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Rocuronium bromide crystal form

A technology of rocuronium bromide and crystal form, which is applied in the directions of organic active ingredients, muscular system diseases, neuromuscular system diseases, etc. Ammonium has strong static electricity and other problems, and achieves the effect of saving storage and transportation costs, low static electricity and low cost.

Active Publication Date: 2020-05-26
CHENGDU SINO STRONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] 3. The produced rocuronium bromide has strong static electricity, which is not conducive to crushing and packaging, subpackaging, and is not conducive to the production and operation of raw materials and preparations
[0009] The rocuronium bromide prepared by the technical scheme reported in the literature is an amorphous substance with poor stability. Generally, it is stored by freezing airtight shading below -20°C, or introducing acetic acid in the refining process to improve its stability to a certain extent, but did not fundamentally solve the problem
Existing technical schemes all can increase storage transportation cost greatly

Method used

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  • Rocuronium bromide crystal form
  • Rocuronium bromide crystal form
  • Rocuronium bromide crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1: the preparation of rocuronium bromide

[0055] Add 500g of dichloromethane to the 1000ml flask, add (2β,3α,5α,16β,17β)-17-acetoxy-3-hydroxyl-2-(4-morpholinyl)-16-(1-pyrrolidine Base) androstane 100g, stir until the solid is completely dissolved, add 100g sodium carbonate and 100g 3-bromopropene, and react at 20-30°C. After the reaction was completed, the inorganic salt was removed by filtration, the filter cake was washed with dichloromethane, and the filtrate was dropped into 4000 g of ether, stirred and dispersed, filtered, washed, and dried under reduced pressure at 45 to 50° C. to obtain 119 g of rocuronium bromide, with a yield of 95.2%. 98.5% purity.

Embodiment 2

[0056] Embodiment 2: the preparation of rocuronium bromide crystal form A

[0057] Add 10 g of low-purity rocuronium bromide prepared in Example 1 to 50 g of acetone, 1 g of methanol, and 2.5 g of ether, stir at 20 to 30 ° C to dissolve the solid, stir and crystallize at -20 to -15 ° C for 48 hours, filter, Dry under reduced pressure at 10-20°C to obtain 6.78g of high-purity rocuronium bromide, with a yield of 67.8%, the largest single impurity 0.015%, and the total impurity 0.040%.

[0058] After testing, its HPLC detection spectrum is as follows figure 1 As shown, the infrared spectrum is as figure 2 As shown, the crystallinity photograph observed under the microscope is as follows image 3 As shown, the X-ray powder diffraction pattern is shown in Figure 4 shown.

Embodiment 3

[0059] Embodiment 3: the preparation of rocuronium bromide crystal form A

[0060] 15g of rocuronium bromide prepared according to the method of Example 1 was added to 70g of acetone, 3.2g of ethanol, and 2.8g of ether, stirred at 20 to 30°C to dissolve the solid, and stirred and crystallized at -25 to -20°C for 48 hours. Filtration, air-drying at 10-20°C gave 7.92 g of crystal form A of rocuronium bromide, with a yield of 52.8%, the largest single impurity being 0.014%, and the total impurity being 0.038%.

[0061] After detection, its HPLC collection of illustrative plates and figure 1 Basically the same, the infrared spectrum and figure 2 Basically the same, X-ray powder diffraction pattern and Figure 4 Basically the same.

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Abstract

The invention discloses a crystal form A of rocuronium bromide. Cu-Kalpha radiation is used; an X-ray powder diffraction pattern expressed by a 2theta angle has characteristic diffraction peaks at positions of 8.0 + / - 0.2 degrees, 11.1 + / - 0.2 degrees, 15.4 + / - 0.2 degrees, 15.9 + / - 0.2 degrees, 17.1 + / - 0.2 degrees, 18.2 + / - 0.2 degrees, 19.0 + / - 0.2 degrees, 19.6 + / - 0.2 degrees, 20.2 + / - 0.2 degrees, 22.0 + / - 0.2 degrees, 22.8 + / - 0.2 degrees and 25.4 + / - 0.2 degrees. The preparation method of the rocuronium bromide crystal form is simple, and the rocuronium bromide crystal form has good stability and is more beneficial to production, storage and transportation.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a crystal form of rocuronium bromide. Background technique [0002] Muscle relaxants are necessary adjuvant drugs for anesthesia in surgical operations, and are used in large amounts. At present, the common ones are rocuronium bromide, vecuronium bromide, succinylcholine, and atracurium bromide. Rocuronium Bromide (Chinese name: Rocuronium bromide), chemical name 1-[(2β,3α,5α,16β,17β)-17-(acetyloxy)-3-hydroxy-2-(4-morpholinyl) Androstan-16-yl]-1-(2-propenyl)pyrrolidine bromide is a steroidal non-depolarizing muscle relaxant developed by Organon in the Netherlands. Because rocuronium has the fastest onset of action and no side effects such as releasing histamine, it becomes the most promising drug among similar drugs. Since the development of Organon in the Netherlands, it has been marketed in more than 40 countries and regions including the Netherlands, Belgium, Germany, the United Stat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J43/00A61K31/58A61P21/02A61P23/00
CPCA61P21/02A61P23/00C07B2200/13C07J43/003
Inventor 匡建明王成刚刘力超高建李有章伍伟
Owner CHENGDU SINO STRONG PHARMA
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