38 results about "Rocuronium Bromide" patented technology

The invention provides a bromide type muscle relaxant, which mainly comprises a method for synthesizing rocuronium bromide, vecuronium bromide, pancuronium bromide and pipecuronium bromide , and is mainly characterized by adopting a ketene as an acylating agent during the process of transforming 5Alpha-androstane -2-alkene-17-alkone to 17-acetoxyl group-5Alpha- androstane-2, and 16-diene, adopting a stress kettle as a reactor when realizing the step of ring-opening and condensation of the 2 Alpha and 3 Alpha-epoxy compound, and adding a solid catalyst and a desiccant in the last step of operation of rocuronium bromide to greatly improve the reaction yield and the quality of products. The technology provided by the invention can shorten the synthesis time of the bromide type muscle relaxant, simplify the operation steps, improve the quality of products and reduce the production cost.

The invention provides a stable rocuronium bromide composition for vein, which contains rocuronium bromide with treating effective dose, EDTA-2Na-Ca or EDTA-2Na and a pH value buffer system. The EDTA-2Na-Ca or the EDTA-2Na delays the hydrolysis of a rocuronium bromide 17-bit ester bond of the composition in the processes of preparation and storage; and on one hand, medicine liquid can resist the high temperature in the processes of hot press and sterilization, on the other hand, the content of rocuronium bromide deacetyl impurities in the composition in the process of storage is reduced. The invention also provides a reasonable method for preparing the medicine liquid, which can reduce the generation of the rocuronium bromide hydrolysis impurities in the process of preparation. The reduction of the rocuronium bromide hydrolysis impurities improves the quality controllability of the composition and ensures the safety and effectiveness of clinical use.

The invention relates to a preparation method of bulk drugs, in particular to a preparation method of rocuronium bromide crystalline hydrate, which comprises the following steps of: preparing the rocuronium bromide aqueous solution with 2-15 percent of weight volume percent concentration, freezing the aqueous solution to ice under -50-30 DEG C, decompressing and heating up to 30-50 DEG C under vacuum state, keeping 10-20 hours of temperature-rise period and preserving heat for 10-30 hours in vacuum at the temperature. The rocuronium bromide crystalline hydrate prepared by the method enhances the stability of the rocuronium bromide bulk drugs, improves the particle exterior of the rocuronium bromide and effectively reduces the excessive organic residue of the rocuronium bromide bulk drugs.

The invention encompasses processes for synthesizing 1-[17β-acetyloxy-3α-hydroxy-2β-(4-morpholinyl)-5α-androstan-16β-yl]-1-(2-propenyl)pyrrolidinium bromide (rocuronium bromide) and intermediates thereof.

Provided is a method for purifying rocuronium bromide, which comprises: formulating crude rocuronium bromide to be purified into an aqueous solution, distilling off excess residue solvents at reduced pressure, absorbing by adding active carbon or silica gel, then filtrating, quick freezing the filtrate into ice, and then lyophilizing to obtain rocuronium bromide.

The invention discloses a method for preparing rocuronium bromide midbody compound crystal, which is characterized in that compound 2beta-(4-morpholinyl)-16beta-(1-pyrrolidyl)-5alpha-androstane-3alpha, 17beta-glycol is adopted as raw material to be proceeded with acylation reaction and then to be refined to obtain crystal powder compound 2beta-(4 - morpholinyl)-16beta-(1 - pyrrolidinyl)-5alpha-Androstane-3alpha, 17beta-diol - 2 acetate with high purity. With the method, the fallow crystal powder compound with high purity can be prepared, and conditions are created for synthesizing high-quality rocuronium bromide.

The invention belongs to the technical field of biological medicine, and relates to a water-soluble cucurbit [8] urea sulfonate derivative serving as a neuromuscular blocker antagonist as well as a preparation method and application thereof. The water-soluble cucurbit [8] urea sulfonate derivative is obtained by taking cucurbit [8] urea as a raw material and introducing a water-soluble side chain group through a chemical reaction; a hydrophobic cavity of the water-soluble cucurbit [8] urea sulfonate derivative can be combined with neuromuscular blockers including cis-asatracurium besylate, rocuronium bromide, vecuronium bromide and pantocuronium bromide in a water phase through interaction of hydrophobic agents, so that antagonism is achieved. Experiments show that the water-soluble cucurbit [8] uril derivative can efficiently antagonize various neuromuscular blockers in a living body, is high in universality and low in biotoxicity, and is an ideal neuromuscular blocker antagonist.

