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Details for Patent: 7,871,598

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Details for Patent: 7,871,598

Title:Stable metal ion-lipid powdered pharmaceutical compositions for drug delivery and methods of use
Abstract: Microparticle compositions comprising metal ion-lipid complexes for drug delivery are described including methods of making the microparticle compositions and methods of treating certain conditions and disease states by administering the microparticle compositions. The metal ion-lipid complexes can be combined with various drugs or active agents for therapeutic administration. The microparticle compositions of the present invention have superior stability to other microparticle compositions resulting in a microparticle composition with longer shelf life and improved dispersability. The microparticle compositions of the present invention have a transition temperature T.sub.m of at least 20.degree. C. above the recommended storage temperature (Tst) for drug delivery.
Inventor(s): Dellamary; Luis A. (San Marcos, CA), Riess; Jean (Falicon, FR), Schutt; Ernest G. (San Diego, CA), Weers; Jeffry G. (Half Moon Bay, CA), Tarara; Thomas E. (Burlingame, CA)
Assignee: Novartis AG (Basel, CH)
Filing Date:May 10, 2000
Application Number:09/568,818
Claims:1. A powder composition comprising a plurality of microparticles, the microparticles comprising an active agent and a metal ion-lipid complex, and the powder composition has a metal ion concentration of greater than 0 and up to and including 25% w/w, and a lipid concentration of 25-90% w/w, and wherein the density of the microparticles as measured by He displacement is 0.5-2.0 g/ml and the T.sub.g of the microparticles is at least 2.degree. C. greater than that of microparticles without the metal ion.

2. The powder composition of claim 1 wherein the lipid component comprises a mixture of at least two lipids.

3. The powder composition of claim 1 wherein the lipid comprises a phospholipid.

4. The powder composition of claim 1 wherein the metal ions are chosen from the group consisting of lanthanide metals, actinide metals, group IIa and IIIb metals, transition metals or mixtures thereof.

5. The powder composition of claim 4 wherein the metal ion is chosen from the group consisting of calcium, zinc, aluminum, iron and magnesium, their water soluble salts and mixtures thereof.

6. The powder composition of claim 1 wherein the metal ion has more than a one positive charge.

7. The powder composition of claim 3 wherein the phospholipid is selected from the group consisting of dipalmitoylphosphatidylcholine, distearoylphosphatidylcholine, and dimyristoylphosphatidylcholine.

8. The powder composition of claim 7 wherein the microparticle has a phospholipid concentration from about 20-90% w/w.

9. The powder composition of claim 1 wherein the active agent is selected from the group consisting of antiallergics, antifungals, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, leukotriene inhibitors or antagonists, antihistamines, antiinflammatories, antineoplastics, anticholingerics, anesthetics, antituberculars, imaging agents, cardiovascular agents, enzymes, steroids, DNA, RNA, viral vectors, antisense agents, proteins, peptides, immunoglobulins, and combinations thereof.

10. The powder composition of claim 1 wherein the active agent is selected from the group consisting of albuterol, budesonide, fluticasone, salmeterol, formoterol, nicotine, triamcinolone, dexamethasone, beclomethasone, gentamicin, ciprofloxacin, paclitaxel, amphotericin, amikacin, tobramycin, insulin, human growth hormone, and salts thereof.

11. The powder composition of claim 1 further comprising a surfactant selected from the group consisting of nonionic detergents, nonionic block copolymers, ionic surfactants and combinations thereof.

12. The powder composition of claim 11 wherein the surfactant is selected from the group consisting of sorbitan esters, ethoxylated sorbitan esters, fatty acid salts, sugar esters, ethylene oxides, and combinations thereof.

13. The powder composition of claim 1 further comprising a polymer selected from the group consisting of polysaccharides, polyvinyl alcohol, polyvinyl pyrrolidone, polylactides, polyglycolides, polyethylene glycol, cyclodextrins, starches, carboxymethylcellulose, hydroxylmethyl cellulose or mixtures thereof.

14. The powder composition of claim 1 wherein the microparticles are administered by inhalation.

15. The powder composition of claim 14 comprising a mean volume aerodynamic particle size of 0.5-7 microns.

16. The powder composition of claim 15 wherein the microparticle is administered via a dry powder inhaler.

17. The powder composition of claim 15 wherein the microparticle is administered via a metered dose inhaler.

18. The powder composition of claim 1 in table or capsule form for oral administration.

19. A powder composition comprising a plurality of microparticles, the microparticles comprising an active agent, a metal ion, and a phospholipid, wherein the metal ion forms a coordination bond with the phospholipid, and the powder composition has a metal ion concentration of greater than 0 and up to and including 25% w/w, and a phospholipid concentration of 25-90% w/w, and wherein the density of the particle as measured by He displacement is at least 0.5-2.0 g/ml and the transition temperature of the microparticle exceeds its storage temperature by at least 20.degree. C.

