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JP2007063144A - Liquid composition - Google Patents

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JP2007063144A
JP2007063144A JP2005247332A JP2005247332A JP2007063144A JP 2007063144 A JP2007063144 A JP 2007063144A JP 2005247332 A JP2005247332 A JP 2005247332A JP 2005247332 A JP2005247332 A JP 2005247332A JP 2007063144 A JP2007063144 A JP 2007063144A
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hydroxy
decenoic acid
liquid composition
surfactant
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JP4911278B2 (en
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Motohisa Ookubo
始久 大久保
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Taisho Pharmaceutical Co Ltd
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Abstract

<P>PROBLEM TO BE SOLVED: To provide a liquid composition which improves the stability of 10-hydroxy-2-decenoic acid, even when containing a surfactant having a polyoxyethylene group. <P>SOLUTION: A method for stabilizing 10-hydroxy-2-decenoic acid comprises adding one or more galenicals selected from the group consisting of Atractylodis rhizome, Cnidium officinale rhizome, Cordyceps sinensis Sacc., and bupleuri radix to a liquid composition containing a surfactant having a polyoxyethylene group and the 10-hydroxy-2-decenoic acid. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

本発明は、10−ヒドロキシ−2−デセン酸が安定化された液体組成物に関する。   The present invention relates to a liquid composition in which 10-hydroxy-2-decenoic acid is stabilized.

10−ヒドロキシ−2−デセン酸は、ローヤルゼリーに特異的に含まれている有機酸であり、抗腫瘍作用、菌発育阻止作用を持つと言われている。ローヤルゼリーは蛋白質、脂質、炭水化物をはじめ、ビタミン類、ミネラル類、アミノ酸類、脂肪酸等の栄養成分をバランスよく含み、滋養、強壮、体質改善等広範な薬理作用を示すなど高度の機能性を有することから健康食品、医薬品、化粧品として利用されている。   10-Hydroxy-2-decenoic acid is an organic acid specifically contained in royal jelly, and is said to have antitumor activity and fungal growth inhibition activity. Royal jelly contains protein, lipid, carbohydrates, vitamins, minerals, amino acids, fatty acids and other nutritional components in a well-balanced manner, and has a high degree of functionality such as nourishment, toughness, constitution improvement, etc. It is used as health food, pharmaceuticals and cosmetics.

しかしながら、10−ヒドロキシ−2−デセン酸の安定性に関する研究は、ほとんど行われておらず、単一水溶液(クエン酸緩衝液)中では安定であるが、ドリンク剤等の製剤に他の成分と共に配合した場合に、その安定性が損なわれることが知られていた。   However, there has been almost no research on the stability of 10-hydroxy-2-decenoic acid, and it is stable in a single aqueous solution (citrate buffer). It has been known that when blended, the stability is impaired.

従来、栄養補給や疾病の治療等を目的として、ビタミンA、ビタミンE等の脂溶性薬物がドリンク剤等の液剤に配合されているが、このような脂溶性薬物を液剤に安定に配合するためには、可溶化剤として界面活性剤を添加する必要がある。一般的に、ドリンク剤のような内服液剤においては、安全性の観点から、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレングリセリン脂肪酸エステル等が用いられている(特許文献1参照)。   Conventionally, fat-soluble drugs such as vitamin A and vitamin E have been blended into liquids such as drinks for the purpose of nutritional supplementation and disease treatment, etc., in order to stably blend such fat-soluble drugs into liquids. It is necessary to add a surfactant as a solubilizer. Generally, in an internal liquid such as a drink, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene glycerin fatty acid ester and the like are used from the viewpoint of safety (Patent Document 1). reference).

また、従来、ローヤルゼリーを配合したドリンク剤(特許文献2参照)が知られているが、10−ヒドロキシ−2−デセン酸と、ビタミンA、ビタミンE等の脂溶性薬物を配合した液剤については知られていない。   Conventionally, drinks containing royal jelly (see Patent Document 2) are known, but liquids containing 10-hydroxy-2-decenoic acid and fat-soluble drugs such as vitamin A and vitamin E are known. It is not done.