The invention discloses a preparation method of a rocuronium bromide intermediate 5alpha-sterane-2-ene-17-one. The specific steps include: sequentially adding epiandrosterone TS, a solvent and a phasetransfer catalyst into a reaction bottle, performing heating to a reaction temperature of 90-120DEG C, carrying out stirring reaction, and conducting post-treatment purification to obtain the 5alpha-sterane-2-ene-17-one. The method provided by the invention greatly shortens the reaction time, reduces byproducts, enhances the yield, reduces three wastes, lowers the production cost, is suitable forindustrial production, and has obvious social and economic benefits.

The invention discloses a new compound for muscle relaxation antagonism. The new compounds of theta type, beta type, gamma type, lambda type, kappa type, nu type, tau type, omega type, upsilon type and the like of sugammadex sodium have less hygroscopicity and better storage stability, are more beneficial to quality control of medicines and preparations and the like, and are suitable for preparingspecific binding neuromuscular block antagonists. And the compound can be applied to drugs for antagonizing treatment or prevention of neuromuscular block induced by rocuronium bromide or vecuroniumbromide and the like.

The invention provides a novel rocuronium bromide preparation. The rocuronium bromide preparation contains rocuronium bromide, has a pH of 4 or less, and does not contain a buffering agent.

The invention belongs to the technical field of raw material medicine preparation, and particularly relates to a single crystal culture method for a rocuronium bromide starting raw material (LK-7). According to the technical scheme, the method comprises the following steps: firstly, dissolving a certain amount of LK-7 solid in a proper amount of organic solvent at a certain temperature to obtain an LK-7 solution with a certain concentration, and meanwhile, ensuring that the obtained solution is clear and transparent without any macroscopic particles; and culturing the LK-7 single crystal by adopting a volatile solvent method. The invention provides a culture method of an LK-7 single crystal, and provides a scientific method for quality control of an initial bulk drug LK-7, especially for confirmation of an absolute configuration of a chiral center.

The invention provides a method for detecting a rocuronium bromide intermediate and impurities, which adopts a high performance liquid chromatography to detect and analyze the rocuronium bromide intermediate, an impurity 1, an impurity 2, an impurity 3 and an impurity 4. According to the method, known impurities can be accurately detected, the main peak of the intermediate and the peak of the known impurities can be effectively separated, and the method is a brand-new detection and analysis method beneficial to quality control of the rocuronium bromide intermediate. The method is high in sensitivity, wide in linear range, good in specificity and repeatability and easy and convenient to operate.

The invention provides a preparation method of rocuronium bromide. The preparation method comprises the following steps: step 1, reacting a raw material compound I with acetyl chloride to obtain a compound II; 2, dropwise adding a hydrochloric acid solution into the compound II obtained in the step 1 to carry out a hydrolysis reaction, performing standing for layering, removing part of an organiclayer, adjusting the pH value of the residual reaction solution to 7-9 by using a sodium carbonate aqueous solution, separating out an organic phase, and treating to obtain a compound III; 3, adding dichloromethane, anhydrous magnesium sulfate and alkaline aluminum oxide into the compound III and allyl bromide, carrying out a quaternization reaction under the nitrogen flow, filtering under the protection of nitrogen after the reaction is completed, concentrating a filtrate to obtain a concentrate, pulping the concentrate by using a dichloromethane-methyl tert-butyl ether-ethyl acetate system,separating out solids, and carrying out freeze drying to obtain a rocuronium bromide pure product. The purity of the prepared bulk drug product is greater than or equal to 99.8% (according to a USP40correction result), the maximum impurity content is less than or equal to 0.1% (according to the USP40 correction result), and the solvent residue sum is less than or equal to 0.5%.