JP6795316B2 - L−アスパラギン酸またはその塩、及びニコチンアミドを含有する口腔ケア用組成物 - Google Patents
L−アスパラギン酸またはその塩、及びニコチンアミドを含有する口腔ケア用組成物 Download PDFInfo
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- JP6795316B2 JP6795316B2 JP2016053518A JP2016053518A JP6795316B2 JP 6795316 B2 JP6795316 B2 JP 6795316B2 JP 2016053518 A JP2016053518 A JP 2016053518A JP 2016053518 A JP2016053518 A JP 2016053518A JP 6795316 B2 JP6795316 B2 JP 6795316B2
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- Prior art keywords
- oral
- nicotinamide
- salt
- aspartic acid
- sodium
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- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 description 1
- 235000011180 diphosphates Nutrition 0.000 description 1
- ZPWVASYFFYYZEW-UHFFFAOYSA-L dipotassium hydrogen phosphate Chemical compound [K+].[K+].OP([O-])([O-])=O ZPWVASYFFYYZEW-UHFFFAOYSA-L 0.000 description 1
- 229910000396 dipotassium phosphate Inorganic materials 0.000 description 1
- 235000019797 dipotassium phosphate Nutrition 0.000 description 1
- IKALZAKZWHFNIC-JIZZDEOASA-L dipotassium;(2s)-2-aminobutanedioate Chemical compound [K+].[K+].[O-]C(=O)[C@@H](N)CC([O-])=O IKALZAKZWHFNIC-JIZZDEOASA-L 0.000 description 1
- SZXQTJUDPRGNJN-UHFFFAOYSA-N dipropylene glycol Chemical compound OCCCOCCCO SZXQTJUDPRGNJN-UHFFFAOYSA-N 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 235000019414 erythritol Nutrition 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 229940009714 erythritol Drugs 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 229960004756 ethanol Drugs 0.000 description 1
- 235000019441 ethanol Nutrition 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 description 1
- 239000004403 ethyl p-hydroxybenzoate Substances 0.000 description 1
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 description 1
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
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- 150000004673 fluoride salts Chemical class 0.000 description 1
- 239000004088 foaming agent Substances 0.000 description 1
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- 239000008369 fruit flavor Substances 0.000 description 1
- 206010018388 glossodynia Diseases 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 235000012907 honey Nutrition 0.000 description 1
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- 230000006872 improvement Effects 0.000 description 1
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 description 1
- 229960000367 inositol Drugs 0.000 description 1
- 229940113094 isopropylparaben Drugs 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- 239000000845 maltitol Substances 0.000 description 1
- 235000010449 maltitol Nutrition 0.000 description 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
- 229940035436 maltitol Drugs 0.000 description 1
- JCQLYHFGKNRPGE-HFZVAGMNSA-N maltulose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 JCQLYHFGKNRPGE-HFZVAGMNSA-N 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 239000001525 mentha piperita l. herb oil Substances 0.000 description 1
- 229940080927 menthol 10 mg Drugs 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 229960002216 methylparaben Drugs 0.000 description 1
