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2-(alpha-hydroxy pentyl) benzoate controlled-release tablet and preparation method thereof

A benzoate and hydroxypentyl technology, which is applied in the field of 2-(α-hydroxypentyl)benzoate controlled-release tablets and their preparation, can solve the problems of inability to exert long-term effects and short half-life, and achieve shortening Medication cycle, maintenance of blood drug concentration, and effect of increasing compliance

Inactive Publication Date: 2014-08-20
YUNNAN HAOPY PHARM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it highlights the short half-life of PHPB, the fast metabolism in animals, and the quick-acting advantages of being easy to act quickly, it cannot give full play to its long-acting advantages

Method used

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  • 2-(alpha-hydroxy pentyl) benzoate controlled-release tablet and preparation method thereof
  • 2-(alpha-hydroxy pentyl) benzoate controlled-release tablet and preparation method thereof
  • 2-(alpha-hydroxy pentyl) benzoate controlled-release tablet and preparation method thereof

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preparation example Construction

[0021] Described preparation method specifically comprises:

[0022] a. Pass 2-(α-hydroxypentyl) benzoate, slow and controlled release framework materials and auxiliary materials through 80-mesh sieve respectively, and then mix in a mixer for at least 30 minutes to achieve uniformity;

[0023] b. The stabilizer and auxiliary materials are also passed through a 80-mesh sieve, and then dissolved with a wetting agent and mixed evenly;

[0024] c. Send the mixed solid material to the wet granulator with a vacuum feeder, then add the prepared wetting agent to the wet granulator through the compressed air through the pressure tank, and mix in the wet granulator At least 15 minutes, pass through a 12-18 mesh sieve through a granulator to make granules. The granules enter the fluidized drying bed for 40 minutes by gravity or vacuum, and the drying temperature is controlled below 65 ° C. The dried granules pass through the lifting transfer machine Enter the granulator, the granulated ...

Embodiment 1

[0043] prescription:

[0044] Potassium Hydroxypentyl Benzoate (PHPB) raw material: 100mg

[0045] Disodium hydrogen phosphate-sodium hydroxide: 10mg

[0046] HPMC: 10mg

[0047] Hydroxypropyl Cellulose - Hydroxypropyl Methyl Cellulose Phthalate: 100mg

[0048] Magnesium stearate: 5mg

[0049] Purified water 1-2ml, ethanol 3-5ml

[0050] Coating material: cellulose acetate 1-2mg

[0051] 1. Pass potassium hydroxypentyl benzoate (PHPB), hydroxypropyl cellulose-hydroxypropyl methyl cellulose phthalate through an 80-mesh sieve and add to a three-dimensional mixer to mix for 30±10 minutes.

[0052] 2. Pass disodium hydrogen phosphate-sodium hydroxide and HPMC through 80-mesh sieve respectively, dissolve in ethanol and set aside.

[0053] 3. Mix the two ethanol solutions in 2 for later use.

[0054] 4. Put the material formed in 1 into a wet granulator, then add the wetting agent in 3 and mix for at least 15 minutes to make a soft material.

[0055] 5. Make the soft material ...

Embodiment 2

[0061] Potassium hydroxypentylbenzoate (PHPB) raw material: 100mg

[0062] Disodium hydrogen phosphate-sodium hydroxide: 10mg

[0063] Microcrystalline Cellulose: 15mg

[0064] CMC: 80mg

[0065] Magnesium stearate: 5mg

[0066] Purified water 1-2ml, ethanol 3-5ml

[0067] Coating material: acrylic resin IV No. 1-2mg

[0068] 1. Pass potassium hydroxypentyl benzoate (PHPB), CMC, and microcrystalline cellulose through an 80-mesh sieve first, then add to a three-dimensional mixer and mix for 30±10 minutes.

[0069] 2. Pass disodium hydrogen phosphate-sodium hydroxide through an 80-mesh sieve and dissolve it in ethanol for later use.

[0070] 3. Reserve the ethanol solution in 2.

[0071] 4. Put the material formed in 1 into a wet granulator, then add the wetting agent in 3 and mix for at least 15 minutes to make a soft material.

[0072] 5. Make the soft material into wet granules through the granulator.

[0073] 6. Dry the wet granules; the drying temperature is 45-70°C...

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Abstract

The present invention discloses a 2-(alpha-hydroxy pentyl) benzoate controlled-release tablet and a preparation method thereof. The controlled-release tablet comprises a tablet core and a coating film wrapping the tablet core. The tablet core is characterized by containing an effective amount of 2-(alpha-hydroxy pentyl) benzoate, a stabilizer and 0.1-10% of a controlled-release skeleton material, and the tablet core coats with an enteric film coating. The preparation method of the invention is as below: evenly mixing 2-(alpha-hydroxy pentyl) benzoate, the stabilizer, the controlled-release skeleton material and auxiliary materials, wherein the stabilizer and auxiliary materials are respectively mixed with a wetting agent, then mixed together and added into a well mixed material to prepare a soft material; granulating, drying and adding the rest of the auxiliary materials; and tabletting and coating the tablet core with the film coating. The invention employs specific technological process to release the drug at a constant speed in the body, reaches the effects of sustained, long-term and low-toxicity blood concentration, shortens medication cycle, increases patient compliance, and brings convenience to the patients.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a 2-(α-hydroxypentyl) benzoate controlled-release tablet and a preparation method thereof. Background technique [0002] Taking a comprehensive view of the research on new drugs for the treatment of ischemic cerebrovascular disease at home and abroad, despite long-term efforts to explore, the results are not significant. There are very few drugs for the treatment of ischemic cerebrovascular disease, especially those with definite curative effect and little side effects. Most patients cannot receive effective treatment. Therefore, clinically, there is a great demand for the research and development of new drugs against cerebral ischemic injury. In recent years, scholars from various countries have conducted in-depth discussions on the pathophysiology of ischemic brain injury, and have gradually shifted from seeking drugs with a single target to finding new drugs tha...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/192A61P9/10
Inventor 李彪王涌杨云
Owner YUNNAN HAOPY PHARM LTD
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