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CN108113962A - A kind of method for reducing the oral preparation of Chinese traditional medicinal astringent taste containing polyphenol - Google Patents

A kind of method for reducing the oral preparation of Chinese traditional medicinal astringent taste containing polyphenol Download PDF

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CN108113962A
CN108113962A CN201810155552.8A CN201810155552A CN108113962A CN 108113962 A CN108113962 A CN 108113962A CN 201810155552 A CN201810155552 A CN 201810155552A CN 108113962 A CN108113962 A CN 108113962A
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extract
astringent taste
aqueous solution
oral
liquid
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CN108113962B (en
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张定堃
林俊芝
韩雪
韩丽
杨明
段渠
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Chengdu University of Traditional Chinese Medicine
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/47Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/82Theaceae (Tea family), e.g. camellia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds

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Abstract

The invention discloses a kind of methods for reducing the oral preparation of Chinese traditional medicinal astringent taste containing polyphenol, belong to field of traditional Chinese medicine pharmacy, the present invention provides a kind of methods for the astringent taste for reducing the Chinese medicine containing polyphenol, take the extract of the Chinese medicine containing polyphenol, pH is adjusted to 4~4.5 to get the Chinese medical extract of astringent taste is reduced.The present invention also provides a kind of oral preparation of Chinese traditional medicinal containing polyphenol for reducing astringent taste, it is prepared by following methods:Taking reduces the Chinese medical extract of astringent taste made from preceding method, along with oral formulations are prepared in pharmaceutically acceptable auxiliary material.The method of the present invention by the pH of the extract of the pharmaceutical composition containing polyphenol by being adjusted to 4~4.5, while ensure that ingredient stability, unexpectedly significantly reduce the original astringent taste of drug, improve the compliance of patient's medication, it avoids and adds in a large amount of corrigents, the dosage of sweetener in prescription is reduced, reduces production cost;Taste masking effect is apparent, does not increase the dosage of patient, simple and practical.

Description

A kind of method for reducing the oral preparation of Chinese traditional medicinal astringent taste containing polyphenol
Technical field
The invention belongs to field of traditional Chinese medicine pharmacy, are related to a kind of method for reducing the oral preparation of Chinese traditional medicinal astringent taste containing polyphenol, More particularly to a kind of Polyphenols taste masking preparation.
Background technology
Astringent taste is since epithelial cell is exposed to corrugation, the sensation shunk caused by polyphenol solution.This is one group complicated Sensation, be related to the drying of oral surfaces, the deflation of coarse and oral mucosa and muscle, towing or corrugated sensation.Strictly Ground says, astringent taste is a kind of sensation or tactile rather than the sense of taste, is generated not by the taste bud acted on tongue, simply by In resulting from oral cavity, and it is mistaken for the sense of taste.
One of the true flavour of astringent taste as Chinese medicine has certain generality in Chinese medicine and Chinese patent drug.Rich in more The drug of aldehydes matter can generate apparent astringent taste during taking, and seriously affect the compliance that patient takes, constrain more The expansion of phenols pharmaceutical market share.Therefore, adverse drug taste is effectively covered, product quality is improved, is subject to medicine further Learn the attention of practitioner.
It is sheltered for astringent taste, mostly using the side such as adsorption clarification, calcium salt or gelatin precipitation, macroreticular resin separation in food industry Formula is separated off part polyphenol.But pharmaceutically, there is polyphenols exact anti-oxidant, antibacterial, anti peroxidation of lipid to damage The effect of wound, antitumor isoreactivity are important material base.It is simple seriously to be damaged using the technology mode of " separation, impurity removal " The performance of drug effect, and in pharmaceutical preparation, belong to the major change on drug substance basis.
101573046 A of patent CN are coated polyphenols using encapsulated material and use in the prior art It is cyclodextrin encapsulated to wait technology modes, and release and action of the drug in oral cavity can be substantially reduced, on the one hand it is unfavorable for mouth disease Treatment;On the other hand the great change of main component absorption features and bioavilability can be caused.
And increase sweetener dosage merely, in addition to increasing part sense of taste disturbing effect, astringent taste masking effect is not obvious, And drugloading rate can be reduced, increase dose.
To sum up, the research preparation and production practices of astringent taste problem long-standing problem oral preparation of Chinese traditional medicinal becomes and restricts in astringent taste The bottleneck problem of medicine development.
The content of the invention
Polyphenol generate astringent taste basic principle be polyphenol phenolic hydroxyl group and mammalian saliva in Pro-rich albumen Generation complexing, generation are precipitated and caused, and essence is exactly the mistake that sialoprotein forms hydrophobic complexes with polyphenol substance Journey.Factors can have an impact the process, cause including individual difference different to the susceptibility of astringent taste;It is polyphenol concentration, more Phenols type;Reaction time, temperature, pH etc..