特開2002−128672号公報JP 2002-128672 A 特開2005−35979号公報JP 2005-35979 A

本発明者らが脂溶性薬物及びローヤルゼリーを配合したドリンク剤を開発しようとしたところ、以下の欠点が判明した。すなわち、10−ヒドロキシ−2−デセン酸と、脂溶性薬物の可溶化剤であるポリオキシエチレン基を有する界面活性剤を液剤に配合することにより、10−ヒドロキシ−2−デセン酸の安定性が著しく低下することが判明した。   When the present inventors tried to develop a drink containing a fat-soluble drug and royal jelly, the following drawbacks were found. That is, by adding 10-hydroxy-2-decenoic acid and a surfactant having a polyoxyethylene group, which is a solubilizer of a fat-soluble drug, to the liquid agent, the stability of 10-hydroxy-2-decenoic acid is improved. It turned out to be significantly reduced.

本発明は、ポリオキシエチレン基を有する界面活性剤が配合されていても10−ヒドロキシ−2−デセン酸の安定性が改善された液体組成物を提供することを目的とする。   An object of the present invention is to provide a liquid composition in which the stability of 10-hydroxy-2-decenoic acid is improved even when a surfactant having a polyoxyethylene group is blended.

上記課題を解決するために、本発明者は鋭意検討を重ねた結果、白ジュツ、川キュウ、冬虫夏草、柴胡からなる群より選ばれる1種又は2種以上を配合することにより、ポリオキシエチレン基を有する界面活性剤を含有する溶液中で10−ヒドロキシ−2−デセン酸を安定化できることを見出し、本発明を完成した。   In order to solve the above-mentioned problems, the present inventor has conducted extensive studies, and as a result, polyoxyethylene is blended by blending one or more selected from the group consisting of white jutsu, river cucumber, cordyceps, and shiihu. The present invention was completed by finding that 10-hydroxy-2-decenoic acid can be stabilized in a solution containing a surfactant having a group.

すなわち、本発明は以下の通りである。
(1)白ジュツ、川キュウ、冬虫夏草、柴胡からなる群より選ばれる1種又は2種以上の生薬、10-ヒドロキシ-2-デセン酸、及び、ポリオキシエチレン基を有する界面活性剤を含有する液体組成物。
(2)ポリオキシエチレン基を有する界面活性剤が、ポリオキシエチレン硬化ヒマシ油である上記(1)に記載の液体組成物。
(3)ポリオキシエチレン基を有する界面活性剤と10-ヒドロキシ-2-デセン酸を含む液体組成物に、白ジュツ、川キュウ、冬虫夏草、柴胡からなる群より選ばれる1種又は2種以上の生薬を添加することによる10-ヒドロキシ-2-デセン酸の安定化方法。
That is, the present invention is as follows.
(1) Contains one or more herbal medicines selected from the group consisting of white jutsu, river cucumber, cordyceps sinensis, and shiihu, 10-hydroxy-2-decenoic acid, and a surfactant having a polyoxyethylene group Liquid composition.
(2) The liquid composition according to the above (1), wherein the surfactant having a polyoxyethylene group is polyoxyethylene hydrogenated castor oil.
(3) A liquid composition containing a surfactant having a polyoxyethylene group and 10-hydroxy-2-decenoic acid, one or more selected from the group consisting of white jutsu, river cucumber, cordyceps and saiko Of 10-hydroxy-2-decenoic acid by adding a crude drug of

本発明により、ポリオキシエチレン基を有する界面活性剤を配合した液体組成物においても10−ヒドロキシ−2−デセン酸を安定に配合することができた。   According to the present invention, 10-hydroxy-2-decenoic acid can be stably blended even in a liquid composition blended with a surfactant having a polyoxyethylene group.

