JPH02262510A - Dentifrice composition - Google Patents
Dentifrice compositionInfo
- Publication number
- JPH02262510A JPH02262510A JP1261050A JP26105089A JPH02262510A JP H02262510 A JPH02262510 A JP H02262510A JP 1261050 A JP1261050 A JP 1261050A JP 26105089 A JP26105089 A JP 26105089A JP H02262510 A JPH02262510 A JP H02262510A
- Authority
- JP
- Japan
- Prior art keywords
- dried
- activity
- extract
- pericarp
- hederagenin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 23
- 239000000551 dentifrice Substances 0.000 title abstract 4
- NTWLPZMPTFQYQI-UHFFFAOYSA-N (3alpha)-olean-12-ene-3,23-diol Natural products C1CC(O)C(C)(CO)C2CCC3(C)C4(C)CCC5(C)CCC(C)(C)CC5C4=CCC3C21C NTWLPZMPTFQYQI-UHFFFAOYSA-N 0.000 claims abstract description 18
- GCGBHJLBFAPRDB-UHFFFAOYSA-N Hederagenin Natural products CC1(C)CCC2(CCC3(C)C4CCC5C(C)(CO)C(O)CCC5(C)C4CC=C3C2C1)C(=O)O GCGBHJLBFAPRDB-UHFFFAOYSA-N 0.000 claims abstract description 18
- GCGBHJLBFAPRDB-KCVAUKQGSA-N Scutellaric acid Natural products CC1(C)CC[C@@]2(CC[C@@]3(C)[C@@H]4CC[C@H]5[C@@](C)(CO)[C@H](O)CC[C@]5(C)[C@H]4CC=C3[C@@H]2C1)C(=O)O GCGBHJLBFAPRDB-KCVAUKQGSA-N 0.000 claims abstract description 18
- PGOYMURMZNDHNS-MYPRUECHSA-N hederagenin Chemical compound C1C[C@H](O)[C@@](C)(CO)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CCC(C)(C)C[C@H]5C4=CC[C@@H]3[C@]21C PGOYMURMZNDHNS-MYPRUECHSA-N 0.000 claims abstract description 18
- 241000580938 Sapindus Species 0.000 claims abstract description 9
- 240000008027 Akebia quinata Species 0.000 claims abstract description 7
- 229940034610 toothpaste Drugs 0.000 claims description 17
- 239000000606 toothpaste Substances 0.000 claims description 17
- 241000196324 Embryophyta Species 0.000 claims description 7
- 239000004615 ingredient Substances 0.000 claims description 7
- 241000722953 Akebia Species 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract description 19
- 230000000694 effects Effects 0.000 abstract description 18
- 230000003110 anti-inflammatory effect Effects 0.000 abstract description 9
- 235000007756 Akebia quinata Nutrition 0.000 abstract description 6
- 101710081722 Antitrypsin Proteins 0.000 abstract description 6
- 230000001475 anti-trypsic effect Effects 0.000 abstract description 6
- 239000002753 trypsin inhibitor Substances 0.000 abstract description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 6
- 206010061218 Inflammation Diseases 0.000 abstract description 5
- 238000010438 heat treatment Methods 0.000 abstract description 5
- 201000001245 periodontitis Diseases 0.000 abstract description 5
- 239000002904 solvent Substances 0.000 abstract description 5
- 230000000288 anti-kallikrein effect Effects 0.000 abstract description 4
- 239000000706 filtrate Substances 0.000 abstract description 4
- 230000004054 inflammatory process Effects 0.000 abstract description 4
- 239000000843 powder Substances 0.000 abstract description 4
- 244000025254 Cannabis sativa Species 0.000 abstract 3
- 239000002674 ointment Substances 0.000 abstract 2
- 238000001914 filtration Methods 0.000 abstract 1
- 239000000463 material Substances 0.000 abstract 1
- 239000012254 powdered material Substances 0.000 abstract 1
- 235000019441 ethanol Nutrition 0.000 description 11
- 238000000605 extraction Methods 0.000 description 9
- 229940012957 plasmin Drugs 0.000 description 6
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- 102000009123 Fibrin Human genes 0.000 description 4
- 108010073385 Fibrin Proteins 0.000 description 4
- BWGVNKXGVNDBDI-UHFFFAOYSA-N Fibrin monomer Chemical compound CNC(=O)CNC(=O)CN BWGVNKXGVNDBDI-UHFFFAOYSA-N 0.000 description 4
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 4
- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 description 4
- 229950003499 fibrin Drugs 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- 239000003205 fragrance Substances 0.000 description 3
- 230000007062 hydrolysis Effects 0.000 description 3
