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WO2000059507A1 - Obesity preventives - Google Patents

Obesity preventives Download PDF

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Publication number
WO2000059507A1
WO2000059507A1 PCT/JP1999/001748 JP9901748W WO0059507A1 WO 2000059507 A1 WO2000059507 A1 WO 2000059507A1 JP 9901748 W JP9901748 W JP 9901748W WO 0059507 A1 WO0059507 A1 WO 0059507A1
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Prior art keywords
biotin
obesity
weight gain
intake
preventives
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Ceased
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PCT/JP1999/001748
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French (fr)
Japanese (ja)
Inventor
Kazumi Osada
Kenji Tsunoda
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Taisho Pharmaceutical Co Ltd
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Taisho Pharmaceutical Co Ltd
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Priority to JP9276089A priority Critical patent/JPH11116478A/en
Application filed by Taisho Pharmaceutical Co Ltd filed Critical Taisho Pharmaceutical Co Ltd
Priority to AU29614/99A priority patent/AU2961499A/en
Priority to PCT/JP1999/001748 priority patent/WO2000059507A1/en
Publication of WO2000059507A1 publication Critical patent/WO2000059507A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents

Definitions

  • the present invention relates to an antiobesity agent containing piotin as an active ingredient.
  • the present inventors have found that in the course of a study on the physiological role of biotin, the rate of weight gain of a model animal to which biotin was administered was significantly suppressed, and completed the present invention based on such findings.
  • the present invention is an antiobesity agent characterized by using biotin as an active ingredient.
  • Pyotin is a type of coenzyme known as vitamin H. It is well known that it acts as an essential coenzyme of lupoxylase. In terms of physiological effects, effects on cell growth and DNA synthesis have been reported, and a wide variety of research reports have been made on deficiency of biotin, including dermatitis, hair loss, and ataxia.
  • biotin significantly suppresses undesired weight gain caused by ingesting a high calorie single meal, ie, that biotin has an obesity-preventing effect. That is, the prevention of obesity according to the present invention refers to an effect of suppressing an undesired increase in weight that is observed when calories are excessively consumed, as described above.
  • the antiobesity agent of the present invention can be prepared in the form of a solid preparation or a liquid preparation as long as it can be taken orally.
  • a solid preparation containing biotin any of powder, granule and tablet forms can be prepared by a general production method.
  • Liquid preparations can also be prepared by mixing with commonly used bases and active ingredients.
  • the intake of It is preferably at least 200 g, preferably at least 400 g per day. With an intake of less than 200 X g, the effect of biotin on suppressing weight gain is not fully exerted.
  • microcrystalline cellulose and biotin were uniformly mixed in advance, other components were additionally mixed and granulated to prepare a high calorie granule.
  • microcrystalline cellulose and biotin were uniformly mixed in advance, other components were additionally mixed and granulated to prepare a high calorie granule.
  • Example 1 The following test was performed using an SD rat (oss) body weight of 400 g.
  • the animals of Example 1, Example 2, and Comparative Example 1 were each fed 10 g Z days each in three groups of six animals each. Since egg white, which is a protein source in each diet, has the property of adsorbing biotin, the comparative example in which 150 g of biotin adsorbed on 2 O mg of egg white was added was used as a blank for the amount of biotin. . Therefore, the amount of effective biotin contained in each example is equivalent to 50 g / 100 g of the bait in Example 1 and to 600 g / 100 g of the bait in Example 2.
  • FIG. 1 shows the average food consumption of the granules of Examples and Comparative Examples in each SD rat group from day 60 to day 70 after the start of the test. The vertical line on the graph indicates the standard deviation.
  • FIG. 2 is a graph showing the average weight gain of the SD rats fed with biotin for 70 days, in which the vertical axis represents the weight gain and the horizontal axis represents the experimental period (weeks).
  • indicates the results when the granules of Comparative Example 1 were used
  • indicates the results when the granules of Example 1 were used
  • indicates the results when the granules of Example 2 were used.

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  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

To provide oral preparations having an effect of preventing obesity based on a principle different from promotion of exercise or restriction of caloric intake. By taking obesity preventives containing biotin as the active ingredient, undesirable weight gain is effectively prevented.

