Claims for Patent: 12,427,104

Summary for Patent: 12,427,104

Title:	Injectable carboplatin formulations
Abstract:	Described herein are injectable carboplatin formulations, comprising: about 10 mg/mL of carboplatin; and a pharmaceutically acceptable vehicle; wherein the formulation has a pH of from about 5 to about 7; wherein the formulation has a dissolved oxygen level of not less than about 28 ppm; wherein the formulation is filled in a vial at a fill volume of from about 1 mL to about 70 mL in a vial having a capacity of from about 1 mL to about 100 mL; wherein the vial has head space ranging from about 20% to about 82%; and wherein the headspace comprises oxygen gas in an amount effective to maintain a 1,1-cyclobutanedicarboxylic acid level of not more than 1.0%, based on the weight of carboplatin, and a total degradation impurity level at not more than 2.5%, based on the weight of carboplatin, when stored at room temperature for 24 months.
Inventor(s):	Mukteeshwar Gande, Praveen Reddy Billa, Venkata S. Varanasi, Samir Chimanlal Mehta
Assignee:	Ingenus Pharmaceuticals LLC
Application Number:	US19/097,811
Patent Claims:	1. A stable injectable carboplatin formulation, comprising: about 10 mg/mL of carboplatin, or a pharmaceutically acceptable derivative thereof; a pharmaceutically acceptable vehicle; wherein the formulation has a pH of from about 5 to about 7; wherein the formulation has a dissolved oxygen level of not less than about 28 ppm; wherein the formulation is filled in a glass vial selected from: (i) a vial having a capacity of about 5 mL and a fill volume of from about 2.15 mL to about 2.35 mL with a headspace of from about 77% to about 82%; (ii) a vial having a capacity of about 10 mL and a fill volume of from about 8.2 mL to about 8.8 mL with a headspace of from about 47% to about 58%; and (iii) a vial having a capacity of about 50 mL and a fill volume of from about 50.2 mL to about 55.3 mL with a headspace of from about 20% to about 30%; and wherein the headspace comprises oxygen gas in an amount effective to maintain a 1,1-cyclobutanedicarboxylic acid level of not more than 1.0%, based on the weight of carboplatin, and a total degradation impurity level at not more than 2.5%, based on the weight of carboplatin, when stored at room temperature for 24 months. 2. The formulation of claim 1, wherein the pharmaceutically acceptable vehicle comprises Water for Injection (WFI). 3. The formulation of claim 1, wherein the formulation provides a Waste Reduction Efficiency Factor (WREF) of up to about 500%. 4. The formulation of claim 1, wherein the formulation retains its stability for at least eight (8) hours after dilution with 5% D5W or 0.9% Sodium Chloride Injection, USP. 5. A method for enhancing patient and/or healthcare provider compliance with an injectable carboplatin formulation, comprising: (i) preparing an injectable carboplatin formulation according to claim 1; (ii) calculating a therapeutically effective dose of carboplatin based on body surface area (BSA), glomerular filtration rate (GFR), and/or target area under the curve (AUC); (iii) administering said therapeutically effective dose of carboplatin to a patient in need thereof; wherein said therapeutically effective dose of carboplatin is provided in from about 1 to about 15 vials; and wherein said injectable carboplatin formulation according to claim 1 provides a WREF up to about 500%. 6. A process for preparing a formulation according to claim 1, comprising the steps of: (i) admixing carboplatin, or a pharmaceutically acceptable derivative thereof, with an oxygen enriched aqueous solvent to form a solution wherein the level of dissolved oxygen in said solution is not less than 28 ppm; (ii) sterilizing said solution; (iii) filling the sterilized solution of step (ii) into a glass vial, flushing and filling the available head space with oxygen; and (iv) stoppering and sealing said glass vial. 7. A method for treating recurrent ovarian carcinoma, comprising: administering a therapeutic dose of an injectable carboplatin formulation according to claim 1 to a patient in need thereof, on day 1, every 4 weeks; wherein said therapeutic dose of carboplatin is 360 mg/m2 IV; and wherein said therapeutic dose is provided by from about 1 vial to about 15 vials; and wherein the method provides a WREF up to about 500%. 8. The method according to claim 7, wherein the therapeutic dose is provided by from about 1 vial to about 10 vials. 9. A method for treating advanced ovarian cancer, comprising: administering a therapeutic dose of an injectable carboplatin formulation according to claim 1, in combination with cyclophosphamide, to a patient in need thereof, on day 1, every 4 weeks for 6 cycles; wherein said therapeutic does of carboplatin is 300 mg/m2 IV; and wherein said therapeutic dose is provided using from about 1 vial to about 15 vials; and wherein the method provides a WREF up to about 500%. 10. The method according to claim 9, wherein the therapeutic dose is provided by from about 1 vial to about 10 vials.