JP2008169168A - Bone density increasing agent - Google Patents
Bone density increasing agent Download PDFInfo
- Publication number
- JP2008169168A JP2008169168A JP2007005396A JP2007005396A JP2008169168A JP 2008169168 A JP2008169168 A JP 2008169168A JP 2007005396 A JP2007005396 A JP 2007005396A JP 2007005396 A JP2007005396 A JP 2007005396A JP 2008169168 A JP2008169168 A JP 2008169168A
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- JP
- Japan
- Prior art keywords
- glucosamine
- bone density
- salt
- increasing agent
- bone
- 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.)
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- 230000037182 bone density Effects 0.000 title claims abstract description 44
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 claims abstract description 33
- MSWZFWKMSRAUBD-UHFFFAOYSA-N beta-D-galactosamine Natural products NC1C(O)OC(CO)C(O)C1O MSWZFWKMSRAUBD-UHFFFAOYSA-N 0.000 claims abstract description 31
- 229960002442 glucosamine Drugs 0.000 claims abstract description 31
- 235000013305 food Nutrition 0.000 claims abstract description 16
- 150000002301 glucosamine derivatives Chemical class 0.000 claims abstract description 15
- 150000003839 salts Chemical class 0.000 claims abstract description 10
- 238000001727 in vivo Methods 0.000 claims abstract description 8
- 239000000203 mixture Substances 0.000 claims description 17
- 239000004480 active ingredient Substances 0.000 claims description 8
- 208000001132 Osteoporosis Diseases 0.000 abstract description 9
- 210000000845 cartilage Anatomy 0.000 abstract description 7
- 230000002265 prevention Effects 0.000 abstract description 4
- 210000000988 bone and bone Anatomy 0.000 abstract description 3
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 208000010392 Bone Fractures Diseases 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 description 10
- 241001465754 Metazoa Species 0.000 description 7
- 235000013402 health food Nutrition 0.000 description 6
- 230000000694 effects Effects 0.000 description 5
- 239000003814 drug Substances 0.000 description 4
- 239000000546 pharmaceutical excipient Substances 0.000 description 4
- 229920002683 Glycosaminoglycan Polymers 0.000 description 3
- 241000282412 Homo Species 0.000 description 3
- 241000699670 Mus sp. Species 0.000 description 3
- OVRNDRQMDRJTHS-UHFFFAOYSA-N N-acelyl-D-glucosamine Natural products CC(=O)NC1C(O)OC(CO)C(O)C1O OVRNDRQMDRJTHS-UHFFFAOYSA-N 0.000 description 3
- OVRNDRQMDRJTHS-FMDGEEDCSA-N N-acetyl-beta-D-glucosamine Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-FMDGEEDCSA-N 0.000 description 3
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- CBOJBBMQJBVCMW-BTVCFUMJSA-N (2r,3r,4s,5r)-2-amino-3,4,5,6-tetrahydroxyhexanal;hydrochloride Chemical compound Cl.O=C[C@H](N)[C@@H](O)[C@H](O)[C@H](O)CO CBOJBBMQJBVCMW-BTVCFUMJSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 2
- LCTONWCANYUPML-UHFFFAOYSA-N Pyruvic acid Chemical compound CC(=O)C(O)=O LCTONWCANYUPML-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
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- 230000037396 body weight Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
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- 230000001054 cortical effect Effects 0.000 description 2
- 239000000284 extract Substances 0.000 description 2
- 230000037406 food intake Effects 0.000 description 2
- 229960001911 glucosamine hydrochloride Drugs 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 description 2
- 235000012054 meals Nutrition 0.000 description 2
- 235000013336 milk Nutrition 0.000 description 2
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- 230000003449 preventive effect Effects 0.000 description 2