- 238000006460 hydrolysis reaction Methods 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 238000000746 purification Methods 0.000 description 3
- NWUYHJFMYQTDRP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;1-ethenyl-2-ethylbenzene;styrene Chemical compound C=CC1=CC=CC=C1.CCC1=CC=CC=C1C=C.C=CC1=CC=CC=C1C=C NWUYHJFMYQTDRP-UHFFFAOYSA-N 0.000 description 2
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 2
- 239000004378 Glycyrrhizin Substances 0.000 description 2
- 241001602876 Nata Species 0.000 description 2
- 241001093760 Sapindaceae Species 0.000 description 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 2
- 150000001298 alcohols Chemical class 0.000 description 2
- 229960000458 allantoin Drugs 0.000 description 2
- TUFYVOCKVJOUIR-UHFFFAOYSA-N alpha-Thujaplicin Natural products CC(C)C=1C=CC=CC(=O)C=1O TUFYVOCKVJOUIR-UHFFFAOYSA-N 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 description 2
- 229960004949 glycyrrhizic acid Drugs 0.000 description 2
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 description 2
- 235000019410 glycyrrhizin Nutrition 0.000 description 2
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 description 2
- 239000003456 ion exchange resin Substances 0.000 description 2
- 229920003303 ion-exchange polymer Polymers 0.000 description 2
- 238000000691 measurement method Methods 0.000 description 2
- NROKBHXJSPEDAR-UHFFFAOYSA-M potassium fluoride Chemical compound [F-].[K+] NROKBHXJSPEDAR-UHFFFAOYSA-M 0.000 description 2
- 239000002994 raw material Substances 0.000 description 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 2
- 241000894007 species Species 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 229930007845 β-thujaplicin Natural products 0.000 description 2
- 229920000936 Agarose Polymers 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108010049003 Fibrinogen Proteins 0.000 description 1
- 102000008946 Fibrinogen Human genes 0.000 description 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
- 102100038124 Plasminogen Human genes 0.000 description 1
- 108010051456 Plasminogen Proteins 0.000 description 1
- 241000580955 Sapindus mukorossi Species 0.000 description 1
- 102100032491 Serine protease 1 Human genes 0.000 description 1
- 101710151387 Serine protease 1 Proteins 0.000 description 1
- 239000004902 Softening Agent Substances 0.000 description 1
- 108090000190 Thrombin Proteins 0.000 description 1
- 101710119665 Trypsin-1 Proteins 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 239000003792 electrolyte Substances 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 1
- 229940012952 fibrinogen Drugs 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 238000002372 labelling Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- 238000010899 nucleation Methods 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 239000011698 potassium fluoride Substances 0.000 description 1
- 235000003270 potassium fluoride Nutrition 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 239000000344 soap Substances 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- -1 softeners Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 229960004072 thrombin Drugs 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Cosmetics (AREA)
Abstract
Description
【発明の詳細な説明】
（産業上の利用分野）
この発明は歯ミガキ組成物に係り、その目的は歯周炎な
どの歯ぐきの炎症等を防止する抗炎症効果に優れた歯ミ
ガキ組成物の提供にある。Detailed Description of the Invention (Industrial Application Field) The present invention relates to a toothpaste composition, and its purpose is to provide a toothpaste composition with excellent anti-inflammatory effects to prevent gum inflammation such as periodontitis. On offer.
（従来技術及びその問題点）
歯ミガキ組成物の一形態としての歯ミガキは歯周炎など
の歯ぐきの炎症を防止する抗炎症、あるいは細菌発育阻
害などの殺菌の効果を奏する成分が内包され、歯周炎用
歯ミガキとされることが多い。(Prior art and its problems) Toothpaste, which is one form of toothpaste composition, contains ingredients that have anti-inflammatory effects to prevent gum inflammation such as periodontitis, or have sterilizing effects such as inhibiting bacterial growth. It is often used as a toothpaste for periodontitis.
