IP Library Granted Patent US 10,993,952
Granted Patent B2
US 10,993,952 · App. 15/551,507 · Granted May 4, 2021

Stable ready to use cyclophosphamide liquid formulations

Inventors: Kocherlakota Chandrashekhar (Secunderabad, IN); Banda Nagaraju (Hyderabad, IN)
Assignee: LEIUTIS PHARMACEUTICALS PVT. LTD.
A61K31/675A61K9/0019A61K9/08A61K47/10
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Quick Facts
Patent No.
US 10,993,952
App. No.
15/551,507
Granted
May 4, 2021
Kind
B2
Abstract

The present invention relates to stable ready to use liquid formulations of Cyclophosphamide for parenteral use. The ready to use composition comprises Cyclophosphamide dissolved in a solvent system comprising a solvent, cosolvent(s) and antioxidant(s).

Claims (19)

1. A stable liquid parenteral formulation of cyclophosphamide comprising

i) cyclophosphamide in a concentration of about 12% to about 23% based on total formulation weight;

ii) an ethanol content of about 70% to about 75% based on total formulation weight;

iii) both polyethylene glycol and propylene glycol, wherein a polyethylene glycol to propylene glycol mass ratio is between approximately 1.0:1.0 to approximately 2.0:1.0; and

iv) about 3.4% to about 8.8% based on total formulation weight of polyethylene glycol

v) about 3.4% to about 4.4% based on total formulation weight of propylene glycol

vi) wherein, after storage for 7 days at 40° C./75% RH, decomposition to form any of the following impurities is less than 0.5%:

a) bis(2-chloroethyl)amine hydrochloride;

b) 3-(2-chloroethyl)-2-oxo-2-hydroxy-1,3,6,2-oxadiazaphosphonane; and

c) 3-[2-(2-chloroethylamino)ethyl amino] propyl dihydrogen phosphate dihydrochloride.

2. The formulation of claim 1 , further comprising an antioxidant.

3. The formulation of claim 2 , wherein the antioxidant is monothioglycerol at concentration of about 0.01% to about 0.02% by total formulation weight.

4. A stable liquid parenteral formulation of cyclophosphamide comprising

i. cyclophosphamide in a concentration of about 23% based on total formulation weight

ii. an ethanol content of about 70% based on total formulation weight;

iii. both polyethylene glycol and propylene glycol, wherein a polyethylene glycol to propylene glycol mass ratio is about 1.0:1.0; and

iv. about 3.4% to about 8.8% based on total formulation weight of polyethylene glycol

v. about 3.4% to about 4.4% based on total formulation weight of propylene glycol, and

vi. about 0.02% based on total formulation weight of monothioglycerol.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 9, 2024
From: LEIUTIS PHARMACEUTICALS LLP
To: INGENUS PHARMACEUTICALS, LLC
Reel/Frame 067935/0049 →
NUNC PRO TUNC ASSIGNMENT Recorded May 25, 2022
From: LEIUTIS PHARMACEUTICALS LLP
To: LEIUTIS PHARMACEUTICALS LLP; INGENUS PHARMACEUTICALS, LLC
Reel/Frame 060015/0501 →
CHANGE OF NAME Recorded Jun 15, 2021
From: LEIUTIS PHARMACETICALS PRIVATE LIMITED
To: LEIUTIS PHARMACEUTIALS LLP
Reel/Frame 056549/0347 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 19, 2017
From: CHANDRASHEKHAR, KOCHERLAKOTA; NAGARAJU, BANDA
To: LEIUTIS PHARMACEUTICALS PVT. LTD.
Reel/Frame 043620/0180 →
Priority Claims (2)
IN 735/CHE/2015 · Feb 16, 2015 · national
IN 3117/CHE/2015 · Jun 22, 2015 · national
Continuity (1)
Related Publication 20180055861A1 · Mar 1, 2018
Cited By (2)
US 12,329,767 US 12,453,737