- 239000000047 product Substances 0.000 description 2
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- KIUKXJAPPMFGSW-DNGZLQJQSA-N (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-carboxylic acid Chemical compound 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 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 description 1
- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 description 1
- 239000001606 7-[(2S,3R,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-3-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-2-yl]oxy-5-hydroxy-2-(4-hydroxyphenyl)chroman-4-one Substances 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- JMGZEFIQIZZSBH-UHFFFAOYSA-N Bioquercetin Natural products CC1OC(OCC(O)C2OC(OC3=C(Oc4cc(O)cc(O)c4C3=O)c5ccc(O)c(O)c5)C(O)C2O)C(O)C(O)C1O JMGZEFIQIZZSBH-UHFFFAOYSA-N 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 229920001287 Chondroitin sulfate Polymers 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- 229920000045 Dermatan sulfate Polymers 0.000 description 1
- 244000068988 Glycine max Species 0.000 description 1
- 235000010469 Glycine max Nutrition 0.000 description 1
- QUQPHWDTPGMPEX-UHFFFAOYSA-N Hesperidine Natural products C1=C(O)C(OC)=CC=C1C1OC2=CC(OC3C(C(O)C(O)C(COC4C(C(O)C(O)C(C)O4)O)O3)O)=CC(O)=C2C(=O)C1 QUQPHWDTPGMPEX-UHFFFAOYSA-N 0.000 description 1
- 235000019766 L-Lysine Nutrition 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- OVRNDRQMDRJTHS-CBQIKETKSA-N N-Acetyl-D-Galactosamine Chemical compound CC(=O)N[C@H]1[C@@H](O)O[C@H](CO)[C@H](O)[C@@H]1O OVRNDRQMDRJTHS-CBQIKETKSA-N 0.000 description 1
- MBLBDJOUHNCFQT-UHFFFAOYSA-N N-acetyl-D-galactosamine Natural products CC(=O)NC(C=O)C(O)C(O)C(O)CO MBLBDJOUHNCFQT-UHFFFAOYSA-N 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose 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)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- 229930003316 Vitamin D Natural products 0.000 description 1
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- QUQPHWDTPGMPEX-UTWYECKDSA-N aurantiamarin Natural products COc1ccc(cc1O)[C@H]1CC(=O)c2c(O)cc(O[C@@H]3O[C@H](CO[C@@H]4O[C@@H](C)[C@H](O)[C@@H](O)[C@H]4O)[C@@H](O)[C@H](O)[C@H]3O)cc2O1 QUQPHWDTPGMPEX-UTWYECKDSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 238000009395 breeding Methods 0.000 description 1
- 230000001488 breeding effect Effects 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 239000005018 casein Substances 0.000 description 1
- BECPQYXYKAMYBN-UHFFFAOYSA-N casein, tech. Chemical compound NCCCCC(C(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(CC(C)C)N=C(O)C(CCC(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(C(C)O)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(COP(O)(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(N)CC1=CC=CC=C1 BECPQYXYKAMYBN-UHFFFAOYSA-N 0.000 description 1
- 235000021240 caseins Nutrition 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 229940059329 chondroitin sulfate Drugs 0.000 description 1
- APSNPMVGBGZYAJ-GLOOOPAXSA-N clematine Natural products COc1cc(ccc1O)[C@@H]2CC(=O)c3c(O)cc(O[C@@H]4O[C@H](CO[C@H]5O[C@@H](C)[C@H](O)[C@@H](O)[C@H]5O)[C@@H](O)[C@H](O)[C@H]4O)cc3O2 APSNPMVGBGZYAJ-GLOOOPAXSA-N 0.000 description 1
- 210000002808 connective tissue Anatomy 0.000 description 1
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- 230000003247 decreasing effect Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- AVJBPWGFOQAPRH-FWMKGIEWSA-L dermatan sulfate Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@H](OS([O-])(=O)=O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](C([O-])=O)O1 AVJBPWGFOQAPRH-FWMKGIEWSA-L 0.000 description 1