Chinese medicine polyphenol has common feature in structure, contains substantial amounts of polynary phenolic hydroxyl group;It is carried in the Chinese medicine rich in polyphenol It takes in liquid, medicinal extract, solution often shows acidity, and pH is 2.5-3 or so;In addition preparation often adds the acidic excipients such as citric acid Increase flavor.The present invention controls the application of acidic excipient oral effectively to reduce creatively by adjusting medicinal extract, the pH of solution The astringent taste of preparation.For this purpose, by substantial amounts of experimental study, it has unexpectedly been found that the pH before regulation and control preparations shaping reduces acidic excipient Use, the good oral formulations of astringent taste masking effect can be made.
In order to solve the problems, such as the astringent taste of long-standing problem oral preparation of Chinese traditional medicinal, the present invention provides a kind of reductions to contain polyphenol The method of oral preparation of Chinese traditional medicinal astringent taste.Specially:
The present invention provides a kind of methods for the astringent taste for reducing the Chinese medicine containing polyphenol, take the extraction of the Chinese medicine containing polyphenol PH is adjusted to 4~4.5 to get the Chinese medical extract of astringent taste is reduced by object.
Further, the extract of the Chinese medicine containing polyphenol is tea polyphenol extract object, three fruit soup, three Le are starched, Pu Gong English extract, tranquilization paste, Fructus Hippophae extractum, Shanlu Tea extract for dropping, Fructus chebulae immaturus extract, emblic extract or Nuodikang oral liquid.
Further, the pH is 4.5.
Further, the adjusting pH is to adjust liquid or alkali grain using alkalescence.
Preferably, it is aqueous sodium carbonate, sodium bicarbonate aqueous solution or sodium hydrate aqueous solution that the alkalescence, which adjusts liquid,; And/or the alkali grain is sodium carbonate particle or sodium bicarbonate particle.
It is furthermore preferred that the alkalescence adjusts aqueous sodium carbonate, the bicarbonate of 0.1~1g/mL that liquid is 0.1~1g/mL The sodium hydrate aqueous solution of sodium water solution or 0.1~1g/mL.
Even more preferably, the alkalescence adjusts aqueous sodium carbonate, the bicarbonate of 0.5g/mL that liquid is 0.5g/mL The sodium hydrate aqueous solution of sodium water solution or 0.5g/mL.
The present invention also provides a kind of oral preparation of Chinese traditional medicinal containing polyphenol for reducing astringent taste, it is by following methods system It is standby to obtain:The extract of the Chinese medicine containing polyphenol is taken, pH is adjusted to 4~4.5 to get the Chinese medical extract of astringent taste is reduced, Along with oral formulations are prepared in pharmaceutically acceptable auxiliary material.
Further, the extract of the Chinese medicine containing polyphenol is tea polyphenol extract object, three fruit soup, three Le are starched, Pu Gong English extract, tranquilization paste, Fructus Hippophae extractum, Shanlu Tea extract for dropping, Fructus chebulae immaturus extract, emblic extract or Nuodikang oral liquid.
Further, the pH is 4.5.
Further, the adjusting pH is to adjust liquid or alkali grain using alkalescence.
Preferably, it is aqueous sodium carbonate, sodium bicarbonate aqueous solution or sodium hydrate aqueous solution that the alkalescence, which adjusts liquid,; And/or the alkali grain is sodium carbonate particle or sodium bicarbonate particle.
It is furthermore preferred that the alkalescence adjusts aqueous sodium carbonate, the bicarbonate of 0.1~1g/mL that liquid is 0.1~1g/mL The sodium hydrate aqueous solution of sodium water solution or 0.1~1g/mL.
Even more preferably, the alkalescence adjusts aqueous sodium carbonate, the bicarbonate of 0.5g/mL that liquid is 0.5g/mL The sodium hydrate aqueous solution of sodium water solution or 0.5g/mL.
Further, the oral formulations for granule, lozenge, chewable tablets, lozenge, oral liquid, pill, tablet, powder, Mixture, syrup, electuary, paste or sublimed preparation.
Preferably, the oral formulations are tea polyphenol extract object, three fruit soup lozenges, three Le starch oral liquid, jian Tablets, Pu Public English particle, tranquilization paste, five tastes sea-buckthorn dissipate, double mountain particles, zangqingguo tablets, throat smoothing tablet with emblic or Nuodikang oral liquid.