Description

明 細 書  Specification

肥満防止剤  Antiobesity agent

技術分野 Technical field

本発明は、 ピオチンを有効成分とした肥満防止剤に関する。 背景技術  The present invention relates to an antiobesity agent containing piotin as an active ingredient. Background art

現代社会の高力口リ一型食生活のもたらす問題の一つに、 カロリ一過剰摂取に 基づく体重の増加、 いわゆる肥満が挙げられる。 肥満は、 運動不足と相まって、 糖尿病、 動脈硬化、 高血圧等の、 種々の生活習慣病の引き金となるといわれてい る。  One of the problems brought about by the high-strength diet of modern society is weight gain due to excessive intake of calories, so-called obesity. Obesity, combined with lack of exercise, is said to trigger various lifestyle-related diseases such as diabetes, arteriosclerosis, and high blood pressure.

肥満は、 摂取カロリー量が消費カロリー量を上回ることが、 その根本原理であ る。 従って、 食事を介したカロリー摂取量を抑制し、 運動などによってカロリー 消費を促進すれば、 理論上は解消される。 しかし、 実際上はその実行は困難を伴 う場合が多い。 特に運動機能に支障を有する者にとっては、 運動を必須とする先 の方法は事実上実行不可能である。  The basic principle of obesity is that the calorie intake exceeds the calorie consumption. Therefore, if caloric intake through diet is suppressed and caloric consumption is promoted by exercise or the like, it is theoretically eliminated. However, in practice it is often difficult. Particularly for those with motor function impairment, the above methods that require exercise are virtually impractical.

そのため、 運動を必須とする肥満の解消方法の他に、 天然由来の食成分や非消 化性成分を用いた栄養学的な方法や、 手術等の物理的な方法など、 数多くの肥満 解消法が提案されている。  Therefore, in addition to the method of eliminating obesity that requires exercise, there are many other methods of eliminating obesity, such as nutritional methods using natural food ingredients and non-degradable ingredients, and physical methods such as surgery. Has been proposed.

また、 肥満を防止する方法も数多く提案されているが、 これらの多くは、 非消 化性の食物または低力口リ一食物を摂取することによる、 カロリ一摂取量の抑制 をその原理とするものであり、 この点において、 肥満の解消方法と変わるところ がない。 発明の開示  Many methods for preventing obesity have also been proposed, but most of them are based on the suppression of caloric intake by ingesting non-extinguishing foods or low-strength foods. In this respect, there is no difference from the method of eliminating obesity. Disclosure of the invention

本発明者らは、 ピオチンの生理学的役割についての研究過程において、 ビォチ ンを投与したモデル動物の体重増加率が有意に抑制されることを見出し、 係る知 見を基に本発明を完成した。  The present inventors have found that in the course of a study on the physiological role of biotin, the rate of weight gain of a model animal to which biotin was administered was significantly suppressed, and completed the present invention based on such findings.

即ち本発明は、 ピオチンを有効成分とすることを特徴とする肥満防止剤である。 ピオチンはビタミン Hとして知られる補酵素の一種であり、 生体内の 4種の力 ルポキシラーゼの必須の補酵素として作用していることがよく知られている。 ま た、 生理作用としては、 細胞増殖や D N A合成に対する影響が報告されており、 またピオチンの欠乏により、 皮膚炎や脱毛、 運動失調症など多岐に渡る研究報告 も為されている。 That is, the present invention is an antiobesity agent characterized by using biotin as an active ingredient. Pyotin is a type of coenzyme known as vitamin H. It is well known that it acts as an essential coenzyme of lupoxylase. In terms of physiological effects, effects on cell growth and DNA synthesis have been reported, and a wide variety of research reports have been made on deficiency of biotin, including dermatitis, hair loss, and ataxia.

