Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF32 Cites 64 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 specialized equipment and incurs significant expense.
Curiously, however, commercial development of propylene glycol formulations have heretofore not been reported.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Liquid formulations of bendamustine
  • Liquid formulations of bendamustine
  • Liquid formulations of bendamustine

Examples

Experimental program
Comparison scheme
Effect test

examples

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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Temperatureaaaaaaaaaa
Fractionaaaaaaaaaa
Fractionaaaaaaaaaa
Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com