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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 a long treatment course for cardiovascular and cerebrovascular diseases, increase the pain of patients, there is no public report on oral preparations of puerarin, etc., and achieves improved oral bioavailability and increased permeability. Sexual and qualitatively stable effects

Inactive Publication Date: 2003-02-05
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

[0024] Embodiment 1: puerarin granules

[0025] Put puerarin and soybean lecithin in a ratio of 2:1 by weight, and dissolve them in 10 times acetone under the condition of reflux and stirring at 50°C. After reacting for 120 minutes, evaporate the solvent to dryness, and dry in vacuum at 50°C for 10 hours to obtain the puerarin-phospholipid complex. Grind through a 120-mesh sieve; mix 150g of puerarin-phospholipid complex with 600g of micropowdered silica gel, 1500g of lactose, and 600g of starch, and then mix 1,000g of 50% ethanol and 180g of polysorbate 80 (molecular weight: 1309.7) and add to the mixture , mix evenly, then use 200g of 70% syrup to make the soft material of binder system, pass through 20 mesh sieves to make granules, dry at 55°C for 6 hours, cross 20 mesh sieves for granulation, and measure the content of puerarin in the granules by HPLC. Add 3 g of talcum powder, pack and seal 0.1 g of puerarin per bag to obtain puerarin granules.

Embodiment 2

[0026] Embodiment 2: puerarin granules

[0027] 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

[0028] Embodiment 3: puerarin granules

[0029] 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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Abstract

The present invention uses puerarin as main medicine, phospholipid as absorption-promoting agent, polysorbate 80 as solubilization agent, and the weight ratio of puerarin and phospholipid is 1-20:1-4, and the weight ratio of puerarin and polysorbate 80 is 1-20:1-15, and adopts a certain preparation method to obtain the invented puerarin oral preparation which can be made into granules, tablet, capsule and soft capsule, etc. Said invention also provides its preparation method, including preparation of puerarin and phospholipid composite and its preparation. Said invention preparation is stable in quality, has no toxicity and irritation to body, and its biological utilization rate can be obviously raised.

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 Applications(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
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