JP2011148776A - Liquid preparation composition - Google Patents

Liquid preparation composition Download PDF

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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
liquid preparation
liquid composition
extract
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Takashi Domoto
隆史 堂本
Takuto Takei
拓人 武井
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Taisho Pharmaceutical Co Ltd
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Taisho Pharmaceutical Co Ltd
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Abstract

<P>PROBLEM TO BE SOLVED: To provide a liquid preparation improving the bitter taste of a Coptis japonica extract. <P>SOLUTION: The liquid preparation composition is characterized by compounding a Coptis japonica extract and aspartic acid or its salt. Preferably, the liquid preparation composition is characterized by compounding 1 pt.mass of the Coptis japonica extract with ≥2 pts.mass of the aspartic acid or its salt. <P>COPYRIGHT: (C)2011,JPO&INPIT

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.

特開平8−242809号公報JP-A-8-242809 特開平5−255126号公報Japanese Patent Laid-Open No. 5-255126

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.

Figure 2011148776
Figure 2011148776

Figure 2011148776
Figure 2011148776

Figure 2011148776
Figure 2011148776

<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.

Figure 2011148776
Figure 2011148776

Figure 2011148776
Figure 2011148776

Figure 2011148776
比較例1のオウレンエキス配合液剤では強い苦味が認められたが、実施例1のようにアスパラギン酸を添加することで苦味が顕著に抑制された。比較例2〜4において添加したグリシン、クエン酸、又はリンゴ酸では十分な苦味抑制効果が認められなかった。オウレンエキス1質量部に対してアスパラギン酸を2質量部以上含有させることにより苦味が顕著に抑制された(実施例2〜4)。表6より、pH3.0〜4.5の範囲で苦味が顕著に抑制された(実施例5〜7)。
Figure 2011148776
Although a strong bitter taste was recognized in the liquid composition of the aurene extract of Comparative Example 1, bitterness was significantly suppressed by adding aspartic acid as in Example 1. The glycine, citric acid, or malic acid added in Comparative Examples 2 to 4 did not show a sufficient bitter taste suppressing effect. Bitterness was remarkably suppressed by containing 2 parts by mass or more of aspartic acid with respect to 1 part by mass of the aurene extract (Examples 2 to 4). From Table 6, bitterness was remarkably suppressed in the range of pH 3.0 to 4.5 (Examples 5 to 7).

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.

Claims (2)

オウレンエキス及びアスパラギン酸又はその塩を配合することを特徴とする液剤組成物。 A liquid preparation composition comprising an oren extract and aspartic acid or a salt thereof. 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、請求項1に記載の液剤組成物。 The liquid composition according to claim 1, wherein 2 parts by mass or more of aspartic acid or a salt thereof is blended with 1 part by mass of auren extract.
JP2010283967A 2009-12-22 2010-12-21 Liquid preparation composition Pending JP2011148776A (en)

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Cited By (5)

* Cited by examiner, † Cited by third party
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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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