The present invention provides a kind of method for reducing the oral preparation of Chinese traditional medicinal astringent taste containing polyphenol, by the way that polyphenol will be contained The pH of the extract of pharmaceutical composition is adjusted to 4~4.5, while ensure that ingredient stability, unexpectedly significantly drops The low original astringent taste of drug improves the compliance of patient's medication, avoids and adds in a large amount of corrigents, reduces sweet tea in prescription The dosage of taste agent, reduces production cost;Taste masking effect is apparent, does not increase the dosage of patient, simple and practical.
The technique has a very important significance the production of Chinese medicine preparation, and can be used for preparing a variety of traditional handicrafts can not The peroral dosage form (solution sensory issues) of realization, in particular for some specific crowds (old man that such as children and swallowing have any problem) Special form (such as granule, dispersible tablet preparation), it is easy to operate, it is of low cost, be conducive to mass produce, have good Application prospect, be widely portable to the fields such as food, tea beverage, grape wine, drug.
Obviously, the above according to the present invention according to the ordinary technical knowledge and customary means of this field, is not departing from Under the premise of the above-mentioned basic fundamental thought of the present invention, the modification, replacement or change of other diversified forms can also be made.
The specific embodiment of form by the following examples remakes further specifically the above of the present invention It is bright.But the scope that this should not be interpreted as to the above-mentioned theme of the present invention is only limitted to following example.It is all to be based on the above of the present invention The technology realized all belongs to the scope of the present invention.
Description of the drawings
Fig. 1 is the three fruit soup of taste masking of different pH processing and the fluorescence spectra of former three fruit soup and beta-casein reaction system.
Fig. 2 is the combining information of three fruit soup and beta-casein.
Fig. 3 is finger-print before and after three fruit soup lozenge taste maskings.
Fig. 4 is the principal component analysis result of three fruit soup medicinal extract and screening main component figure under condition of different pH.
Fig. 5 is finger-print before and after three fruit soup buccal tablet taste maskings.
Fig. 6 is the volunteer VAS scoring Contrast on effect of three kinds of prescriptions.
Specific embodiment
The raw material that is used in the specific embodiment of the invention, equipment are known product, are obtained by buying commercial product.
1) material and reagent
Myrobalan (lot number Z00216N01), emblic (lot number Z16116N01), terminaliae billericae,fructus (lot number Z10016N01), are purchased from Sichuan golden mean of the Confucian school pharmaceutcal corporation, Ltd is respectively the drying and ripening of combretaceae plant myrobalan Terminalia chebula Retz Fruit, the dry mature fruit of euphorbia plant emblic Phyllanthus emblica and combretaceae plant adjoin Li Le The dry mature fruit of Terminalia bellirica (Gaertn.) Roxb..
Beta-casein (purity >=98%, Sigma company, lot number SLBN8470V), artificial saliva (the permanent science and technology of Dongguan City letter Co., Ltd, lot number XH-002), three Le slurry anti-fatigue liquid (the magnificent pharmaceutical Co. Ltd in Sichuan, lot number 1403003) is soluble Starch (Xilong Chemical Co., Ltd, lot number 130824), dextrin (Tianjin Heng Xing chemical reagent Manufacturing Co., Ltd, batch Number 20170411), sucrose (Xilong Chemical Co., Ltd, lot number 140301), citric acid (the western limited public affairs of Gansu Province chemical industry share Department, lot number 110720), menthol (Shanghai Yuan Ye bio tech ltd, lot number JM0524RB13), tea polyphenols (Shang Haiyuan Leaf bio tech ltd, lot number Y23D6B8012).
2) key instrument
Cary Eclipse types sepectrophotofluorometer (VARIAN companies of the U.S.), thunder magnetic PHS-3C types pH meter (Shanghai instrument Electric scientific instrument limited company), TURBISCAN LAB analysis of stability analyzer (French Formulation companies), Agilent 1260 high performance liquid chromatographs (Agilent scientific & technical corporation of the U.S.).
Embodiment 1:PH adjusts the improvement to three fruit soup buccal tablet astringent tastes
1st, the preparation of three fruit soup medicinal extract
2 parts of myrobalan, 1 part of terminaliae billericae,fructus, 1 part of emblic are weighed, 10 times of amount water is added in, at 100 DEG C, extracts twice, every time 1h.Extracting solution is merged, is concentrated into relative density between 1.20~1.30, obtains three fruit soup medicinal extract.
2nd, the preparation of three fruit soup taste masking medicinal extract
Utilize the Na of 0.5g/mL2CO3Medicinal extract pH is adjusted respectively to 2.5,3.5,4.5,5.5 and 6.5, distinguished by aqueous solution Prepare three fruit soup taste masking medicinal extract.Then starch, dextrin, sucrose are added in, softwood processed, 16 mesh sieve whole grains, equal increments add in stearic Sour magnesium;Menthol is molten to peppermint oil dementholized, it is uniformly sprayed onto in above-mentioned particle, mixing, tabletting, sterilization, packaging, inspection storage, i.e., , preparation specification is 1g/ pieces.In terms of 1000, wherein containing three fruit soup taste masking medicinal extract 600g, starch 300g, dextrin 100g, sucrose 50g, menthol 10g, peppermint oil dementholized 5mL, magnesium stearate 6g.
