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A method for reducing the astringent taste of traditional Chinese medicine oral preparations containing polyphenols

A technology for oral preparations and traditional Chinese medicines, which is applied in the field of polyphenols taste-masking preparations, can solve the problems that plague the research, preparation and production practice of traditional Chinese medicine oral preparations, changes in absorption routes and bioavailability, and the masking effect of astringency is not obvious. Application prospects, beneficial to large-scale production, and the effect of ensuring the stability of ingredients

Active Publication Date: 2021-06-25
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Patent CN 101573046 A uses encapsulation materials to coat polyphenols, and adopts cyclodextrin inclusion and other process methods in the prior art, which will significantly reduce the release and onset of drugs in the oral cavity. On the one hand, it is not conducive to the oral cavity. The treatment of diseases; on the other hand, it will cause major changes in the absorption route and bioavailability of the main components
[0006] However, simply increasing the dosage of sweeteners, in addition to increasing part of the taste interference effect, has no obvious astringent masking effect, and will reduce the drug loading and increase the dosage.
[0007] In summary, the astringent taste problem has long plagued the research, preparation and production practice of oral preparations of traditional Chinese medicines, and has become a bottleneck problem restricting the development of astringent Chinese medicines.

Method used

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  • A method for reducing the astringent taste of traditional Chinese medicine oral preparations containing polyphenols
  • A method for reducing the astringent taste of traditional Chinese medicine oral preparations containing polyphenols
  • A method for reducing the astringent taste of traditional Chinese medicine oral preparations containing polyphenols

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: pH adjustment improves the astringency of Sanguotang buccal tablets

[0044] 1. Preparation of Sanguo Decoction Extract

[0045]Weigh 2 parts of myrobalan, 1 part of myrobalan, and 1 part of emblica, add 10 times the amount of water, and extract twice at 100 ° C, each time for 1 hour. The extracts are combined and concentrated until the relative density is between 1.20 and 1.30 to obtain the three fruit soup extract.

[0046] 2. Preparation of the taste-masking extract of Sanguo Decoction

[0047] Using 0.5g / mL Na 2 CO 3 aqueous solution, adjust the pH of the extract to 2.5, 3.5, 4.5, 5.5 and 6.5, respectively, and prepare the taste-masking extract of Sanguo Decoction. Then add starch, dextrin, and sucrose to make soft materials, granulate with a 16-mesh sieve, and add magnesium stearate in an equal amount; dissolve menthol into peppermint oil, spray evenly into the above-mentioned granules, mix well, press into tablets, and sterilize , packaged, inspect...

Embodiment 2

[0072] Example 2 pH adjustment and removal of citric acid improve the astringency of Sanguotang buccal tablets

[0073] Based on the influence of pH on astringent taste, it is speculated that citric acid may affect the astringent taste perception of Sanguotang buccal tablets. Therefore, compared with the original prescription (pH3.5, prescription 1, the pH here is the pH of the original extract), the original prescription removes citric acid (pH3.5, prescription 2), and the original prescription increases the pH (pH4.5, prescription 3 ).

[0074] Taste evaluation was carried out by VAS volunteer scoring method. Each of 12 volunteers was given 1 piece of taste-masked buccal tablet and original buccal tablet, put it in the mouth for 2 minutes, spit it out, rinsed the mouth, and scored according to the expression of the volunteers against the VAS table. See Table 1 and Figure 6 .

[0075] Table 1 Comparison of the prescriptions of three kinds of Sanguotang buccal tablets

...

Embodiment 3

[0081] Embodiment 3: pH adjustment improves the astringent taste of Sanle pulp

[0082] Get Sanle pulp oral liquid stock solution (medicine liquid for preparing oral liquid), adopt 0.5g / mL Na 2 CO 3 The aqueous solution adjusts the pH of the extract to 5 to obtain the concentrated juice of the three-leaf pulp with masking taste. Take the same amount of Sanle pulp oral liquid stock solution and taste-masked Sanle pulp concentrated juice, add the same amount of L-arginine, L-aspartic acid, honey and other auxiliary materials, mix, sterilize, pack, and inspect Stored in, acquired, the preparation specification is 15mL / bottle, and the taste-masked Sanle Porridge Oral Liquid and the original San Le Porridge Oral Liquid are obtained.

[0083] 12 volunteers were given 10mL of taste-masked Sanlejiang Oral Liquid and the original Sanlejiang Oral Liquid, put it in the mouth for 30 seconds, spit it out, and rinsed the mouth. The results showed that the astringent taste of Sanlejiang Or...

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Abstract

The invention discloses a method for reducing the astringency of polyphenol-containing traditional Chinese medicine oral preparations, which belongs to the field of traditional Chinese medicine pharmacy. The invention provides a method for reducing the astringency of polyphenol-containing traditional Chinese medicine. and adjust the pH to 4-4.5 to obtain a traditional Chinese medicine extract with reduced astringency. The present invention also provides a traditional Chinese medicine oral preparation containing polyphenols with reduced astringency, which is prepared by the following method: take the traditional Chinese medicine extract with reduced astringency prepared by the aforementioned method, and add pharmaceutically acceptable Oral formulations are prepared with accepted excipients. The method of the present invention adjusts the pH of the extract of the pharmaceutical composition containing polyphenols to 4-4.5, while ensuring the stability of the components, unexpectedly greatly reduces the original astringent taste of the medicine, and improves the patient's ability to take medicine. It has good compliance, avoids the addition of a large amount of flavoring agents, reduces the dosage of sweeteners in the prescription, and reduces the production cost; the taste masking effect is obvious, and the dosage of the patients is not increased, which is simple and practical.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a method for reducing the astringency of polyphenol-containing traditional Chinese medicine oral preparations, in particular to a polyphenol taste-masking preparation. Background technique [0002] Astringency is due to the wrinkled, constricted sensation of epithelial cells exposed to polyphenol solutions. This is a complex set of sensations involving dryness, roughness of the oral surfaces, and sensations of tightening, dragging, or wrinkling of the oral mucosa and muscles. Strictly speaking, astringency is a feeling or touch, not taste, and is not produced by acting on the taste buds on the tongue, but is mistaken for taste because it is produced in the mouth. [0003] As one of the true tastes of traditional Chinese medicine, astringency has certain universality in Chinese medicinal materials and Chinese patent medicines. Drugs rich in polyphenols will pro...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/02A61K36/47A61K36/82
CPCA61K9/0053A61K36/185A61K36/47A61K36/82A61K47/02A61K2300/00
Inventor 张定堃林俊芝韩雪韩丽杨明段渠
Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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