従来より このような抗炎症などの効果を奏するものと
してはグリチルリチン、アラントイン、ヒノキチオール
などの成分が配合されている。Conventionally, ingredients such as glycyrrhizin, allantoin, and hinokitiol have been blended as ingredients that have such anti-inflammatory effects.
しかし、これらグリチルリチン、アラントイン、ヒノキ
チオールなどの抗炎症剤の抗炎症効果は不′充分なもの
であり、上記問題を解決するには至っていない。However, the anti-inflammatory effects of these anti-inflammatory agents such as glycyrrhizin, allantoin, and hinokitiol are insufficient, and the above-mentioned problems have not yet been solved.
（発明の解決課題）
上記問題に鑑み、業界では、歯周炎などの歯ぐきの炎症
等を防止する抗炎症効果に優れた歯ミガキ組成物の創出
が望まれている。(Problems to be Solved by the Invention) In view of the above-mentioned problems, there is a desire in the industry to create a toothpaste composition with excellent anti-inflammatory effects to prevent gum inflammation such as periodontitis.
（発明の解決手段）
即ち、この発明はムクロジ（Ｓａｐｉｎｄｕｓ ｍｕｋ
ｕｒｏｓｓｉ Ｇａｅｒｔｎ）の果皮及び／又はアケビ
（Ａｋｅｂｉａ ｑｕｉｎａｔａ Ｄｅｃｎｅ）の全草
から抽出されたヘデラゲニン（式■）を含む抽出物を必
須成分としてなる歯ミガキ組成物。(Solution Means of the Invention) That is, the present invention solves the problem of Sapindus mukuroji.
A toothpaste composition comprising, as an essential component, an extract containing hederagenin (formula 2) extracted from the pericarp of Akebia quinata Decne and/or the whole plant of Akebia quinata Decne.
（式１）
が抗プラスミン活性、抗力リクレン活性、抗トリプシン
活性に優れ、つまり抗炎症効果に優れていることを見出
し、この発明の完成に至った。It was discovered that (Formula 1) has excellent anti-plasmin activity, anti-recreation activity, and anti-trypsin activity, that is, it has excellent anti-inflammatory effects, leading to the completion of this invention.
（発明の構成）
この発明で使用するムクロジ（Ｓａｐｉｎｄｕｓ ｍｕ
ｋｕｒ。(Structure of the Invention) Sapindus mukuro used in this invention
kur.
ｓｓｉ Ｇａｅｒｔｎ）とは、ムクロジ科、ムクロジ属
に分類される落葉喬木でその果実の果皮を主としてこの
発明には好適に使用する。ssi Gaertn) is a deciduous tree classified into the family Sapindaceae and the genus Sapindica, and the pericarp of its fruit is preferably used mainly in the present invention.
尚、この発明においてはムクロジ科、ムクロジ属のムク
ロジ（Ｓａｐｉｎｄｕｓ ｍｕｋｕｒｏｓｓｉ Ｇａｅ
ｒｔｎ）およびその近縁種、亜種の果皮の使用も可能で
ある。In addition, in this invention, Sapindus mukurossi (Sapindus mukurossi Gae) belonging to the family Sapindaceae and the genus Sapindus
rtn) and its related species and subspecies can also be used.
因にこのムクロジの種子は従来正月の羽根つきの玉に使
用されているもので、果皮は石鹸の代用等としてのみ使
用されていたことがある。Incidentally, the seeds of this Sapindica tree have traditionally been used to make feathered balls for the New Year, and the peel has only been used as a substitute for soap.
また、この発明で使用するアケビ（Ａｋｅｂｉａ ｑｕ
ｉｎａｔａ Ｄｅｃｎｅ）はアケビ科アケビ属に分類さ
れる植物であって、その茎、根、葉、種子などの全草が
この発明に係る歯ミガキ組成物の必須配合成分の原料と
して好適に使用することができる。In addition, Akebia qu used in this invention.
inata Decne) is a plant classified into the family Akebiaceae, and the whole plant including stems, roots, leaves, and seeds can be suitably used as a raw material for the essential ingredients of the toothpaste composition according to the present invention. I can do it.
