CN1471403A - 用于减少斑块和结石的含有海藻的口服制剂 - Google Patents
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Abstract
用于减少哺乳动物例如人、猫或狗中斑块和/或结石,例如菌斑、动脉硬化斑、动脉粥样硬化斑、胸膜斑、牙结石、肾结石、胆结石和前列腺结石的口服制剂,其中含有囊叶藻属,尤其是岩衣藻海藻或其提取物。本发明口服制剂适用于治疗哺乳动物个体中的斑块和/或结石的预防和/或治疗方法。
Description
本发明涉及用于减少哺乳动物斑块和/或结石的口服制剂。更具体来说,本发明涉及囊叶藻属(Ascophyllum sp.)海藻或其提取物在制备用于减少哺乳动物斑块和/或结石的口服制剂中的应用,包含囊叶藻属海藻或其提取物作为活性组分的单位剂量的口服制剂,和治疗哺乳动物个体中斑块和/或结石的预防和/或治疗方法。
发明背景
牙结石是影响哺乳动物例如人、猫和狗的身体不适。专业人员认为牙结石是钙化的细菌沉积物。据认为当不能除去这样的沉积物时会出现牙结石。牙结石非常牢固地附着在牙齿表面上,并且普通的人不能自己除去牙结石。迄今为止,已知除去牙结石的唯一方法是牙科医生或牙齿卫生人员使用器械通过机械手段将其除去或者使用超声波仪器通过振动将其除去。牙结石不带来任何疼痛,但是在将其除去时经常会带来疼痛。其使得牙齿卫生保健更困难并应当除去。
斑块是形成牙结石和发展成龋齿所必需的。然而,不是所有斑块都发展成结石,这可能是由于在唾液和/或牙周渗出物中有某些保护机制所致。对于这样的保护机制的特征的认识尚不充分。饮食构成可能很重要。
不是每个人都有牙结石。尽管牙齿卫生保健做得很不好,但是有些人可以一生都没有牙结石。对于这一点的原因是未知的,但是可以设想唾液的化学组成起了重要作用。因此,应当能够用化学手段对抗牙结石的形成。已经作了很多尝试来施用化学制剂,以希望局部影响牙结石形成过程。但是迄今为止没有取得任何成功。
发明描述
本发明提供了减少、或甚至是消除菌斑和龋齿,以及动脉硬化斑、动脉粥样硬化斑、胸膜斑、肾结石、胆结石和前列腺结石的手段。
本发明是基于用狗和人进行的经验研究,已经确认,服用含有海藻粗粉的包衣片剂几周后,所述狗和人的牙结石消除了。其中所述包衣片剂是被吞咽下去,而不是让它们首先在口腔中施加任何局部作用。因此可以推断,对牙结石的作用依赖于血液、唾液和从牙床囊流出的流体所介导的影响。很明显,从片剂释放出的化学组分经由某些流体打破了保持牙结石与牙床表面附着的化学键。然而,作用机制是未知的。
在初始的经验研究和下述实验中,所用的海藻是囊叶藻属,即岩衣藻(Ascophyllum nodosum)。所分析的岩衣藻的组成如表1所示。在整个欧洲能够从商业上获得该海藻已有30多年的历史。其含有大量营养素,并且可视为饮食补充物。
因此,本发明一个方面涉及囊叶藻属海藻或其提取物在制备用于减少哺乳动物斑块和/或结石的口服制剂中的应用。
在本说明书和权利要求书中,应当理解,囊叶藻属海藻提取物是能够减少哺乳动物斑块和/或结石的任何合成或分离的海藻部分。
在优选的本发明实施方案中,所述哺乳动物选自人、猫和狗。
在另一实施方案中,口服制剂选自粉剂、悬浮液、片剂、包衣片剂和胶囊。因为据认为海藻的味道缺乏吸引力,优选通过在包衣片剂或胶囊中提供海藻,或者通过向粉剂、悬浮液或未包衣片剂中加入香料或芳香剂来遮蔽海藻的味道。应当使用形成各种口服制剂所需的常用添加剂。
在优选的本发明实施方案中,斑块选自菌斑、动脉硬化斑、动脉粥样硬化斑和胸膜斑,结石选自牙结石、肾结石、胆结石和前列腺结石。
在最优选的实施方案中,海藻是岩衣藻。
例如,岩衣藻海藻具有下列分析的化学组成:
20-26%酯化形式的硫酸化糖醛酸类化合物、5-8%甘露醇、2-5%昆布多糖(Laminaran)、5-15%岩藻多糖(Fucoidin)、2.5-3.5%S、2-3%K、3-4%Cl、3-4%Na、0.5-1%Mg、1-3%Ca、0.1-0.15%P和40-100mg/kg Br、1-10mg Co、1-10mg Cu、150-1000mg Fe、10-50mg Mn、700-1200mg I、20-200mg Zn、0.3-1mg Mo、2-5mg Ni、15-50mg Ba、1.5-3mg V和500-2000mg/kg抗坏血酸、150-300mg/kg生育酚类化合物、30-60mg/kg胡萝卜素类化合物、10-30mg/kg烟酸、0.1-0.4mg/kg生物素、0.2-1mg/kg叶酸、5-10mg/kg核黄素、1-5mg/kg硫胺素、0.004mg/kg维生素B12和10mg/kg维生素K。
本发明的另一方面涉及单位剂量的口服制剂,其中含有哺乳动物斑块和/或结石减少量的囊叶藻属海藻或其提取物作为活性组分。
在优选的实施方案中,哺乳动物斑块和/或结石减少量的囊叶藻属海藻是250mg-1g海藻/单位剂量。囊叶藻属海藻优选是岩衣藻。
