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2-(alpha-hydroxypentyl) benzoate dispersible tablet and preparation method thereof

A technology of benzoate and hydroxypentyl group, applied in the field of medicine, can solve the problems of affecting the therapeutic effect of drugs, increase toxic and side effects, deficiency, etc., and achieve the effects of quick action, improved solubility and dissolution rate, and improved stability.

Inactive Publication Date: 2015-04-15
YUNNAN HAOPY PHARM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the process of preparing 2-(α-hydroxypentyl)benzoate preparations, it may cause the transformation of 2-(α-hydroxypentyl)benzoate, which will affect the therapeutic effect of the drug and even increase the toxic and side effects
At present, some conventional tablets and capsules of 2-(α-hydroxypentyl)benzoate have appeared on the market, but they are far from meeting the actual needs of the market, especially in the urgent need to exert drug effects and improve bioavailability very lacking

Method used

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  • 2-(alpha-hydroxypentyl) benzoate dispersible tablet and preparation method thereof
  • 2-(alpha-hydroxypentyl) benzoate dispersible tablet and preparation method thereof
  • 2-(alpha-hydroxypentyl) benzoate dispersible tablet and preparation method thereof

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preparation example Construction

[0026] The preparation method of the 2-(α-hydroxypentyl) benzoate dispersible tablet of the present invention requires the control of relative humidity ≤40% and temperature ≤30°C in the preparation environment, which specifically includes the following steps:

[0027] method one:

[0028] A. Granulation: Weigh 2-(α-hydroxypentyl) benzoate, stabilizer and auxiliary materials according to the formula ratio, mix them in a multi-dimensional mixer for 20-40 minutes, pass through a 100-mesh vibrating sieve, and enter the wet process In the granulator, add 2-(α-hydroxypentyl) benzoate, stabilizer and wetting agent with a weight ratio of 2~4:1 to the total weight of auxiliary materials under stirring, and continue to stir for 20~40min to make soft material , Pass through 18 mesh sieve, make wet granules, enter fluidized bed and dry at 60~70℃ for 30~50min, use 20 mesh sieving machine to sizing, add 2-(α-hydroxypentyl)benzene in mixer 0.5-10% of the total weight of the formate, stabilizer a...

Embodiment 1

[0049] 1. Prescription: 1000 tablets

[0050] Potassium 2-(α-hydroxypentyl) benzoate (PHPB) raw material: 100g

[0051] MCC, CMS-Na, PPVP, dextrin: 50g each

[0052] Disodium hydrogen phosphate-sodium hydroxide: 1g

[0053] 95% edible ethanol: 100ml

[0054] Magnesium stearate: 5g

[0055] 2. Preparation process:

[0056] (1) Environmental requirements: relative humidity ≤40%, temperature ≤30℃

[0057] (2) Weigh out 2-(α-hydroxypentyl) benzoate, MCC, CMS-Na, PPVP, dextrin, and sodium hydroxide.

[0058] (3) Put the above materials in a V-type mixer and mix them for 30 minutes, then pass through a 100-mesh shaking sieve for use.

[0059] (4) The above-mentioned materials that have passed through the vibrating sieve are fed into the warm granulator by vacuum, and 95% edible ethanol is added under stirring, and the stirring is continued for 30 minutes to make soft materials, pass through 18 mesh sieve, and make wet granules The granules enter the fluidized bed, the drying temperature of the fl...

Embodiment 2

[0062] 1. Prescription:

[0063] Potassium 2-(α-hydroxypentyl) benzoate (PHPB) raw material: 100g

[0064] MCC, CMS-Na, PPVP, dextrin: 50g each

[0065] Sodium hydroxide: 1g

[0066] A small amount of silica gel: 5g

[0067] 2. Preparation process:

[0068] (1) Environmental requirements: relative humidity ≤40%, temperature ≤30℃

[0069] (2) Weigh the prescription amount of 2-(α-hydroxypentyl) benzoate, MCC, CMS-Na, PPVP, dextrin, sodium hydroxide, and a small amount of silica gel.

[0070] (3) Put the above materials in a V-type mixer for 30 minutes, mix them evenly, and pass through a 120-mesh vibrating screen for later use.

[0071] (4) It is obtained by pressing with a tablet press.

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Abstract

The invention discloses a 2-(alpha-hydroxypentyl) benzoate dispersible tablet and preparation method thereof. The 2-(alpha-hydroxypentyl) benzoate dispersible tablet comprises 20-80wt% of 2-(alpha-hydroxypentyl) benzoate, 0.5-20% of a stabilizer and 20-80% of an auxiliary material. In the preparation method, requirements on a preparation environment are as follows: the relative humidity is lower than or equal to 40%, and the temperature is lower than or equal to 30 DEG C; the preparation method comprises the steps of granulating and tabletting or directly tabletting. The 2-(alpha-hydroxypentyl) benzoate dispersible tablet can make up defects of the existing 2-(alpha-hydroxypentyl) benzoate preparation, improves the solubility and the dissolution rate of a drug and is quick-acting and high in bioavailability; more importantly, after adoption of the dispersible tablet preparation, the defect that the 2-(alpha-hydroxypentyl) benzoate is prone to change in the preparation process is overcome, the drug quality is ensured and the stability is improved.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a 2-(α-hydroxypentyl) benzoate dispersible tablet and a preparation method thereof. Background technique [0002] 2-(α-hydroxypentyl) benzoate, chemical name: racemic 2-(α-hydroxypentyl) benzoate, is a neuroprotective agent for acute ischemic cerebrovascular disease, its main mechanism is : Expand cerebral blood vessels, increase cerebral blood flow, inhibit platelet aggregation and thrombosis, protect mitochondrial function and resist neuronal apoptosis caused by various factors. [0003] Looking at the domestic and foreign research on new drugs for the treatment of ischemic cerebrovascular disease, despite long-term efforts to explore, the results are not significant. There are few drugs used to treat ischemic cerebrovascular disease, especially those with definite curative effect and low side effects. Most patients do not receive effective treatment. Therefore, there i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/192A61P25/00A61P9/08A61P7/02A61P9/10
Inventor 李彪王涌杨云
Owner YUNNAN HAOPY PHARM LTD