5 results about "Zopiclone" patented technology

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.

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.

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.