- 210000000258 minor salivary gland Anatomy 0.000 description 1
- 229910000402 monopotassium phosphate Inorganic materials 0.000 description 1
- 235000019796 monopotassium phosphate Nutrition 0.000 description 1
- 235000019799 monosodium phosphate Nutrition 0.000 description 1
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 1
- 208000030194 mouth disease Diseases 0.000 description 1
- 229960003512 nicotinic acid Drugs 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 229940041672 oral gel Drugs 0.000 description 1
- 229940095353 oral granules Drugs 0.000 description 1
- 229940041667 oral paste Drugs 0.000 description 1
- 210000003681 parotid gland Anatomy 0.000 description 1
- 235000015927 pasta Nutrition 0.000 description 1
- 235000019477 peppermint oil Nutrition 0.000 description 1
- 208000028169 periodontal disease Diseases 0.000 description 1
- 229960005323 phenoxyethanol Drugs 0.000 description 1
- PJNZPQUBCPKICU-UHFFFAOYSA-N phosphoric acid;potassium Chemical compound [K].OP(O)(O)=O PJNZPQUBCPKICU-UHFFFAOYSA-N 0.000 description 1
- RNAICSBVACLLGM-GNAZCLTHSA-N pilocarpine hydrochloride Chemical compound Cl.C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C RNAICSBVACLLGM-GNAZCLTHSA-N 0.000 description 1
- 229960002139 pilocarpine hydrochloride Drugs 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- YHLBDCUXFZRLFT-UHFFFAOYSA-N propane-1,1-diol;propane-1,3-diol Chemical compound CCC(O)O.OCCCO YHLBDCUXFZRLFT-UHFFFAOYSA-N 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- MUPFEKGTMRGPLJ-ZQSKZDJDSA-N raffinose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO[C@@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O2)O)O1 MUPFEKGTMRGPLJ-ZQSKZDJDSA-N 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 208000026451 salivation Diseases 0.000 description 1
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 235000002639 sodium chloride Nutrition 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 229940010747 sodium hyaluronate Drugs 0.000 description 1
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
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- 230000004936 stimulating effect Effects 0.000 description 1
- 230000035882 stress Effects 0.000 description 1
- 210000003670 sublingual gland Anatomy 0.000 description 1
- 210000001913 submandibular gland Anatomy 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 235000019669 taste disorders Nutrition 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- CCXAYLQLOLXXKE-DWJAGBRCSA-K trisodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4s,5s,6s)-2-[[(3s,4ar,6ar,6bs,8as,11s,12ar,14ar,14bs)-11-carboxylato-4,4,6a,6b,8a,11,14b-heptamethyl-14-oxo-2,3,4a,5,6,7,8,9,10,12,12a,14a-dodecahydro-1h-picen-3-yl]oxy]-6-carboxylato-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-t Chemical compound [Na+].[Na+].[Na+].O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C([O-])=O)C([O-])=O)[C@@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O CCXAYLQLOLXXKE-DWJAGBRCSA-K 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Cosmetics (AREA)
Description
(1)L−アスパラギン酸またはその塩、及びニコチンアミドを含有する口腔ケア用組成物。
(2)L−アスパラギン酸またはその塩が、L−アスパラギン酸ナトリウムである(1)に記載の組成物。
(3)口腔ケアが、口腔内湿潤または/及び口腔内洗浄である(1)または(2)に記載の組成物。
(4)L−アスパラギン酸またはその塩、及びニコチンアミドを含有する口腔ケア用組成物。
