Two-phase release preparation containing zolpidem or salt of zolpidem and preparation method thereof

Abstract

The invention discloses a two-phase release preparation containing zolpidem or salt of zolpidem, which is characterized by comprising a normal medicine-containing fast release preparation and enteric fast release preparation and being suitable for respectively releasing zolpidem or salt of zolpidem in two preset periods of time. More than 90% dose of the normal medicine-containing fast release preparation is released within 30 minutes in 0.01M of hydrochloric acid buffer solution at 37 DEG C, and more than 90% dose of the enteric fast release preparation is released within 30 minutes in phosphate buffer solution of 6.8 potential of hydrogen (pH) at 37 DEG C. The two-phase release preparation containing zolpidem or salt of zolpidem is specific to the sleep characteristics of a patient with sleep difficulties and early waking, and has effects on patients with both sleeping difficulties and early waking simultaneously.

Description

technical field [0001] The invention relates to a biphasic release preparation of zolpidem or a salt thereof, and also relates to a preparation method of the biphasic release preparation of zolpidem or a salt thereof. Background technique [0002] Insomnia is a common sleep disorder, which is caused by various reasons, such as difficulty in falling asleep, shallow sleep or too short sleep frequency, early awakening and insufficient sleep time or poor quality. Common causes of insomnia mainly include environmental factors, individual factors, physical factors, mental factors, emotional factors and so on. Among them, early awakening refers to the phenomenon of waking up 2-3 hours or more earlier than the normal situation more than four times a week, and cannot fall back to sleep again. People with insomnia often have trouble falling asleep and waking up early at the same time. The effective action time of most sleeping pills is generally 4-6 hours. Taking the medicine before...

AI Technical Summary

Problems solved by technology

Therefore, continuous dosing with sustained-release formulations, especially at times when patients would be sleeping peacefully, is unnecessary

After 3-4 hours, it is often at a loss to wake up early because the drug has been released and the effective drug concentration cannot be reached

At the same time, due to the long release time of sustained-release preparations and the individual differences of patients, it is difficult to effectively control a reasonable blood drug concentration level, resulting in symptoms such as dizziness in most patients the next morning, affecting normal work and life.

[0005] In addition, CN101574328 discloses a time-selected pulse-release pellet of zolpidem salt, the outer layer of which is a time-lag layer coated with a low-permeability acrylic resin containing a quaternary ammonium salt group, which controls the middle layer. The release of drugs and organic acids, after a period of time lag to release drugs, this time-selected pulse release pellets only for the symptoms of early awakening, and have no therapeutic effect on the difficulty in falling asleep that often accompany early awakening symptoms

Images