20. The powder composition of claim 19 wherein the lipid component is comprised of a mixture of at least two lipids.

21. The powder composition of claim 19 wherein the lipid comprises a phospholipid.

22. The powder composition of claim 21 wherein the phospholipid is selected from the group consisting of dipalmitoylphosphatidylcholine, distearoylphosphatidylcholine, and dimyristoylphosphatidylcholine.

23. The powder composition of claim 22 wherein the microparticle has a phospholipid concentration of from about 20-90% w/w.

24. The powder composition of claim 19 wherein the metal ions are chosen from the group consisting of lanthanide metals, actinide metals, group IIa and IIIb metals, transition metals or mixtures thereof.

25. The powder composition of claim 24 wherein the metal ion is chosen from the group consisting of calcium, zinc, aluminum, iron and magnesium, their water soluble salts and mixtures thereof.

26. The powder composition of claim 19 wherein the metal ion has more than a one positive charge.

27. The powder composition of claim 19 wherein the active agent is selected from the group consisting antiallergics, antifungals, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, leukotriene inhibitors or antagonists, antihistamines, antiinflammatories, antineoplastics, anticholingerics, anesthetics, antituberculars, imaging agents, cardiovascular agents, enzymes, steroids, DNA, RNA, viral vectors, antisense agents, proteins, peptides, immunoglobulins, and combinations thereof.

28. The powder composition of claim 19 wherein the active agent is selected from the group consisting of albuterol, budesonide, fluticasone, salmeterol, formoterol, nicotine, triamcinolone, dexamethasone, beclomethasone, gentamicin, ciprofloxacin, paclitaxel, amphotericin, amikacin, tobramycin, insulin, human growth hormone, and salts thereof.

29. The powder composition of claim 19 further comprising a surfactant selected from the group consisting of nonionic detergents, nonionic block copolymers, ionic surfactants and combinations thereof.

30. The powder composition of claim 29 wherein the surfactant is selected from the group consisting of sorbitan esters, ethoxylated sorbitan esters, fatty acid salts, sugar esters, ethylene oxides, and combinations thereof.

31. The powder composition of claim 19 further comprising a polymer selected from the group consisting of polysaccharides, polyvinyl alcohol, polyvinyl pyrrolidone, polylactides, polyglycolides, polyethylene glycol, cyclodextrins, starches, carboxymethylcellulose, hydroxymethyl cellulose or mixtures thereof.

32. The powder composition of claim 1 wherein the microparticles are administered by inhalation.

33. The powder composition of claim 32 comprising a mean volume aerodynamic particle size of 0.5-7 microns.

34. The powder composition of claim 32 wherein the microparticle is administered via a dry powder inhaler.

35. The powder composition of claim 32 wherein the microparticle is administered via a metered dose inhaler.

36. The powder composition of claim 19 in tablet or capsule form for oral administration.

37. The powder composition of claim 19 wherein the T.sub.g of the microparticle is at least 2.degree. C. greater than that of particles without the metal ion.

38. The powder composition of claim 1 wherein the lipid is zwitterionic.

39. The powder composition of claim 19 wherein the lipid is zwitterionic.

40. The powder composition of claim 1 wherein the microparticles are suspended in a fluorocarbon or fluoroalkane containing propellant.

41. The powder composition of claim 19 wherein the microparticles are suspended in a fluorocarbon or fluoroalkane containing propellant.

42. A powder composition comprising a plurality of microparticles, the microparticles comprising an active agent and a metal ion-lipid complex, and the powder composition has a metal ion concentration of greater than 0 and up to and including 25% w/w, and a lipid concentration of 25-90% w/w, wherein the T.sub.g of the microparticles is at least 2.degree. C. greater than that of microparticles without the metal ion, and wherein the active agent is selected from the group consisting of albuterol, budesonide, fluticasone, salmeterol, formoterol, nicotine, triamcinolone, dexamethasone, beclomethasone, gentamicin, ciprofloxacin, paclitaxel, amphotericin, amikacin, tobramycin, insulin, human growth hormone, and salts thereof.

43. The powder composition of claim 42 wherein the microparticles are suspended in a fluorocarbon or fluoroalkane containing propellant.
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