本発明で用いる10−ヒドロキシ−2−デセン酸は、公知の化合物であり、ローヤルゼリーからの抽出物もしくは合成品のいずれであってもよく、又は、これを含むローヤルゼリーの形態で配合されてもよい。その配合量は、製剤全体に対して、1×10-5〜1.0w/v%、好ましくは1×10-5〜1×10-1w/v%、さらに好ましくは、5×10-4w/v%〜3×10-2w/v%である。1×10−5w/v%未満であると液剤に配合したときの10−ヒドロキシ−2−デセン酸又はこれを含むローヤルゼリーの薬理作用を発現しにくくなり、1.0w/v%を超えて配合すると内服液剤としたときに風味の点から好ましくないからである。 10-Hydroxy-2-decenoic acid used in the present invention is a known compound, and may be an extract from a royal jelly or a synthetic product, or may be formulated in the form of a royal jelly containing the same. . The amount is 1 × 10 −5 to 1.0 w / v%, preferably 1 × 10 −5 to 1 × 10 −1 w / v%, more preferably 5 × 10 − 4 w / v% to 3 × 10 −2 w / v%. When it is less than 1 × 10 −5 w / v%, it becomes difficult to express the pharmacological action of 10-hydroxy-2-decenoic acid or a royal jelly containing the same when blended in a liquid, and exceeds 1.0 w / v%. This is because when blended, it is not preferable from the viewpoint of flavor when it is used as an internal solution.

本発明におけるポリオキシエチレン基を有する界面活性剤は、例えば、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレングリセリン脂肪酸エステル等が挙げられるが、可溶化力が優れている点からポリオキシエチレン硬化ヒマシ油が特に好ましい。   Examples of the surfactant having a polyoxyethylene group in the present invention include polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene glycerin fatty acid ester, and the like, but the solubilizing power is excellent. To polyoxyethylene hydrogenated castor oil is particularly preferred.

本発明における生薬は、白ジュツ、川キュウ、冬虫夏草、柴胡からなる群より1種又は2種以上を選択することができる。   The herbal medicine in this invention can select 1 type (s) or 2 or more types from the group which consists of white jutsu, river cucumber, cordyceps and saiko.

生薬の配合量は、10−ヒドロキシ−2−デセン酸1重量部に対して、白ジュツが原生薬換算量で1〜20000重量部、好ましくは10〜2000重量部、川キュウが原生薬換算量で0.1〜10000重量部、好ましくは1〜1000重量部、冬虫夏草が原生薬換算量で0.1〜12000重量部、好ましくは1〜1200重量部、柴胡が原生薬換算量で0.2〜40000重量部、好ましくは2〜4000重量部である。   The compounding amount of the crude drug is 1 to 20000 parts by weight, preferably 10 to 2000 parts by weight in terms of the bulk drug, and 10 to 2000 parts by weight in terms of the bulk drug, based on 1 part by weight of 10-hydroxy-2-decenoic acid. 0.1 to 10000 parts by weight, preferably 1 to 1000 parts by weight, Cordyceps is 0.1 to 12000 parts by weight in terms of active ingredient, preferably 1 to 1200 parts by weight, and Shiba is 0. 2 to 40,000 parts by weight, preferably 2 to 4000 parts by weight.

配合する生薬は、エキスの形態が好ましい。エキスの製造は通常の方法、例えば、抽出溶媒を用いて、適当な温度(低温又は加熱)にて、生薬原料から抽出する方法などにより行う。抽出溶媒は生薬に応じて適宜選択できるが、好ましくは、水、親水性溶媒(特にエタノール)およびこれらの混合溶媒が用いられる。本発明のエキスとしては、液状抽出物をそのまま使用できるほか、水などで希釈したもの、液状抽出物の濃縮物、液状抽出物の乾固物としても使用できる。すなわち、本発明のエキスは、乾燥エキス、軟エキス、流エキス、チンキなどいずれのものも包含する。   The herbal medicine to be blended is preferably in the form of an extract. The extract is produced by an ordinary method, for example, a method of extracting from a crude drug raw material at an appropriate temperature (low temperature or heating) using an extraction solvent. The extraction solvent can be appropriately selected according to the crude drug, but preferably water, a hydrophilic solvent (especially ethanol) and a mixed solvent thereof are used. As the extract of the present invention, a liquid extract can be used as it is, and it can also be used as a diluted product of water or the like, a concentrate of a liquid extract, or a dried product of a liquid extract. That is, the extract of the present invention includes any of a dry extract, a soft extract, a flow extract, a tincture and the like.