- 229940051593 dermatan sulfate Drugs 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- IVTMALDHFAHOGL-UHFFFAOYSA-N eriodictyol 7-O-rutinoside Natural products OC1C(O)C(O)C(C)OC1OCC1C(O)C(O)C(O)C(OC=2C=C3C(C(C(O)=C(O3)C=3C=C(O)C(O)=CC=3)=O)=C(O)C=2)O1 IVTMALDHFAHOGL-UHFFFAOYSA-N 0.000 description 1
- 229930003935 flavonoid Natural products 0.000 description 1
- 150000002215 flavonoids Chemical class 0.000 description 1
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- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
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- 229940025878 hesperidin Drugs 0.000 description 1
- VUYDGVRIQRPHFX-UHFFFAOYSA-N hesperidin Natural products COc1cc(ccc1O)C2CC(=O)c3c(O)cc(OC4OC(COC5OC(O)C(O)C(O)C5O)C(O)C(O)C4O)cc3O2 VUYDGVRIQRPHFX-UHFFFAOYSA-N 0.000 description 1
- QUQPHWDTPGMPEX-QJBIFVCTSA-N hesperidin Chemical compound C1=C(O)C(OC)=CC=C1[C@H]1OC2=CC(O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@@H](CO[C@H]4[C@@H]([C@H](O)[C@@H](O)[C@H](C)O4)O)O3)O)=CC(O)=C2C(=O)C1 QUQPHWDTPGMPEX-QJBIFVCTSA-N 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 229920002674 hyaluronan Polymers 0.000 description 1
- 229960003160 hyaluronic acid Drugs 0.000 description 1
- 150000003840 hydrochlorides Chemical class 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 229910017053 inorganic salt Inorganic materials 0.000 description 1
- 235000015110 jellies Nutrition 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 244000144972 livestock Species 0.000 description 1
- 229940049920 malate Drugs 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 210000001161 mammalian embryo Anatomy 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 235000020124 milk-based beverage Nutrition 0.000 description 1
- 229930019673 naringin Natural products 0.000 description 1
- DFPMSGMNTNDNHN-ZPHOTFPESA-N naringin Chemical compound O[C@@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@H]1O[C@H]1[C@H](OC=2C=C3O[C@@H](CC(=O)C3=C(O)C=2)C=2C=CC(O)=CC=2)O[C@H](CO)[C@@H](O)[C@@H]1O DFPMSGMNTNDNHN-ZPHOTFPESA-N 0.000 description 1
- 229940052490 naringin Drugs 0.000 description 1
- ARGKVCXINMKCAZ-UHFFFAOYSA-N neohesperidine Natural products C1=C(O)C(OC)=CC=C1C1OC2=CC(OC3C(C(O)C(O)C(CO)O3)OC3C(C(O)C(O)C(C)O3)O)=CC(O)=C2C(=O)C1 ARGKVCXINMKCAZ-UHFFFAOYSA-N 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 229940107700 pyruvic acid Drugs 0.000 description 1
- FDRQPMVGJOQVTL-UHFFFAOYSA-N quercetin rutinoside Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC=2C(C3=C(O)C=C(O)C=C3OC=2C=2C=C(O)C(O)=CC=2)=O)O1 FDRQPMVGJOQVTL-UHFFFAOYSA-N 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- IKGXIBQEEMLURG-BKUODXTLSA-N rutin Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@@H]1OC[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](OC=2C(C3=C(O)C=C(O)C=C3OC=2C=2C=C(O)C(O)=CC=2)=O)O1 IKGXIBQEEMLURG-BKUODXTLSA-N 0.000 description 1
- ALABRVAAKCSLSC-UHFFFAOYSA-N rutin Natural products CC1OC(OCC2OC(O)C(O)C(O)C2O)C(O)C(O)C1OC3=C(Oc4cc(O)cc(O)c4C3=O)c5ccc(O)c(O)c5 ALABRVAAKCSLSC-UHFFFAOYSA-N 0.000 description 1
- 235000005493 rutin Nutrition 0.000 description 1
- 229960004555 rutoside Drugs 0.000 description 1
- 235000013580 sausages Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
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- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
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- 238000012353 t test Methods 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
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Landscapes
- Fodder In General (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
本発明は、グルコサミン塩の新規な用途、即ち、大腿骨等の骨格を形成する骨の骨密度を向上させるための用途に関するものである。 The present invention relates to a novel use of glucosamine salt, that is, a use for improving the bone density of bone forming a skeleton such as a femur.
