Non-sizing pipecuronium and preparation method and purpose thereof

A pipecuronium bromide and amorphous technology, which is applied in the field of amorphous pipecuronium bromide and its preparation, can solve the problems of poor resolubility of pipecuronium bromide powder injections and pain in patients, and improve resolubility and reduce Residue of organic solvents, effect of increasing water solubility

Active Publication Date: 2013-10-30
SICHUAN CREDIT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies have shown that the reconstitution of pipecuronium bromide powder injection is not good and may cause pain to patients when used

Method used

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  • Non-sizing pipecuronium and preparation method and purpose thereof
  • Non-sizing pipecuronium and preparation method and purpose thereof
  • Non-sizing pipecuronium and preparation method and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The preparation of embodiment 1 pipecuronium bromide amorphous substance of the present invention

[0051] Dissolve 200 g of pipecuronium bromide in 600 ml of water with stirring, bubble and saturate with nitrogen for 2 min, and filter. The filtrate was extracted twice with 800 ml of ethyl acetate, and the organic layer was discarded to obtain an aqueous layer.

[0052] The treated aqueous layer solution was quickly frozen to -40°C, kept at a constant temperature for 4 hours, and the solution was frozen into a solid. Vacuumize the system to a vacuum degree below 20Pa, heat up gradually to -20°C, keep the temperature for 4 hours; raise the temperature to -10°C, keep the temperature for 6 hours; raise the temperature to 0°C, keep the temperature for 8 hours; naturally rise to room temperature, keep the temperature for 10 hours, That is, 185 g of the pipecuronium bromide was obtained with a yield of 92.5% and a melting point range of 267-270° C. (decomposition).

[0053]...

Embodiment 2

[0063] Embodiment 2 The preparation of pipecuronium bromide amorphous substance of the present invention

[0064] Dissolve 200 g of pipecuronium bromide in 500 ml of water with stirring, bubble and saturate with nitrogen for 2 min, and filter. The filtrate was extracted twice with 600 ml of cyclohexane, and the organic layer was discarded to obtain an aqueous layer.

[0065] The treated aqueous layer solution was quickly frozen to -40° C., kept at a constant temperature for 2 hours, and the solution was frozen into a solid. Vacuumize the system to below 18Pa, heat gradually to -20°C, keep the temperature for 4 hours; raise the temperature to -10°C, keep the temperature for 6 hours; raise the temperature to 0°C, keep the temperature for 8 hours; naturally rise to room temperature, keep the temperature for 10 hours, That is, 185 g of the pipecuronium bromide was obtained as a white solid with a yield of 92.5%, a purity of 99.8%, and a melting point range of 268-270° C. (decompo...

Embodiment 3

[0066] Embodiment 3 The preparation of pipecuronium bromide amorphous substance of the present invention

[0067] 500ml of water was saturated with nitrogen, 200g of pipecuronium bromide was added, and stirred to dissolve. Filter and extract twice with 500 ml of diethyl ether, discard the organic layer, and then saturate the aqueous layer with nitrogen for 1 minute.

[0068] The treated aqueous solution was quickly frozen to -40°C and kept at a constant temperature for 2 hours to freeze solid. The system is evacuated to below 40Pa, and the temperature is gradually raised to -20°C and kept at a constant temperature for 4 hours; the temperature is raised to -10°C and kept at a constant temperature for 6 hours; the temperature is raised to 0°C and kept at a constant temperature for 8 hours; naturally rises to room temperature and kept at a constant temperature for 8 hours, that is 188 g of the pipecuronium bromide was obtained as a white solid with a yield of 94.0%, a purity of ...

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Abstract

The invention discloses non-sizing pipecuronium. The X-ray powder diffraction of the pipecuronium has no characteristic peak, preferably, the X-ray powder diffraction is shown as the picture 1. A preparation method and the purpose of the pipecuronium are further provided. The non-sizing pipecuronium improves water solubility and greatly improves product repeated solubility under the condition that stability of the existing products is maintained, thereby facilitating use of powder injection agents. Simultaneously, the preparation method of the non-sizing pipecuronium is convenient to operate and capable of effectively removing organic solvent in the pipecuronium, remarkably reducing residual of the organic solvent and greatly improving medicine safety.

Description

technical field [0001] The present invention relates to amorphous pipecuronium bromide and its preparation method and use. Background technique [0002] Pipecuronium bromide, chemical name 2β,16β-bis(4'-dimethyl-1'-piperazinyl)-3α,17β-diacetoxy-5α-androster dibromide, CAS No. 52212- 02-9, molecular formula C 35 h 62 Br 2 N 4 o 4 , molecular weight: 762.7, its structure is shown in formula (1), [0003] [0004] Picuronium bromide is a steroidal long-acting nondepolarizing muscle relaxant that is highly selective for striated muscle. There is no cardiovascular adverse reaction and no release of histamine at the clinically applied dose. It is mainly excreted through the kidneys in its original form, and there is no obvious accumulation effect after repeated administration. Patients with coronary artery bypass grafting can still maintain stable hemodynamics even if they are injected with a large dose (0.15mg / kg), so it becomes the preferred muscle relaxant for patient...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J43/00A61K31/58A61P21/02
Inventor 傅霖李晓莉陈刚
Owner SICHUAN CREDIT PHARMA
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