38 results about "Ropivacaine hydrochloride" patented technology

Disclosed herein is hyperbaric solution for injection of Ropivacaine Hydrochloride which comprises Ropivacaine Hydrochloride; a base / acid to adjust the pH and a baricity adjuster to modify Baricity of the injection solution.

The invention discloses a temperature-sensitive gel for ropivacaine long-acting injection and a preparation method thereof. The gel comprises main ingredients ropivacaine, ropivacaine hydrochloride or ropivacaine mesylate; Glycolide molar ratio 2-3:1, PLGA-PEG-PLGA copolymer with PEG molecular weight of 1000, PEG accounts for 18-30% of the total mass of the copolymer; water for injection, normal saline or pH adjustment solution. The preparation method is to fully swell the copolymer in a solvent, add the main drug, and sterilize through a filter membrane. The temperature-sensitive gel is convenient for administration, gels rapidly at body temperature and exerts a slow-release effect. The drug release in vitro is ≤35-45%, 48 hours ≥65%-75%, and 72 hours ≥80%, which is in line with local anesthetics. After a single injection of continuous analgesia 48h design requirements. Pharmacodynamic studies have shown that the ropivacaine temperature-sensitive gel group can significantly prolong the maintenance time of the drug effect, and can continuously exert an analgesic effect for 48 hours.

The invention relates to a ropivacaine hydrochloride injection and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The injection contains ropivacaine hydrochloride and a stabilizer, the mass ratio of the two is 1:1-1.6; the stabilizer is one of trehalose and trehalose sodium sulfate or a mixture of the two in any proportion . The ropivacaine hydrochloride injection of the present invention, due to the structural characteristics of trehalose and its unique biological characteristics, can inhibit the enantiomeric transformation of ropivacaine hydrochloride in aqueous solution, and enhance the strength of ropivacaine hydrochloride. The stability of the injection solves the problems of poor stability, light and heat resistance, and easy freezing of the ropivacaine hydrochloride injection, and obtains satisfactory technical results.

The invention provides a ropivacaine hydrochloride sodium chloride injection and a preparation method thereof. The method comprises the process steps of: burdening, carbon adsorption, rough filtering, fine filtering, filling, sterilizing, lamp detecting, packing and the like. The prepared ropivacaine hydrochloride sodium chloride injection has a definite medicinal effect and high safety; the test result of each index in a stability test is accordant with specifications, and the defects of the requirement of repeated injection, inconvenience in using, easiness in increasing secondary pollution by freeze-dried powder and the like existing in a ropivacaine water injection are overcome; the ropivacaine hydrochloride sodium chloride injection is particularly suitable for a patient using an analgesia pump; during use in a large volume, an instant stable concentration is kept for a medicinal liquid, so that a remarkable postoperative analgesic effect is achieved, and the requirement of an opioid medicament is remarkably lowered; and moreover, the effect can be enhanced rapidly by administrating in a self-pressing way.

The invention provides a ropivacaine hydrochloride impurity and a preparation method thereof. The structural formula of the ropivacaine hydrochloride impurity is shown in formula I. The ropivacaine hydrochloride impurity of the present invention is a kind of impurity discovered by the inventor during the research process. A new compound, the impurity of ropivacaine hydrochloride of the present invention is of great significance for quality control in the synthesis process of ropivacaine hydrochloride, and the inventors have found through research that the impurity of ropivacaine hydrochloride with structural formula such as formula I has excellent The anesthetic performance can be used for a new kind of anesthetic. The method of the present invention is simple in operation and mild in conditions. It only needs to mix the reaction raw materials to generate ropivacaine hydrochloride impurities. It does not need to control temperature and other conditions, and the preparation method has low cost and no side reactions. The impurity of pivacaine has high purity and high yield, which is beneficial to reduce the cost of quality control analysis of ropivacaine hydrochloride.

The invention provides a method for preparing hydrochloric acid ropivacaine. Part of parameters and conditions in the prior art are improved, and optimization is performed through the following steps that intermediate (I) separation pH and separation extracting solvent are selected; a catalyst and the usage quantity of the catalyst in a resolution agent are selected; refining solvent is selected. In this way, the yield and purity of the prepared hydrochloric acid ropivacaine are high, the purity reaches up to over 99% under the optimal condition, the percentage of dextrorotary isomer is reduced below 0.5%, standard requirements are completely met, and the hydrochloric acid ropivacaine is suitable for industrial production.

