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A kind of vecuronium bromide freeze-dried preparation and preparation method thereof

A technology of freeze-dried preparations and vecuronium bromide, which is applied in the direction of freeze-dried delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of blood vessel irritation, injection pain, etc., and reduce irritation, injury, and side effects Reduced effect

Active Publication Date: 2011-12-21
XIAN LIBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Vecuronium bromide is an alkaline compound with amino groups. The traditional formula needs to add strong acid to increase the solubility of vecuronium bromide, so the preparation after dissolution is acidic (research shows that the pH of vecuronium bromide electrolyte solution is 4.3 [22][23] ), causing severe irritation to blood vessels, causing injection pain [24][25][26]

Method used

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  • A kind of vecuronium bromide freeze-dried preparation and preparation method thereof
  • A kind of vecuronium bromide freeze-dried preparation and preparation method thereof
  • A kind of vecuronium bromide freeze-dried preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Prescription:

[0031]

[0032] method:

[0033] Accurately measure 4mg of vecuronium bromide and 50mg of vitamin E into 10ml of water for injection, heat to 60°C and stir for about 10-20min to dissolve completely. Take another 10ml of water for injection, add 20mg of polyethylene glycol-200 and 15mg of glycerin, and stir to dissolve. Then slowly add polyethylene glycol-200 and glycerin aqueous solution into the vecuronium bromide and vitamin E aqueous solution cooled to normal temperature under stirring, stir evenly until completely dissolved, finally add 200mg glycine, adjust the water for injection to 50ml , stirred for a period of time, sterile filtered, freeze-dried and packaged.

Embodiment 2

[0035] Prescription:

[0036]

[0037] method:

[0038] Accurately measure 4mg of vecuronium bromide and 50mg of vitamin E into 10ml of water for injection, heat to 60°C and stir for about 10-20min to dissolve completely. Take another 10ml of water for injection, add 20mg of polyethylene glycol-400 and 15mg of glycerin, and stir to dissolve. Then slowly add polyethylene glycol-400 and glycerin aqueous solution into the vecuronium bromide and vitamin E aqueous solution cooled to normal temperature under stirring, stir evenly until completely dissolved, and finally add 600mg of glutamic acid to adjust the amount of water for injection to 50ml, stirred for a period of time, sterile filtered, freeze-dried and packaged.

Embodiment 3

[0040] Prescription:

[0041]

[0042] method:

[0043] Accurately measure 4mg of vecuronium bromide and 50mg of vitamin E into 10ml of water for injection, heat to 60°C and stir for about 10-20min to dissolve completely. Take another 10ml of water for injection, add 20mg of polyethylene glycol-600 and 15mg of glycerin, and stir to dissolve. Then slowly add polyethylene glycol-600 and glycerin aqueous solution into the vecuronium bromide and vitamin E aqueous solution cooled to normal temperature under stirring, stir evenly until completely dissolved, finally add 800mg of tryptophan, adjust the water volume for injection to 50ml, stirred for a period of time, sterile filtered, freeze-dried and packaged.

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Abstract

The invention discloses a novel vecuronium bromide freeze-dried preparation and a preparation method thereof. The novel preparation comprises the main components of vecuronium bromide, a freeze-dried excipient, polyethylene glycol playing a role in re-dissolving assistance, vitamin E playing a role in anti-oxidation, and glycerol serving as an isotonic regulator. According to the formula, the vecuronium bromide is developed into the novel freeze-dried preparation, and the process is simple. The novel vecuronium bromide freeze-dried preparation can improve the pH value of re-dissolved preparation solution to make the pH value reach or be close to the physiological pH range of blood, avoids or reduces stimulations caused by the preparation to a blood vessel, alleviates injection pains, and simultaneously can ensure that a medicament compound is fully dissolved to prevent insoluble substances from causing side effect injuries to a body.

Description

1. Technical field [0001] The invention belongs to the series of medical drugs, and relates to a short-acting non-depolarizing muscle relaxant of monoquaternary ammonium steroids, in particular to a freeze-dried drug preparation for injection. Specifically, it is a novel freeze-dried preparation of vecuronium bromide and a preparation method thereof. 2. Background technology [0002] Vecuronium (Vec) is a clinically commonly used short- and medium-acting non-depolarizing muscle relaxant [1] , which is similar in structure to pancuronium bromide, blocks the transmission between nerve endings and striated muscle by competing with acetylcholine for nicotinic receptors located on the motor endplate of striated muscle [2][3][4] . Vecuronium bromide slightly affects circulatory function [5][6] , no histamine release [7][8] , has very weak blocking effect on autonomic ganglion [9][10] , is the only muscle relaxant that has the least cardiovascular adverse reactions among muscl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/58A61K47/40A61P21/02A61K47/34A61K47/22A61K47/18A61K47/36A61K47/38A61K47/10
Inventor 陈涛王汝涛王惟娇胡慧静
Owner XIAN LIBANG PHARMA
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