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Vecuronium bromide compound and production method thereof

A technology of vecuronium bromide and its compound, which is applied in the field of medicine, can solve the problems of low purity of vecuronium bromide, achieve the effects of reducing toxic and side effects, improving clinical adverse reactions, easy control and industrial production

Active Publication Date: 2012-07-25
灵康药业集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to overcome the defects of the above-mentioned prior art, especially the defect of low purity of vecuronium bromide prepared by the prior art, the invention provides a method for preparing a high-purity vecuronium bromide compound

Method used

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  • Vecuronium bromide compound and production method thereof
  • Vecuronium bromide compound and production method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0039] Accurately weigh 10 g of vecuronium bromide with a purity of 86% prepared according to the method of CN101684139A and dissolve it in 50 ml of dichloromethane, stir vigorously to make it completely dissolved, filter with suction, discard solid impurities, and collect the filtrate.

[0040] Inject the dichloromethane solution of vecuronium bromide into Baker column chromatography special neutral alumina with a particle size of 50-200 μm, a pore size of 6 nm, and pH 7.0, then pump in dichloromethane for elution, and collect vecuronium bromide The ammonium elution fraction was concentrated under reduced pressure at 30°C, and the concentrate was collected.

[0041] Raise the temperature of the dichloromethane solution of vecuronium bromide to 70°C and keep it for 1 hour, then add absolute ethanol which accounts for 1.5 times the volume of the vecuronium bromide dichloromethane solution, and reduce the temperature to 45-50°C within 1 hour °C, then lower the temperature to 22-...

Embodiment 2

[0047] Accurately weigh 10 g of vecuronium bromide raw material with a purity of 92% (Anhui Wellman Pharmaceutical Co., Ltd., H20093826) and dissolve it in 200 ml of dichloromethane, stir vigorously to make it completely dissolved, filter with suction, discard solid impurities, and collect the filtrate.

[0048] Inject the dichloromethane solution of vecuronium bromide into Baker column chromatography special neutral alumina with a particle size of 50-200 μm, a pore size of 6 nm, and pH 7.0, then pump in dichloromethane for elution, and collect vecuronium bromide The ammonium elution fraction was concentrated under reduced pressure at 40°C, and the concentrate was collected.

[0049] Raise the temperature of the dichloromethane solution of vecuronium bromide to 65°C and keep it for 2 hours, then add absolute ethanol twice the volume of the vecuronium bromide dichloromethane solution, and lower the temperature to 48-50°C within 1 hour °C, then lower the temperature to 20-24 °C ...

Embodiment 3

[0051] Accurately weigh 10 g of vecuronium bromide raw material with a purity of 93% (Shanxi Boda Pharmaceutical Co., Ltd., H20083095) and dissolve it in 100 ml of dichloromethane, stir vigorously to make it completely dissolved, filter with suction, discard solid impurities, and collect the filtrate.

[0052] Inject the dichloromethane solution of vecuronium bromide into ICN allumina N fine-pore neutral alumina with a particle size of 18-63 μm, a pore size of 6 nm, and pH 7.5, then pump in dichloromethane for elution, and collect vecuronium bromide The ammonium elution fraction was concentrated under reduced pressure at 35°C, and the concentrate was collected.

[0053] Raise the temperature of the dichloromethane solution of vecuronium bromide to 66°C and keep it for 1.5 hours, then add anhydrous ethanol which accounts for 3 times the volume of the vecuronium bromide dichloromethane solution, and drop the temperature to 48-48°C within 1 hour 50°C, then reduce the temperature ...

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Abstract

The present invention relates to a high purity vecuronium bromide compound with the structural formula shown in the specification, and also relates to a production method of the vecuronium bromide compound. The production method comprises the following steps: 1) dissolving the vecuronium bromide used as a raw material into a proper amount of dichloromethane, vigorously stirring up, leaching the mixture, and discarding solid impurities from the mixture to obtain a vecuronium bromide dichloromethane solution; 2) loading the vecuronium bromide dichloromethane solution on a chromatography column, collecting the elution portion of vecuronium bromide, and concentrating the elution portion at reduced pressure to obtain the vecuronium bromide dichloromethane solution; and 3) adding absolute ethyl alcohol into the vecuronium bromide dichloromethane solution at a temperature not higher than 70 DEG C, lowering the temperature at gradient, recrystallizing the mixture and drying the recrystallized products to obtain vecuronium bromide. By utilizing the production method, the impurity and quality of the products are increased, and the side-effect is reduced, thus the production method is suitable for industrial mass production.

Description

technical field [0001] The invention relates to a high-purity vecuronium bromide compound and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Vecoronium Bromide, CAS No.: 50700-72-6, chemical name 1-((3α,17β-diacetyl-2βpiperidinyl-5α-androstyl-16βhydroxy)-1-methanol Base piperidine ammonium bromide salt), Chinese synonyms: Wansi Song; Nuokoulong; Nuocolon; VBMC; nc-45; orgnc45; norcuron; Musculax; Muscurate; vecuronium; 34 h 57 BrN 2 o 4 , the molecular weight is 637.74, and the structural formula is as follows: [0003] [0004] Vecuronium bromide is a non-depolarizing diaminoandrostane muscle relaxant used for endotracheal intubation and maintenance of anesthesia. It is an adjuvant drug for general anesthesia that can promote skeletal muscle relaxation. It acts quickly after intravenous injection, works on the vagus nerve of the heart five times, does not release histamine, and has stable cardiovascular fun...

Claims

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Application Information

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IPC IPC(8): C07J43/00
Inventor 陶灵刚
Owner 灵康药业集团股份有限公司
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