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Zalaipulong injection

A technology for zaleplon and injection preparations, applied in the field of chemical pharmaceutical preparations, can solve the problems of withdrawal symptoms, large side effects, addiction and the like, and achieve the effects of small dose, fast onset, and few side effects

Inactive Publication Date: 2006-06-14
SHANDONG CHENGCHUANG PHARMA R&D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this type of drug has relatively large side effects, common adverse reactions are drowsiness, dizziness and fatigue, long-term continuous drug use can cause dependence and addiction, withdrawal symptoms may occur after drug withdrawal, etc.
Compared with this, the new sedative-hypnotic drug with less side effects-zaleplon only has oral tablets and capsules. Compared with injection preparations, it has the disadvantages of slow onset of action and large dosage. Therefore, it is necessary to develop a clinical Zaleplon injection preparation with fast onset of action, small dosage and few side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Zaleplon 5g, add 1200ml of ethanol and stir to dissolve it properly, then add 400ml of propylene glycol, mix well, heat to dissolve; add 200ml of phosphate buffer (pH about 6.8) to adjust the pH to 7.1, add water for injection to 10000ml, stir uniform. Add 0.1% (g / ml) active carbon, stir and adsorb for 30 minutes, decarbonize, filter, carefully filter, fill and seal in ampoules by 1ml / branch, and sterilize at 115° C. for 30 minutes to obtain the injection of the present invention.

Embodiment 2

[0018] Zaleplon 1g, add 240ml of ethanol and stir to dissolve it in an appropriate amount, add 80ml of polyethylene glycol, then add 4 drops of polysorbate and mix well, heat to dissolve; add 40ml of phosphate buffer (pH about 6.8) to adjust the pH For 7.1, add water for injection to 2000ml, and stir well. Add 0.1% (g / ml) active carbon, stir and adsorb for 30 minutes, decarbonize, filter, carefully filter, fill and seal in ampoules by 2ml / support, and sterilize at 115° C. for 30 minutes to obtain the injection of the present invention.

Embodiment 3

[0020] Zaleplon 2g, add 480ml of ethanol and stir to dissolve it in an appropriate amount, add 80ml of propylene glycol and 80ml of polyethylene glycol, mix well, heat to dissolve; add 40ml of borate buffer solution (pH about 7.0) to adjust the pH to 7.3, add Water for injection to 4000ml, stir well. Add 0.1% (g / ml) gac to stir and adsorb for 30 minutes, decarbonize, filter, carefully filter, fill and seal in ampoules by 4ml / support, and sterilize at 115° C. for 30 minutes to obtain the injection of the present invention.

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PUM

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Abstract

A Zhalaipulong injection for the inducing of general anesthesia and treating epilepsy, convulsion, and minimal convulsion caused by tetanus contains proportionally the Zhalaipulong as active component and the solvent chosen from water-soluble or water-insoluble solvent and the water for injection.

Description

technical field [0001] The invention relates to a zaleplon injection preparation, which belongs to the field of chemical drug preparations. Background technique [0002] At present, the commonly used sedative and hypnotic drugs in clinic are benzodiazepines, such as diazepam and amobarbital, etc. These drugs have residual effects, addiction, dependence, secondary insomnia and other adverse reactions after drug withdrawal . Compared with benzodiazepines, the new non-benzodiazepine drugs developed and marketed in recent years have a highly selective effect on benzodiazepine ω1 receptors, and do not produce adverse reactions caused by benzodiazepine receptor stimulation. ;Plasma half-life is short, side effects such as sequelae are small; slow-wave sleep time is significantly shortened, and fast-wave sleep time is not affected. Representative drugs mainly include zolpidem, levopiclone, and zaleplon, among which zaleplon has the characteristics of short half-life and rapid ons...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P25/20
Inventor 王志刚岳珍
Owner SHANDONG CHENGCHUANG PHARMA R&D