(5)更に、L−メントールを含有する(4)に記載の組成物。
(6)L−アスパラギン酸またはその塩が、L−アスパラギン酸ナトリウムである(4)または(5)に記載の組成物。
(7)口腔ケアが、口腔内湿潤または/及び口腔内洗浄である(4)乃至(6)のいずれか1に記載の組成物。
(1)被験物質
ニコチンアミドは東京化成工業社製、L−アスパラギン酸ナトリウムはペプチド研究所製を使用した。
Slc:Wistar雄ラット[日本エスエルシー(株)]6週齢を購入し、検疫・馴化を行った。
検疫・馴化期間(6日間)を終了したラットをウレタン及びα−クロラロースを腹腔内投与し麻酔を行い、気道確保のために気管カニューレを実施し、投与液の胃内流入を防ぐため、食道を縫合糸で結紮した。
次に、ニコチンアミド、L−アスパラギン酸ナトリウム、またはニコチンアミドとL−アスパラギン酸ナトリウムの1:1の混合物を媒体(4%カルボキシメチルセルロースナトリウム水溶液:CMC水溶液と称す)を用いて160mg/mLに調製した被験物質投与液をマイクロピペットで口腔内に100μL投与した。また、対照として、媒体(4%CMC水溶液)を口腔内に100μL投与した。
媒体または被験物質投与10分後に、風袋重量測定済みの綿球を用いて、口腔内の媒体または投与液を拭い取った。拭き取り後の重量から風袋と媒体または被験物質投与液の重量を差し引いて、投与中の唾液分泌量を概算した。
口腔内の媒体または投与液を拭い取った直後に、口腔内に風袋重量測定済みの綿球を入れた。いずれの群についても、10分ごとに綿球を交換し、交換後の重量との差し引きで唾液分泌量を測定した。測定は30分後まで実施した。
各被験物質及び対照(媒体)投与後30分の総唾液分泌量の測定結果(いずれもn=4)を、それぞれ表1及び図1に示す。
図及び表より、ニコチンアミドとL−アスパラギン酸ナトリウムを併用することで優れた唾液分泌促進作用が発現するという意外な結果が得られた。
(1)被験物質
ニコチンアミドは東京化成工業社製、L−アスパラギン酸ナトリウムはペプチド研究所製、L−メントールは鈴木薄荷社製を使用した。
Slc:Wistar雄ラット[日本エスエルシー(株)]6週齢を購入し、検疫・馴化を行った。
検疫・馴化期間(6日間)を終了したラットをウレタン及びα−クロラロースを腹腔内投与し麻酔を行い、気道確保のために気管カニューレを実施し、投与液の胃内流入を防ぐため、食道を縫合糸で結紮した。 次に、媒体(4%CMC水溶液)を用いて、ニコチンアミド75mg/mL及びL−アスパラギン酸ナトリウム75mg/mLの混合物、ニコチンアミド75mg/mL、L−アスパラギン酸ナトリウム75mg/mLとL−メントール10mg/mLの混合物をそれぞれ調製して被験物質投与液とし、マイクロピペットで口腔内に100μL投与した。また、対照として、媒体(4%CMC水溶液)を口腔内に100μL投与した。
媒体または被験物質投与10分後に、風袋重量測定済みの綿球を用いて、口腔内の媒体または投与液を拭い取った。拭き取り後の重量から風袋と媒体または被験物質投与液の重量を差し引いて、投与中の唾液分泌量を概算した。
口腔内の媒体または投与液を拭い取った直後に、口腔内に風袋重量測定済みの綿球を入れた。いずれの群についても、10分ごとに綿球を交換し、交換後の重量との差し引きで唾液分泌量を測定した。
各被験物質及び対照(媒体)投与後30分の総唾液分泌量の測定結果(いずれもn=4)を、それぞれ表2及び図2に示す。
図及び表より、ニコチンアミドとL−アスパラギン酸ナトリウムにL−メントールを併用することでさらに優れた唾液分泌促進作用が発現するという意外な結果が得られた。
表3の成分及び分量をとり、常法に従って練歯磨を製造する。
表4の成分及び分量をとり、常法に従って液体歯磨を製造する。
表5の成分及び分量をとり、常法に従って洗口液を製造する。
表6の成分及び分量をとり、常法に従って口腔内用軟膏を製造する。
表7の上記成分及び分量をとり、日局製剤総則「ガム剤」の項に準じてガム剤を製造する。
表8の成分及び分量をとり、日局製剤総則「トローチ剤」の項に準じてトローチ剤を製造する。
表9の成分及び分量をとり、日局製剤総則「口腔用スプレー剤」の項に準じて口腔内用スプレー剤を製造する。
表10の成分及び分量をとり、日局製剤総則「口腔用錠剤」の項に準じて口腔内用錠剤を製造する。
表11の成分及び分量をとり、日局製剤総則「舌下錠」の項に準じて口腔内用錠剤を製造する。
表12の成分及び分量をとり、日局製剤総則「バッカル錠」の項に準じて口腔内用錠剤を製造する。
表13の成分及び分量をとり、日局製剤総則「付着錠」の項に準じて口腔内用錠剤を製造する。
Claims (4)
- L−アスパラギン酸またはその塩、及びニコチンアミドを含有する唾液分泌促進するための口腔ケア用医薬組成物(医薬部外品を含む)。
- 更に、L−メントールを含有する請求項1に記載の医薬組成物(医薬部外品を含む)。
- L−アスパラギン酸またはその塩が、L−アスパラギン酸ナトリウムである請求項1または2に記載の医薬組成物(医薬部外品を含む)。
- 口腔ケアが、口腔内湿潤または/及び口腔内洗浄である請求項1乃至3のいずれか1項に記載の医薬組成物(医薬部外品を含む)。
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DE3532860C1 (de) * | 1985-09-14 | 1987-03-12 | Blendax Werke Schneider Co | Mittel zur oralen Hygiene |
JPH089531B2 (ja) * | 1987-07-28 | 1996-01-31 | 株式会社資生堂 | 口腔用組成物 |
JPH10298048A (ja) * | 1997-04-30 | 1998-11-10 | Lion Corp | 歯周病細菌内毒素中和剤、歯周病原因菌付着抑制剤及び口腔用組成物 |
JP2004244404A (ja) * | 2002-12-19 | 2004-09-02 | Lion Corp | 練歯磨組成物 |
EP1682641B1 (en) * | 2003-11-04 | 2007-06-27 | Firmenich Sa | Flavor ingredients for cooling preparations |
US20110014136A1 (en) * | 2008-02-08 | 2011-01-20 | Colgate-Palmolive Company | Oral care product and methods of use and manufacture thereof |
JP5467800B2 (ja) * | 2009-05-14 | 2014-04-09 | ロート製薬株式会社 | 唾液分泌促進剤及び唾液分泌促進用組成物 |
JP2014139163A (ja) * | 2012-12-19 | 2014-07-31 | Daiichi Sankyo Healthcare Co Ltd | 体液分泌促進剤 |
JP2015096473A (ja) * | 2013-11-15 | 2015-05-21 | 第一三共ヘルスケア株式会社 | 唾液分泌促進剤及びそれを含有する口腔用組成物 |
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