IP Library › Patent Application 16859443
Patent Application
App. No. 16/859,443

DEPOT FORMULATIONS

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Patent No.
US None
App. No.
16/859,443
Abstract

Pharmaceutical compositions comprising an active pharmaceutical ingredient, a high viscosity liquid carrier material, a hydrophobic solvent, and a hydrophilic solvent are disclosed. Also disclosed are methods of manufacturing and using the compositions. The compositions are suitable for use, e.g., as depot formulations.

Claims (44)

1 . A composition comprising:

sirolimus present in an amount ranging from about 1 wt % to about 10 wt %, based on weight of the composition;

sucrose acetate isobutyrate (SAIB) present in an amount ranging from about 0.1 wt % to about 10 wt %, based on weight of the composition;

benzyl benzoate present in an amount ranging from about 30 wt % to about 60 wt %, based on weight of the composition;

ethanol present in an amount ranging from about 1 wt % to about 10 wt %, based on weight of the composition;

polyethylene glycol (PEG) present in an amount ranging from about 30 wt % to about 60 wt %, based on weight of the composition; and

vitamin E present in an amount ranging up to 5 wt %, based on weight of the composition.

2 - 5 . (canceled)

6 . The composition of claim 1 , wherein the composition comprises from about 1 wt % to about 5 wt % of the sirolimus, based on weight of the composition.

7 - 9 . (canceled)

10 . The composition of claim 1 , wherein the benzyl benzoate is present in an amount ranging from about 35 wt % to about 45 wt %, based on weight of the composition.

11 - 20 . (canceled)

21 . The composition of claim 1 , wherein the PEG is present in an amount ranging from about 35 wt % to about 50 wt %, based on weight of the composition.

22 . The composition of claim 21 , wherein the PEG is present in an amount ranging from about 40 wt % to about 50 wt %, based on weight of the composition.

23 - 24 . (canceled)

25 . The composition of claim 1 , wherein the vitamin E is present in an amount ranging from about 0.1 wt % to about 5 wt %, based on weight of the composition.

26 . The composition of claim 1 , wherein the vitamin E is present in an amount ranging from about 0.5 wt % to about 2 wt %, based on weight of the composition.

27 . The composition of claim 1 , wherein the composition has a weight ratio of SAIB:vitamin E ranging from about 0.5 to about 10.

28 . (canceled)

29 . The composition of claim 1 , wherein:

the sirolimus is present in an amount ranging from about 1 wt % to about 5 wt %, based on weight of the composition;

the benzyl benzoate is present in an amount ranging from about 30 wt % to about 45 wt %, based on weight of the composition;

the PEG is present in an amount ranging from about 40 wt % to about 50 wt %, based on weight of the composition; and

the vitamin E is present in an amount ranging from about 0.5 wt % to about 2 wt %, based on weight of the composition.

30 . The composition of claim 1 , the composition consisting essentially of:

sirolimus in an amount ranging from about 1 wt % to about 5 wt %, based on weight of the composition;

SAM in an amount ranging from about 0.1 wt % to about 10 wt %, based on weight of the composition;

benzyl benzoate in an amount ranging from about 30 wt % to about 45 wt %, based on weight of the composition;

ethanol in an amount ranging from about 1 wt % to about 10 wt %, based on weight of the composition;

PEG400 in an amount ranging from about 40 wt % to about 50 wt %, based on weight of the composition; and

vitamin E in an amount ranging from about 0.5 wt % to about 2 wt %, based on weight of the composition.

31 - 33 . (canceled)

34 . The composition of claim 1 , wherein the composition is pharmaceutically acceptable.

35 - 38 . (canceled)

39 . The composition of claim 1 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.

40 . The composition of claim 6 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.

41 . The composition of claim 10 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.

42 . The composition of claim 21 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.

43 . The composition of claim 22 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.

44 . The composition of claim 25 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.

45 . The composition of claim 26 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.

46 . The composition of claim 27 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.

47 . The composition of claim 29 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.

48 . The composition of claim 30 , wherein at least 98% of the sirolimus in the composition remains after storage in a 2 mL crimp sealed glass vial for 18 weeks at 5° C./60% RH.