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Preparation method of racemic 2-(α-hydroxypentyl) benzoate tablets

A technology of benzoate tablets and hydroxypentyl, which is applied in the field of preparation of racemic 2-benzoate tablets, and can solve problems such as poor stability and easy degradation

Active Publication Date: 2016-03-09
山西首智生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention provides a racemic 2-(α-hydroxypentyl) benzoate in order to solve the problem that the active ingredient racemic 2-(α-hydroxypentyl)benzoate is prone to degradation and poor stability in the preparation process of conventional tablets, and provides a racemic 2-(α-hydroxypentyl) The preparation method of pentyl) benzoate sheet

Method used

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  • Preparation method of racemic 2-(α-hydroxypentyl) benzoate tablets
  • Preparation method of racemic 2-(α-hydroxypentyl) benzoate tablets
  • Preparation method of racemic 2-(α-hydroxypentyl) benzoate tablets

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Effect test

Embodiment 1

[0034] Prescription composition (1000 tablets)

[0035] Core weight

[0036] Potassium 2-(α-hydroxypentyl)benzoate 100g

[0037] Preparation method: control the water content of the main ingredient below 1%, and directly compress it with a common tablet machine or a high-speed tablet machine to obtain a tablet with a hardness of 3-8 kg; dissolve the coating material in water or ethanol, and give The obtained tablets are coated to obtain racemic 2-(α-hydroxypentyl)potassium benzoate tablets.

Embodiment 2

[0039] Prescription composition (1000 tablets)

[0040]

[0041] Preparation method: use disodium hydrogen phosphate-sodium hydroxide to adjust the pH value to 12.0 as a solvent, prepare 6% HPMC aqueous solution, and prepare 6% HPMC aqueous solution and ethanol at a ratio of 1:1 to obtain 3% HPMC Add the main ingredient to obtain the soft material, granulate, dry (control the moisture content below 1%), and granulate; the obtained granules are mixed with magnesium stearate; with an ordinary tablet press or a high-speed tablet press, Obtain a tablet with a hardness of 3-g kg; dissolve the coating material in water or ethanol, and coat the obtained tablet to obtain racemic 2-(α-hydroxypentyl)potassium benzoate tablets.

Embodiment 3

[0043] Prescription composition (1000 tablets)

[0044]

[0045]Preparation method: dissolve the main ingredient in water, adjust the pH value to 12.0, add medicinal starch, stir with HPMC, obtain solid powder by spray drying, freeze drying or rotary evaporation, and control the moisture content below 1%; directly Compress tablets with a common tablet press or a high-speed tablet press to obtain a tablet with a hardness of 3 to 8 kg; dissolve the coating material in water or ethanol, and coat the obtained tablet to obtain racemic 2-(α- Hydroxypentyl) Potassium Benzoate Tablets.

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Abstract

The invention relates to a racemic 2-(alpha-hydroxyl amyl) benzoate tablets and a preparation method thereof, aiming at solving the problem that an active ingredient, namely racemic 2-(alpha-hydroxyl amyl) benzoate is easy to degrade and has low stability in a conventional tablet preparation technology. According to the preparation method of the racemic 2-(alpha-hydroxyl amyl) benzoate tablets, crude drug powder is directly tabletted or an alkalization treatment process is adopted in a preparation technology, so that the stability of the main drug of the racemic 2-(alpha-hydroxyl amyl) benzoate tablets is obviously improved; and the preparation method is suitable for preparation of the tablets.

Description

technical field [0001] The invention relates to a preparation method of racemic 2-(alpha-hydroxypentyl)benzoate tablets. Background technique [0002] Racemic 2-(α-hydroxypentyl)benzoate is the drug precursor of racemic butylphthalide, which can be rapidly converted into racemic butylphthalide in the body to exert its drug effect. After intragastric administration of racemic 2-(α-hydroxypentyl)benzoate to rats or Beagle dogs, it can be rapidly converted into racemic butylphthalide in the body, and the drug of racemic butylphthalide in plasma- The area under the time curve is increased by 40% (rats) and 100% (Beagle dogs) compared with the plasma drug-time area under the curve of the direct oral administration of equimolar concentration of racemic butylphthalide. Pharmacodynamic studies have shown that racemic 2-(α-hydroxypentyl)benzoate has similar or stronger biological effects to racemic butylphthalide. [0003] As early as in the patent CN01109795.7 applied by the Insti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/36A61K9/32A61K31/235A61K31/24A61K31/5375A61K47/38A61K47/36A61K47/34A61K47/32
CPCA61K9/2009A61K9/2054A61K9/2059A61K9/28A61K31/192
Inventor 刘宇航韩亚雄高哲伟
Owner 山西首智生物科技有限公司
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