3rd, fluorescence spectrometry
1.2mgmL is configured using artificial saliva-1Beta-casein solution and 0.4mgmL-1Three fruit soup solution of taste masking With former three fruit soup solution.
The beta-casein solution of 1mL is added in 10 containers, then be separately added into 0,10,20,40,80,100,200, 400th, the three fruit soup standard solution of 600,1000 μ L, manually saliva be settled to 2mL, mixing is placed in 30 DEG C of water-bath and reacts It is taken out after 30min, in being detected on sepectrophotofluorometer, setting excitation wavelength is 280nm, scans the transmitting light of 287-450nm Spectrum, observes the variation of fluorescence intensity.
(1) three fruit soup and beta-casein temper go out constant
Three fruit soup and beta-casein the temper constant that goes out can be obtained by below equation:
F0/(F0- F)=1/ (fK [Q])+1/f
In formula, F0Mei temper is illustrated respectively in F to go out beta-casein fluorescence intensity of the agent He temper goes out in the presence of agent, [Q] Shi temper goes out agent concentration, and K Shi temper goes out constant, and f is that Ji temper goes out agent fluorescence fraction, with F0/(F0- F) it maps to 1/ [Q], Fig. 1 is obtained, is cut Away from being K with the ratio between slope.
Fig. 1 is the three fruit soup of taste masking of different pH processing and the fluorescence spectra of former three fruit soup and beta-casein reaction system. In Fig. 1, pH2.5 (A), former medicinal extract (B), pH4.5 (C), pH5.5 (D), pH6.5 (E), pH3.5/20 DEG C (F);(a) β-junket egg In vain, (b-j) beta-casein and 0.024,0.048,0.096,0.193,0.242,0.484,0.968,1.453and 2.421mM Three fruit soup reaction systems.
The combining information of (2) three fruit soup and beta-casein
The combining information of three fruit soup and beta-casein can be reflected by Fig. 2 and below equation:
Log[(F0- F)/F]=log Ka+nlog[Q]
In formula, KaIt is binding constants, n is the binding site number of each beta-casein molecule.
At 20 DEG C and 30 DEG C, the K between three fruit soup and beta-caseinaRespectively 3.08 × 104M-1With 10.06 × 104M-1。 With the rise of temperature, KaIncrease, show to have in the form of covalent in cohesive process of the three fruit soup with beta-casein existing for phase Interaction, wherein what is played a major role is with interaction existing for non-ionic form.
Binding constants are the results show that KaValue is affected by pH, is ordered as with reference to power:pH3.5>pH6.5>pH5.5> pH2.5>pH4.5.Wherein, KaBigger, then the combination of polyphenol and beta-casein is bigger in three fruit soup of surface, so as to confirm three fruit soup Astringent taste it is also stronger.Ranking results show that the three fruit soup of pH4.5 and protein binding are most weak, so as to which its astringent taste is minimum.
4th, finger-print Study on Similarity
Chromatographic condition:Agilent1200 high performance liquid chromatographs (band autosampler, vacuum degassing machine, quaternary pump, column Incubator etc.), Welchrom C18Chromatographic column (4.6mm × 250mm, 5 μm), mobile phase are 0.1% phosphoric acid water (A)-methanol (B) (ladder Degree elutes:0-6min, 5%B;6-15min, 5%-7%B;15-20min, 7%-15%B;20-25min, 15%-21%B; 25-31min, 21%-22%B;31-41min, 22%B;41-45min, 22%-32%B;45-60min, 32%-65%B; 60-65min, 65%-5%B), Detection wavelength 270nm, flow velocity 1.0mL/min, 30 DEG C of column temperature, 10 μ L of sample size.
The result is shown in Fig. 3 for the similarity evaluation of finger-print under the conditions of each pH.As seen from the figure, compared with former medicinal extract, pH is adjusted The similarity of medicinal extract changes afterwards, and when pH is 2.5~5.5, for coefficient of similarity more than 0.996, similarity is very high, says Significant change does not occur for the ratio of bright ingredient, ensure that the stability of ingredient;When pH continues rise, coefficient of similarity starts to drop Low, for example, when pH is 6.5, the coefficient of similarity with former medicinal extract is only 0.94, illustrates that apparent change has occurred in the ratio of some ingredients Change, most notably the peak of liquid phase retention time 77min.
