Polymorphic forms of sodium benzoate and uses thereof

a technology of sodium benzoate and polymorphism, applied in the field of polymorphic forms of sodium benzoate, can solve the problems of lagged effectiveness of cns disorders treatment, reduce symptoms, signs or causes of the condition, delay or minimize one or more symptoms, and improve the overall treatment

Active Publication Date: 2018-12-06
SYNEURX INT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0039]A “therapeutically effective amount” of a polymorphic form of sodium benzoate described herein is an amount sufficient to provide a therapeutic benefit in the treatment of a condition or to delay or minimize one or more symptoms associated with the condition. A therapeutically effective amount of a polymorphic form means an amount of therapeutic agent, alone or in combination with other therapies, which provides a therapeutic benefit in the treatment of the condition. The term “therapeutically effective amount” can encompass an amount that improves overall therapy, reduces or avoids symptoms, signs, or causes of the condition, and / or enhances the therapeutic efficacy of another therapeutic agent.

Problems solved by technology

The development of effective therapies for CNS disorders has lagged behind other therapeutic areas due to the complexity of such disorders and the lack of efficient technology for delivering therapeutic agents through the blood-brain barrier.

Method used

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  • Polymorphic forms of sodium benzoate and uses thereof
  • Polymorphic forms of sodium benzoate and uses thereof
  • Polymorphic forms of sodium benzoate and uses thereof

Examples

Experimental program
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Effect test

example 1

on of Polymorphic Form #1 of Sodium Benzoate

[0136]199.93 mg of sodium benzoate was placed in a flask and 4 mL of methanol was added to dissolve the sodium benzoate. Unless otherwise indicated, commercially available sodium benzoate was purchased from Merck, Formosa Laboratories Inc., or Sigma Aldrich, and solvents were purchased from vendors such as Acros, Merck, and Sigma Aldrich. The solution thus formed was kept stirring for 10 min and then filtered to remove any insoluble ingredients. The filtrate was evaporated by rotary evaporation to form solid sodium benzoate in a polymorphic form. The solid obtained was analyzed by XRPD, TGA, and DSC as described below.

[0137]Thermogravimetric Analysis (TGA).

[0138]Total weight loss was obtained on a TA Instrument TGA Model Q500. The sample was heated in an opened aluminum pan at the heating rate of 10° C. / min up to the final temperature.

[0139]Differential Scanning Calorimetry.

[0140]Thermal analysis was performed using a TA Instrument DSC Mod...

example 2

on of New Polymorphic Form #2

[0144]2.005 mg of commercially available sodium benzoate was placed in a round bottom flask followed by the addition of 150 mL of acetonitrile. The suspension thus formed was kept stirring for 2 days and filtered to collect solid sodium benzoate thus formed. The solid sodium benzoate, in a polymorphic form, was also analyzed by XRPD, TGA, and DSC and the results are shown in FIGS. 4-6.

example 3

on of New Polymorphic Form #3

[0145]2.006 g of commercially available sodium benzoate was placed in a round bottom flask and 150 mL of isobutanol was added. The suspension thus formed was kept stirring for 6 days and filtered afterwards. The solid sodium benzoate thus formed was collected and analyzed by XRPD, TGA, and DSC. The results are shown in FIGS. 7-9.

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Abstract

The present disclosure provides polymorphic forms of sodium benzoate with a X-ray diffraction pattern comprising characteristic peaks at a reflection angle 2θ of approximately 5.9, 30.2, and 31.2 degrees; or a X-ray diffraction pattern comprising characteristic peaks at a reflection angle 2θ of approximately 3.7, 5.9, and 26.6 degrees. Also provided herein are methods of preparing the polymorphic forms of sodium benzoate and uses thereof in treating and / or reducing the risk for a neuropsychiatric disorder (e.g., schizophrenia, psychotic disorders, depressive disorders, or Alzheimer's disease).

Description

RELATED APPLICATION[0001]The present application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Application No. 62 / 412,160, filed Oct. 24, 2016, which is herein incorporated by reference in its entirety.BACKGROUND OF THE INVENTION[0002]The central nervous system (CNS) includes the brain and spinal cord. The CNS is vulnerable to various disorders, which may be caused by various factors, including trauma, infections, degeneration, structural defects and / or damages, tumors, blood flow disruption, and autoimmune disorders. Symptoms of a CNS disorder would depend on the area of the nervous system that is involved and the cause of the disorder.[0003]The development of effective therapies for CNS disorders has lagged behind other therapeutic areas due to the complexity of such disorders and the lack of efficient technology for delivering therapeutic agents through the blood-brain barrier. As such, it is of great interest to develop new treatment approaches for CNS disorders.S...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07C63/08C07C51/41A61K31/192A61K45/06A23L33/16
CPCC07C63/08C07C51/41A61K31/192A23V2002/00A23L33/16C07B2200/13A61K45/06C07C51/43A61K31/198A61K31/445A61K31/5513A61K31/7024A61K9/28A61P1/00A61P25/00A61P25/14A61P25/16A61P25/18A61P25/22A61P25/24A61P25/26A61P25/28A61P29/02A61P43/00A61K2300/00
Inventor TSAI, GUOCHUAN EMILWANG, CHING-CHENGHSIEH, TIEN-LAN
Owner SYNEURX INT
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