グルコサミンは，結合組織や軟骨組織に多く分布し，各器官の強度，柔軟性，弾力性を維持するのに寄与している。また、グルコサミンは軟骨グリコサミノグリカンの前駆物質であり、生体内でN−アセチル‐グルコサミンやN−アセチル‐ガラクトサミンに変換された後，ヒアルロン酸やコンドロイチン硫酸，デルマタン硫酸などの軟骨グリコサミノグリカンの構成成分として取り込まれることから，近年，変形性関節症への予防・治療効果が注目されている（例えば特許文献３）。そして，日本とアメリカでは健康食品として，またヨーロッパではすでに変形性関節症の治療薬として実際に使用されている。そのため，関節軟骨の修復作用を中心にグルコサミンの研究が行われてきた。そして今までの研究によって，グルコサミンが関節軟骨におけるグリコサミノグリカンの合成を高めることと，その分解を抑制することが明らかにされた。
また、グルコサミン塩、特に硫酸塩または塩酸塩等は特許文献１もしくは特許文献２等に開示された方法で製造され、該USPにはカプセル剤または錠剤等の形で、関節症治療剤等として使用されることが開示されている。しかしながら、グルコサミンが骨密度を向上させる作用のあることは全く知られていない。
従来、骨密度向上剤としては一般的に、乳抽出物、大豆胚抽出物、ビタミン類、ミネラル類などが知られている。また、ピルビン酸や、フラボノイド類、好ましくはヘスペリジン、ナリンジンまたはルチンが骨密度向上に有効であることが知られている（特許文献４および５）。
In addition, glucosamine salts, especially sulfates or hydrochlorides, etc. are produced by the method disclosed in Patent Document 1 or Patent Document 2, etc., and are used as therapeutic agents for arthritis in the form of capsules or tablets in the USP. Is disclosed. However, it is not known at all that glucosamine has an effect of improving bone density.
Conventionally, milk extract, soybean embryo extract, vitamins, minerals and the like are generally known as bone density improvers. Further, it is known that pyruvic acid and flavonoids, preferably hesperidin, naringin or rutin are effective in improving bone density (Patent Documents 4 and 5).
骨粗鬆症は近年高齢者の増加と共に増加傾向にあり、その予防治療は大きな問題となっている。そして、骨粗鬆症の治療剤として従来、カルシウム剤、活性ビタミン剤、女性ホルモン剤などが使用されている。しかしながら、骨粗鬆症が発症してからの治療よりも、医療費の抑制等の観点から、最近予防が重視されてきている。そのため、食事や運動等が推奨されているが、それと共に、より副作用等の恐れがなく、食事などと共に容易に摂取することができ、かつ予防的効果を達成しうる薬剤等の開発が望まれている。特に、最近若い女性等において、食事の偏食や運動不足などから骨密度の低下している人が多く見られ、これらの人は骨粗鬆症における潜在的な予備群と見られている。従ってこれらの人の骨密度を向上させることは、将来の骨粗鬆症を予防する意味で、非常に重要である。 In recent years, osteoporosis has been increasing with the number of elderly people, and its preventive treatment has become a big problem. Conventionally, calcium agents, active vitamin agents, female hormone agents, and the like have been used as therapeutic agents for osteoporosis. However, prevention has recently been emphasized from the viewpoint of medical cost control, etc., rather than treatment after osteoporosis develops. For this reason, meals and exercise are recommended, but development of drugs that can be easily taken with meals and that can achieve a preventive effect is desired. ing. In particular, among young women, etc., there are many people who have decreased bone density due to unbalanced diet and lack of exercise, and these people are regarded as a potential reserve group in osteoporosis. Therefore, it is very important to improve the bone density of these people in terms of preventing future osteoporosis.
本発明者らは、生体内において、軟骨等に多く存在し、毒性もなく、健康食品などとして、最近多用されているグルコサミンに注目し、研究したところ、意外にも、グルコサミンには、軟骨でない骨格を形成している通常の骨自体の骨密度を向上させる作用のあることを見出し、本発明を完成した。 The present inventors have focused on and studied glucosamine, which is frequently present in the living body in cartilage and the like, has no toxicity, and is frequently used as a health food. Surprisingly, glucosamine is not cartilage. The present invention has been completed by finding that it has the effect of improving the bone density of the normal bone itself forming the skeleton.
即ち本発明は
（１）グルコサミン若しくはその塩または生体内で分解されてそれらを生成しうるグルコサミン誘導体を有効成分とする骨密度向上剤、
（２）グルコサミン若しくはその塩または生体内で分解されてそれらを生成しうるグルコサミン誘導体を有効成分とする骨密度向上組成物、
（３）骨密度向上飲食品または飼料である上記（１）に記載の骨密度向上組成物、
（４）有効成分がグルコサミン塩である上記（１）に記載の骨密度向上剤または（２）若しくは（３）に記載の骨密度向上組成物、
に関するものである。
That is, the present invention provides (1) a bone density improver comprising, as an active ingredient, glucosamine or a salt thereof or a glucosamine derivative that can be decomposed in vivo to produce them,
(2) A composition for improving bone density, comprising as an active ingredient a glucosamine or a salt thereof or a glucosamine derivative that can be decomposed in vivo to produce them,
(3) The bone density improving composition according to (1), which is a bone density improving food or drink or feed,
(4) The bone density improving agent according to (1) or (2) or (3), wherein the active ingredient is a glucosamine salt,
It is about.