5th, HPLC component metabolics profile combination principal component analysis
Using HPLC component metabolic profile combination principal component analysis, the larger substance of research composition transfer.As shown in figure 4, Fig. 4-A illustrate the principal component analysis of three fruit soup medicinal extract under condition of different pH as a result, as seen from the figure, when pH is increased to 6.5, with The distance of former medicinal extract (pH3.5) gradually becomes remote, and whole similitude is prompted to reduce, and when pH is in the range of 2.5~5.5, with original The distance of medicinal extract (pH3.5) is close, illustrates that whole similitude is very high.Partial least squares discriminant analysis (PLS-DA) is carried out to screen Main component (Fig. 4-B), it is exactly the peak of retention time 77min to find main difference ingredient, carries out reference substance and points out, and finding should Ingredient is ellagic acid.
6th, fungistatic effect measures
Three fruit soup taste masking buccal tablets (pH4.5) and former piece are placed in dissolving device, respectively at 0.5,1,1.5,2,2.5, 3min is sampled, spare after crossing 0.22 μm of miillpore filter.
After staphylococcus aureus and Candida albicans culture to a certain concentration, it is applied to respectively on solid medium, The scraps of paper are put in culture medium with tweezers, 5 μ L, tri- fruit decoction of medicinal ingredients liquid is drawn in the scraps of paper, cultivates at a suitable temperature.After a certain period of time, Taking-up sends out measurement antibacterial circle diameter with right-angled intersection, with the presence or absence of inhibition zone and the bacteriostatic activity of size evaluation drug.The result is shown in Fig. 5, the results showed that the bacteriostatic activity no significant difference of three fruit soup before and after taste masking.
7th, astringent taste measures
Everyone 1 taste masking buccal tablet (pH4.5) of 12 volunteers and stomodaeum lozenge are given, is spued after being put into oral cavity 2min, It gargles, as a result thinks that astringent taste is substantially reduced, be easily accepted by.Compared to original prescription, tablet recipe is sucked using three fruit soup of new process, Supplementary product consumption reduces, and the amount of corrigent is significantly reduced, and stable components, and bacteriostatic activity is without significant change.
Embodiment 2pH adjusts and removes improvement of the citric acid to three fruit soup lozenge astringent tastes
Based on pH to the affecting laws of astringent taste, thus it is speculated that the astringent taste that citric acid may influence three fruit soup lozenges perceives.Therefore, it is right Than original prescription (pH3.5, prescription 1, pH is the pH of former medicinal extract herein), original prescription removal citric acid (pH3.5, prescription 2), original place Side rises pH (pH4.5, prescription 3).
Mouthfeel evaluation is carried out using VAS volunteer's point system.Give everyone 1 taste masking buccal tablet of 12 volunteers and stomodaeum Lozenge spues after being put into oral cavity 2min, gargles, and according to volunteer's expression, control VAS tables score.Three kind of three fruit soup lozenge Prescription comparison is shown in Table 1 and Fig. 6.
1 three kind of three fruit soup of table is compared containing tablet recipe
Prescription Former medicinal extract Medicinal extract after pH rises Citric acid VAS volunteer scores
Prescription 1 (original prescription) + - + 8.58±1.10
Prescription 2 (removal citric acid) + - - 7.91±1.31
Prescription 3 (pH4.5) - + + 4.92±0.90
From result, by prescription 2 compared with original prescription (prescription 1), after removing citric acid, astringent taste reduces, and two groups have system Meter learns difference.On the basis of original prescription (prescription 1), heightening pH to 4.5, in the case where not removing citric acid, astringent taste is shown prescription 3 Writing reduces.I.e. in original prescription, citric acid is directly removed, astringent taste reduces, but unobvious;And prescription 3 can by adjusting pH to 4.5 So that astringent taste significantly reduces, it is with obvious effects.
The three fruit soup of 2 difference pH of table are compared containing tablet recipe
Prescription VAS volunteer scores
Prescription 1 (pH 2.5) 7.94±1.40
Prescription 2 (pH 3.5) 5.94±0.87
Prescription 3 (pH 4) 4.67±0.91
Prescription 4 (pH 4.5) 4.21±0.63
Prescription 5 (pH 5.5) 5.07±1.13
Prescription 6 (pH 6) 6.32±1.19
Prescription 7 (pH 6.5) 6.59±1.05
As shown in Table 2, when pH is 4~4.5, astringent taste significantly reduces.And when pH is 2.5~5.5, coefficient of similarity exists More than 0.996, similarity is very high, illustrates that significant change does not occur for the ratio of ingredient, that is, ensure that the stability of ingredient;Cause This, is adjusted to 4~4.5 by pH, can both ensure the stability of ingredient, can also reduce astringent taste.
