Liquid formulations of bendamustine

a technology of liquid formulation and bendamustine, which is applied in the direction of biocide, drug composition, animal husbandry, etc., can solve the problems of inability to commercialize the development of propylene glycol formulations, time-consuming and cumbersome lyophilization of bendamustine powder, and high cost of lyophilization of solids on a commercial scal

Inactive Publication Date: 2011-08-04
CEPHALON INC
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

The reconstitution of the bendamustine lyophilized powder is time consuming and cumbersome.
Moreover, lyophilization of solids on a commercial scale requires spe

Method used

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  • Liquid formulations of bendamustine
  • Liquid formulations of bendamustine
  • Liquid formulations of bendamustine

Examples

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Solubility and Stability of Bendamustine Hydrochloride in Polar Aprotic Solvents

[0034]Equilibrium solubility was determined for solvents including 1-methyl-2-pyrrolidone (NMP), 1,3-dimethyl-2-imidazolidinone (DMI), dimethylacetamide (DMA), dimethyl sulfoxide (DMSO), acetone, tetrahydrofuran (THF), dimethylformamide (DMF), and propylene carbonate (PC). The solubility of bendamustine hydrochloride was also determined for two solutions, 25 mg / mL niacinamide in DMA and 66% DMA / 34% propylene glycol (PG). A saturated solution of bendamustine hydrochloride was made in triplicate for each solvent or solution and mixed on a Lab-Quake with gentle mixing and low shear for 3 days at room temperature. A sample of each suspension was put into a microcentrifuge tube and spun at 10,000 rpm for 5 min on an Eppendorf microcentrifuge. The supernatant was removed and put into a clean vial. Each solution was diluted with sample solvent: 50% NMP / 50% 0.1% trifluoroacetic acid in water. A reverse phase met...

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Abstract

Stable liquid formulations of bendamustine, and pharmaceutically acceptable salts thereof, and polar aprotic solvents, are described.

Description

TECHNICAL FIELD OF THE INVENTION[0001]The present invention relates to liquid formulations of bendamustine, and the pharmaceutical salts thereof.BACKGROUND OF THE INVENTION[0002]Bendamustine, (4-{5-[bis(2-chloroethyl)amino]-1-methyl-2-benzimidazolyl}butyric acidis an atypical structure with a benzimidazole ring, which structure includes an active nitrogen mustard. Bendamustine was initially synthesized in 1963 in the German Democratic Republic and was available from 1971 to 1992 in that location under the name Cytostasan®. Since that time, it has been marketed in Germany under the tradename Ribomustin®. It is currently available for use in the United States under the tradename Treanda® (Cephalon, Inc., Frazer, Pa.). It has been widely used to treat chronic lymphocytic leukemia, Hodgkin's disease, non-Hodgkin's lymphoma, multiple myeloma, and breast cancer.[0003]Like other nitrogen mustards, bendamustine hydrolyzes in aqueous solution, with the major degradant being the primary alcoh...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A61P35/00
CPCA61K9/08A61K31/4184A61K47/10A61K47/40A61K47/20A61K47/22A61K47/18A61P35/00A61P35/02A61K9/0019
Inventor DRAGER, ANTHONY S.LABELL, RACHEL Y.PATEL, PIYUSH R.
Owner CEPHALON INC
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