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Puerarin oral preparation and its preparation method

An oral preparation, puerarin technology, applied in the field of medicine, can solve the problems of increasing patient suffering, long treatment period for cardiovascular and cerebrovascular diseases, and no public reports of puerarin oral preparations, etc., to increase permeability and oral bioavailability Improve and increase the effect of water solubility and dispersibility

Inactive Publication Date: 2005-06-15
山东淄博新达制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the long course of treatment for cardiovascular and cerebrovascular diseases, administration in the form of injections brings more inconvenience to patients and increases the suffering of patients to a certain extent.
There is no public report of puerarin oral preparations

Method used

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  • Puerarin oral preparation and its preparation method
  • Puerarin oral preparation and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: puerarin granules

[0026] Dissolve puerarin and soybean lecithin in a ratio of 2:1 by weight in 10 times acetone under reflux and stirring at 50°C, react for 120 minutes, evaporate the solvent to dryness, and dry in vacuum at 50°C for 10 hours to obtain the puerarin-phospholipid complex , ground through a 120 mesh sieve; get 150g puerarin phospholipid complex and mix with 600g micropowder silica gel, 1500g lactose, 600g starch, get 50% ethanol 1000g and 180g polysorbate 80 (molecular weight is 1309.7) and mix and add the above mixture Middle, mix well, then use 200g of 70% syrup as binder to make soft material, pass through 20-mesh sieve to make granules, dry at 55°C for 6 hours, pass through 20-mesh sieve for granulation, and measure the content of puerarin in the granules by HPLC , add talcum powder 3g, pack and seal puerarin granule containing 0.1g puerarin per bag.

Embodiment 2

[0027] Embodiment 2: puerarin granules

[0028] Put puerarin and soybean lecithin in a ratio of 1:1 by weight, and dissolve them in 10 times absolute ethanol under reflux and stirring at 50°C. After reacting for 60 minutes, evaporate the ethanol to dryness, and vacuum-dry at 50°C for 10 hours to obtain puerarin phospholipids. The compound was ground through a 120-mesh sieve; 200g of the puerarin phospholipid compound was mixed with 400g of micropowdered silica gel, 1800g of lactose, and 800g of starch, and 300g of 50% ethanol and 150g of polysorbate 80 were taken and added to the mixture after mixing. Mix evenly, then use 300g of 70% syrup as a binder to make soft materials, pass through a 20-mesh sieve to make granules, dry at 55°C for 6 hours, pass through a 20-mesh sieve for granulation, and measure the content of puerarin in the granules by HPLC. Talcum powder 4g, pack and seal puerarin granules by containing 0.1g puerarin in every bag.

Embodiment 3

[0029] Embodiment 3: puerarin granules

[0030] Put puerarin and soybean lecithin in a ratio of 1:2 by weight, and dissolve them in 20 times absolute ethanol under the condition of reflux and stirring at 50°C. After reacting for 60 minutes, evaporate the ethanol to dryness, and vacuum-dry at 50°C for 10 hours to obtain the puerarin-phospholipid compound Grind and pass through a 120-mesh sieve; take 300g of puerarin phospholipid complex, mix with 500g of micropowder silica gel, 2000g of lactose, and 800g of starch, and then take 800g of 50% ethanol and 250g of polysorbate 80, mix them, and add them to the above mixture. , then use 400g of 70% syrup as a soft material for binder system, pass through a 20-mesh sieve to make granules, dry at 55°C for 6 hours, pass through a 20-mesh sieve for granulation, measure the content of puerarin in the granules by HPLC, add talcum powder 10g, packed and sealed with 0.1g puerarin per bag to obtain puerarin granules.

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PUM

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Abstract

Puerarin oral preparations and a preparation method thereof belong to the technical field of medicines. The puerarin oral preparation of the present invention uses puerarin as the main agent, phospholipids as the absorption-promoting agent, polysorbate 80 as the solubilizer, and the weight ratio of puerarin and phospholipids is (1-20): (1-4), The weight ratio of puerarin and polysorbate 80 is (1-20): (1-15). Puerarin oral preparations include puerarin granules, puerarin tablets, puerarin capsules, and puerarin soft capsules. The preparation method of the puerarin oral preparation comprises the preparation of the puerarin phospholipid complex and the preparation of the preparation. Puerarin is made into a complex with phospholipids first, which can improve the fat solubility of puerarin, and then mixed with polysorbate, can increase the water solubility and dispersion of puerarin, and increase the permeability to the gastrointestinal mucosa, that is, The oral absorption of puerarin can be improved, the obtained preparation has stable properties, is non-toxic and non-irritating to the body, and the oral bioavailability is significantly improved.

Description

(1) Technical field [0001] The invention relates to an oral preparation made by using the traditional Chinese medicine puerarin as an active ingredient and a preparation method thereof, belonging to the technical field of medicine. (2) Background technology [0002] The active ingredients of traditional Chinese medicine puerarin can be used to treat coronary heart disease, angina pectoris and other diseases related to cardiocerebral circulation, as well as retinal artery and vein occlusion, sudden deafness and other diseases. Puerarin is an isoflavone glycoside isolated from the dried root of the leguminous plant Pueraria lobata (Willd.) Ohwi, the chemical name is 4,7-dihydroxy-8-β-D-glucosyl isoflavone In 1993, the Ministry of Health approved puerarin (raw material) and its injection for clinical treatment. As a vasodilator, the drug is used to treat coronary heart disease, angina pectoris and other diseases related to cardio-cerebral circulation disorders, and has achieve...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/7048A61P9/10
Inventor 娄红祥翟光喜孙隆儒
Owner 山东淄博新达制药有限公司