Embodiment 3:PH adjusts the improvement to three Le slurry astringent taste
Three Le slurry oral liquid stoste (liquid for preparing oral liquid) is taken, using the Na of 0.5g/mL2CO3Aqueous solution adjusts extraction Liquid pH to 5 obtains three Le of taste masking slurry inspissated juice.Three Le of equivalent is taken to starch oral liquid stoste, three Le of taste masking slurry inspissated juice respectively, then The auxiliary materials such as same amount of L-arginine, ASPARTIC ACID, honey are added in, mixing, sterilization, packaging, inspection storage both obtain, system Agent specification starches oral liquid for 15mL/ bottles to get three Le of taste masking and former three Le starch oral liquid.
It gives everyone three Le of 10mL taste maskings of 12 volunteers slurry oral liquid and starches oral liquid with former three Le, after being put into oral cavity 30s It spues, gargles, as a result think that the astringent taste of three Le slurry oral liquid is down to 5.88 by 7.31, astringent taste significantly reduces, and mouthfeel is more easily accepted by.
Embodiment 4
(1) pH adjusts the improvement to tea extract astringent taste
Green tea is taken, is added water to cook, is filtered, merging filtrate adds the Na of 0.5g/mL2CO3Aqueous solution adjusts pH to alkalescence, stands, Sediment adds the HCl of 1mol/L to adjust pH to acidity, filters, filtrate is shaken with ethyl acetate and extracted, and solvent is recovered under reduced pressure, and is used The Na of 0.5g/mL2CO3Aqueous solution adjusts pH to 5, dry, pulverize, both.
Everyone 0.5g taste maskings tea extract of 12 volunteers and former extract are given, spues, gargles after being put into oral cavity 30s Mouthful, as a result think that the astringent taste of tea extract is down to 6.06 by 8.48, astringent taste significantly reduces, and mouthfeel is more easily accepted by.
(2) pH adjusts the improvement to jian Tablets astringent taste
Above-mentioned taste masking tea extract and tealeaves original extract are taken, is separately added into the microcrystalline cellulose of equivalent (in 80- When 100 DEG C of dryings 4 are small) 100g, starch 94g, with 40% alcohol granulation, low temperature drying adds in magnesium stearate 1.5g, mixing, pressure 1000 are made, has both obtained taste masking piece and former piece.
Everyone 1 taste masking piece of 12 volunteers and former piece are given, spues, gargles after being put into oral cavity 30s, as a result think heart and brain The taste masking piece of strong piece is down to 5.30 compared with the astringent taste of former piece by 7.12, and the astringent taste of the taste masking piece of jian Tablets significantly reduces, mouth Sense is more easily accepted by.
To sum up, the present invention provides a kind of method for reducing the oral preparation of Chinese traditional medicinal astringent taste containing polyphenol, adjusted by alkalescence The pH of the extract of pharmaceutical composition containing polyphenol is adjusted to 4~4.5 by section liquid, and pharmaceutical chemistry ingredient becomes without apparent at this time Change, i.e., while ensure that ingredient stability, unexpectedly significantly reduce the original astringent taste of drug, improve patient's clothes The compliance of medicine avoids and adds in a large amount of corrigents, reduces the dosage of sweetener in prescription, reduce production cost;Taste masking It is with obvious effects, do not increase the dosage of patient, it is simple and practical.
The technique has a very important significance the production of Chinese medicine preparation, and can be used for preparing a variety of traditional handicrafts can not The peroral dosage form (solution sensory issues) of realization, in particular for some specific crowds (old man that such as children and swallowing have any problem) Special form (such as granule, dispersible tablet preparation), it is easy to operate, it is of low cost, be conducive to mass produce, have good Application prospect, be widely portable to the fields such as food, tea beverage, grape wine, drug.

Claims (10)

  1. A kind of 1. method for the astringent taste for reducing the Chinese medicine containing polyphenol, it is characterised in that:The extract of the Chinese medicine containing polyphenol is taken, PH is adjusted to 4~4.5 to get the Chinese medical extract of astringent taste is reduced.
  2. 2. according to the method described in claim 1, it is characterized in that:The extract of the Chinese medicine containing polyphenol carries for tea polyphenols Take object, three fruit soup, three Le slurries, dandelion extract, tranquilization paste, Fructus Hippophae extractum, Shanlu Tea extract for dropping, Fructus chebulae immaturus extract, emblic Seed extract or Nuodikang oral liquid.
  3. 3. according to the method described in claim 1, it is characterized in that:The pH is 4.5.