因にこの発明においてはアケビ（Ａｋｅｂｉａ ｑｕｉ
ｎａｔａ Ｄｅｃｎｅ）の同属植物、ミツバアケビ（Ａ
ｋｅｂｉａ ｑｕｉｎａｔａ Ｄｅｃｎｅ）、ゴヨウア
ケビ（Ａｋｅｂｉａ ｐｅｎｔａｐｈｙｌｌａＭａｋｉ
ｎｏ）等の近縁種、亜種なとの茎、葉、種子等も好適に
使用することができる。Incidentally, in this invention, Akebia qui
Akebi (A. nata Decne)
kebia quinata Decne), Akebia pentaphyllaMaki
Stems, leaves, seeds, etc. of closely related species and subspecies such as No. 1 can also be suitably used.
この発明においては、このような原料植物を利用してこ
の発明の必須成分とするヘデラゲニンを含む抽出物を調
製する。In this invention, such a raw material plant is used to prepare an extract containing hederagenin, which is an essential component of this invention.
この発明において、ヘデラゲニン（式■）を含む抽出物
とはへデラゲニンを１００％含む抽出物である必要はな
く、少なくとも天然存在率である１〜２％より目的意識
的にエキス中の配合率か増大している抽出物であればよ
い。In this invention, the extract containing hederagenin (formula ■) does not necessarily have to be an extract containing 100% hederagenin, but it is intended to intentionally increase the blending ratio in the extract from at least the natural abundance of 1 to 2%. Any extract that has been expanded is sufficient.
このようなヘデラゲニンを調製する方法としては、出発
植物を生のまま、乾燥物或いは乾燥粉砕物を使用し、含
水アルコール（エチルアルコール、エタノール、イソプ
ロピルアルコール）あるいは水を溶媒として加熱抽出す
る。As a method for preparing such hederagenin, a starting plant is used in its raw state, dried, or dried and pulverized, and heated and extracted using hydrous alcohol (ethyl alcohol, ethanol, isopropyl alcohol) or water as a solvent.
この加熱抽出としては、含水アルコールの濃度によって
も異なるが、通常は含水アルコールの濃度を５０乃至８
０％とした場合には、６０℃で３時間程度抽出すればよ
い。This heating extraction differs depending on the concentration of hydrous alcohol, but usually the concentration of hydrous alcohol is 50 to 8.
When the content is 0%, extraction may be performed at 60°C for about 3 hours.
尚、抽出溶媒は含水アルコ−、ルに限定されることはな
く、水もしくは水を含まないアルコールを用いてもよい
。The extraction solvent is not limited to hydrous alcohols, and water or water-free alcohols may also be used.
また、加熱抽出条件としては、前記条件以外に常温で抽
出してもよく、その場合には一昼夜程度処理するのが望
ましい。Further, as the heating extraction conditions, extraction at room temperature may be performed in addition to the above-mentioned conditions, and in that case, it is preferable to perform the treatment for about one day and night.
このように抽出処理して、抽出液を濾別する。After the extraction process is carried out in this manner, the extract is filtered.
この濾液の段階でもこの発明の必須成分として使用でき
る。This filtrate stage can also be used as an essential component of this invention.
次いで、この濾液を６０℃以下の温度で加温しながら減
圧濃縮し、°約１７５０程度に濃縮して、軟エキスを調
製する。Next, this filtrate is concentrated under reduced pressure while heating at a temperature of 60° C. or lower to about 1750° C. to prepare a soft extract.
得られた軟エキスを５％前後の鉱酸（ＨＣＩ、Ｈ２ＳＯ
。The obtained soft extract was mixed with around 5% mineral acid (HCI, H2SO
.
ＨＮＯｓ）を、濾液の容積にして１０〜２０倍量加え、
加熱して加水分解を行い、加水分解後アルカリで中和し
、その後減圧濃縮し、その残査を得る。HNOs) was added in an amount 10 to 20 times the volume of the filtrate,
Hydrolysis is carried out by heating, and after the hydrolysis, it is neutralized with an alkali, and then concentrated under reduced pressure to obtain the residue.