本発明によれば、グルコサミンを骨密度向上剤、または飲食品（栄養補助食品、健康食品、機能性食品等も含む）として、摂取することにより、容易に骨密度を向上させることができるので、ヒトの骨折の予防や骨粗鬆症の予防に効果があると考えられる。また、本発明においては、ヒトばかりでなく、他の温血動物、例えば家畜、ペット等における骨密度向上剤または骨密度向上飼料などとしても使用することができる。 According to the present invention, by ingesting glucosamine as a bone density improver or food and drink (including nutritional supplements, health foods, functional foods, etc.), bone density can be easily improved, It is thought to be effective in preventing human fractures and osteoporosis. In the present invention, it can be used not only as a human but also as a bone density improving agent or bone density improving feed in other warm-blooded animals such as livestock and pets.
本発明を以下により詳しく説明する。
本発明において、有効成分として使用されるグルコサミンは、フリーであっても、その塩（薬理学上許容される塩）であってもまた、生体内（特に胃等の消化管内）で加水分解されてグルコサミンまたはその塩となるＮ−アセチルグルコサミン等のグルコサミン誘導体であっても良い。好ましい有効成分としては、グルコサミン塩またはＮ−アセチルグルコサミンを挙げることができ、より好ましくはグルコサミン塩である。
グルコサミン塩としては薬理学的に許容されるものであれば特に制限はなく、無機酸塩、有機酸塩いずれも使用できるが一般的には硫酸塩もしくは塩酸塩等の無機塩が使用され、本発明においては塩酸塩が好ましい。有機酸塩としては例えば酢酸塩、クエン酸塩、コハク酸塩またはリンゴ酸塩等が挙げられる。
以下本明細書において単にグルコサミンという場合、フリーのグルコサミン、その塩および生体内でグルコサミンを生成しうる誘導体を含めた意味で使用するものとする。
The invention is described in more detail below.
In the present invention, glucosamine used as an active ingredient is hydrolyzed in vivo (particularly in the digestive tract such as the stomach), whether it is free or a salt thereof (pharmacologically acceptable salt). It may be a glucosamine derivative such as N-acetylglucosamine which becomes glucosamine or a salt thereof. Preferable active ingredients include glucosamine salt or N-acetylglucosamine, more preferably glucosamine salt.
The glucosamine salt is not particularly limited as long as it is pharmacologically acceptable, and either an inorganic acid salt or an organic acid salt can be used, but generally an inorganic salt such as sulfate or hydrochloride is used. In the invention, hydrochloride is preferred. Examples of the organic acid salt include acetate, citrate, succinate and malate.
Hereinafter, when simply referred to as glucosamine in the present specification, it is meant to include free glucosamine, a salt thereof, and a derivative capable of producing glucosamine in vivo.
本発明の骨密度向上剤において、グルコサミンは、単独でそのまま使用してもよいが、通常グルコサミンを担体、賦形剤、助剤（矯味剤、香料、甘味料、結合剤）等の医薬用又は食品用等に使用される添加剤と共に常法に従って、液剤又は固形剤例えば錠剤、顆粒剤、粉剤、カプセル剤、ゼリー剤等に製剤して、または健康食品、機能性食品、栄養補助食品または一般食品用の飲食物等として、組成物の形で使用することが出来る。なお、本明細書において飲食品といった場合、通常の飲食品と共に、健康食品、機能性食品および栄養補助食品等をも含むものとする。
坦体又は賦形剤としては、水、糖類、などの医薬製剤または健康食品に用いられる賦形剤、担体等を挙げることが出来る。骨密度向上剤におけるグルコサミンの含量は、特に限定はなく、通常０．０５％（質量％：以下同じ）以上、好ましくは１％以上で、最大１００％までよい。
従って、本発明における骨密度向上剤または骨密度向上組成物は、該効果を発揮する限り、グルコサミン単独、賦形剤などの添加剤を混合して製剤化したもの、また飲食品などと混合したもの、何れであってもよい。
本発明における骨密度向上剤または骨密度向上組成物においては、ビタミンＣおよび/またはビタミンＤ等を、骨密度向上用に併用添加してもよいが、本発明においては特に併用添加しなくても骨密度を向上させることができる。
In the bone density improving agent of the present invention, glucosamine may be used alone as it is, but usually glucosamine is used for pharmaceuticals such as carriers, excipients, auxiliaries (flavoring agents, fragrances, sweeteners, binders) or the like. According to conventional methods with additives used for food, etc., formulated into liquids or solids such as tablets, granules, powders, capsules, jellies, etc., health foods, functional foods, dietary supplements or general It can be used in the form of a composition as food or drink for food. In addition, in this specification, a food / beverage product includes a health food, a functional food, a nutritional supplement, and the like together with a normal food / beverage product.
Examples of the carrier or excipient include excipients and carriers used in pharmaceutical preparations such as water and saccharides or health foods. The content of glucosamine in the bone density improver is not particularly limited, and is usually 0.05% (mass%: the same applies hereinafter) or more, preferably 1% or more, and may be up to 100%.
Therefore, as long as the bone density improving agent or bone density improving composition of the present invention exerts the effect, it is formulated with a mixture of glucosamine alone, additives such as excipients, and mixed with food and drink. Or any of them.
In the bone density improving agent or bone density improving composition of the present invention, vitamin C and / or vitamin D may be added together for improving bone density, but in the present invention, it is not particularly necessary to add together. Bone density can be improved.
グルコサミン塩を飲食品に配合して本発明における骨密度向上用組成物として摂取する場合は、適当に飲食物と混合して摂取すれば良く、グルコサミン塩を混合しうる飲食物は特に限定されず、牛乳などの乳飲料、ドリンク剤等の飲料やハム、ソーセージ等の食物などを挙げることが出来る。
これらの食品に対するグルコサミン塩の添加量は特に限定されないが通常食品全体に対して０．０５％ 以上、好ましくは０．１％以上、上限は特に無いが味覚等の点から通常１０％以下、好ましくは５％以下、更に好ましくは４％ 以下である。
本発明でのグルコサミン塩の投与量は通常成人当たり１日０．３g以上、より好ましくは０．５g以上、更に好ましくは１g以上で、上限は毒性もほとんどないので特に制限はないが、通常２０g以下、好ましくは１０g以下、更に好ましくは５g以下程度である。また、ヒト以外の温血動物の場合には、１ｍｇ〜５ｇ／ｋｇ・day、好ましくは１０ｍｇ〜２ｇ／ｋｇ・day程度である。
When the glucosamine salt is blended in a food or drink and taken as a composition for improving bone density in the present invention, it may be taken by appropriately mixing with the food or drink, and the food or drink that can be mixed with the glucosamine salt is not particularly limited. And milk beverages such as milk, beverages such as drinks, and foods such as ham and sausage.
The amount of glucosamine salt added to these foods is not particularly limited, but is usually 0.05% or more, preferably 0.1% or more, and the upper limit is not particularly limited, but usually 10% or less from the viewpoint of taste, etc. Is 5% or less, more preferably 4% or less.
The dose of glucosamine salt in the present invention is usually 0.3 g or more per day per adult, more preferably 0.5 g or more, and further preferably 1 g or more. The upper limit is not particularly limited because there is almost no toxicity, but usually 20 g. The amount is preferably 10 g or less, more preferably about 5 g or less. In the case of warm-blooded animals other than humans, the dose is about 1 mg to 5 g / kg · day, preferably about 10 mg to 2 g / kg · day.
本発明の骨密度向上剤または組成物は、上記したように、経口摂取により、ヒトまたは家畜若しくはペット等の温血動物の骨密度を増加させることができ、骨折、骨粗鬆症等の予防にきわめて有用と考えられる。
次に、本発明を実施例により、具体的に説明する。
As described above, the bone density improving agent or composition of the present invention can increase the bone density of humans or warm-blooded animals such as domestic animals or pets by ingestion, and is extremely useful for the prevention of fractures, osteoporosis and the like. it is conceivable that.
Next, the present invention will be specifically described by way of examples.
グルコサミン投与による、ＤＤＹマウスでの骨密度の向上
ＤＤＹマウス（８週齢：雌）３匹を１群（平均体重３０ｇ／１匹）として、完全精製飼料（AIN-93組成）の餌をもとに、全体に対して０．２％となるグルコサミン塩酸塩を配合した下記組成の餌を、自由摂取により与え、４週間飼育した。１匹の１日当たりのグルコサミンの平均摂取量は０．０１ｇであった。
対照として、グルコサミンの代わりに、グルコースを０．２％配合した飼料を与え、ＤＤＹマウス（８週齢：雌）３匹を１群（平均体重３０ｇ／１匹）として、グルコサミン投与群と全く同様に飼育した。
餌組成
成分 配合量（g/Kg(餌））
カゼイン ２００
Ｌ−リジン ３
セルロース ５０
蔗糖 ９７
コーンスターチ ５３０
コーンオイル ７０
AIN-93 ミネラルミックス ３５
AIN-93 ビタミンミックス １０
本発明：グルコサミン(GlcN) ２
（対照：グルコース (Glu) ２）
４週間飼育後、各群における大腿骨の骨密度を、実験動物用Ｘ線ＣＴ（商品名：ラシータ：ＬＣＴ−１００、アロカ株式会社製）にて測定した。その結果を下表に示す
皮質骨密度ｍｇ／ｃｍ３ 全骨密度ｍｇ／ｃｍ３
GlcN投与群（本発明） 840.1 657.8
(SD 27.88 28.68)
Glu投与群（対照） 810.4 648.8
(SD 25.46 27.75 )
上表より、明らかなように、グルコサミン塩酸塩投与群では、４週間の投与で、対照投与群に比して、皮質骨密度において、２９．６５ｍｇ／ｃｍ３ 増加しており、全骨密度においても８．９２５ｍｇ／ｃｍ３ 増加している。これらの値は有意差検定(t検定）でも明らかに有意な差であった（P<0.01)。
Improvement of bone density in DDY mice by administration of glucosamine Three DDY mice (8 weeks old: female) as one group (average body weight 30 g / 1), based on the feed of a completely purified diet (AIN-93 composition) In addition, a feed having the following composition containing 0.2% of glucosamine hydrochloride based on the whole was given by free intake and bred for 4 weeks. The average daily intake of glucosamine per animal was 0.01 g.
As a control, instead of glucosamine, a diet containing 0.2% glucose was given, and three DDY mice (8 weeks old: female) were used as one group (average body weight 30 g / one), exactly the same as the glucosamine administration group. I was reared.
Bait composition Ingredients Amount (g / Kg (bait))
Casein 200
L-lysine 3
Cellulose 50
Sucrose 97
Cornstarch 530
Corn oil 70
AIN-93 Mineral Mix 35
AIN-93 Vitamin Mix 10
The present invention: Glucosamine (GlcN) 2
(Control: glucose (Glu) 2)
After breeding for 4 weeks, the bone density of the femur in each group was measured by X-ray CT for experimental animals (trade name: Lasita: LCT-100, manufactured by Aloka Co., Ltd.). The results are shown in the table below.
Cortical bone density mg / cm 3 Total bone density mg / cm 3
GlcN administration group (present invention) 840.1 657.8
(SD 27.88 28.68)
Glu administration group (control) 810.4 648.8
(SD 25.46 27.75)
As is apparent from the above table, in the glucosamine hydrochloride administration group, the cortical bone density increased by 29.65 mg / cm 3 compared to the control administration group in the administration for 4 weeks, and in the total bone density Also increased by 8.925 mg / cm 3 . These values were also clearly significant in the significant difference test (t test) (P <0.01).
本発明の骨密度向上剤または組成物は、経口摂取により、ヒトを含む温血動物の骨密度を増加させることができるもので、該動物の骨折および骨粗鬆症等の予防にきわめて有用である。 The bone density improving agent or composition of the present invention can increase the bone density of warm-blooded animals including humans by ingestion, and is extremely useful for prevention of fractures and osteoporosis of the animals.
Claims (4)
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| RU2843456C1 (en) * | 2020-05-22 | 2025-07-14 | Сосьете Де Продюи Нестле С.А. | Use of breast milk oligosaccharides in nutritional compositions for improving bone tissue development and/or bone strength |
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