本发明另一方面涉及治疗有此需要的哺乳动物个体中斑块和/或结石的预防和/或治疗方法,包括给所述个体施用单位剂量的本发明口服制剂。
下面用附图描述和实验进一步举例说明本发明,但是本发明的保护范围不限于所公开的本发明实施方案。
附图描述
附图1表示的是,服用CalcOFF-一种本发明片剂2个月后,在30个人中在3颗牙齿上的结石的程度的图。
附图2表示的是,服用CalcOFF 2个月后,在30个人中在3颗牙齿上的斑块的程度的图。
附图3表示的是,服用CalcOFF 2个月后,在30个人中的牙结石质量的图。
在附图1和2中,OHI-s是口腔卫生保健指数,其描述了牙齿表面上斑块或结石的程度。其细分为4个等级:0代表没有斑块,1代表在<1/3表面上有斑块,2代表在<2/3表面上有斑块,3代表在>2/3牙齿表面上有斑块。
实验
除了所述的初始经验研究以外,又进行了如下所公开的多个实验。
用于实验中的口服制剂是包衣片剂形式的剂量单位,称为CalcOFF,并且由下列成分组成:岩衣藻干粉 250mg磷酸二钙 130mg微晶纤维素 116.8mg硬脂酸镁 3.2mg
用过去形成了结石并且在基准时具有口腔结石的30名成人患者进行实验。他们得到免费的CalcOFF样本,并同意在2个月的时间内每天服用2片。
在基准时和2个月后,一名牙科医生记录在第26、31和11颗牙齿上的龈上结石和斑块的程度(Greene and Wermillion指数,即口腔卫生保健指数=OHI-s)。OHI-s结果分别作为斑块指数(PLA)和结石指数(CAI)记录。
统计学方法:通过方差分析对在基准时与在2个月后记录的值之间的差异进行统计学评价。
结果:表2和3,以及附图1和2证实了在所有测试的牙齿上,斑块和结石的程度都大大显著减小。需要强调的是,解释表3的数据在某种程度上是基于牙科医生的主观判断。
如附图3所示,CalcOFF片剂对结石的影响在个体间有差异。在16个人中,结石消失了,或者其程度减小了。在12个人中,记录仅有小的减少,但是结石非常软,并且易于除去,甚至由患者除去。有两例没有产生任何作用。这种效果差异最有可能是由于矿化水平不同所致。
2个月的试验后,仍然具有结石的某些患者同意在接下来的8周内将CalcOFF片剂的剂量从每天2片增加至每天4片。该试验仍然进行,但是很明显,现在他们正更快地释放结石。因此,似乎效果是剂量依赖性的。
在其它情况中,基准2个月后,由牙科医生除去结石,并且患者继续服用CalcOFF片剂。新结石的形成是零或者与以前年度相比显著减慢。
CalcOFF片剂对斑块形成有显著作用(附图2)。在服用该片剂的2个月期间,斑块减少了71-87%。依据表2,服用该片剂之前与之后的差异在测定的所有牙齿上都非常显著。最有可能的是,服用CalcOFF片剂几天后已经实现了作用。
两名患者也患有肾结石。令人惊奇的是,他们注意到在他们的尿中有沉淀,这意味着他们的肾结石降解了。
这些发现表明,除了牙结石以外,CalcOFF还能有效地抗其它结石形成,以及除了牙齿斑块以外,还能有效地抗其它斑块形成。
所记录的已有结石的减少与观察到的斑块减少以及在施用本发明制剂期间很少形成新的结石这一观察结果相一致。
每日摄取该海藻不但可以减轻具有结石的成人中的斑块和结石程度,而且还可以预防形成新的斑块和结石。
表1.所分析的岩衣藻的组成水 12-15%Ash 17-20%藻酸 20-26%甘露醇 5-8%昆布多糖 2-5%纤维 <8%蛋白 5-10%醚提取物 2-4%岩藻多糖 10%S 2.5-3.5%K 2-3%Cl 3.1-4.4%Na 3-4%Mg 0.5-0.9%Ca 1-3%P 0.1-0.15%Br 40-100mg/kgCo 1-10mg/kgCu 1-10mg/kgFe 150-1000mg/kgMn 10-50mg/kgI 700-1200mg/kgZn 20-200mg/kgMo 0.3-1mg/kgNi 2-5mg/kgBa 15-50mg/kgV 1.5-3mg/kg抗坏血酸 500-2000mg/kg生育酚类化合物 150-300mg/kg胡萝卜素 30-60mg/kg烟酸 10-30mg/kg生物素 0.1-0.4mg/kg叶酸 0.2-1mg/kg核黄素 5-10mg/kg硫胺素 1-5mg/kg维生素B12 0.004mg/kg维生素K 10mg/kg表2.在服用CalcOFF之前和2个月后,在30个人中在第26、31和11颗牙齿上的牙结石的程度牙齿编号26
CAI SD在基准时 0.96 0.5272个月后 0.57 0.503 差异41% P<0.0021牙齿编号31在基准时 1.13 0.5712个月后 0.76 0.504 差异30% P<0.011牙齿编号11在基准时 0.41 0.5682个月后 0.14 0.350 差异68% P<0.009表3.在服用CalcOFF之前和2个月后,在30个人中在第26、31和11颗牙齿上的斑块的程度牙齿编号26