  4. 4. according to the method described in claim 1, it is characterized in that:The adjusting pH is to adjust liquid or alkalescence using alkalescence Grain;Preferably, it is aqueous sodium carbonate, sodium bicarbonate aqueous solution or sodium hydrate aqueous solution that the alkalescence, which adjusts liquid,;And/or The alkali grain is sodium carbonate particle or sodium bicarbonate particle;It is furthermore preferred that it is 0.1~1g/mL's that the alkalescence, which adjusts liquid, The sodium hydrate aqueous solution of aqueous sodium carbonate, the sodium bicarbonate aqueous solution of 0.1~1g/mL or 0.1~1g/mL;Further more Preferably, the alkalescence adjusts aqueous sodium carbonate, the sodium bicarbonate aqueous solution or 0.5g/mL of 0.5g/mL that liquid is 0.5g/mL Sodium hydrate aqueous solution.
  5. 5. a kind of oral preparation of Chinese traditional medicinal containing polyphenol for reducing astringent taste, it is characterised in that:It is prepared by following methods It arrives:The extract of the Chinese medicine containing polyphenol is taken, pH is adjusted to 4~4.5 to get the Chinese medical extract of astringent taste is reduced, then is added Oral formulations are prepared in upper pharmaceutically acceptable auxiliary material.
  6. 6. oral preparation of Chinese traditional medicinal according to claim 5, it is characterised in that:The extract of the Chinese medicine containing polyphenol is Tea polyphenol extract object, three fruit soup, three Le slurries, dandelion extract, tranquilization paste, Fructus Hippophae extractum, Shanlu Tea extract for dropping, myrobalan extraction Object, emblic extract or Nuodikang oral liquid.
  7. 7. oral preparation of Chinese traditional medicinal according to claim 5, it is characterised in that:The pH is 4.5.
  8. 8. oral preparation of Chinese traditional medicinal according to claim 5, it is characterised in that:The adjusting pH be using alkalescence adjust liquid or Alkali grain;Preferably, it is aqueous sodium carbonate, sodium bicarbonate aqueous solution or sodium hydrate aqueous solution that the alkalescence, which adjusts liquid,; And/or the alkali grain is sodium carbonate particle or sodium bicarbonate particle;It is furthermore preferred that the alkalescence adjust liquid for 0.1~ The sodium hydrate aqueous solution of the aqueous sodium carbonate of 1g/mL, the sodium bicarbonate aqueous solution of 0.1~1g/mL or 0.1~1g/mL;Into One step it is furthermore preferred that the alkalescence adjust liquid be the aqueous sodium carbonate of 0.5g/mL, 0.5g/mL sodium bicarbonate aqueous solution or The sodium hydrate aqueous solution of 0.5g/mL.
  9. 9. oral preparation of Chinese traditional medicinal according to claim 5, it is characterised in that:The oral formulations are granule, lozenge, nozzle Chew piece, lozenge, oral liquid, pill, tablet, powder, mixture, syrup, electuary, paste or sublimed preparation.
  10. 10. oral preparation of Chinese traditional medicinal according to claim 9, it is characterised in that:The oral formulations for tea polyphenol extract object, Three fruit soup lozenges, three Le slurry oral liquid, jian Tablets, dandelion granule, tranquilization paste, five tastes sea-buckthorn dissipate, double mountain particles, myrobalan Lozenge, throat smoothing tablet with emblic or Nuodikang oral liquid.
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109999201A (en) * 2019-04-19 2019-07-12 成都中医药大学 A kind of novel taste masking companion agent and application thereof
CN111419791A (en) * 2019-03-22 2020-07-17 成都中医药大学 Method for inhibiting generation of oral liquid precipitate
CN115734713A (en) * 2020-06-29 2023-03-03 富士胶片株式会社 Method for preparing purified extract of Salacia plant

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1104912A (en) * 1994-01-07 1995-07-12 周荣华 Oral liquid for invigorating kidney and strengthening yang and its production method
CN101404990A (en) * 2006-03-16 2009-04-08 诺瓦提斯公司 Solid dosage form containing a taste masked active agent
