.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 8,722,700

« Back to Dashboard

Claims for Patent: 8,722,700

Title:CCI-779 formulations for parenteral administration
Abstract: This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent.
Inventor(s): Rubino; Joseph T. (Towaco, NJ), Siskavich; Victoria (Lyon Mountain, NY), Harrison; Maureen M. (Sugar Loaf, NY), Gandhi; Pooja (Highland Mills, NY)
Assignee: Wyeth LLC (Madison, NJ)
Application Number:13/892,389
Patent Claims: 1. A method for administering a parenteral CCI-779 formulation to a subject in need thereof, said method comprising: (i) mixing CCI-779 with about 15 to about 60% w/v of dehydrated ethanol, about 0.01 to about 0.1% of d,1-.alpha.-tocopherol, about 0.001 to about 0.005% w/v of citric acid, and about 15 to about 60% w/v of propylene glycol to provide a cosolvent concentrate comprising about 1 to about 25 mg/mL of CCI-779; (ii) mixing about 15 to about 60% w/v of polysorbate 80, about 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol to provide a diluent; (iii) mixing said cosolvent concentrate and said diluent; and (iv) administering the product of step (iii) to said subject.

2. The method according to claim 1, wherein the ratio of said cosolvent concentrate to diluent is about 1:1.5 to about 1:2.

3. The method according to claim 1, wherein said parenteral CCI-779 formulation is administered by direct injection.

4. The method according to claim 1, further comprising: (v) mixing the product of step (iii) with water.

5. The method according to claim 4, wherein said water is a sterile infusion fluid.

6. The method according to claim 5, wherein said parenteral CCI-779 formulation is administered by intravenous infusion.

7. The method according to claim 1, wherein said cosolvent concentrate comprises about 25 mg/mL CCI-779, about 40% w/v of dehydrated ethanol, about 0.075% w/v of d,1-.alpha.-tocopherol, 0.0025% w/v of citric acid, and about 35% w/v propylene glycol.

8. The method according to claim 1, wherein said diluent comprises 20% w/v of dehydrated ethanol, about 40% w/v of polysorbate 80, and about 40% w/v of polyethylene glycol 400.

9. A CCI-779 direct injection fluid, said fluid comprising: (i) about 1 to about 25 mg/mL of CCI-779; (ii) about 0.01 to about 0.1% w/v of d,1-.alpha.-tocopherol; (iii) about 0.001 to about 0.005% w/v of citric acid; (iv) about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol; and (v) about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400.

10. The CCI-779 direct injection fluid according to claim 9, wherein the ratio of dehydrated ethanol to propylene glycol in component (vi) is about 1.4:1.

11. The CCI-779 direct injection fluid according to claim 9, wherein the ratio of polysorbate 80 to polyethylene glycol 400 in component (v) is about 1:1.

12. The CCI-779 direct injection fluid according to claim 9, wherein the ratio of mixture (iv) to mixture (i) is about 50:1.

13. The CCI-779 direct injection fluid according to claim 9, wherein the ratio of mixture (vi) to component (i) is about 50:1.

14. The CCI-779 direct injection fluid according to claim 9, comprising about 1% w/v of CCI-779, about 0.03% w/v of d,1-.alpha.-tocopherol, about 0.001% w/v of citric acid, about 28% w/v of dehydrated ethanol, about 20% w/v of propylene glycol, about 24% w/v of polysorbate 80, and about 25% w/v of polyethylene glycol 400.

15. A CCI-779 intravenous infusion solution comprising: (i) about 1 to about 25 mg/mL of CCI-779, about 0.01 to about 0.1% w/v of d,1-.alpha.-tocopherol, about 0.001 to about 0.005% w/v of citric acid, about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol, and about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400; and (ii) a sterile infusion fluid.

16. The CCI-779 intravenous infusion solution according to claim 15, wherein the ratio of dehydrated ethanol to propylene glycol is about 1.4:1.

17. The CCI-779 intravenous infusion solution according to claim 15, wherein the ratio of polysorbate 80 to polyethylene glycol 400 is about 1:1.

18. The CCI-779 intravenous infusion solution according to claim 15, wherein the ratio of the combination of dehydrated ethanol and propylene glycol to CCI-779 is about 50:1.

19. The CCI-779 intravenous infusion solution according to claim 15, wherein the ratio of the combination of polysorbate 80 and polyethylene glycol 400 to CCI-779 is about 50:1.

20. The CCI-779 intravenous infusion solution according to claim 15, wherein said component (i) comprises about 1% w/v of CCI-779, about 0.03% w/v of d,1-.alpha.-tocopherol, about 0.001% w/v of citric acid, about 28% w/v of dehydrated ethanol, about 20% w/v of propylene glycol, about 24% w/v of polysorbate 80, and about 25% w/v of polyethylene glycol 400.

21. A method of solubilizing CCI-779 in a solution, said method comprising mixing about 1 to about 25 mg/mL of CCI-779, about 0.01 to about 0.1% w/v of d,1-.alpha.-tocopherol, about 0.001 to about 0.005% w/v of citric acid, about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol, and about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400.

22. A method of stabilizing a solution comprising CCI-779, said method comprising mixing about 1 to about 25 mg/mL of said CCI-779 with about 15 to about 60% w/v of dehydrated ethanol, about 0.01 to about 0.1% of of d,1-.alpha.-tocopherol, about 0.001 to about 0.005% w/v of critic acid, and about 15 to about 60% w/v of propylene glycol.

23. A method of stabilizing a solution comprising CCI-779, said method comprising mixing about 1 to about 25 mg/mL of said CCI-779 with about 0.01 to about 0.1% w/v of d,1-.alpha.-tocopherol, about 0.001 to about 0.005% w/v of citric acid, about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol, and about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400.

24. A method of preventing precipitation of CCI-779 in an aqueous infusion solution or blood, said method comprising: (i) mixing CCI-779 with about 15 to about 60% w/v of dehydrated ethanol, about 0.01 to about 0.1% of d,1-.alpha.-tocopherol, about 0.001 to about 0.005% w/v of citric acid, and about 15 to about 60% w/v of propylene glycol to provide a cosolvent concentrate comprising about 1 to about 25 mg/mL of CCI-779; (ii) mixing about 15 to about 60% w/v of polysorbate 80, about 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol to provide a diluent; (iii) mixing said cosolvent concentrate and said diluent; and (iv) adding the product of step (iii) to said aqueous infusion solution or blood.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc