JP2011148776A - Liquid preparation composition - Google Patents
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- JP2011148776A JP2011148776A JP2010283967A JP2010283967A JP2011148776A JP 2011148776 A JP2011148776 A JP 2011148776A JP 2010283967 A JP2010283967 A JP 2010283967A JP 2010283967 A JP2010283967 A JP 2010283967A JP 2011148776 A JP2011148776 A JP 2011148776A
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- bitterness
- aspartic acid
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- 239000007788 liquid Substances 0.000 title claims abstract description 24
- 239000000203 mixture Substances 0.000 title claims abstract description 22
- 239000000284 extract Substances 0.000 claims abstract description 16
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims abstract description 15
- 235000003704 aspartic acid Nutrition 0.000 claims abstract description 13
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 150000003839 salts Chemical class 0.000 claims abstract description 9
- 235000019658 bitter taste Nutrition 0.000 abstract description 21
- 241000218203 Coptis japonica Species 0.000 abstract description 4
- 238000013329 compounding Methods 0.000 abstract 2
- 229960005261 aspartic acid Drugs 0.000 description 11
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 239000003814 drug Substances 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 238000011156 evaluation Methods 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 239000008213 purified water Substances 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 235000013305 food Nutrition 0.000 description 3
- AKYHKWQPZHDOBW-UHFFFAOYSA-N (5-ethenyl-1-azabicyclo[2.2.2]octan-7-yl)-(6-methoxyquinolin-4-yl)methanol Chemical compound OS(O)(=O)=O.C1C(C(C2)C=C)CCN2C1C(O)C1=CC=NC2=CC=C(OC)C=C21 AKYHKWQPZHDOBW-UHFFFAOYSA-N 0.000 description 2
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 2
- CKLJMWTZIZZHCS-UHFFFAOYSA-N D-OH-Asp Natural products OC(=O)C(N)CC(O)=O CKLJMWTZIZZHCS-UHFFFAOYSA-N 0.000 description 2
- 239000001576 FEMA 2977 Substances 0.000 description 2
- 239000004471 Glycine Substances 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- CKLJMWTZIZZHCS-UWTATZPHSA-N L-Aspartic acid Natural products OC(=O)[C@H](N)CC(O)=O CKLJMWTZIZZHCS-UWTATZPHSA-N 0.000 description 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 2
- 229940024606 amino acid Drugs 0.000 description 2
- 235000001014 amino acid Nutrition 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- LOUPRKONTZGTKE-UHFFFAOYSA-N cinchonine Natural products C1C(C(C2)C=C)CCN2C1C(O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-UHFFFAOYSA-N 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 241000411851 herbal medicine Species 0.000 description 2
- 230000000968 intestinal effect Effects 0.000 description 2
- 239000001630 malic acid Substances 0.000 description 2
- 235000011090 malic acid Nutrition 0.000 description 2
- 229960003110 quinine sulfate Drugs 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 239000000341 volatile oil Substances 0.000 description 2
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 229920002527 Glycogen Polymers 0.000 description 1
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 description 1
- 241000218201 Ranunculaceae Species 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 244000269722 Thea sinensis Species 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- YBHILYKTIRIUTE-UHFFFAOYSA-N berberine Chemical compound C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 YBHILYKTIRIUTE-UHFFFAOYSA-N 0.000 description 1
- 229940093265 berberine Drugs 0.000 description 1
- QISXPYZVZJBNDM-UHFFFAOYSA-N berberine Natural products COc1ccc2C=C3N(Cc2c1OC)C=Cc4cc5OCOc5cc34 QISXPYZVZJBNDM-UHFFFAOYSA-N 0.000 description 1
- 235000013361 beverage Nutrition 0.000 description 1
- 229960001948 caffeine Drugs 0.000 description 1
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 description 1
- 229940126678 chinese medicines Drugs 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 239000003797 essential amino acid Substances 0.000 description 1
- 235000020776 essential amino acid Nutrition 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 229940096919 glycogen Drugs 0.000 description 1
- 239000012676 herbal extract Substances 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 239000003002 pH adjusting agent Substances 0.000 description 1
- QUCQEUCGKKTEBI-UHFFFAOYSA-N palmatine Chemical compound COC1=CC=C2C=C(C3=C(C=C(C(=C3)OC)OC)CC3)[N+]3=CC2=C1OC QUCQEUCGKKTEBI-UHFFFAOYSA-N 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 229940109850 royal jelly Drugs 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 235000011496 sports drink Nutrition 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
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- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Description
本発明は、医薬品、医薬部外品及び食品等の分野における液剤組成物に関する。 The present invention relates to a liquid composition in the fields of pharmaceuticals, quasi drugs and foods.
オウレンは整腸薬として健胃、消化不良や下痢の改善等に広く利用されてきた。また、各種漢方の構成生薬としても知られている。 Ouren has been widely used as an intestinal agent for improving the stomach, digestive disorders and diarrhea. It is also known as a herbal medicine for various Chinese medicines.
オウレンを含有する液剤には、通常オウレンエキスが使用されているが、水溶液に溶かした場合に強い苦味が生じるという問題があった。このような苦味に関する問題を解決する方法として、モノ又はジグリセリドとポリカルボン酸とのエステルを配合する方法(特許文献1)、精油又は精油成分を配合する方法(特許文献2)等が報告されている。しかしこれらの技術を使用しても、マスキング効果が十分でないという問題があった。 An oren extract is usually used as a liquid agent containing aurene, but there is a problem that a strong bitter taste occurs when it is dissolved in an aqueous solution. As a method for solving such a bitterness problem, a method of blending an ester of mono- or diglyceride and polycarboxylic acid (Patent Document 1), a method of blending essential oil or an essential oil component (Patent Document 2), etc. have been reported. Yes. However, even if these techniques are used, there is a problem that the masking effect is not sufficient.
本発明の目的は、苦味を有するオウレンエキスを日常的に無理なく多量に摂取することができるように、苦味をマスキングしたオウレンエキス配合液剤を提供することである。 An object of the present invention is to provide an agate extract-containing liquid that masks bitterness so that abundantly can be ingested in a large amount on a daily basis.
本発明者は、上記課題を解決するために鋭意検討した結果、意外にもアスパラギン酸又はその塩を配合することにより、オウレンエキスが溶解した際に生じる苦味が改善されることを見いだし、本発明を完成した。 As a result of intensive studies to solve the above-mentioned problems, the present inventor has unexpectedly found that the bitterness produced when the aurene extract is dissolved is improved by blending aspartic acid or a salt thereof. Was completed.
すなわち、本発明は、
(1)オウレンエキス及びアスパラギン酸又はその塩を含有することを特徴とする液剤組成物、又は
(2)オウレンエキス1質量部に対して、アスパラギン酸又はその塩を2質量部以上配合することを特徴とする、(1)に記載の液剤組成物である。
That is, the present invention
(1) A liquid drug composition characterized by containing an oren extract and aspartic acid or a salt thereof, or (2) 2 parts by mass or more of aspartic acid or a salt thereof with respect to 1 part by mass of an oren extract. The liquid composition according to (1), which is characterized.
本発明により、オウレンエキスの苦味が改善された極めて服用しやすい液剤組成物を提供することができた。 INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide a liquid composition that is extremely easy to take and has improved bitterness of the auren extract.
本発明で用いるオウレンはキンポウゲ科の植物のオウレン(Coptis japonica)の根茎である。オウレンはベルベリン、パルマチン、オウレニン、コプチシンなどの成分を含有し、健胃、整腸などの作用を有する。オウレンエキスは、前記オウレンを通常の方法を用いて抽出することにより得られる。抽出溶媒として、例えば、メタノール、エタノール等の低級アルコール、水等、もしくはその混合物を用いることが出来る。 The auren used in the present invention is the rhizome of Coptis japonica, a plant of the family Ranunculaceae. Ouren contains components such as berberine, palmatin, Ourenin, and Copticin, and has effects such as healthy stomach and intestinal regulation. Ouren extract is obtained by extracting the above-mentioned Ouren using a conventional method. As the extraction solvent, for example, a lower alcohol such as methanol or ethanol, water, or a mixture thereof can be used.
アスパラギン酸は、グリコーゲン産生性の非必須アミノ酸で、アミノ酸輸液や経口・経腸栄養剤等、食品、医薬品の広い分野で使用されている。アスパラギン酸は、好ましくはL−アスパラギン酸であり、ナトリウム塩やカリウム塩などの塩を使用しても同様の効果を得ることができる。 Aspartic acid is a glycogen-producing non-essential amino acid and is used in a wide range of food and pharmaceutical fields such as amino acid infusions and oral and enteral nutrients. Aspartic acid is preferably L-aspartic acid, and the same effect can be obtained even when a salt such as sodium salt or potassium salt is used.
本発明における液剤組成物において、アスパラギン酸の配合量はオウレンエキス1質量部に対してアスパラギン酸を0.1〜500質量部であり、好ましくは1〜100質量部であり、さらに好ましくは2〜100質量部である。この配合量により、オウレンにより生じる苦味を効果的に低減する液剤組成物を提供することができる。 In the liquid composition of the present invention, the amount of aspartic acid is 0.1 to 500 parts by weight, preferably 1 to 100 parts by weight, more preferably 2 to 1 part by weight of aspartic acid. 100 parts by mass. With this blending amount, it is possible to provide a liquid composition that effectively reduces the bitterness caused by the aurene.
本発明における液剤組成物のpHは、特に限定されないが、好ましくは2.5〜7.0であり、より好ましくは3.0〜6.0であり、さらに好ましくは3.0〜4.5である。
本発明の液剤組成物のpHを上記範囲に保つために、必要に応じて有機酸等のpH調整剤を配合することができる。また、その他の成分として、ビタミン類、他のミネラル類、アミノ酸及びその塩類、生薬、生薬抽出物、カフェイン、ローヤルゼリー等を本発明の効果を損なわない範囲で適宜に配合することができる。さらに必要に応じて、抗酸化剤、着色剤、香料、矯味剤、界面活性剤、溶解補助剤、保存剤、甘味料等の添加物を本発明の効果を損なわない範囲で適宜に配合することができる。
The pH of the liquid composition in the present invention is not particularly limited, but is preferably 2.5 to 7.0, more preferably 3.0 to 6.0, and still more preferably 3.0 to 4.5. It is.
In order to keep the pH of the liquid composition of the present invention in the above range, a pH adjuster such as an organic acid can be blended as necessary. In addition, as other components, vitamins, other minerals, amino acids and salts thereof, herbal medicines, herbal extracts, caffeine, royal jelly, and the like can be appropriately blended as long as the effects of the present invention are not impaired. Furthermore, if necessary, additives such as antioxidants, colorants, fragrances, flavoring agents, surfactants, solubilizers, preservatives, sweeteners and the like are appropriately blended within a range not impairing the effects of the present invention. Can do.
本発明の液剤組成物は、常法により調製することができ、その方法は特に限定されるものではない。通常、各成分をとり適量の精製水で溶解した後、pHを調整し、更に精製水を加えて容量調整し、必要に応じてろ過、殺菌処理を行うことにより本発明の液剤組成物を得ることができる。 The liquid composition of the present invention can be prepared by a conventional method, and the method is not particularly limited. Usually, after each component is taken and dissolved in an appropriate amount of purified water, the pH is adjusted, the volume is further adjusted by adding purified water, and the liquid composition of the present invention is obtained by performing filtration and sterilization treatment as necessary. be able to.
本発明の液剤組成物は、内服液剤組成物であり、ドリンク剤、シロップ等の医薬品及び医薬部外品の他、健康飲料、茶飲料、スポーツドリンク等の食品領域における各種飲料として提供することができる。 The liquid composition of the present invention is a liquid composition for internal use, and can be provided as various beverages in food areas such as health drinks, tea drinks, sports drinks, in addition to pharmaceuticals and quasi drugs such as drinks and syrups. it can.
以下に実施例及び試験例を示し、本発明をより詳細に説明する。
<実施例>
(1)苦味の評価
精製水にオウレンエキス(松浦薬業(株))10mgを溶かし、その溶液に表1〜3に示す配合量のL−アスパラギン酸、グリシン、クエン酸、又はリンゴ酸を添加・溶解させた。さらに精製水を加えて全量100mLとし、塩酸及び水酸化ナトリウムでpH3〜4.5に調整した。各試験液をガラスビンに充填後殺菌し、表1〜3に示す実施例1〜7及び比較例1〜7の液剤組成物を得た。
The following examples and test examples illustrate the present invention in more detail.
<Example>
(1) Evaluation of bitterness 10 mg of auren extract (Matsuura Pharmaceutical Co., Ltd.) is dissolved in purified water, and the amounts of L-aspartic acid, glycine, citric acid, or malic acid shown in Tables 1 to 3 are added to the solution. -Dissolved. Further, purified water was added to make a total volume of 100 mL, and the pH was adjusted to 3 to 4.5 with hydrochloric acid and sodium hydroxide. Each test solution was filled in a glass bottle and sterilized to obtain liquid composition of Examples 1 to 7 and Comparative Examples 1 to 7 shown in Tables 1 to 3.
<試験例>
各液剤組成物約10mLを5秒間口に含んだ時に感じる苦味の最大値について、成人男女からなるパネルにより評価した。評価方法は、以下のスタンダードに対する相対評価とした。
<Test example>
The maximum bitterness felt when about 10 mL of each liquid composition was included in the mouth for 5 seconds was evaluated by a panel of adult men and women. The evaluation method was relative evaluation with respect to the following standards.
スタンダードは、0.006、0.012、 0.020、 0.031、0.050mM 硫酸キニーネとした。各濃度の硫酸キニーネを服用した際の苦味をそれぞれ苦味強度1〜5に設定し、「0.006mMよりも苦味が弱い」場合を苦味強度0、「0.050mMよりも苦味が強い」場合を苦味強度6に設定した。 The standard was 0.006, 0.012, 0.020, 0.031, 0.050 mM quinine sulfate. The bitterness when taking quinine sulfate of each concentration is set to bitterness intensity 1 to 5, respectively, when “bitterness is weaker than 0.006 mM”, bitterness intensity is 0, “bitterness is stronger than 0.050 mM” The bitterness intensity was set to 6.
5名の評価結果の平均値を表4〜5に,2名の評価結果の平均値を表6に示す。 Tables 4 to 5 show the average values of the evaluation results of the five people, and Table 6 shows the average values of the evaluation results of the two people.
本発明により、オウレンエキスにより生じる苦味が改善された、極めて服用しやすい液剤組成物を提供することが可能となった。 According to the present invention, it is possible to provide a liquid composition that is improved in bitterness caused by an aurene extract and that is extremely easy to take.
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103417661A (en) * | 2013-08-13 | 2013-12-04 | 吴中区胥口精益生物医药研究所 | Rhizoma coptidis essence and preparation method thereof |
CN105055995A (en) * | 2015-08-10 | 2015-11-18 | 孙霞 | Traditional Chinese medicine used for treating spleen-stomach disharmony |
CN106727295A (en) * | 2016-12-28 | 2017-05-31 | 江西济民可信药业有限公司 | A kind of normal open oral liquid for relaxation and preparation method thereof |
RU2667638C2 (en) * | 2013-04-29 | 2018-09-21 | Кореа Юнайтед Фарм. Инк. | Oral formulation comprising extract of coptis rhizome having masked bitter taste |
JP2019011279A (en) * | 2017-06-30 | 2019-01-24 | 小林製薬株式会社 | Diarrhea inhibitor |
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JPH05255126A (en) * | 1992-03-04 | 1993-10-05 | Zeria Pharmaceut Co Ltd | Bitter taste-reducing composition |
JP2000270804A (en) * | 1999-03-26 | 2000-10-03 | Snow Brand Milk Prod Co Ltd | Agent for reducing or removing bitterness of sweetener with high sweetness |
JP2003231631A (en) * | 2001-12-03 | 2003-08-19 | Eisai Co Ltd | Gustatory improving composition |
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2010
- 2010-12-21 JP JP2010283967A patent/JP2011148776A/en active Pending
Patent Citations (4)
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JPS5417014B2 (en) * | 1974-03-09 | 1979-06-27 | ||
JPH05255126A (en) * | 1992-03-04 | 1993-10-05 | Zeria Pharmaceut Co Ltd | Bitter taste-reducing composition |
JP2000270804A (en) * | 1999-03-26 | 2000-10-03 | Snow Brand Milk Prod Co Ltd | Agent for reducing or removing bitterness of sweetener with high sweetness |
JP2003231631A (en) * | 2001-12-03 | 2003-08-19 | Eisai Co Ltd | Gustatory improving composition |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
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RU2667638C2 (en) * | 2013-04-29 | 2018-09-21 | Кореа Юнайтед Фарм. Инк. | Oral formulation comprising extract of coptis rhizome having masked bitter taste |
CN103417661A (en) * | 2013-08-13 | 2013-12-04 | 吴中区胥口精益生物医药研究所 | Rhizoma coptidis essence and preparation method thereof |
CN105055995A (en) * | 2015-08-10 | 2015-11-18 | 孙霞 | Traditional Chinese medicine used for treating spleen-stomach disharmony |
CN106727295A (en) * | 2016-12-28 | 2017-05-31 | 江西济民可信药业有限公司 | A kind of normal open oral liquid for relaxation and preparation method thereof |
JP2019011279A (en) * | 2017-06-30 | 2019-01-24 | 小林製薬株式会社 | Diarrhea inhibitor |
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