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Claims for Patent: 6,592,903

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Claims for Patent: 6,592,903

Title: Nanoparticulate dispersions comprising a synergistic combination of a polymeric surface stabilizer and dioctyl sodium sulfosuccinate
Abstract:Disclosed are solid dose nanoparticulate compositions comprising a poorly soluble active agent, at least one polymeric surface stabilizer, and dioctyl sodium sulfosuccinate (DOSS). The solid dose compositions exhibit superior redispersibility of the nanoparticulate composition upon administration to a mammal, such as a human or animal. The invention also describes methods of making and using such compositions.
Inventor(s): Ryde; Niels P. (Malvern, PA), Ruddy; Stephen B. (Schwenksville, PA)
Assignee: Elan Pharma International Ltd. (Shannon, IE)
Application Number:10/075,443
Patent Claims: 1. A nanoparticulate dispersion comprising: (a) a poorly soluble active agent; (b) at least one polymeric surface stabilizer adsorbed on the surface of the active agent; and (c) about 0.1% to about 20% w/w of dioctyl sodium sulfosuccinate (DOSS), wherein the effective average particle size of the poorly soluble active agent in the nanoparticulate dispersion is less than about 1 micron.

2. The dispersion of claim 1, wherein the active agent is present in an amount of about 99.8% to about 0.1% (w/w).

3. The dispersion of claim 1, wherein the active agent is present in an amount of about 80% to about 5% (w/w).

4. The dispersion of claim 1, wherein the active agent is present in an amount of about 50% to about 10% (w/w).

5. The dispersion of claim 1, wherein the at least one polymeric surface stabilizer is present in an amount of about 0.01% to about 90% (w/w).

6. The dispersion of claim 1, wherein the at least one polymeric surface stabilizer is present in an amount of about 1% to about 75% (w/w).

7. The dispersion of claim 1, wherein the at least one polymeric surface stabilizer is present in an amount of about 10% to about 60% (w/w).

8. The dispersion of claim 1, wherein DOSS is present in an amount of about 1% to about 10% (w/w).

9. The dispersion of claim 1, wherein the effective average particle size of the nanoparticulate dispersion is less than about 800 nm.

10. The dispersion of claim 1, wherein the effective average particle size of the nanoparticulate dispersion is less than about 600 nm.

11. The dispersion of claim 1, wherein the effective average particle size of the nanoparticulate dispersion is less than about 400 nm.

12. The dispersion of claim 1, wherein the effective average particle size of the nanoparticulate dispersion is less than about 200 nm.

13. The dispersion of claim 1, wherein the active agent is selected from the group consisting of a crystalline phase, a semi-crystalline phase, and an amorphous phase.

14. The dispersion of claim 1, wherein the active agent is selected from the group consisting of proteins, peptides, nucleotides, anti-obesity drugs, nutraceuticals, corticosteroids, elastase inhibitors, analgesics, anti-fungals, oncology therapies, anti-emetics, analgesics, cardiovascular agents, anti-inflammatory agents, anthelmintics, anti-arrhythmic agents, antibiotics, anticoagulants, antidepressants, antidiabetic agents, antiepileptics, antihistamines, antihypertensive agents, antimuscarinic agents, antimycobacterial agents, antineoplastic agents, immunosuppressants, antithyroid agents, antiviral agents, anxiolytics, sedatives, astringents, beta-adrenoceptor blocking agents, blood products and substitutes, cardiac inotropic agents, contrast media, corticosteroids, cough suppressants, diagnostic agents, diagnostic imaging agents, diuretics, dopaminergics, haemostatics, immuriological agents, lipid regulating agents, muscle relaxants, parasympathomimetics, parathyroid calcitonin and biphosphonates, prostaglandins, radio-pharmaceuticals, sex hormones, anti-allergic agents, stimulants and anoretics, sympathomimetics, thyroid agents, vasodilators, and xanthines.

15. The dispersion of claim 1, wherein the active agent is ketoprofen.

16. The dispersion of claim 1, wherein the active agent is a MAP kinase inhibitor.

17. The dispersion of claim 1, wherein the active agent is an angiogenesis inhibitor.

18. The dispersion of claim 1, wherein the at least one polymeric surface stabilizer is selected from the group consisting of polyvinylpyrrolidone, cellulose ethers, polysaccharides, random copolymers of vinyl acetate and vinyl pyrrolidone, polyvinyl alcohol, and copolymers of vinyl acetate and vinyl alcohol.

19. The dispersion of claim 18, wherein the at least one polymeric surface stabilizer is selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methylcellulose, carboxymethyl cellulose, methyl cellulose, hydroxyethyl cellulose, dextrin, guar gum, starch, and a copolymer of 1-vinyl-2-pyrrolidone and vinyl acetate in a mass proportion of 3:2.

20. A pharmaceutical composition comprising the dispersion of claim 1, and one or more pharmaceutically acceptable excipients.

21. A method of making a nanoparticulate dispersion comprising: (a) dispersing particles of a poorly soluble active agent in a liquid dispersion medium; and (b) applying mechanical means in the presence of grinding media to reduce the effective average particle size of the active agent in the liquid dispersion medium to less than about 1 micron, wherein at least one polymeric surface stabilizer and dioctyl sodium sulfosuccinate are added to the liquid dispersion medium before or after milling.

22. The method of claim 21, wherein the active agent is present in an amount of about 99.8 to about 0.1% (w/w).

23. The method of claim 21, wherein the at least one polymeric surface stabilizer is present in an amount of about 0.01% to about 90% (w/w).

24. The method of claim 21, wherein DOSS is added in an amount of about 0.1% to about 20% (w/w).

25. The method of claim 21, wherein DOSS is added in an amount of about 1.0% to about 10% (w/w).

26. The method of claim 21, wherein the active agent is selected from the group consisting of a crystalline phase drug, a semi-crystalline phase drug, and an amorphous phase drug.

27. The method of claim 21, wherein the effective average particle size of the resultant nanoparticulate dispersion is less than about 800 nm.

28. The method of claim 21, wherein the effective average particle size of the resultant nanoparticulate dispersion is less than about 600 nm.

29. The method of claim 21, wherein the effective average particle size of the resultant nanoparticulate dispersion is less than about 400 nm.

30. The method of claim 21, wherein the effective average particle size of the nanoparticulate dispersion is less than about 200 nm.

31. The dispersion of claim 1, wherein the active agent is selected from the group consisting of ketoprofen, a MAP kinase inhibitor, and an angiogenesis inhibitor.

32. The pharmaceutical composition of claim 20, wherein the active agent is selected from the group consisting of ketoprofen, a MAP kinase inhibitor, and an angiogenesis inhibitor.

33. The method of claim 21, wherein the active agent is selected from the group consisting of ketoprofen, a MAP kinase inhibitor, and an angiogenesis inhibitor.
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