PLI SD在基准时 0.85 0.4562个月后 0.11 0.362 差异87% P<0.0001牙齿编号31在基准时 0.70 0.5352个月后 0.10 0.305 差异86% P<0.0001牙齿编号11在基准时 0.48 0.5802个月后 0.15 0.362 差异71% P<0.001
Claims (10)
1.囊叶藻属海藻或其提取物在制备用于减少哺乳动物斑块和/或结石的口服制剂中的应用。
2.权利要求1的应用,其中所述哺乳动物选自人、猫和狗。
3.权利要求1或2的应用,其中所述口服制剂选自粉剂、悬浮液、片剂、包衣片剂和胶囊。
4.权利要求1-3任一项的应用,其中所述斑块选自菌斑、动脉硬化斑、动脉粥样硬化斑和胸膜斑,所述结石选自牙结石、肾结石、胆结石和前列腺结石。
5.权利要求1-4任一项的应用,其中所述海藻是岩衣藻。
6.权利要求5的应用,其中所述岩衣藻海藻具有下列分析的化学组成:
20-26%酯化形式的硫酸化糖醛酸类化合物、5-8%甘露醇、2-5%昆布多糖(Laminaran)、5-15%岩藻多糖、2.5-3.5%S、2-3%K、3-4%Cl、3-4%Na、0.5-1%Mg、1-3%Ca、0.1-0.15%P和40-100mg/kg Br、1-10mg Co、1-10mg Cu、150-1000mg Fe、10-50mg Mn、700-1200mg I、20-200mg Zn、0.3-1mgMo、2-5mg Ni、15-50mg Ba、1.5-3mg V和500-2000mg/kg抗坏血酸、150-300mg/kg生育酚类化合物、30-60mg/kg胡萝卜素类化合物、10-30mg/kg烟酸、0.1-0.4mg/kg生物素、0.2-1mg/kg叶酸、5-10mg/kg核黄素、1-5mg/kg硫胺素、0.004mg/kg维生素B12和10mg/kg维生素K。
7.单位剂量的口服制剂,其中含有哺乳动物斑块和/或结石减少量的囊叶藻属海藻或其提取物作为活性组分。
8.权利要求7的单位剂量的口服药物,其中所述哺乳动物斑块和/或结石减少量的囊叶藻属海藻是250mg-1g海藻/单位剂量。
9.权利要求7或8的单位剂量的口服制剂,其中所述囊叶藻属海藻是岩衣藻。
10.治疗有此需要的哺乳动物个体中斑块和/或结石的预防和/或治疗方法,包括给所述个体施用权利要求7-9任一项的单位剂量的口服制剂。
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SE0003907A SE0003907D0 (sv) | 2000-10-27 | 2000-10-27 | Komposition för eliminering av tandsten ur munnen |
SE00039073 | 2000-10-27 |
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CN1471403A true CN1471403A (zh) | 2004-01-28 |
CN1230195C CN1230195C (zh) | 2005-12-07 |
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EP (1) | EP1328285B1 (zh) |
JP (1) | JP4648611B2 (zh) |
KR (1) | KR100890723B1 (zh) |
CN (1) | CN1230195C (zh) |
AT (1) | ATE319463T1 (zh) |
AU (1) | AU2001290473A1 (zh) |
BR (1) | BRPI0114933B8 (zh) |
CA (1) | CA2426936C (zh) |
CY (1) | CY1105379T1 (zh) |
DE (1) | DE60117824T2 (zh) |
DK (1) | DK1328285T3 (zh) |
ES (1) | ES2260286T3 (zh) |
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MX (1) | MXPA03003699A (zh) |
NO (1) | NO329352B1 (zh) |
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PT (1) | PT1328285E (zh) |
RU (1) | RU2275218C2 (zh) |
SE (1) | SE0003907D0 (zh) |
SK (1) | SK287572B6 (zh) |
WO (1) | WO2002034279A1 (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103877195A (zh) * | 2013-11-15 | 2014-06-25 | 东南大学 | 一种用于治疗肾结石的中药配方组成及其服用方法 |