この残査を再度含水アルコールに溶解した後、イオン交
換樹脂を通して精製し、この発明の必須成分とするヘデ
ラゲニンを得ることができる。This residue is redissolved in hydrous alcohol and purified through an ion exchange resin to obtain hederagenin, which is an essential component of the present invention.
このようにして得たヘデラゲニンは乾燥粉末状で或いは
、軟エキス状で歯ミガキ組成物に配合すればよい。The hederagenin thus obtained may be incorporated into a toothpaste composition in the form of a dry powder or a soft extract.
この発明において歯ミガキ組成物とするには、例えば他
の常用成分、柔軟剤、溶剤、油指、香料、抗軟化剤を適
宜調合してもよく、またこのヘデラゲニンは歯ミガキ組
成物に配合する際には、少なくとも乾燥物に換算して、
５０ｍｇ〜５０００ｍｇ程度となるように配合すればよ
い。In order to obtain a toothpaste composition in the present invention, for example, other commonly used ingredients, softeners, solvents, oils, fragrances, and anti-softening agents may be appropriately added, and this hederagenin is also incorporated into the toothpaste composition. In some cases, at least in terms of dry matter,
What is necessary is just to mix|blend so that it may become about 50 mg - 5000 mg.
以下この発明の処方例を記載する。Prescription examples of this invention will be described below.
処方例１ 練り歯磨
炭酸カルシウム ３９．０％ソル
ビット ２２．０カルボキ
シメチルセルロースナトリウム１．１ラウリル硫酸ナト
リウム １．３サツカリン
０．１香 料
１．０抽 出 物
１．０パラオキシ
安息香酸エチル ０．０１水
残部処方例２ 粉歯磨
炭酸カルシウム ７５．０％グリ
でリン 】０．０抽
出 物 ２
．０香 料
１．０パラオキシ安息香酸エチル
０．０５ラウリル硫酸ナトリウム １．
３サツカリン ０．１水
残部次にこの発明の実
施例及び試験例を記載することにより、この発明の効果
をより一層明確なものとする。Formulation example 1 Toothpaste calcium carbonate 39.0% Sorbitol 22.0 Sodium carboxymethyl cellulose 1.1 Sodium lauryl sulfate 1.3 Saccharin
0.1 fragrance
1.0 extract
1.0 Ethyl paraoxybenzoate 0.01 Water
Remaining formulation example 2 Powdered toothpaste calcium carbonate 75.0% phosphorus] 0.0 extraction
Exhibit 2
．． 0 fragrance
1.0 Ethyl paraoxybenzoate
0.05 Sodium lauryl sulfate 1.
3 Satukarin 0.1 Water
The effects of the present invention will be made clearer by describing Examples and Test Examples of the present invention.
実施例１
ムクロジ（Ｓａｐｔｎｄｕｓ ｍｕｋｕｒｏｓｓｉ Ｇ
ａｅｒｔｎ）の乾燥粉砕果皮１ｋｇを５０％含水アルコ
ール１０Ｉ！で６０℃、３ｈｒ加熱抽出し、抽出液を６
０℃以下で５０分の１の容量に減圧濃縮して軟エキスを
得た。Example 1 Saptundus mukurossi G
aertn) 1 kg of dried and crushed peel of 50% hydroalcohol 10 I! Heat extraction at 60℃ for 3 hours, and extract the extract at 60℃ for 3 hours.
A soft extract was obtained by concentrating under reduced pressure at 0°C or lower to 1/50th the volume.
この軟エキスに、１０倍量の５％ＨＣＩを加え、加水分
解した。To this soft extract, 10 times the amount of 5% HCI was added and hydrolyzed.
加水分解後、５％ＮａＯＨで残存ＨＣＩを中和点まで中
和した。After hydrolysis, residual HCI was neutralized with 5% NaOH to the neutralization point.
得られた反応液を１１５０容量に減圧濃縮し、その残部
に５０％含水エタノールを１０倍量加え、エタノール可
溶分イオン交換樹脂を充填し、カラム内に通液して精製
して、白色粉末１８ｇを得た。（実施例１のＡ）
尚、精製前のエキスを実施例１のＢとした。The resulting reaction solution was concentrated under reduced pressure to 1150 volumes, 10 times the volume of 50% aqueous ethanol was added to the remaining volume, the ethanol-soluble portion was filled with ion exchange resin, and the liquid was passed through a column for purification to obtain a white powder. 18g was obtained. (A in Example 1) The extract before purification was designated as B in Example 1.