The invention relates to a freeze-dried ropivacaine hydrochloride composition for injection. The freeze-dried ropivacaine hydrochloride composition comprises ropivacaine hydrochloride and lactose, for example, 75 parts by weight of ropivacaine hydrochloride and 20-60 parts by weight of lactose. The composition is basically prepared by a method comprising the following steps: weighing a formulated amount of ropivacaine hydrochloride and lactose, adding an appropriate amount of injection water, and stirring for dissolution; adding active carbon into a medicinal solution obtained in the previous step, stirring, and filtering to remove carbon; refilling the injection water to a full formulated amount, stirring uniformly, measuring the pH value of the solution and optionally measuring the content of active ingredients, and adjusting the pH value to 4.0-6.0 by using a pH value regulator if necessary; carrying out sterilization and filtration on the medicinal solution, and filling the solution into a penicillin bottle; and carrying out freeze-drying to remove water, and carrying out tamponment. The freeze-dried ropivacaine hydrochloride composition for injection, provided by the invention, has excellent pharmaceutical properties as described in the specification.

The invention belongs to the technical field of injection production, and particularly relates to a ropivacaine hydrochloride sodium chloride injection and a preparation process. The ropivacaine hydrochloride injection comprises 0.40 g of ropivacaine hydrochloride and 1.72 g of sodium chloride in every 200 ml of the ropivacaine hydrochloride injection, and injection water is added to 200 ml of the ropivacaine hydrochloride injection. In addition, the preparation device comprises a machine body assembly, an injection storage box, a sterile filling mechanism, a cover pressing mechanism and a control box, the sterile filling mechanism comprises a conveying pump, the conveying pump is connected with a liquid conveying main pipe, and the lower end of the liquid conveying main pipe is connected with a plurality of liquid conveying branch pipes at intervals; the ropivacaine hydrochloride sodium chloride injection provided by the invention is clear in drug effect and high in safety, determination results of various indexes in a stability test all meet regulations, and the preparation device ensures the product quality of the prepared injection, so that the drug effect of the injection is clear, and the safety is high.

The invention belongs to the field of chemical synthesis technology, and concretely relates to a preparation method of a ropivacaine hydrochloride impurity F (8aS)-2-(2,6-dimethylphenyl)-3,3-dimethyl-imidazo[1,5-a]pyridine-1(5H)-ketone. (S)-N-(2',6'-dimethylphenl)-2-piperidine carboxamide and acetone are used as raw materials, a condensation reaction is carried out with an acidic condition in order to remove one water molecule, a solution is distilled, treatment is adjusted with alkaline, the impurity F crude product is obtained, then refining is carried out, and the high-purity ropivacaine hydrochloride impurity F is obtained. The method has the advantages of short synthetic route, simple operation, and high product purity; and a qualified impurity reference substance is provided for quality control of ropivacaine hydrochloride.

The invention relates to a freeze-drying ropivacaine hydrochloride composition for injection and a quality control method thereof. The composition is prepared from ropivacaine hydrochloride and lactose, for example, the composition is prepared from, by weight, 75 parts of ropivacaine hydrochloride and 20-60 parts of lactose. The composition is basically prepared through the following steps that ropivacaine hydrochloride and lactose are weighed according to the amount in the prescription, a proper amount of injection water is added, and stirring is carried out to dissolve the mixture; active carbon is added in the medicine liquor obtained in the last step, stirring is carried out, and filtering is carried out to remove carbon; injection water is supplemented to the full amount of the prescription, the mixture is stirred evenly, the pH value of the solution is measured, the content of active ingredients is optionally measured, and the pH is regulated with an acid-base regulator if necessary; the medicine liquor is sterilized, filtered and then poured into penicillin bottles; freeze-drying is carried out to remove moisture, plugs are pressed, and the freeze-drying ropivacaine hydrochloride composition is obtained. The freeze-drying ropivacaine hydrochloride composition has the excellent pharmaceutical properties stated in the description, and the quality control method has excellent methodological performance.

The invention relates to a method for preparing and purifying a ropivacaine hydrochloride intermediate. The method uses a single chiral raw material L-piperidine formic acid hydrochloride and 2,6-dimethylaniline to prepare a single chiral intermediate Body (-)-(2S)-N-(2,6-dimethylphenyl) piperidine-2-carboxamide can reduce resolution steps; the present invention further adopts non-polar solvent to intermediate (-) -(2S)-N-(2,6-dimethylphenyl) piperidine-2-carboxamide is refined to reduce related impurities. The preparation method of the present invention has simple and convenient post-processing, high product purity, and After refining, the purity reaches over 99.5%, the single impurity is less than 0.1%, and the total yield is greater than 80%, which is suitable for large-scale industrial production.