Racemic 2-(alpha-hydroxyl amyl) benzoate tablets and preparation method thereof

A technology of benzoate tablet and hydroxypentyl group, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of easy degradation and poor stability.

Active Publication Date: 2013-06-05
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) Amyl) benzoate tablet and preparation method thereof

Method used

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  • Racemic 2-(alpha-hydroxyl amyl) benzoate tablets and preparation method thereof
  • Racemic 2-(alpha-hydroxyl amyl) benzoate tablets and preparation method thereof
  • Racemic 2-(alpha-hydroxyl amyl) benzoate tablets and preparation method thereof

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Comparison scheme
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 the tablet with a common tablet press or a high-speed tablet press 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 water content below 1%), and granulate; mix the obtained granules with magnesium stearate; use a common tablet press or a high-speed tablet press, A tablet with a hardness of 3-8 kg is obtained; the coating material is dissolved in water or ethanol, and the obtained tablet is coated to obtain a racemic 2-(alpha-hydroxypentyl)potassium benzoate tablet.

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, and 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 racemic 2-(α-hydroxypentyl) benzoate tablet and a preparation method thereof. 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 th...

Claims

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Application Information

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