dispersions may be directly administered to the lung of a patient using an endotracheal tube or bronchoscope.
Inventor(s): Dellamary; Luis A. (San Marcos, CA), Tarara; Thomas E. (San Diego, CA), Kabalnov; Alexey (Corvallis, OR), Weers; Jeffry G. (San Diego, CA), Schutt; Ernest G. (San Diego, CA)
Assignee: Inhale Therapeutic Systems, Inc. (San Carlos, CA)
Filing Date:Dec 22, 1998
Application Number:09/218,209
Claims:1. A method for delivering one or more bioactive agents comprising the steps of: providing a stabilized dispersion comprising a nonaqueous suspension medium having dispersed therein a plurality of perforated microstructures wherein said suspension medium substantially permeates said perforated microstructures, and wherein said perforated microstructures comprise a bioactive agent; and administering by liquid dose instillation a therapeutically effective amount of said stabilized dispersion to at least a portion of the nasal or pulmonary passages of a patient in need thereof.

2. The method of claim 1 wherein a surfactant is incorporated into said perforated microstructures.

3. The method of claim 2 wherein said surfactant is selected from the group consisting of phospholipids, nonionic detergents, nonionic block copolymers, ionic surfactants, biocompatible fluorinated surfactants and combinations thereof.

4. The method of claim 1 wherein said suspension medium and said perforated microstructures have a refractive index differential of less than about 0.5.

5. The method of claim 1wherein said perforated microstructures further comprise hollow porous microspheres.

6. The method of claim 1 wherein said bioactive agent is selected from the group consisting of antiallergics, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, leukotriene inhibitors or antagonists, antihistamines, anti-inflammatories, antineoplastics, anticholinergics, anesthetics, anti-tuberculars, imaging agents, cardiovascular agents, enzymes, steroids, genetic material, viral vectors, antisense agents, proteins, peptides and combinations thereof.

7. The method of claim 6 wherein said bioactive agent is gentamicin.

8. The method of claim 1 wherein said nonaqueous suspension medium comprises a liquid fluorochemical.

9. The method of claim 8 wherein said liquid fluorochemical comprises perfluorooctyl bromide.

10. A method for stabilizing a dispersion by reducing attractive van der Waals forces comprising the steps of: providing a plurality of perforated microstructures comprising at least one bioactive agent; combining the perforated microstructures with a nonaqueous suspension medium comprising at least one liquid fluorochemical wherein said suspension medium substantially permeates said perforated microstructures.

11. The method of claim 10 wherein said perforated microstructures have a mean density selected to provide a density differential with that of the suspension medium of less than 0.6 g/cm.sup.3.

12. The method of claim 10 wherein the dispersion comprises a creaming time of greater than 30 minutes.

13. The method of claim 10 wherein the dispersion comprises a creaming time of greater than 60 minutes.

14. The method of claim 10 wherein a surfactant is incorporated into said perforated microstructures.

15. The method of claim 10 wherein said perforated microstructures further comprise hollow porous microspheres.

16. The method of claim 10 wherein said bioactive agent is selected from the group consisting of antiallergics, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, leukotriene inhibitors or antagonists, antihistamines, anti-inflammatories, antineoplastics, anticholinergics, anesthetics, anti-tuberculars, imaging agents, cardiovascular agents, enzymes, steroids, genetic material, viral vectors, antisense agents, proteins, peptides and combinations thereof.

17. The method of claim 10 wherein said liquid fluorochemical comprises perfluorooctyl bromide.

18. A stabilized dispersion for the delivery of a bioactive agent by liquid dose instillation comprising a nonaqueous suspension medium having dispersed therein a plurality of perforated microstructures comprising at least one bioactive agent wherein said suspension medium substantially permeates said perforated microstructures.

19. The dispersion of claim 18 wherein the perforated microstructures have a mean diameter of 1-30 .mu.m.

20. The dispersion of claim 18 wherein a surfactant is incorporated into said perforated microstructures.

21. The dispersion of claim 20 wherein said surfactant is present in said perforated microstructures in an amount greater than 10% w/w.

22. The dispersion of claim 20 wherein said surfactant is present in said perforated microstructures in an amount greater than 20% w/w.

23. The dispersion of claim 20 wherein said surfactant comprises a phospholipid.

24. The dispersion of claim 18 wherein said perforated microstructures further comprise hollow porous microspheres.

25. The dispersion of claim 18 wherein said bioactive agent is selected from the group consisting of antiallergics, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, leukotriene inhibitors or antagonists, antihistamines, anti-inflammatories, antineoplastics, anticholinergics, anesthetics, anti-tuberculars, imaging agents, cardiovascular agents, enzymes, steroids, genetic material, viral vectors, antisense agents, proteins, peptides and combinations thereof.

26. The dispersion of claim 25 wherein the bioactive agent is gentamicin.

27. The dispersion of claim 18 wherein said perforated microstructures have a mean density selected to provide a density differential with that of the suspension medium of less than 0.6 g/cm.sup.3.

28. The dispersion of claim 18 wherein said liquid fluorochemical has a vapor pressure 5-760 torr at 25.degree. C.

29. The dispersion of claim 28 wherein said liquid fluorochemical comprises perfluorooctyl bromide.

30. A method for delivering one or more bioactive agents comprising the steps of: providing a stabilized dispersion comprising a nonaqueous suspension medium having dispersed therein a plurality of perforated microstructures, which displace a volume of suspension medium, wherein the volume of suspension medium displaced by the perforated microstructure is less than 70% of the average particle volume of the perforated microstructure, and wherein said perforated microstructures comprise a bioactive agent; and administering by liquid dose instillation a therapeutically effective amount of said stabilized dispersion to at least a portion of the nasal or pulmonary passages of a patient in need thereof.

31. A stabilized dispersion for the delivery of a bioactive agent by liquid dose instillation comprising a nonaqueous suspension medium having dispersed therein a plurality of perforated microstructures, which displace a volume of suspension medium, comprising at least one bioactive agent wherein the volume of suspension medium displaced by the perforated microstructure is less than 70% of the average particle volume of the perforated microstructure.
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