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Sustained release preparation used for treating alzheimer's disease, and preparation method thereof

A technology of sustained-release preparations and sustained-release materials, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pill delivery, etc. smooth and complete effect

Inactive Publication Date: 2016-11-30
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to this patent prescription, the two sustained-release preparations were prepared, and the release was measured according to the first method (basket method) in the 2010 edition of Chinese Pharmacopoeia Appendix X C "Dissolution Determination". The results showed that the two sustained-release preparations in vitro The cumulative release percentages are all lower than 90%, which does not meet the requirement of "in vitro cumulative release percentages reaching over 90%" in Appendix XIX D of the 2010 Chinese Pharmacopoeia "Guiding Principles for Sustained Release, Controlled Release, and Delayed Release Preparations". For specific data, see the instructions attached Figure 7

Method used

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  • Sustained release preparation used for treating alzheimer's disease, and preparation method thereof
  • Sustained release preparation used for treating alzheimer's disease, and preparation method thereof
  • Sustained release preparation used for treating alzheimer's disease, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: The formulation of the sustained-release formulation of 2-(4-methylthiazol-5-yl)ethyl nitrate hydrochloride is as follows:

[0026]

[0027] Taking the preparation of 10,000 2-(4-methylthiazol-5-yl)ethyl nitrate hydrochloride sustained-release preparations as an example, all the excipients were crushed separately and passed through a 100-mesh nylon sieve. Take the main medicine and grind to powder. According to the prescription composition in Example 1, 441.0g of 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride, 450.0g of hydroxypropyl methylcellulose K100M, 417.0 lactose, 139.5g micro Crystal cellulose PH101, mix well, make soft material with 4% povidone ethanol solution, granulate with 20-mesh sieve, dry at 50°C, granulate with 18-mesh sieve, add 7.5g magnesium stearate and 45.0g dioxide Silicon, mix well, press with φ7 punch. The 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride sustained-release preparation is obtained. The release rate was determi...

Embodiment 2

[0028] Example 2: The formulation of the sustained-release formulation of 2-(4-methylthiazol-5-yl)ethyl nitrate hydrochloride is as follows:

[0029]

[0030] Taking the preparation of 10,000 2-(4-methylthiazol-5-yl)ethyl nitrate hydrochloride sustained-release preparations as an example, all the excipients were crushed separately and passed through a 100-mesh nylon sieve. Take the main medicine and grind to powder. According to the prescription composition in Example 2, 441.0g of 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride, 300.0g of hydroxypropyl methylcellulose K100M, 529.5g of lactose, and 177.0g were respectively weighed out. Microcrystalline cellulose PH101, mix well, make soft material with 4% povidone ethanol solution, granulate with 20 mesh sieve, dry at 50°C, granulate with 18 mesh sieve, add 7.5g magnesium stearate and 45.0g sodium bicarbonate Silicon oxide, mix well, press with φ7 punch. The 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride sustained-rel...

Embodiment 3

[0031] Example 3: The formulation of the sustained-release formulation of 2-(4-methylthiazol-5-yl)ethyl nitrate hydrochloride is as follows:

[0032]

[0033]

[0034] Taking the preparation of 10,000 2-(4-methylthiazol-5-yl)ethyl nitrate hydrochloride sustained-release preparations as an example, all the excipients were crushed separately and passed through a 100-mesh nylon sieve. Take the main medicine and grind to powder. According to the prescription composition in Example 3, 441.0g of 2-(4-methylthiazol-5-yl)ethyl nitrate hydrochloride, 150.0g of hydroxypropyl methylcellulose K100M, 642.0g of lactose, and 214.5g were respectively weighed out. Microcrystalline cellulose PH101, mix well, make soft material with 4% povidone ethanol solution, granulate with 20 mesh sieve, dry at 50°C, granulate with 18 mesh sieve, add 7.5g magnesium stearate and 45.0g sodium bicarbonate Silicon oxide, mix well, press with φ7 punch. The 2-(4-methylthiazol-5-yl) ethyl nitrate hydrochloride susta...

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PUM

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Abstract

The invention relates to a sustained release preparation, and a preparation method thereof. The sustained release preparation contains 0.1 to 0.5% of nitric acid-2-(4-methylthiazole-5-yl) ethyl ester hydrochloride or nitric acid-2-(4-methylthiazole-5-yl) ethyl ester maleate as the main drug; and a main sustained-release material is prepared from hydroxypropyl methyl cellulose, a filling agent, a lubricating agent, and a binding agent or a wetting agent. The nitric acid-2-(4-methylthiazole-5-yl) ethyl ester hydrochloride or nitric acid-2-(4-methylthiazole-5-yl) ethyl ester maleate sustained release preparation is prepared via wet granulation; influences of gastrointestinal peristalsis speed on the release behavior of the sustained release preparation are few; sustained release is realized; relatively stable blood concentration can be maintained; action time is relatively long; less toxic and side effect is caused; and the sustained release preparation is convenient to use. The sustained release preparation is used for preventing and / or treating alzheimer's disease.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates 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] With such as NMDA receptor and gamma-aminobutyric acid type A (GABA A ) Receptors and other amino acid neurotransmitters interact with receptors. The compound is also known to stimulate soluble uridine acyl cyclase (GCase) in the brain. Therefore, this compound is suitable for neuroprotection and realization of cognitive enhancement. See, for example, U.S. Patent No. 6,310,052. It has been found that the new solid form of 2-(4-methylthiazol-5-yl)ethyl nitrate can be prepared as the maleate salt form. See Chinese Patent No. 201180041035.4. The patent describes two formulations of sustained-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/426A61K47/38A61P25/28
CPCA61K31/426A61K9/2054
Inventor 高钟镐黄伟王晓良王琰黄海洪彭英陈丽青
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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