53 results about "Vincamine" patented technology

The invention relates to a vincamine preparation method in the field of compound preparation. The vincamine preparation method includes the steps of (1), tabersonine preparation, (2), vincadifformine preparation, (3), monoperoxy maleic acid preparation and (4), vincamine preparation. The vincamine preparation method has the advantages of easy availability to raw materials, simplicity and convenience in reaction process operation, high safety, low cost, high product yield, high quality and suitability for industrial production.

Pharmaceutical compositions and methods for treating or preventing an inflammatory condition in a patient are disclosed. The pharmaceutical compositions and methods include the use of vincamine or a vincamine derivative, either alone or in combination with one or more additional therapeutic agents, including a steroid (preferably a corticosteroid), an angiotensin II receptor (type 1) antagonist, an angiotensin-converting enzyme (ACE) inhibitor, and a non-steroidal anti-inflammatory drug.

The invention discloses a vincamine sustained-release pellet preparation, which comprises main medicines of vincamine, acid blank pellet cores, an adhesive and a diluent in a weight ratio of (1-10): (10-20): (1-10): (20-200), wherein the acid blank pellet cores consist of blank pellet cores and an organic acid covered on the blank pellet cores. The invention provides the vincamine preparation which can be stably released under the pH of 1.5-7.4, the release pH dependency of the conventional vincamine sustained-release preparation is solved, the vincamine preparation can be released stably and slowly in stomach and intestinal tracts, and the pharmaceutical effect is lasting. Moreover, the invention also discloses a preparation method for the vincamine sustained-release pellet preparation. The preparation method is simple, good in repeatability, high in production efficiency and suitable for industrialized mass production. The prepared medicine-carrying pellets are smooth and round, are released uniformly under the pH of 1.5-7.4, and are high in stability.

The invention discloses a preparation method of high-purity vinpocetine. The preparation method comprises the following steps: S1, preparing vincamine, wherein tabersonine is dissolved, a hydrogenation reaction is performed under the catalysis of palladium and carbon to obtain vincadifformine, the vincadifformine is oxidized to obtain a vincadifformine nitric oxide, and an intermediate vincamine is obtained from the vincadifformine nitric oxide reaction liquid under the catalysis of an acid; S2, dewatering the vincamine by using toluene as a solvent and adding a dewatering agent to obtain apovincamine; and S3, on the basis of the step S2, carrying out a transesterification reaction by taking ethanol as a solvent, using dichloromethane as a cosolvent and using sodium ethoxide / sodium methoxide as a catalyst to obtain a vinpocetine crude product, and re-crystallizing with ethanol to obtain vinpocetine. The process provided by the invention has the advantages of simple production operation, avoidance of high-toxicity reagents, less impurity of the obtained product, high production efficiency, simple and convent operation and environmental friendliness, wherein the purity of the productis more than 99.9%, the quality of the product is higher than the quality of the product obtained by the original research factory, and the medicinal requirements are met.

The invention discloses a synthesis method of vinpocetine. The synthesis method comprises adding vincamine into a three-neck flask, adding toluene into the three-neck bottle, stirring the mixture in ice water bath, dropwise adding polyphosphoric acid, placing the mixture into oil bath after half an hour, installing a water separator and a condensation tube, pumping to be vacuum, replacingnitrogen for two times, and performing reaction for 8 hours at the temperature of 120 DEG C; drying solvent by distillation after reaction is finished, adding ethanol and water, simultaneously dropwise adding caustic soda solution, utilizing saturated potassium carbonate solution to regulate pH to be 12 when the pH is 9, separating out solid, filtering and performing vacuum drying to obtain apovincamine; and adding absolute ethyl alcohol into the three-neck bottle, stirring the mixture in the ice water bath for one hour, then adding caustic alcohol into the mixture, adding the apovincamine after half an hour's stirring, placing a reaction bottle in the oil bath, performing reaction for 12 hours at the temperature of 80 DEG C, then steaming out solvent, adding the solvent into hydrochloric acid, extracting the mixture through ethyl acetate, adjusting pH value of the water phase to 12, separating out solid, filtering and drying to obtain the vinpocetine. The synthesis method is few in reaction step, low in energy consumption and less in environment pollution, recrystallization is not needed, and the purity of the vinpocetine can reach 99.5%.