Families Citing this family (11)
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US6932980B1 (en) * | 2001-01-18 | 2005-08-23 | Richard Sayre | Method of making microalgal-based animal foodstuff supplements, microalgal-supplemented animal foodstuffs and method of animal nutrition |
AU2001269936A1 (en) | 2000-06-20 | 2002-01-02 | Phycotransgenics, Llc | Transgenic algae for delivering antigens to an animal |
US20050267091A1 (en) * | 2004-05-25 | 2005-12-01 | Roger Berlin | Compositions containing policosanol and niacin and/or niacin derivatives and their pharmaceutical uses |
DE102004043945A1 (de) * | 2004-09-11 | 2006-03-30 | Henkel Kgaa | Mund-, Zahn- und Zahnprotesenpflegemittel enthaltend die Plaquebildung inhibierende Substanzen |
EA011286B1 (ru) * | 2007-08-29 | 2009-02-27 | Общество С Ограниченной Ответственностью "Вдс" | Таблетка для профилактики и лечения заболеваний зубов и пародонта |
FR2931071B1 (fr) * | 2008-05-14 | 2010-08-13 | Roquette Freres | Confiserie aux algues pour la prevention des infections buccodentaires |
US20100183523A1 (en) | 2009-01-22 | 2010-07-22 | Wagner Richard E | Dental composition and method |
EP2210582B1 (en) * | 2009-01-22 | 2019-09-18 | Solarvest Bioenergy Inc. | Dental composition comprising algae and method for producing thereof |
FR2968558B1 (fr) | 2010-12-14 | 2013-03-22 | Ys Lab | Composition a base d'extrait d'algues a usage bucco-dentaire |
US8916179B2 (en) * | 2011-10-25 | 2014-12-23 | T.F.H. Publications, Inc. | Ascophyllum nodosum animal chews |
WO2020260955A2 (en) * | 2019-03-27 | 2020-12-30 | UPL Corporation Limited | Plant treatment composition and method |
Family Cites Families (16)
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JPS56117777A (en) * | 1980-02-15 | 1981-09-16 | Takanori Koshiro | Diuretic health food |
JPS56113269A (en) * | 1980-02-15 | 1981-09-07 | Takanori Koshiro | Healthful food for promoting urination |
FR2513122A1 (fr) * | 1981-09-23 | 1983-03-25 | Goemar Sa | Nouveaux medicaments a base d'extraits d'algues, et formulations correspondantes |
