10 results about "Zopiclone" patented technology

The invention belongs to the technical field of pharmaceutical preparations, and particularly discloses a pharmaceutical composition of eszopiclone and a preparation method of the pharmaceutical composition, and the pharmaceutical composition comprises the following components by weight: 3-5% of eszopiclone; 65-85% of lactose; 5-25% of corn starch; 5-25% of pregelatinized starch; 0.5 to 5% of povidone K30; 0.5-5% of carboxymethyl starch sodium; 0.1-1% of silicon dioxide; and 0.25-5% of magnesium stearate. According to the preparation method provided by the invention, the main drug eszopiclone and lactose are mixed through an equivalent progressive increase method, and then the mixture is mixed with other diluents, disintegrants and adhesives to prepare wet granules, so that non-uniform dispersion of the main drug with a small proportion in the auxiliary materials can be avoided, the content uniformity of the product is ensured, and the problems in the background technology can be effectively solved.

The invention relates to a preparation method of a zopiclone related substance N-acetyl zopiclone, which comprises the following steps: dispersing or dissolving N-demethylated zopiclone or a salt thereof serving as a raw material in a solvent, and adding an acetylation reagent for reflux reaction in the presence of a basic catalyst. According to the synthesis method, the reaction endpoint can be judged through visual inspection of solution clarification, the purity of the crude product is high, the yield is high, the reaction condition is mild, the impurity content of the product is low, the synthesis method is suitable for production amplification, and the product is suitable for being used as a zopiclone impurity standard substance.

This invention belongs to the field of clinical efficacy evaluation technology, specifically relating to a method and system for evaluating the efficacy of oral antisleep granules combined with acupoint application in treating insomnia of the heart-kidney disharmony type. The method includes the following steps: selecting subjects to form an observation group and a control group; the control group receiving oral zopiclone tablets; the observation group receiving the same treatment as the control group, combined with oral antisleep granules and acupoint application; observing and comparing indicators: comparing the indicators of the control group before and after treatment with those of the observation group before and after treatment to obtain the efficacy difference between the two groups. The indicators include: a Traditional Chinese Medicine (TCM) syndrome score, where a scale is used to score difficulty falling asleep, shallow sleep with easy awakening / difficulty falling back asleep after waking, early awakening, and lower back and knee weakness. The efficacy evaluation method and system of this application can evaluate the efficacy of oral antisleep granules combined with acupoint application in treating insomnia of the heart-kidney disharmony type.

The present invention addresses the problem of providing: a novel alkyne derivative or a pharmaceutically acceptable salt thereof; and a medicine containing said compound as an active ingredient.　This alkyne derivative or a pharmaceutically acceptable salt thereof exhibited an activity characteristic with respect to an α1 subunit in a GABAAα1β2γ2PAM test, showed, like eszopiclone, a decrease in the awake period and the REM sleep period, an increase in the Non-REM sleep period, and shortening of sleep onset latency, in a sleep test, and showed a weaker bitterness than eszopiclone in a bitterness test. Therefore, this compound has an excellent characteristic in which bitterness is reduced compared to eszopiclone, and is useful as a medicine such as an agent for ameliorating or treating sleep disorders.

The invention belongs to the technical field of medicine detection, and particularly discloses a method for detecting related substances of an eszopiclone intermediate YZ2, which comprises the following steps of: preparing a test solution: taking a proper amount of eszopiclone intermediate test, and dissolving the eszopiclone intermediate test with acetonitrile to a constant volume; an impurity positioning solution: taking proper amounts of reference substances of impurities C, H and N, and respectively dissolving the reference substances with acetonitrile to a constant volume; the determination method comprises the following steps: respectively and precisely measuring the test solution and the three impurity positioning solutions, injecting into a high performance liquid chromatograph, and recording chromatograms; and carrying out peak positioning on the three impurities according to the chromatogram of the impurity positioning solution, analyzing the chromatogram of the test solution, and calculating according to a peak area normalization method to obtain the content of each related substance in the eszopiclone intermediate. According to the present invention, the high performance liquid chromatography is adopted, and the contents of the effective components and the impurities in the eszopiclone intermediate are analyzed, such that the purity of the eszopiclone intermediate can be monitored, the quality can be ensured, and the production process can be evaluated.