本発明の液剤組成物は、飲料としたときの防腐性、風味等を考慮し、通常pH2〜7、好ましくはpH2.5〜6程度である。   The liquid composition of the present invention is usually about pH 2 to 7, preferably about pH 2.5 to 6, considering antiseptic properties and flavor when used as a beverage.

本発明の液体組成物は、乳糖、ショ糖、果糖、ブドウ糖、ソルビトール、マルチトール、エリスリトール、キシリトール、トレハロース、ステビア抽出物、スクラロース、アセスルファムカリウム等を甘味剤またはエネルギー源として配合することが出来る。   The liquid composition of the present invention can contain lactose, sucrose, fructose, glucose, sorbitol, maltitol, erythritol, xylitol, trehalose, stevia extract, sucralose, acesulfame potassium, etc. as a sweetening agent or energy source.

また、その他の成分として、ビタミン類、ミネラル類、生薬および生薬抽出物、カフェイン、コンドロイチン硫酸ナトリウムなどを本発明の効果を損なわない範囲で配合することが出来る。   As other components, vitamins, minerals, herbal medicines and herbal extracts, caffeine, sodium chondroitin sulfate, and the like can be blended as long as the effects of the present invention are not impaired.

また、必要に応じて他の公知の添加剤、例えば、抗酸化剤、着色剤、香料、矯味剤、保存料、pH調整剤などの製剤技術一般に使用される物質を配合することができ、また、界面活性剤などを溶解補助剤として本発明の効果を損なわない範囲で配合することができる。   In addition, other known additives, for example, antioxidants, coloring agents, flavoring agents, flavoring agents, preservatives, pH adjusting agents, and other substances commonly used in pharmaceutical technology can be blended as necessary. Further, a surfactant or the like can be added as a solubilizing agent within a range not impairing the effects of the present invention.

本発明の液体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させた後、pHを調整し、残りの精製水を加えて全量調整する。   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 with an appropriate amount of purified water, the pH is adjusted, and the remaining purified water is added to adjust the total amount.

本発明の液体組成物は、例えば健康飲料、栄養補給飲料などの各種飲料、ドリンク剤、シロップ剤などの医薬品や医薬部外品の内服液剤に適用できる。   The liquid composition of the present invention can be applied to, for example, various beverages such as health beverages and nutritional supplement beverages, pharmaceuticals such as drinks and syrups, and internal solutions for quasi drugs.

以下実施例および比較例により、本発明を詳細に説明する。   Hereinafter, the present invention will be described in detail by way of examples and comparative examples.

表1の処方に従い常法により、液体組成物を得た。
ただし、10−ヒドロキシ−2−デセン酸は、生ローヤルゼリー200mgに10倍量の精製水を加え、クエン酸NaでpH5.0に調整し、90度で30分加温攪拌後に遠心分離(日立工機製Himac CT5DL、ロータ:RT3S(スイング)、3000rpm×20分)し、上澄み液から得た。
A liquid composition was obtained by a conventional method according to the formulation in Table 1.
However, 10-hydroxy-2-decenoic acid was added to 200 mg of fresh royal jelly with 10 times the amount of purified water, adjusted to pH 5.0 with sodium citrate, heated at 90 degrees for 30 minutes and then centrifuged (Hitachi Machined Himac CT5DL, rotor: RT3S (swing), 3000 rpm × 20 minutes) and obtained from the supernatant.

