Aripiprazole formulations having increased injection speeds
The present invention relates to pharmaceutical compositions comprising a compound of Formula (I) that are useful for the intramuscular delivery of antipsychotic drugs using rapid injection rates.
1. A method of treating schizophrenia in a subject in need thereof, comprising intramuscularly administering to said subject a therapeutically effective amount of a pharmaceutical composition at a rapid and continuous rate, wherein said pharmaceutical composition comprises:
(a) 24-30 weight percent of a compound of Formula (I):
wherein n is an integer between 4 and 14;
(b) 0.3-0.4 weight percent sorbitan laurate;
(c) 0.1-0.3 weight percent polysorbate 20; and
(d) an aqueous vehicle;
wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition; and
wherein the pharmaceutical composition has a total injection volume from 1.0 mL to 10 mL.
2. The method of claim 1 , wherein the said pharmaceutical composition comprises:
(a) about 26.6 weight percent Compound 1:
(b) about 0.37 weight percent sorbitan laurate;
(c) about 0.15 weight percent polysorbate 20; and
(d) an aqueous vehicle;
wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition.
3. The method of claim 1 , wherein the pharmaceutical composition has a total injection volume 3.2 mL, 2.4 mL, or 1.6 mL.
4. The method of claim 1 , wherein approximately 3.2 mL of the pharmaceutical composition is injected within 10 seconds, or wherein approximately 2.4 mL of the pharmaceutical composition is injected within 8 seconds, or wherein approximately 1.6 mL of the pharmaceutical composition is injected within 5 seconds.
5. The method of claim 1 , wherein the intramuscular injection rate is selected from the group consisting of: 0.4 mL/s, 0.5 mL/s, 0.6 mL/s, 0.7 mL/s, 0.8 mL/s, and 0.9 mL/s.
6. A method of treating bipolar disorder in a subject in need thereof, comprising intramuscularly administering to said subject a therapeutically effective amount of a pharmaceutical composition at a rapid and continuous rate, wherein said pharmaceutical composition comprises:
(a) 24-30 weight percent of a compound of Formula (I):
wherein n is an integer between 4 and 14;
(b) 0.3-0.4 weight percent sorbitan laurate;
(c) 0.1-0.3 weight percent polysorbate 20; and
(d) an aqueous vehicle;
wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition; and
wherein the pharmaceutical composition has a total injection volume from 1.0 mL to 10 mL.
7. The method of claim 6 , wherein the said pharmaceutical composition comprises:
(a) about 26.6 weight percent Compound 1:
(b) about 0.37 weight percent sorbitan laurate;
(c) about 0.15 weight percent polysorbate 20; and
(d) an aqueous vehicle;
wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition.
8. The method of claim 6 , wherein the pharmaceutical composition has a total injection volume 3.2 mL, 2.4 mL, or 1.6 mL.
9. The method of claim 6 , wherein approximately 3.2 mL of the pharmaceutical composition is injected within 10 seconds, or wherein approximately 2.4 mL of the pharmaceutical composition is injected within 8 seconds, or wherein approximately 1.6 mL of the pharmaceutical composition is injected within 5 seconds.
10. The method of claim 6 , wherein the intramuscular injection rate is selected from the group consisting of: 0.4 mL/s, 0.5 mL/s, 0.6 mL/s, 0.7 mL/s, 0.8 mL/s, and 0.9 mL/s.
11. A method of treating depression in a subject in need thereof, comprising intramuscularly administering to said subject a therapeutically effective amount of a pharmaceutical composition at a rapid and continuous rate, wherein said pharmaceutical composition comprises:
(a) 24-30 weight percent of a compound of Formula (I):
wherein n is an integer between 4 and 14;
(b) 0.3-0.4 weight percent sorbitan laurate;
(c) 0.1-0.3 weight percent polysorbate 20; and
(d) an aqueous vehicle;
wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition; and
wherein the pharmaceutical composition has a total injection volume from 1.0 mL to 10 mL.
12. The method of claim 11 , wherein the said pharmaceutical composition comprises:
(a) about 26.6 weight percent Compound 1:
(b) about 0.37 weight percent sorbitan laurate;
(c) about 0.15 weight percent polysorbate 20; and
(d) an aqueous vehicle;
wherein the percentages of (a), (b), and (c) are relative to the total weight of the composition.
13. The method of claim 11 , wherein the pharmaceutical composition has a total injection volume 3.2 mL, 2.4 mL, or 1.6 mL.
14. The method of claim 11 , wherein approximately 3.2 mL of the pharmaceutical composition is injected within 10 seconds, or wherein approximately 2.4 mL of the pharmaceutical composition is injected within 8 seconds, or wherein approximately 1.6 mL of the pharmaceutical composition is injected within 5 seconds.
15. The method of claim 11 , wherein the intramuscular injection rate is selected from the group consisting of: 0.4 mL/s, 0.5 mL/s, 0.6 mL/s, 0.7 mL/s, 0.8 mL/s, and 0.9 mL/s.