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Preparation method of sofaprodil freeze-dried powder injection as well as product and application thereof

A freeze-dried powder for injection and freeze-drying technology, applied in the field of pharmaceutical preparations, can solve the problems of difficulty in forming uniform and meticulous crystal morphology, layering phenomenon, poor stability, etc., and achieve the effects of good clarity, uniform structure and low moisture content

Pending Publication Date: 2022-02-01
ZHEJIANG APELOA JIAYUAN PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when preparing sofadil for injection by the process used by other varieties in the prior art (for example, the freeze-drying process of fludarabine phosphate in CN104771369B), due to the crystallization behavior of different pharmacodynamic active ingredients when freezing There are differences, which make it difficult for the product to form a uniform and fine crystal form during freeze-drying
In addition, the product precipitates after reconstitution, which has defects such as poor stability and obvious layering in appearance

Method used

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  • Preparation method of sofaprodil freeze-dried powder injection as well as product and application thereof
  • Preparation method of sofaprodil freeze-dried powder injection as well as product and application thereof

Examples

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preparation example Construction

[0045] Specifically, the above-mentioned preparation method comprises the following steps:

[0046] Sofadil is added to the water for injection, dissolved and filtered, the filtrate is adjusted to pH with an aqueous solution of alkaline substances, then added with water for injection to constant volume, filled with an inert gas for protection, and the Sofadil solution is obtained after sterilization and filtration. Freeze-dried, ready to use.

[0047] Unless otherwise specified, the term "water for injection" used in the present invention refers to water that meets the relevant regulations under the item "water for injection" in the Chinese Pharmacopoeia (or as an alternative, the US Pharmacopoeia, the European Pharmacopoeia or the Japanese Pharmacopoeia).

[0048] Unless otherwise specified, the term "dissolving and clearing" (or its full name "dissolving and clarifying") used in the present invention refers to the operation or process of dissolving the sample to be dissolved...

Embodiment 1

[0087] Embodiment 1: the preparation of sofadil.

[0088] According to the method described in CN1309703C, prepare 2-hydroxyl-5-[2,3,5,6-tetrafluoro-4-(trifluoromethyl)benzylamino]benzoic acid:

[0089]5-Aminosalicylic acid (102 g) and triethylamine (100 mL) were dissolved in dry DMF (8000 mL) at room temperature under nitrogen protection, and 2,3,5,6-tetrafluoro-4 was added to the solution. - Trifluoromethylbenzyl bromide (123 g). The reaction mixture was stirred at room temperature for 2 hours, then the solvent was removed in vacuo. Extracted with ethyl acetate / water, the organic layer was washed with water and brine, dried over anhydrous magnesium sulfate, the solvent was distilled off, and the residue was crystallized in ether / n-hexane (1:10) to obtain a white solid 2-hydroxy-5 -[2,3,5,6-Tetrafluoro-4-(trifluoromethyl)benzylamino]benzoic acid (160 g).

[0090] To absolute ethanol (500 mL) was added 2-hydroxy-5-[2,3,5,6-tetrafluoro-4-(trifluoromethyl)benzylamino]benzoic ...

Embodiment 2

[0091] Example 2: Preparation of Sofadil lyophilized powder injection.

[0092] Sofadil (3000g) was dissolved in water for injection (30L), the solution was clear, filtered with a 0.45μm pore size PES material filter membrane, the filtrate was adjusted to pH 8.2 with 0.1mol / L potassium hydroxide aqueous solution, and then added The volume of water for injection was adjusted to 60L, the solution was filled with argon gas protection, and sterilized and filtered with a PES material filter membrane with a pore size of 0.22 μm within 8 hours to obtain the sofadil solution.

[0093] Filling the above-mentioned sofadil solution in a vial, after filling, put the glass bottle into a freeze dryer, and within 30 minutes, the temperature of the plate layer of the freeze dryer was lowered to -50°C, and the temperature was kept for 1 hour; Then, the temperature of the board layer was raised to -5°C, and the temperature was kept for 1 hour; then, the temperature of the board layer was lowere...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a preparation method of a sofaprodil freeze-dried powder injection as well as a product and an application thereof. Specifically, the method disclosed by the invention comprises the following steps: adding the sofaprodil into the water for injection, filtering after dissolving, adjusting the pH value of a filtrate by using an aqueous solution of an alkaline substance, adding the water for injection to a constant volume, introducing inert gas for protection, sterilizing and filtering to obtain a sofaprodil solution, and freeze-drying to obtain the product. The corresponding freeze-dried powder injection is easy to prepare by adopting the method disclosed by the invention, the operation is simple and convenient, the product quality is stable, the controllability is high, and the method is suitable for commercialized mass production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a preparation method of sofadil freeze-dried powder injection, a sofadil freeze-dried powder injection product prepared by the method, and the medical application of the product. Background technique [0002] Sofadil (Salfaprodil), the chemical name is 2-hydroxy-5-[2,3,5,6-tetrafluoro-4-(trifluoromethyl)benzylamino]potassium benzoate, and its structural formula is shown below. [0003] [0004] Sofadil is a moderately potent N-methyl-D-aspartate (NMDA) receptor antagonist and a potent antioxidant with dual neuroprotective effects, simultaneously blocking NMDA receptors It mediates excitotoxicity and the body's oxidative stress response, and its protective effect on neurological function can last for more than 28 days, providing a wide range of neuroprotective effects and expanding the treatment time window. [0005] CN1309703C discloses that sofadil can be u...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K47/02A61K31/196A61P25/28A61P25/16A61P25/08A61P25/00A61P9/10A61P9/02A61P3/08A61P39/00
CPCA61K9/0019A61K9/19A61K47/02A61K31/196A61P25/28A61P25/16A61P25/08A61P25/00A61P9/10A61P9/02A61P3/08A61P39/00A61K31/606
Inventor 詹威强王占国张桅付凌燕林茜陈晓丽吕国杨钟莉银徐新良祝方猛
Owner ZHEJIANG APELOA JIAYUAN PHARMA
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