The invention belongs to the technical field of pharmaceutical chemistry, and particularly discloses a novel zopiclone process impurity and a preparation method thereof.According to the novel zopiclone process impurity and the preparation method thereof, the structure of the impurity with the large content in zopiclone synthesis reaction liquid is confirmed, and the structure of the impurity is # imgabs0. 4-methyl piperazine-1-formyl chloride hydrochloride and DMAP are stirred to react in a reaction solvent, filtering is carried out after the reaction is finished, a filter cake is pulped with a purification solvent, suction filtration and drying are carried out, and the impurities are obtained. The preparation method disclosed by the invention is simple and convenient to operate, low in cost and high in purity, and provides a high-purity impurity sample or standard substance for process research and quality control of zopiclone.

This invention relates to a method for detecting zopiclone impurities, the method comprising the following steps: Step A: preparation of diluent; Step B: preparation of test solution: take zopiclone, add diluent, and dilute to prepare a test solution; Step C: preparation of reference solution: take impurity 6-(5-chloro-2-pyridinyl)-7-ethoxy-5,6-dihydropyrrolo[3,4-b]pyrazin-5-one reference standard and zopiclone reference standard, add diluent, sonicate to dissolve, and prepare a reference solution; Step D: determination method: take the test solution and reference solution respectively, inject them into a high-performance liquid chromatograph, record the chromatogram, and calculate the impurity content; wherein, the chromatographic conditions are: using octadecylsilane-bonded silica gel as the packing material; using acetonitrile-buffered saline solution as the mobile phase; flow rate of 0.5 mL to 2.5 mL per minute; detection wavelength of 280 nm to 320 nm; column temperature of 25 °C to 35 °C; sample chamber temperature of 0 °C to 15 °C; injection volume of 10 to 30 μl.

The present application relates to a preparation method of zopiclone related substance N-acetyl zopiclone, which takes N-desmethyl zopiclone or a salt thereof as a raw material, disperses or dissolves in a solvent, and refluxes in the presence of an alkaline catalyst and by adding an acetylating agent. The synthesis method of the present application realizes the goal of judging the reaction endpoint by visually observing the solution clarity, high purity of the crude product, high yield, mild reaction conditions, low impurity content of the product, and can be suitable for production scale-up and product use as a zopiclone impurity standard.

The invention discloses a detection method of eszopiclone related substances, which comprises the following steps: respectively taking an eszopiclone reference substance, an impurity A reference substance and an impurity B reference substance, and fixing the volume by using a diluent of which the pH value is adjusted to 2.5 to obtain a system applicable solution; preparing an eszopiclone test solution and an eszopiclone reference solution by adopting the diluting agent; and respectively measuring the system applicability solution, the test solution and the reference solution, respectively testing and recording high performance liquid chromatograms, and calculating according to an external standard method to obtain the content of each related substance in eszopiclone. After the pH value of the diluent is adjusted to 2.5, (1) the solution stability is good, and the diluent does not need to be newly prepared temporarily; (2) the positioning retention time of the impurity A is consistent with the retention time of the impurity A in the test sample labeling solution, and the positioning peak retention time of other known impurities is consistent with the retention time of each impurity peak in the test sample labeling solution. The detection method provided by the invention has better durability and higher accuracy.

This invention belongs to the field of drug detection technology, specifically disclosing a method for detecting related substances in eszopiclone intermediate YZ2, comprising the following steps: Test solution: Take an appropriate amount of the eszopiclone intermediate test sample and dissolve and dilute to volume with acetonitrile; Impurity localization solutions: Take appropriate amounts of impurity C, H, and N reference standards and dissolve and dilute to volume with acetonitrile respectively. Determination method: Accurately measure the test solution and the three impurity localization solutions, inject them into a high-performance liquid chromatograph, and record the chromatograms; based on the chromatograms of the impurity localization solutions, locate the peaks of the three impurities, analyze the chromatogram of the test solution, and calculate the content of each related substance in the eszopiclone intermediate using the peak area normalization method. This invention uses high-performance liquid chromatography to monitor the purity of the eszopiclone intermediate by analyzing the content of active ingredients and impurities, ensuring quality and evaluating the production process.