PH-independent zaleplon dipulse release capsule and method for preparing same

A zaleplon, double-release technology, applied in the field of pH-independent double-pulse release capsules and its preparation, can solve the problems of drowsiness, dizziness, inconvenience to patients, and affect the effectiveness of long-release dosage forms, so as to prolong sleep duration Time, increase sleep time, reduce the effect of adverse reactions

Active Publication Date: 2015-03-04
ZHONGSHUAI PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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, 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

Method used

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  • PH-independent zaleplon dipulse release capsule and method for preparing same
  • PH-independent zaleplon dipulse release capsule and method for preparing same
  • PH-independent zaleplon dipulse release capsule and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0078] Example 1: pH-independent double-pulse release capsule of zaleplon and its preparation method

[0079] The zaleplon dual-pulse release capsule of the present invention includes a quick-release tablet and a timing-release tablet. The weight ratio of the active ingredient zaleplon contained in the quick-release tablet and the timing-release tablet is 1:1.

[0080] The preparation method of zaleplon dual-pulse release capsules. The preparation method first uses a tablet press to compress the immediate-release tablets according to the commonly used techniques and methods in pharmaceutics; Use a coating pan to coat, and the coating film is attached to the tablet-containing core to obtain a timely release tablet; the immediate release tablet and the scheduled release tablet prepared above are filled into a capsule to obtain Zaleplon double pulse Release the capsule.

[0081] (1) Preparation of quick-release tablets:

[0082] The raw and auxiliary materials of the immediate-release t...

Example Embodiment

[0091] Example 2: pH-independent double-pulse release capsules of zaleplon and preparation method thereof

[0092] In the zaleplon double-pulse release capsule of the present invention, the weight ratio of the active ingredient zaleplon contained in the immediate-release tablet and the timing-release tablet is 1:1,

[0093] The preparation method of zaleplon dual-pulse release capsules. The preparation method first uses a tablet press to compress the immediate-release tablets according to the commonly used techniques and methods in pharmaceutics; Use a coating pan to coat, and the coating film is attached to the tablet-containing core to obtain a timely release tablet; the immediate release tablet and the scheduled release tablet prepared above are filled into a capsule to obtain Zaleplon double pulse Release the capsule.

[0094] It is basically the same as Example 1, except that:

[0095] The raw and auxiliary materials of the timing release tablet are: zaleplon 125g, filler microc...

Example Embodiment

[0097] Example 3: pH-independent double-pulse release capsules of zaleplon and preparation method thereof

[0098] The zaleplon dual-pulse release capsule of the present invention includes a quick-release tablet and a timing-release tablet. The weight ratio of the active ingredient zaleplon contained in the quick-release tablet and the timing-release tablet is 1:1.

[0099] The preparation method of zaleplon dual-pulse release capsules. The preparation method first uses a tablet press to compress the immediate-release tablets according to the commonly used techniques and methods in pharmaceutics; Use a coating pan to coat, and the coating film is attached to the tablet-containing core to obtain a timely release tablet; the immediate release tablet and the scheduled release tablet prepared above are filled into a capsule to obtain Zaleplon double pulse Release the capsule.

[0100] It is basically the same as Example 1, except that:

[0101] Preparation of double pulse release capsule...

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Abstract

The invention relates to a pH-independent zaleplon-based dipulse release capsule and a method for preparing the same. The contents of the Zaleplon-based dipulse release capsule comprise a quick-release tablet and a timed-release tablet, wherein the quick-release tablet is prepared from the following components in parts by weight: 50-200 parts of zaleplon, 220-880 parts of a filler, 10-40 parts of a binder, 15-60 parts of a disintegrant and 5-20 parts of a lubricant; the timed-release tablet comprises a medicine core and a coating, and the medicine core is prepared from the following components in parts by weight: 125-500 parts of zaleplon, 168-675 parts of a filler, 0-100 parts of a binder, 50-200 parts of a disintegrant and 6-26 parts of a lubricant.

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 ...

Claims

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Application Information

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IPC IPC(8): A61K9/62A61K31/519A61P25/20
Inventor 孙卫东任逢晓于艳玲
Owner ZHONGSHUAI PHARMA SCI & TECH CO LTD
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