New crystal form of vecuronium bromide, and preparation method and use thereof

Abstract

The invention discloses a new crystal form II of vecuronium bromide. There are characteristic peaks at 2theta diffraction angles of 8.3+ / -0.2DEG, 11.7+ / -0.2DEG, 14.1+ / -0.2DEG, 15.7+ / -0.2DEG, 18.0+ / -0.2DEG and 21.3+ / -0.2DEG in the X-ray powder diffraction pattern of the crystal form. The invention also discloses a preparation method of the crystal form and a use of the crystal form. The crystal form II of vecuronium bromide improves the dissolvability of vecuronium bromide, is helpful for mitigating or eliminating the untoward effects of blood vessel irritation and ache initiation during injection, reduces the hydroscopic property of vecuronium bromide, substantially enhances the stability of vecuronium bromide, is in favor of the long term storage of a vecuronium bromide raw material and guarantees the product safety through the change of the crystal form structure. The preparation method of the crystal form II of vecuronium bromide has the advantages of simplicity, convenient operation and high yield, and is benefit for the large scale production of the crystal form II of vecuronium bromide.

Description

technical field [0001] The invention relates to a new crystal form of vecuronium bromide, a preparation method and application of the crystal form. Background technique [0002] Vecuronium bromide (structure shown in formula 1) was first listed in the Netherlands in 1982, and is widely used in clinical practice mainly as an adjuvant to general anesthesia. It belongs to the medium and short-acting non-depolarizing muscle relaxants of monoquaternary ammonium sterols, which can compete with acetylcholine for the nicotinic receptors located on the motor endplate of striated muscles and block the signal transduction between nerve endings and striated muscles. Endotracheal intubation during general anesthesia and muscle relaxation during surgery. Vecuronium bromide will not release histamine after entering the human body, and can effectively reduce possible adverse reactions such as vomiting, aspiration and even hypoxia during intubation. Compared with the existing muscle relaxa...

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Problems solved by technology

Among them, the former is a freeze-dried powder injection, which has disadvantages such as long production cycle, high cost, and unfavorable product cost savings; at the same time, the auxiliary amino acid added in the preparation is unstable, which will accelerate the instability of the drug and increase the preparation cost. (see CN102319215A)

And the latter used additives such as a large amount of cholesterol, phosphatidylethanolamine, soybean lecithin, Tween 80, PVP in the preparation process of liposome injection, and this influenced the curative effect of vecuronium bromide to a certain extent, increased Necessary clinical risks and hidden dangers, and the proportion of each component added in the preparation process must be strictly controlled, otherwise the quality and curative effect of the injection will be greatly reduced

There is no relevant report on the crystal form of vecuronium bromide

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