Figure 2007063144
Figure 2007063144

比較例1及び実施例1から4で得た液体組成物を65℃恒温槽にて1週間保管後、10−ヒドロキシ−2−デセン酸含量を液体クロマトグラフ法により定量した。調製直後の10−ヒドロキシ−2−デセン酸含量に対する65度、7日間後の残存率(%)を表2に示した。その結果、白ジュツ、川キュウ、冬虫夏草、柴胡からなる群より選ばれる1種又は2種以上の生薬を配合することにより、優れた10−ヒドロキシ−2−デセン酸の安定化効果が得られた。   The liquid compositions obtained in Comparative Example 1 and Examples 1 to 4 were stored in a constant temperature bath at 65 ° C. for 1 week, and then the 10-hydroxy-2-decenoic acid content was quantified by liquid chromatography. Table 2 shows the residual rate (%) after 65 days and 7 days with respect to the 10-hydroxy-2-decenoic acid content immediately after preparation. As a result, an excellent 10-hydroxy-2-decenoic acid stabilizing effect can be obtained by blending one or more herbal medicines selected from the group consisting of white jutsu, river cucumber, cordyceps and saiko. It was.

Figure 2007063144
Figure 2007063144

本発明によりポリオキシエチレン基を有する界面活性剤を配合した液体組成物に10−ヒドロキシ−2−デセン酸を安定に配合することが可能になったことから内服液剤等の医薬品や医薬部外品として有用である。
According to the present invention, 10-hydroxy-2-decenoic acid can be stably added to a liquid composition containing a surfactant having a polyoxyethylene group. Useful as.

Claims (3)

白ジュツ、川キュウ、冬虫夏草、柴胡からなる群より選ばれる1種又は2種以上の生薬、10-ヒドロキシ-2-デセン酸、及び、ポリオキシエチレン基を有する界面活性剤を含有する液体組成物。   Liquid composition containing one or more herbal medicines selected from the group consisting of white jutsu, river cucumber, cordyceps sinensis, saiko and 10-hydroxy-2-decenoic acid and a surfactant having a polyoxyethylene group object. ポリオキシエチレン基を有する界面活性剤が、ポリオキシエチレン硬化ヒマシ油である請求項1に記載の液体組成物。   The liquid composition according to claim 1, wherein the surfactant having a polyoxyethylene group is a polyoxyethylene hydrogenated castor oil. ポリオキシエチレン基を有する界面活性剤と10-ヒドロキシ-2-デセン酸を含む液体組成物に、白ジュツ、川キュウ、冬虫夏草、柴胡からなる群より選ばれる1種又は2種以上の生薬を添加することによる10-ヒドロキシ-2-デセン酸の安定化方法。
A liquid composition comprising a surfactant having a polyoxyethylene group and 10-hydroxy-2-decenoic acid, and one or more herbal medicines selected from the group consisting of white jutsu, river cucumber, cordyceps, and shiihou Method for stabilizing 10-hydroxy-2-decenoic acid by adding.
JP2005247332A 2005-08-29 2005-08-29 Liquid composition Expired - Fee Related JP4911278B2 (en)

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH03167113A (en) * 1989-11-24 1991-07-19 Mirubon:Kk Hair regenerating agent
JPH04134032A (en) * 1990-09-25 1992-05-07 Shiga Pref Gov Seiyaku Kk Stable icariin-containing oral solution
JPH0948735A (en) * 1995-08-07 1997-02-18 Kiichi Kubo Production of crude medicine-containing aqueous liquid agent
JPH0959161A (en) * 1995-08-23 1997-03-04 Taisho Pharmaceut Co Ltd Fatigue improving composition
KR20020092082A (en) * 2001-06-02 2002-12-11 김원규 Tonic composition
JP2003231647A (en) * 2002-02-05 2003-08-19 Maruzen Pharmaceut Co Ltd Oral liquid composition

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH03167113A (en) * 1989-11-24 1991-07-19 Mirubon:Kk Hair regenerating agent
JPH04134032A (en) * 1990-09-25 1992-05-07 Shiga Pref Gov Seiyaku Kk Stable icariin-containing oral solution
JPH0948735A (en) * 1995-08-07 1997-02-18 Kiichi Kubo Production of crude medicine-containing aqueous liquid agent
JPH0959161A (en) * 1995-08-23 1997-03-04 Taisho Pharmaceut Co Ltd Fatigue improving composition
KR20020092082A (en) * 2001-06-02 2002-12-11 김원규 Tonic composition
JP2003231647A (en) * 2002-02-05 2003-08-19 Maruzen Pharmaceut Co Ltd Oral liquid composition

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