A kind of pH-independent zaleplon double-pulse release capsule and preparation method thereof

Abstract

The invention relates to a pH-independent double-pulse release capsule with zaleplon as the main drug and a preparation method thereof. The zaleplon double-release capsules of the present invention, the contents of the capsules are composed of quick-release tablets and time-selected release tablets, and the quick-release tablets are composed of the following components in parts by weight: zaleplon 50-200 220-880 parts of filler, 10-40 parts of binder, 15-60 parts of disintegrating agent and 5-20 parts of lubricant. The core is composed of 125-500 parts of zaleplon, 168-675 parts of filler, 0-100 parts of binder, 50-200 parts of disintegrant and 6-26 parts of lubricant in parts by weight.

Description

technical field [0001] The invention relates to a preparation method of pharmaceutical preparations in the field of pharmacy, in particular to a pH-independent double-pulse release capsule with zaleplon as the main ingredient and a preparation method thereof. technical background [0002] Zaleplon is a sedative-hypnotic drug with the chemical name N-[3-(3-cyanopyrazol[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 white or off-white powder; slightly soluble in ethanol or propylene glycol, almost insoluble in water, and the partition coefficient in n-octanol / water is 1.23. [0005] Zaleplon is a sedative-hypnotic drug suitable for the short-term treatment of insomnia with difficulty falling asleep. It exerts its pharmacological effects by acting on the γ-aminobutyric acid-benzodiazepine (GABA-BZ) receptor complex in the body. For the ...

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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, The patient will need to take another preparation to maintain sleep at night, which brings a lot of inconvenience to the patient

Traditionally, middle and long-acting sleeping pills are used. This method often exerts the maximum drug effect in the early stage of sleep, and the therapeutic effect of the drug is significantly reduced in the middle and late stages of sleep. To achieve the therapeutic effect in the middle and late stages of sleep, it is necessary to increase the dosage , which is accompanied by a significant increase in the probability of toxic side effects (symptoms such as headache, drowsiness, dizziness, nausea and vomiting, fatigue, memory difficulties, dreaminess, etc.)

[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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