US 12,220,418 B2
Olanzapine compositions and methods of use
Mélodie Carluer, Jacou (FR); Maria Ferrand, Aniane (FR); Irina Cherniakov, Rehovot (IL); and Anna Elgart Valitsky, Kfar-Saba (IL)
Assigned to MEDINCELL S.A., Jacou (FR)
Filed by MEDINCELL S.A., Jacou (FR)
Filed on Jun. 7, 2024, as Appl. No. 18/736,965.
Application 18/736,965 is a continuation of application No. 18/409,158, filed on Jan. 10, 2024.
Claims priority of provisional application 63/516,283, filed on Jul. 28, 2023.
Claims priority of provisional application 63/479,267, filed on Jan. 10, 2023.
Prior Publication US 2024/0325408 A1, Oct. 3, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/5513 (2006.01); A61K 9/00 (2006.01); A61K 47/20 (2006.01); A61K 47/22 (2006.01); A61K 47/34 (2017.01); A61P 25/18 (2006.01)
CPC A61K 31/5513 (2013.01) [A61K 9/0019 (2013.01); A61K 47/20 (2013.01); A61K 47/22 (2013.01); A61K 47/34 (2013.01); A61P 25/18 (2018.01)] 24 Claims
OG exemplary drawing
 
1. A method of treating schizophrenia in a patient in need thereof, the method comprising subcutaneously administering to the abdomen or upper arm of the patient, once per 28±5 days, 0.9-1.5 mL of a pharmaceutical composition comprising 305 mg of olanzapine per gram of composition, wherein the composition comprises:
30%-32% (w/w) of olanzapine;
52%-54% (w/w) of dimethyl sulfoxide;
12%-14% (w/w) of a diblock copolymer comprising polylactic acid and polyethylene glycol and having a number average molecular weight of 6.5 to 12.5 kg/mol and comprising 75%-84% by weight (w/w) polylactic acid; and
3%-3.5% (w/w) of a triblock copolymer comprising polylactic acid and polyethylene glycol and having a number average molecular weight of 6 to 13 kg/mol and comprising 83%-88% by weight (w/w) polylactic acid;
and wherein the diblock copolymer and triblock copolymer together comprise 15%-17.5% by weight (w/w) of the composition;
wherein the administration of the composition to the patient by subcutaneous injection results in
the patient having an olanzapine plasma Cmax within 11-14 days after the administration;
an olanzapine plasma Cmax of less than 100 ng/mL after any subcutaneous injection administered in the method;
a dose-normalized ratio of AUC∞ after any subcutaneous dose of the composition to the AUCtau of oral olanzapine calculated for 28 days is between 0.97-1.29; and
an olanzapine plasma concentration of at least 10 ng/ml for at least 21 days of the 30 days following any of the subcutaneous injections.