US4775525A (en) * | 1985-12-16 | 1988-10-04 | Ivo Pera | Oral hygiene formulation containing sodium alginate |
JP2691902B2 (ja) * | 1988-01-19 | 1997-12-17 | 日本製粉株式会社 | グルコシルトランスフェラーゼ阻害剤及びう蝕予防口腔用組成物 |
GB8803157D0 (en) * | 1988-02-11 | 1988-03-09 | Nat Res Dev | Denture protection |
US4857331A (en) * | 1988-03-31 | 1989-08-15 | Warner-Lambert Company | Sugarless pectin delivery system |
JP3013060B2 (ja) * | 1991-11-16 | 2000-02-28 | 株式会社ロッテ | 虫歯菌歯牙付着阻害及び脱離のための口腔用組成物 |
DE4219360C2 (de) * | 1992-06-12 | 1994-07-28 | Milupa Ag | Verfahren zur Gewinnung von Lipiden mit einem hohen Anteil von langkettig-hochungesättigten Fettsäuren |
US6255296B1 (en) * | 1994-01-11 | 2001-07-03 | Endomatrix, Inc. | Composition and method for treating a patient susceptible to or suffering from a cardiovascular disorder or disease |
GB2292146A (en) * | 1994-08-11 | 1996-02-14 | Merck & Co Inc | HIV protease inhibitors useful for the treatment of AIDS |
WO1998030228A1 (en) * | 1997-01-13 | 1998-07-16 | Emory University | Compounds and their combinations for the treatment of influenza infection |
US6338856B1 (en) * | 1998-02-27 | 2002-01-15 | Texas Tech University | Seaweed supplement diet for enhancing immune response in mammals and poultry |
US6224871B1 (en) * | 1998-03-11 | 2001-05-01 | Reliv International, Inc. | Dietary supplement for nutritionally promoting healthy joint function |
GB9819530D0 (en) | 1998-09-09 | 1998-10-28 | Smithkline Beecham Plc | Novel compositions and use |
JP4189620B2 (ja) * | 2000-03-01 | 2008-12-03 | ライオン株式会社 | 歯周疾患予防・治療用口腔用組成物 |
-
2000
- 2000-10-27 SE SE0003907A patent/SE0003907D0/xx unknown
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2001
- 2001-09-27 RU RU2003115613/15A patent/RU2275218C2/ru active
- 2001-09-27 EP EP01970473A patent/EP1328285B1/en not_active Expired - Lifetime
- 2001-09-27 KR KR1020037005794A patent/KR100890723B1/ko active IP Right Grant
- 2001-09-27 DK DK01970473T patent/DK1328285T3/da active
- 2001-09-27 JP JP2002537330A patent/JP4648611B2/ja not_active Expired - Lifetime
- 2001-09-27 BR BR0114933-4 patent/BRPI0114933B8/pt not_active IP Right Cessation