（分析方法）
得られた粉末０．１〜０．５ｇを精秤し、３ｍｌのバイ
アルビンに入れ、１％のＰ−ブロム・ツェナシールブロ
マイド（液体クロマト用カルボン酸ラベル化剤）アセト
ニトリル電液１ｍｌを加え、更に少量のフッ化カリ、１
８−クラウン−６・−エーテルを添加（、た。(Analysis method) Precisely weigh 0.1 to 0.5 g of the obtained powder, put it in a 3 ml vial, and add 1% P-brom zenacyl bromide (carboxylic acid labeling agent for liquid chromatography) acetonitrile electrolyte. Add 1 ml, then add a small amount of potassium fluoride, 1
8-crown-6-ether was added.
この状態でｅＯｏＣに加熱し、ｌｈｒ反応させヘデラゲ
ニンのフェナンールエステルを調製し、次の条件で高速
液体クロマト法により分析した。In this state, it was heated to eOoC and subjected to lhr reaction to prepare phenanyl ester of hederagenin, and analyzed by high performance liquid chromatography under the following conditions.
カラム： Ｄｉａｓｉｌ ５−Ｃ１８
移動溶媒：水ニアセトニトリル グラジェント溶出
検 出 ：ＵＶ２５４ｎｍ
流 速： １ ｍ ｌ ／ｍｉｎ
カラム温度：４０℃
実施例１のＡの純度は９８％、実施例１のＢの純度は６
０％であった。Column: Diasil 5-C18 Mobile solvent: Water Niacetonitrile Gradient elution detection: UV254nm Flow rate: 1 ml/min Column temperature: 40°C Purity of A in Example 1 is 98%, purity of B in Example 1 is 6
It was 0%.
実施例２
ムクロジの果皮の代りにアケビＣＡｋｅｂｉａ ｑｕｉ
ｎａｔａ Ｄｅｃｎｅ）の茎、種子の乾燥粉砕物１．５
ｋｇを使用した以外は実施例１と全く同様の抽出操作、
分析をしてヘデラゲニン２０ｇを得た。（実施例２のＡ
）尚、実施例２のＢとしてカラム精製前のエキスを別途
調製した。Example 2 Akebia qui in place of the peel of Sapindium
Dry and crushed stems and seeds of Nata Decne 1.5
The extraction operation was exactly the same as in Example 1 except that kg was used.
After analysis, 20 g of hederagenin was obtained. (A of Example 2
) Note that as B in Example 2, an extract before column purification was separately prepared.
実施例２のＡの純度は９７％、実施例２のＢの純度は７
０％であった。The purity of A in Example 2 is 97%, and the purity of B in Example 2 is 7.
It was 0%.
試験例１ （抗ブラミン活
性、抗力リクレン活性、抗トリプシン活性試験）
実施例で得たヘデラゲニン及びヘデラゲニンを含むエキ
スの抗プラスミン活性、抗力リクレン活性、抗トリプシ
ン活性を調べた。Test Example 1 (Anti-bramin activity, anti-recreane activity, anti-trypsin activity test) The anti-plasmin activity, anti-recreane activity, and anti-trypsin activity of the hederagenin and hederagenin-containing extract obtained in the example were investigated.
指標物質として小野薬品（掬製ガベキセトメシレイト（
薬品）（比較例）のそれぞれの活性とブランクとの差を
１００として実施例で得た各物質の活性度を調べた。As an indicator substance, Ono Pharmaceutical Co., Ltd. (Kiki Sei Setomesylate)
The activity of each substance obtained in the example was investigated by setting the difference between the activity of each drug (comparative example) and the blank as 100.
抗プラスミン、抗カリクレン、抗トリプレシンはいずれ
も抗炎症に寄与する機能である。Anti-plasmin, anti-kallikrein, and anti-trypressin all have functions that contribute to anti-inflammation.
〈抗プラスミン測定方法〉
フィブリン平板法
１％アガロース溶液にフィブリノーゲン（プラスミノー
ゲン除去） ０．４ｇ／１００ｍ Ｉ！ （１００ｕｎ
ｉｔ ／ｍＩ！、）の比率で加え、４０’Ｃ前後で溶か
す。<Anti-plasmin measurement method> Fibrin plate method Fibrinogen (plasminogen removed) in 1% agarose solution 0.4g/100m I! (100un
it/mI! , ) and melt at around 40'C.
この溶液１０ｍ１をシャーレに分生後、トロンビン（ｌ
ｏｏｕｎｉｔ ／ｍ ｌ ） ０．１ｍ Ｒを加え、
よく撹拌しフィブリン平板を作成した。After seeding 10 ml of this solution in a petri dish, thrombin (l
oounit/ml) 0.1m R was added,
The mixture was stirred well and a fibrin plate was prepared.
次に、フィブリン平板に直径７ ｍｍ程度の穴を開け、
プラスミン（１０〜２０ｕｎｉｔ ／ｍβ）とへデラゲ
ニン （２ｍＭ／ Ｄ Ｍ Ｓ （ＮＮ−ジメチハスル
オキザイド）溶液）を同量混合し、そのμｌをフィブリ
ン平板の穴に入れ、３７°Ｃ１１８時間後の溶解面積を
測定し、活性を調べた。Next, a hole with a diameter of about 7 mm was made in the fibrin plate.
Equal amounts of plasmin (10-20 units/mβ) and hederagenin (2mM/DMS (NN-dimethyhasulfoxide) solution) were mixed, μl of the mixture was placed in the hole of a fibrin plate, and the mixture was incubated at 37°C for 118 hours. The dissolution area was measured and the activity was investigated.
（ブランクには、ＤＭＳのみを用いた）〈抗カリクレン
、抗トリプシン測定方法〉合成基質方法
ヘデラゲニン／エタノール（２０ｍＭ）、０．５ｍＡ。(Only DMS was used as a blank) <Anti-kallikrein, anti-trypsin measurement method> Synthetic substrate method Hederagenin/ethanol (20mM), 0.5mA.
ＰＩ（７，４−トリス塩酸バッファー３．８ｍｎ、各酵
素（カリクレン、 ２．５〜５ｕｎｉｔ／ｍβ （ミド
リ十字）、トリプシン１Ｏｕｎｉｔ／１０ ｍｊ７ （
持出製薬））を、０゜５ｍｆの比率で混合し、３７°Ｃ
で５分間インキュベーションを行った。PI (7,4-Tris-HCl buffer 3.8 mn, each enzyme (Kallikrene, 2.5-5 units/mβ (green cross), trypsin 1 unit/10 mj7 (
Mixed pharmaceutical products)) at a ratio of 0°5mf and heated at 37°C.
Incubation was performed for 5 minutes.
次に、合成基質（カリクレン＝ Ｓ −２３０２２５ｍ
ｇ／６．８ｍｆ）、又は（トリプシン−３−２２２２２
５ｍｇ／１７ｍβ）を０．２ｍｊｌ’加え、さらに５分
間インキュベーションを行い、５０％酢酸５ｍｌを加え
反応を止め、４０５ｒ＋ｍの吸光度を測定し、阻害率を
求めた。Next, a synthetic substrate (Kallikrene = S-230225m
g/6.8mf) or (trypsin-3-22222
0.2 mjl' of 5mg/17mβ) was added, the mixture was further incubated for 5 minutes, the reaction was stopped by adding 5ml of 50% acetic acid, and the absorbance at 405r+m was measured to determine the inhibition rate.
（ブランクはエタノールのみを用いた。）結果をまとめ
て第１表に示す。(Only ethanol was used for the blank.) The results are summarized in Table 1.
（発明の効果）
以上詳述した如くこの発明に係る歯ミガキ組成物は、ム
クロジ（ＳａｐｉｎｄｕＳｍｕｋｕｒｏｓｓｉ Ｇａｅ
ｒｔｎ）の果皮及び／又はアケビ（Ａｋｅｂｉａ ｑｕ
ｉｎａｔａ Ｄｅｃｎｅ）の全草から抽出されたヘデラ
ゲニンを含む抽出物を必須成分としてなる歯ミガキ組成
物であるから、前記実施例、試験例の結果から明らかな
如く、この発明の必須配合成分であるヘデラゲニンを含
む物質は抗チロシナーゼ、抗プラスミン、抗カリクレン
、抗トリプシン活性に優れ、つまり抗炎症効果に優れて
いるので、この必須配合成分を配合した歯ミガキ組成物
は優れた抗炎症効果を奏することか判る。(Effects of the Invention) As detailed above, the toothpaste composition according to the present invention can be applied to Sapindu Smukurossi Gae.
rtn) and/or Akebia qu
This toothpaste composition contains an extract containing hederagenin extracted from the whole plant of Inata Decne as an essential component. Substances containing this substance have excellent anti-tyrosinase, anti-plasmin, anti-kallikrein, and anti-trypsin activities, in other words, they have excellent anti-inflammatory effects, so toothpaste compositions containing these essential ingredients can have excellent anti-inflammatory effects. I understand.
Claims (1)
Ｇａｅｒｔｎ）の果皮及び／又はアケビ（Ａｋｅｂｉａ
ｑｕｉｎａｔａＤｅｃｎｅ）の全草から抽出されたヘデ
ラゲニン（式 I ）を含む抽出物を必須成分としてなる
歯ミガキ組成物。 ▲数式、化学式、表等があります▼（式 I ）(1) Sapindus mukurossi
Gaertn pericarp and/or Akebia
A toothpaste composition comprising as an essential ingredient an extract containing hederagenin (formula I) extracted from the whole plant of A. quinata Decne. ▲There are mathematical formulas, chemical formulas, tables, etc.▼ (Formula I)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1261050A JPH02262510A (en) | 1987-08-11 | 1989-10-04 | Dentifrice composition |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP62201177A JPS6442411A (en) | 1987-08-11 | 1987-08-11 | Cosmetic composition |
| JP1261050A JPH02262510A (en) | 1987-08-11 | 1989-10-04 | Dentifrice composition |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP62201177A Division JPS6442411A (en) | 1987-08-11 | 1987-08-11 | Cosmetic composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH02262510A true JPH02262510A (en) | 1990-10-25 |
| JPH0432050B2 JPH0432050B2 (en) | 1992-05-28 |
Family
ID=26512625
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP1261050A Granted JPH02262510A (en) | 1987-08-11 | 1989-10-04 | Dentifrice composition |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH02262510A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002241293A (en) * | 2001-02-13 | 2002-08-28 | Ichimaru Pharcos Co Ltd | Maillard reaction inhibitor |
| WO2004019960A3 (en) * | 2002-08-28 | 2004-05-13 | Lupin Ltd | Herbal extract comprising a mixture of saponins obtained from sapindus trifoliatus for anticonvulsant activity |
| JP2008508263A (en) * | 2004-07-30 | 2008-03-21 | キム、ソンベ | Method for improving antitumor effect of bald radish and composition prepared by the method |
| CN104983612A (en) * | 2015-06-18 | 2015-10-21 | 广州无患子生物科技有限公司 | Plant tooth health care product and preparing method thereof |
-
1989
- 1989-10-04 JP JP1261050A patent/JPH02262510A/en active Granted
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002241293A (en) * | 2001-02-13 | 2002-08-28 | Ichimaru Pharcos Co Ltd | Maillard reaction inhibitor |
| WO2004019960A3 (en) * | 2002-08-28 | 2004-05-13 | Lupin Ltd | Herbal extract comprising a mixture of saponins obtained from sapindus trifoliatus for anticonvulsant activity |
| JP2006501251A (en) * | 2002-08-28 | 2006-01-12 | ルピン・リミテッド | Herbal extract containing a mixture of saponins with anticonvulsant activity obtained from Spindas trifoliatus |
| JP2008508263A (en) * | 2004-07-30 | 2008-03-21 | キム、ソンベ | Method for improving antitumor effect of bald radish and composition prepared by the method |
| CN104983612A (en) * | 2015-06-18 | 2015-10-21 | 广州无患子生物科技有限公司 | Plant tooth health care product and preparing method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0432050B2 (en) | 1992-05-28 |
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