Oral solid preparation released at given time and preparation method thereof

Abstract

The invention relates to a zaleplon preparation released at a given time. The zaleplon preparation is prepared by coating a core or particle containing a tablet. The core or particle containing the tablet comprises the following components in parts by weight: 2-10 parts of zaleplon, 25-35 parts of a filler, 0-5 parts of an adhesive, 4-5 parts of a disintegrant, and 0.4-0.8 part of a lubricant, wherein the coating component comprises the following ingredients in parts by weight: 20-30 parts of glyceryl behenate, 9-10 parts of hydroxypropylcellulose, and 20-30 parts of an opacifier.

Description

technical field [0001] The invention relates to a preparation method of a pharmaceutical preparation in the field of pharmacy, in particular to a time-released oral solid preparation with zaleplon as the main drug and a preparation method. technical background [0002] Zaleplon is a sedative-hypnotic drug with the chemical name N-[3-(3-cyanopyrazo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide. Its molecular formula is: C 17 H 15 N 5 O, the molecular weight is 305.34, and the structural formula is: [0003] [0004] Zaleplon is a white or off-white powder; slightly soluble in ethanol or propylene glycol, almost insoluble in water, with a partition coefficient of 1.23 in n-octanol / water. [0005] Zaleplon is a sedative-hypnotic drug suitable for short-term treatment of insomnia with difficulty falling asleep. It exerts its pharmacological effects by acting on the gamma aminobutyric acid-benzodiazepine (GABA-BZ) receptor complex in vivo. For the regular formulation of z...

AI Technical Summary

Problems solved by technology

Despite the great advancements in available APIs, the inherent properties of such APIs such as short half-lives will largely affect their effectiveness, side effect profile, and patient acceptance

Immediate-release dosage forms of this class of drugs are usually effective, providing rapid release of the drug shortly after ingestion, causing rapid sleep onset; however, the short drug half-life results in short sleep duration or frequent nocturnal waking events, so that the patient will need to take additional preparations at night to maintain sleep

[0009] When most insomnia patients do not complain about difficulty in falling asleep, but only short sleep time and frequent nighttime waking time, insomnia patients especially insomnia occurs at the end of sleep, patients wake up prematurely, and patients who cannot fall asleep again, middle-aged and elderly insomnia Patients often have this form of manifestation. Traditionally, medium and long-acting sleeping pills are used. This method often exerts the maximum efficacy of the drug when the patient does not need the drug (early sleep), and it is accompanied by toxic side effects (symptoms such as headache) , drowsiness, dizziness, nausea and vomiting, fatigue, memory difficulties, dreams and other adverse reactions) the probability of increased, while the effect of drug treatment in the middle and late stages of sleep is reduced

[0010] Zaleplon marketed at home and abroad is oral regular-release tablets and regular-release capsules, the specifications are: 5mg, 10mg, taken before going to bed at night, only to induce sleep, and the short half-life of the drug leads to short sleep duration or frequent sleep Waking up at night, and the release rate of the regular-release dosage form is too fast to cause toxic side effects such as drowsiness and dizziness. To achieve the desired effect, it is necessary to take another preparation in the early morning to maintain sleep, which does not conform to the patient's medication habits and brings inconvenience to the patient.

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