- 2001-09-27 NZ NZ525418A patent/NZ525418A/en not_active IP Right Cessation
- 2001-09-27 CN CNB018180337A patent/CN1230195C/zh not_active Expired - Lifetime
- 2001-09-27 WO PCT/SE2001/002083 patent/WO2002034279A1/en active IP Right Grant
- 2001-09-27 US US10/399,770 patent/US7125555B2/en not_active Expired - Lifetime
- 2001-09-27 PT PT01970473T patent/PT1328285E/pt unknown
- 2001-09-27 SK SK506-2003A patent/SK287572B6/sk not_active IP Right Cessation
- 2001-09-27 ES ES01970473T patent/ES2260286T3/es not_active Expired - Lifetime
- 2001-09-27 DE DE60117824T patent/DE60117824T2/de not_active Expired - Lifetime
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- 2001-09-27 MX MXPA03003699A patent/MXPA03003699A/es active IP Right Grant
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103877195A (zh) * | 2013-11-15 | 2014-06-25 | 东南大学 | 一种用于治疗肾结石的中药配方组成及其服用方法 |
Also Published As
Publication number | Publication date |
---|---|
CA2426936C (en) | 2009-08-25 |
KR20030048082A (ko) | 2003-06-18 |
SK5062003A3 (en) | 2003-08-05 |
SK287572B6 (sk) | 2011-03-04 |
BRPI0114933B1 (pt) | 2018-05-29 |
MXPA03003699A (es) | 2003-08-07 |
DK1328285T3 (da) | 2006-07-17 |
ATE319463T1 (de) | 2006-03-15 |
ES2260286T3 (es) | 2006-11-01 |
WO2002034279A1 (en) | 2002-05-02 |
US7125555B2 (en) | 2006-10-24 |
NO20031808D0 (no) | 2003-04-23 |
PT1328285E (pt) | 2006-07-31 |
CN1230195C (zh) | 2005-12-07 |
BRPI0114933B8 (pt) | 2021-05-25 |
SE0003907D0 (sv) | 2000-10-27 |
EP1328285A1 (en) | 2003-07-23 |
KR100890723B1 (ko) | 2009-03-26 |
DE60117824T2 (de) | 2006-11-02 |
NO20031808L (no) | 2003-04-23 |
RU2275218C2 (ru) | 2006-04-27 |
NO329352B1 (no) | 2010-10-04 |
IS2288B (is) | 2007-10-15 |
JP4648611B2 (ja) | 2011-03-09 |
JP2004512309A (ja) | 2004-04-22 |
NZ525418A (en) | 2004-11-26 |
IS6795A (is) | 2003-04-23 |
CY1105379T1 (el) | 2010-04-28 |
DE60117824D1 (de) | 2006-05-04 |
US20040022806A1 (en) | 2004-02-05 |
CA2426936A1 (en) | 2002-05-02 |
EP1328285B1 (en) | 2006-03-08 |
BR0114933A (pt) | 2004-01-06 |
AU2001290473A1 (en) | 2002-05-06 |
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