Parenteral formulation comprising siponimod

A parenteral and preparation technology, which is applied in the field of cyprinimod pharmaceutical preparations, can solve problems such as insufficient long-term clinical research

Pending Publication Date: 2020-05-05
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to this stability limitation, the corresponding lyophilized formulations are considered insufficiently suitable for long-term clinical studies

Method used

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  • Parenteral formulation comprising siponimod
  • Parenteral formulation comprising siponimod
  • Parenteral formulation comprising siponimod

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0119] Example 1: Parenteral formulations

[0120] Transfer 250 mL of milliQ water to a suitable glass bottle, then add 50 g of hydroxypropyl beta-cyclodextrin. The mixture was stirred at 500 rpm for 30 minutes, forming a clear solution. Add 556 mg (accurately weighed) of 1-{4-[(1E)-N-{[4-cyclohexyl-3-(trifluoromethyl)benzyl]oxy}ethylimidoyl]-2-ethane benzyl}-3-azetidinecarboxylic acid / fumaric acid (2:1) co-crystal, and the mixture was stirred at 500 rpm for 15 minutes to form a suspension. 305 mg of 2-amino-2-(hydroxymethyl)propane-1,3-diol (Tris, trometamol) was added and the mixture was stirred at 500 rpm for 60 minutes, forming a clear solution with a pH of 7.897. Addition of 250 μl of 1 N NaOH, after stirring at 500 rpm for 2 minutes, resulted in a clear solution with a pH of 7.983. 15 g of mannitol was added and the mixture was stirred at 500 rpm for 15 minutes to form a clear solution. MilliQ water was added to give a clear solution with a pH of 8.015 in a volume of...

example 2

[0122] Example 2: Parenteral formulations

[0123] Transfer 250 mL of milliQ water to a suitable glass bottle, then add 50 g of hydroxypropyl beta-cyclodextrin. The mixture was stirred at 500 rpm for 30 minutes, forming a clear solution. Add 556 mg (accurately weighed) of 1-{4-[(1E)-N-{[4-cyclohexyl-3-(trifluoromethyl)benzyl]oxy}ethylimidoyl]-2-ethane benzyl}-3-azetidinecarboxylic acid / fumaric acid (2:1) co-crystal, and the mixture was stirred at 500 rpm for 15 minutes to form a suspension. 305 mg of 2-amino-2-(hydroxymethyl)propane-1,3-diol (Tris, trometamol) was added and the mixture was stirred at 500 rpm for 60 minutes, forming a clear solution with a pH of 7.878. Addition of 250 μl of 1 N NaOH, after stirring at 500 rpm for 2 minutes, resulted in a clear solution with a pH of 7.997. 3 g of sodium chloride was added, and the mixture was stirred at 500 rpm for 15 minutes, forming a clear solution with a pH of 8.112. Addition of 220 μl of 1 N HCl, after stirring at 500 r...

example 3

[0125] Example 3: Parenteral formulations

[0126]

[0127] 1 This composition refers to a nominal volume of 3.5 mL; an overfill of 0.3 mL is not considered.

[0128] 2 1.112 mg / mL of cipnimod / fumaric acid co-crystal corresponds to 1 mg / mL of cipnimod free base.

[0129] 3 Added as a 1N solution

[0130] 4 Packaging material: (i) vial R 6ML / 20MM amber, (ii) STPF LYO CIIR 20MM D21-7S / V10-F322-2W / RS (grey rubber stopper), (iii) AR-KAPPE PP / AL 20MM NATUR / NATUR (aluminum cover with plastic flip disc).

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Abstract

The present invention relates to a pharmaceutical formulation of siponimod which can be administered parenterally. In particular, the present invention relates to a parenteral solution comprising siponimod and a method for preparing said solution.

Description

[0001] The present invention relates to pharmaceutical formulations of siponimod which can be administered parenterally. In particular, the present invention relates to parenteral solutions comprising sipronimod and methods for preparing said solutions. Background technique [0002] The IUPAC name of Sipronimod is 1-{4-[(1E)-N-{[4-cyclohexyl-3-(trifluoromethyl)benzyl]oxy}ethyliminoyl]-2- Ethylbenzyl}-3-azetidinecarboxylic acid, and this compound is represented by the chemical structure according to formula (I): [0003] [0004] Sipronimod (also known as BAF312) is a selective sphingosine-1-phosphate receptor modulator used in the treatment of autoimmune diseases such as multiple sclerosis (MS) for the treatment of neurodegeneration disease. [0005] WO 2004 / 103306 A2 relates to immunosuppressant compounds and methods for their production. In particular, a synthetic route to Sipronimod is described. Furthermore, said document mentions that sipronimod may generally be ad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/397A61K47/40A61K47/26
CPCA61K9/0019A61K47/26A61K9/08A61K47/40A61K31/397A61K47/18A61K31/047A61K31/724
Inventor R·库马M·R·S·库马H·L·G·M·提莫森
Owner NOVARTIS AG
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