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A sustained-release preparation for treating Alzheimer's disease and its preparation method

A slow-release preparation and slow-release material technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pill delivery, etc. It can solve the problems of low bioavailability, low blood drug concentration, and small AUC, etc. problem, achieve the effect of avoiding burst release effect and high physiological tolerance

Active Publication Date: 2021-01-12
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The applied for patent 201610342152.9 describes a sustained-release tablet using hydroxypropyl methylcellulose as a sustained-release material. The in vitro release percentage at the last detection time point (12 hours) is higher than 90%, which meets the requirements for sustained-release preparations in the Chinese Pharmacopoeia. Requirements for in vitro release, but its pharmacokinetic test in Beagle dogs showed lower plasma concentration, lower AUC, and lower bioavailability

Method used

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  • A sustained-release preparation for treating Alzheimer's disease and its preparation method
  • A sustained-release preparation for treating Alzheimer's disease and its preparation method
  • A sustained-release preparation for treating Alzheimer's disease and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: the prescription of 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride slow-release preparation is as follows:

[0034] Dosage of ingredients:

[0035]

[0036]

[0037] Taking the preparation of 10,000 tablets of 2-(4-methylthiazol-5-yl)ethyl nitrate sustained-release preparation as an example, all excipients were pulverized respectively and passed through a 100-mesh nylon sieve. Take the main ingredient and grind it into powder. Take by weighing 499.5g 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride, 750.0g glyceryl behenate, 235.5g microcrystalline cellulose PH101 respectively according to the prescription composition in embodiment 1, mix Evenly, use 4% povidone ethanol solution to make soft material, granulate with 18 mesh sieve, dry at 50°C, granulate with 20 mesh sieve, add 15.0g magnesium stearate, mix evenly, and press with φ7 punch to tablet. The sustained-release preparation of 2-(4-methylthiazol-5-yl)ethyl nitrate hydrochloride wa...

Embodiment 2

[0046] Embodiment 2: the prescription of 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride slow-release preparation is as follows:

[0047] Dosage of ingredients:

[0048]

[0049] Taking the preparation of 10,000 tablets of 2-(4-methylthiazol-5-yl)ethyl nitrate sustained-release preparation as an example, all excipients were pulverized respectively and passed through a 100-mesh nylon sieve. Take the main ingredient and grind it into powder. Take by weighing 499.5g 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride, 120.0g glyceryl behenate, 180.0g hydroxypropyl methylcellulose respectively according to the prescription composition in Example 2 K100M, 685.5g microcrystalline cellulose PH101, mix well, make soft material with 4% povidone ethanol solution, granulate with 18 mesh sieve, dry at 50°C, granulate with 20 mesh sieve, add 15.0g magnesium stearate , mix well, and press the φ7 punch into tablets. The sustained-release preparation of 2-(4-methylthiazol-5-yl)eth...

Embodiment 3

[0054] Embodiment 3: the prescription of 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride slow-release preparation is as follows:

[0055] Dosage of ingredients:

[0056]

[0057] Taking the preparation of 10,000 tablets of 2-(4-methylthiazol-5-yl)ethyl nitrate sustained-release preparation as an example, all excipients were pulverized respectively and passed through a 100-mesh nylon sieve. Take the main ingredient and grind it into powder. Take by weighing 499.5g 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride, 120.0g glyceryl behenate, 300.0g hydroxypropyl methylcellulose respectively according to the prescription composition in Example 3 K15M, 685.5g microcrystalline cellulose PH101, mix well, make soft material with 4% povidone ethanol solution, granulate with 18 mesh sieve, dry at 50°C, granulate with 20 mesh sieve, add 15.0g magnesium stearate , mix well, and press the φ7 punch into tablets. The sustained-release preparation of 2-(4-methylthiazol-5-yl)ethy...

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Abstract

The invention relates to a sustained release preparation and a preparation method thereof. The sustained release preparation contains the following components: nitric acid 2-(4-methylthiazol-5-yl)ethyl ester hydrochloride or nitric acid 2-(4-methylthiazol-5-yl)ethyl ester maleate, a sustained release material, a filler, a lubricant, an adhesive or a wetting agent. The main sustained release material is glyceryl behenate or a mixture of hydroxypropyl methyl cellulose and hydroxypropyl methyl cellulose. The use amount of a main drug in the sustained release preparation is 0.1%-50% of the tabletweight of the sustained release preparation. The release behavior of the nitric acid 2-(4-methylthiazol-5-yl)ethyl ester hydrochloride or nitric acid 2-(4-methylthiazol-5-yl)ethyl ester maleate sustained release preparation prepared through wet granulation is slightly influenced by the creeping speed of a gastrointestinal tract and the like, the sustained release preparation is slowly released, the relatively steady blood concentration can be maintained, and the sustained release preparation has the advantages that the toxic and side effects are small, the taking is convenient, the bioavailability is improved, and the like. The sustained release preparation is used for preventing and / or treating Alzheimer disease. The preparation method is simple and stable in process and easy for batch production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to 2-(4-methylthiazol-5-yl)ethyl nitrate hydrochloride or 2-(4-methylthiazol-5-yl)ethyl nitrate maleic acid Salt sustained-release preparation and preparation method thereof. Background technique [0002] Known compound 2-(4-methylthiazol-5-yl)ethyl nitrate: [0003] [0004] Interacts with amino acid neurotransmitter receptors such as NMDA receptors and gamma-aminobutyric acid type A (GABAA) receptors. The compound is also known to stimulate soluble uridylyl cyclase (GCase) in the brain. Therefore, this compound is suitable for neuroprotection and cognitive enhancement. This compound is also known to stimulate the brain's cognition of soluble urine strength. See, eg, US Patent No. 6,310,052. It has been found that a new solid form of 2-(4-methylthiazol-5-yl)ethyl nitrate can be prepared as the maleate salt. See Chinese Patent No. 201180041035.4. The patent descr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K47/38A61K47/14A61K31/426A61P25/28
CPCA61K9/2013A61K9/2054A61K31/426A61P25/28
Inventor 王晓良高钟镐黄伟王琰黄海洪彭英辛欣郭芳冯茹
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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