CN101474309A (en) * 2009-01-22 2009-07-08 中国人民解放军海军医学研究所 Composition with anti-fatigue and anti-anoxia functions and preparation method thereof
CN101573046A (en) * 2006-12-27 2009-11-04 卡夫食品环球品牌有限责任公司 Reduction of astringency in polyphenol compositions
CN101716220A (en) * 2009-11-20 2010-06-02 杭州平和安康医药科技有限公司 Shielding alkaloid traditional Chinese medicine
CN101966292A (en) * 2010-10-07 2011-02-09 吉林省集安益盛药业股份有限公司 Sugarless Chinese medicinal oral liquid and preparation method thereof
US20110236560A1 (en) * 2010-02-11 2011-09-29 Daniel Perlman Food supplementation with phenolic antioxidants in vinegar
CN102781423A (en) * 2010-02-26 2012-11-14 罗蒂株式会社 Deodorant composition
CN103520471A (en) * 2013-10-21 2014-01-22 海南康芝药业股份有限公司 Bitterness covering agent for Chinese medicine mixture
CN106771018A (en) * 2017-01-20 2017-05-31 成都中医药大学附属医院 A kind of modeling method of Chinese medicine astringent taste evaluation model
CN107712842A (en) * 2017-12-01 2018-02-23 江苏华桑食品科技有限公司 A kind of preparation method of natural locust tree sophora flower flower sauce
CN109862902A (en) * 2016-09-08 2019-06-07 莱拉营养食品有限公司 The smell of native compound shelters preparation

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1104912A (en) * 1994-01-07 1995-07-12 周荣华 Oral liquid for invigorating kidney and strengthening yang and its production method
CN101404990A (en) * 2006-03-16 2009-04-08 诺瓦提斯公司 Solid dosage form containing a taste masked active agent
CN101573046A (en) * 2006-12-27 2009-11-04 卡夫食品环球品牌有限责任公司 Reduction of astringency in polyphenol compositions
CN101474309A (en) * 2009-01-22 2009-07-08 中国人民解放军海军医学研究所 Composition with anti-fatigue and anti-anoxia functions and preparation method thereof
CN101716220A (en) * 2009-11-20 2010-06-02 杭州平和安康医药科技有限公司 Shielding alkaloid traditional Chinese medicine
US20110236560A1 (en) * 2010-02-11 2011-09-29 Daniel Perlman Food supplementation with phenolic antioxidants in vinegar
CN102781423A (en) * 2010-02-26 2012-11-14 罗蒂株式会社 Deodorant composition
CN101966292A (en) * 2010-10-07 2011-02-09 吉林省集安益盛药业股份有限公司 Sugarless Chinese medicinal oral liquid and preparation method thereof
CN103520471A (en) * 2013-10-21 2014-01-22 海南康芝药业股份有限公司 Bitterness covering agent for Chinese medicine mixture
CN109862902A (en) * 2016-09-08 2019-06-07 莱拉营养食品有限公司 The smell of native compound shelters preparation
CN106771018A (en) * 2017-01-20 2017-05-31 成都中医药大学附属医院 A kind of modeling method of Chinese medicine astringent taste evaluation model
CN107712842A (en) * 2017-12-01 2018-02-23 江苏华桑食品科技有限公司 A kind of preparation method of natural locust tree sophora flower flower sauce

Non-Patent Citations (12)

* Cited by examiner, † Cited by third party
Title
ELÍAS OBREQUE-SLIER ,ET AL: "Interactions of enological tannins with the protein fraction of saliva and astringency perception are affected by pH", 《LWT - FOOD SCIENCE AND TECHNOLOGY》 *
姚喆,等: "藏药三果汤散化学与药理研究进展", 《全国第三届药用植物化学与中药新药研发技术创新研讨会》 *
张婷,等: "小分子苦味淬灭剂应用于口服液体制剂的研究概况", 《中国药学杂志》 *
朱彩平,等: "石榴皮多酚提取方法研究进展", 《食品与发酵工业》 *
杨晓雁,等: ""酒度、总酸、pH值以及饮用温度对干红葡萄酒涩味的影响"", 《食品科学》 *
林俊芝,等: ""中药涩味的形成原理及掩蔽技术的研究概况"", 《中草药》 *
柳梅,等: "沙棘叶多酚提取物抗氧化及体外降血糖活性研究", 《天然产物研究与开发》 *
胥佰涛,等: "茶多酚提取方法研究进展", 《茶叶》 *
董科,等: "植物多酚及其提取方法的研究进展", 《食品工业科技》 *
赵生玉,等: "中药制剂掩味评价新方法功能性磁共振成像技术应用的前瞻性分析", 《中草药》 *
郭炳春,等: "余甘子总多酚提取工艺优化研究", 《热带作物学报》 *
黄浩洲,等: "多酚类液体制剂精细制造关键:多元沉淀形成原理与稳态重构", 《药学学报》 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111419791A (en) * 2019-03-22 2020-07-17 成都中医药大学 Method for inhibiting generation of oral liquid precipitate
CN111419791B (en) * 2019-03-22 2022-04-08 成都中医药大学 Method for inhibiting generation of oral liquid precipitate
CN109999201A (en) * 2019-04-19 2019-07-12 成都中医药大学 A kind of novel taste masking companion agent and application thereof
CN109999201B (en) * 2019-04-19 2023-02-17 成都中医药大学 Taste-masking mate agent and application thereof
CN115734713A (en) * 2020-06-29 2023-03-03 富士胶片株式会社 Method for preparing purified extract of Salacia plant

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