Eszopiclone-containing particle and its preparation method

Abstract

The invention relates to an eszopiclone-containing particle and its preparation method. The particle can cover the bitter taste of eszopiclone, has no obvious sandy feeling, has uniform contents and high dissolution rate, and can be used for preparing solid dosage forms such as orally disintegrating tablets, dispersing tablets, suspension granules and the like.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to eszopiclone-containing granules and a preparation method thereof. Background technique [0002] Insomnia is a manifestation of sleep disorders. Insomnia not only causes changes in perception and spirit, but also may cause functional diseases and even induce other diseases, which is a great potential threat to human health. At present, nearly 1 / 4 of the people in the world suffer from insomnia, and more than 10% of people in our country have sleep disorders. When insomnia is severe and sleep hygiene and nonpharmacologic treatments are ineffective, drug therapy is the first choice. [0003] Commonly used sedative and hypnotic drugs such as barbiturates and benzodiazepines often have various side effects, such as causing drowsiness, fatigue, dizziness, ataxia, temporary amnesia and disturbance of consciousness. In severe cases, it may lead to coma and respiratory depress...

AI Technical Summary

Problems solved by technology

[0005] However, eszopiclone can produce extremely strong and persistent bitter taste in the oral cavity, and this shortcoming makes the development of oral formulations of eszopiclone greatly limited

Although the common tablets of eszopiclone currently on the market provide a choice for the application of eszopiclone, the disadvantages and limitations of use of conventional common tablets are also very obvious: 1. It cannot effectively cover the bad taste of the drug, causing disintegration The disintegration and drug dissolution time is longer, and the curative effect is slow; although the film-coated tablet has a taste-masking effect to a certain extent, its disintegration and drug dissolution may be worse; 2. The local concentration of the drug after disintegration is high, which may easily cause gastric Intestinal adverse reactions; 3. It must be swallowed whole, and the elderly, children and other patients with dysphagia have poor compliance; 4. The swallowed tablets may stick to the esophagus, causing foreign body sensation or even drug-induced esophageal damage

In conclusion, ordinary tablets are difficult to maximize the application advantages of eszopiclone

CN1418631A discloses a zopiclone orally disintegrating tablet. Although the tablet is dissolved in the oral cavity and is easy to swallow, the disintegrating tablet cannot effectively cover the bitter taste of zopiclone, and patients have a certain sense of rejection

We have found through experiments that this method has the following defects when it is used to prepare eszopiclone granules: 1. Due to the difference in bulk density between eszopiclone bulk drug and excipient powder, it is easy to stratify in a fluidized state, resulting in poor particle content uniformity; 2. The powder of eszopiclone raw material medicine is easy to fly and adhere to the fluidized bed equipment during the fluidization process, resulting in a large loss

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