The invention relates to a synthetic process for chemical medicines, in particular to a process for preparing vincamine by a semisynthetic method. At present, the process for preparing the vincamine is divided into a total synthetic method and the semisynthetic method, wherein the semisynthetic method has the problems of unstable and inflammable hydrogenation catalyst, large using amount, high hydrogenation pressure, insecurity in the preparation of monoperoxide maleic acid and the like. The process comprises the following steps of: preparing tabersonine vincadifformine hydrochloride, preparing the monoperoxide maleic acid, performing oxidizing reaction, performing reduction reaction and transposition reaction, precipitating ammonia and purifying products, wherein the low-cost and stable Pd / C hydrogenation catalyst is selected to reduce the pressure of the hydrogenation reaction; tabersonine sulfate is replaced by the tabersonine hydrochloride; the monoperoxide maleic acid is preparedby using low-concentration hydrogen peroxide; the reaction temperature is below 0 DEG C, and security coefficients are improved; the temperature of the oxidizing reaction is reduced, and the generation of isomers is reduced; purification and solvent recrystallization are performed by column chromatography; and the quality of the products reaches the pharmaceutical-grade standard.

The invention relates to preparation methods for chiral impurities of vincamine. Through oriented synthesis method and the later column chromatography separation, high purity product of seven chiral impurities can be obtained, and the preparation methods can be used for the qualitative and quantitative analysis of impurities in the production of vincamine, so that the separation and confirmation of the seven chiral impurities in vincamine drugs can be realized, and the drug standard of the vincamine can be enhanced, and therefore, the vincamine with high purity can be obtained. Compared with existing preparation methods for the vincamine, the preparation methods relate to the preparation of seven chiral isomers, and are more complete and simpler in operation.

The invention relates to a special reaction kettle for synthesizing vincamine intermediate vinblastine forming, which comprises a kettle rack, a kettle erected on the kettle rack and a stirring device, the kettle comprises a kettle body and a kettle cover which is hermetically connected with the kettle body, a material outlet is provided at the lower part of the kettle body, a material inlet is provided on the kettle cover, insulation jackets of the steam inlet and condensed water outlet are provided outside the kettle body, particularly, the stirring device is a magnetic stirring device, and comprises a magnetic device arranged at the lower part of the kettle body and a magnetic stir bar which is in the kettle body and rotated by driving of the magnetic device. The reaction kettle of the invention uses the magnetic stirring device to replace traditional mechanical stirring, the reaction kettle has good seal performance and can satisfy the sealing requirement of synthesizing the reaction kettle by catalytic hydrogenation. Simultaneously, the magnetic stirring device can provide the required stirring force for the catalytic hydrogenation reaction, compared with the mechanical stirring mode, the reaction kettle of the present invention has lower energy consumption and is in favor of reducing the production cost.

The invention provides a preparation method for vinpocetine. The method comprises the following steps: with vincamine as a raw material and triethyl formate as an esterification reagent, subjecting vincamine and triethyl formate to a one-step reaction under the action of Lewis acid so as to obtain a crude vinpocetine product; and then carrying out washing with alkali lye, decoloring in alcohol and recrystallization so as to prepare a refined vinpocetine product. Compared with the prior art, the preparation method provided by the invention has the advantages of short process flow, simple operation and suitability for industrial production, and the prepared refined vinpocetine product has yield of more than 89%, a melting point of 148 to 151 DEG C, HPLC of greater than 99%, a whitish color, good quality and low preparation cost.

The invention provides a pervone vincamine injection and a preparation process thereof, relating to the technical field of pervone vincamine injections and preparation processes thereof. The injection is a solution type injection or frozen powder injection, and the solution type injection is divided into a water injection and a drug-carried type infusion solution, wherein the contained active constituent is the pervone vincamine, and the pervone vincamine can exit in the form of soluble salt. The invention has the advantages that compared with the prior art, the injection has the characteristics of unique formulation, convenient use, fast curative effect, safety, reliability and the like, and is applied to the clinical treatment, in particular to the intravenous injection for some patients who can not swallow drugs due to all kinds of reasons or can not carry out the oral administration due to the gastrointestinal tract dysfunction; and the preparation process is simple, convenient and economical, is easy for industrial production, has high economic and social benefits, and solves the key problem that the solubility of the pervone vincamine is lower in water because the pervone vincamine belongs to alkaloids in tryptophane system. It is especially significant to develop a pervone vincamine aqueous solution applied to the clinical treatment.

The invention discloses a production process using a semi-synthetic method to prepare vincamine. The production process comprises the following steps: using a tabersonine salt as a reaction starting raw material, performing hydrogeneration catalytic reduction, enzyme method hydroxylation and rearranged crystallization to obtain vincamine. The process is simple and short in process route; the obtained vincamine is high in yield and good in purity; the whole production process is low in cost and suitable for industrial production; the enzyme method hydroxylation is performed by oxygenase, so that the process is clean, safe and environment-friendly.

The invention discloses a method for detecting isomer impurities in vincamine, which uses high-performance liquid chromatography for detection, uses a CHIRALCEL OD-RH chiral chromatographic column as a chromatographic column, and uses a mixed solution of borax-boric acid buffer and acetonitrile Carry out isocratic elution for mobile phase, record chromatogram, calculate the content of impurity A in vincamine according to the peak area in chromatogram. The method of the invention can quantitatively determine the content of the isomer impurity A in the vincamine raw material, has the advantages of high accuracy and high sensitivity, and is beneficial to the quality control of the vincamine raw material.

The invention provides a method for detecting related substances vinblastine and apovincine in an injection, which uses high performance liquid chromatography to quantitatively identify impurity vinblastine and impurity apovincine in vinpocetine injection , the chromatographic conditions are: the filler of the chromatographic column is cyanosilane bonded silica gel, the flow rate is 0.5-0.7mL min-1, the column temperature is 30-34°C, and the volume ratio is 30-65:65-70 of 0.1 mol / L~0.25mol / L triethylamine solution and ethanol are mobile phases. The present invention uses high performance liquid chromatography to measure the content of impurity vinblastine and impurity apovincine in vinpocetine injection. The method has the advantages of good separation effect, sensitivity and accuracy, and ensures stable and uniform quality of the product. Sexuality and curative effect; The method of the present invention is simple, specificity is strong, reproducibility is good, has guaranteed the quality and curative effect of vinpocetine injection effectively, has very strong practicability.

The invention relates to a crystallizing tank used for vincamine, comprising a tank rack, a tank and a stirring device, wherein the tank and the stirring device are arranged on the tank rack; the tank comprises a tank body and a tank cover connected with the tank body in a sealing mode; the bottom of the tank body is provided with a discharge hole; a dump valve is arranged on the discharge hole; the tank cover is provided with a feeding hole; the circumstance of the tank body is also provided with a jacket with a cooling water inlet and a cooling water outlet; and the discharge valve comprises a valve plate and a filter plate for blocking the discharge hole. Especially, the thickness of the discharge hole is same with that of the bottom of the tank body; and the valve plate is used for blocking an annular continuous arc-shaped surface formed by parts of upper surface of the discharge hole and the inner surface of the bottom of the tank. The crystallizing tank is characterized in that the valve plate of the discharge valve is used for blocking the annular continuous arc-shaped surface formed by parts of upper surface of the discharge hole and the inner surface of the bottom of the tank without any stirring dead corner, and fine-grain crystallization with even particle diameter can be obtained.