本発明者らは、 ピオチンの生理学的役割についての研究過程において、 ビォチ ンを含ませた高カロリー食を摂餌させたラッ卜の体重増加率が、 ピオチンを含ま ない高カロリー食を摂取させたラッ卜のそれに比べ、 有意に低下していることを 見出した。 さらに摂餌中のピオチン量を変化させて体重増加率との相関を調べた ところ、 ピオチンの摂取量に比例して体重増加率も低下することが認められたの である。  In the course of the study on the physiological role of biotin, the present inventors found that rats fed a high-calorie diet containing biotin showed an increase in body weight, and a high-calorie diet without biotin was consumed. It was found to be significantly lower than that of rats. Furthermore, when the correlation with the rate of body weight gain was examined by changing the amount of biotin in the diet, it was found that the rate of body weight gain also decreased in proportion to the amount of biotin taken.

このことは、 高カロり一食を摂取することによる好ましくない体重増加をピオ チンが有意に抑制すること、 すなわちピオチンが肥満防止効果を有することを示 していると考えられる。 即ち、 本発明のいう肥満防止とは、 上述のように、 カロ リーの過剰摂取時に見られる好ましくない体重増加を抑制する効果をいう。  This is considered to indicate that biotin significantly suppresses undesired weight gain caused by ingesting a high calorie single meal, ie, that biotin has an obesity-preventing effect. That is, the prevention of obesity according to the present invention refers to an effect of suppressing an undesired increase in weight that is observed when calories are excessively consumed, as described above.

ピオチンの肥満防止効果、 すなわちカロリーの過剰摂取時に見られる好ましく ない体重増加量の抑制効果に関する生理学的機作については、 いまだ不明な点が 多い。 本発明者らは、 ラットにピオチンを摂取させることにより、 糖代謝の律速 酵素とされている肝臓ダルコキナーゼ活性が上昇することを確認している。 また、 ピオチンが補酵素として作用することにより、 トリカルボン酸サイクル (T C A サイクル) の代謝が活発になることも予想されることから、 体内グルコースの好 気的代謝が、 ピオチンの摂取により促進されるものと考えられる。 その結果、 貯 蔵脂肪の合成が低下し、 貯蔵脂肪の増加による肥満には至らないものと推察され る。  There is still much to be understood about the physiological mechanism of the effect of biotin on obesity, that is, the effect of suppressing unwanted body weight gain during caloric overdose. The present inventors have confirmed that when rats are ingested with biotin, the activity of hepatic dalcokinase, which is a rate-limiting enzyme for glucose metabolism, increases. In addition, since the metabolism of the tricarboxylic acid cycle (TCA cycle) is expected to be activated by the action of biotin as a coenzyme, the aerobic metabolism of glucose in the body is promoted by ingestion of biotin. it is conceivable that. As a result, it is presumed that the synthesis of stored fats decreases and obesity does not result from the increase in stored fats.

本発明における肥満防止剤は、 経口的に摂取可能な剤型であれば、 固形剤、 液 剤何れの形態でも調製することができる。 ピオチンを含有した固形剤の調製では、 散剤、 顆粒剤、 錠剤いずれの剤型でも、 それぞれ一般的な製造方法により調製す ることができる。 また、 液剤の調製もまた、 一般的に汎用される基剤や有効成分 と配合して調製することができる。  The antiobesity agent of the present invention can be prepared in the form of a solid preparation or a liquid preparation as long as it can be taken orally. In the preparation of a solid preparation containing biotin, any of powder, granule and tablet forms can be prepared by a general production method. Liquid preparations can also be prepared by mixing with commonly used bases and active ingredients.

本発明における肥満防止効果を発揮させるためには、 ピオチンの摂取量は成人 1日当たり 2 0 0 g以上、 好ましくは 4 0 0 g以上であることが好ましい。 2 0 0 X gを下回る摂取量では、 ピオチンの体重増加抑制効果が十分には発揮さ れない。 産業上の利用可能性 In order to exert the anti-obesity effect of the present invention, the intake of It is preferably at least 200 g, preferably at least 400 g per day. With an intake of less than 200 X g, the effect of biotin on suppressing weight gain is not fully exerted. Industrial applicability

本発明によれば、 従来のエネルギー摂取抑制とその原理を異にする、 新たな肥 満防止剤を提供することができる。 発明を実施するための最良の形態  According to the present invention, it is possible to provide a new anti-fertility agent having a different principle from that of conventional energy intake suppression. BEST MODE FOR CARRYING OUT THE INVENTION

以下に実施例を示し、 本発明を具体的に説明するが、 本発明は下記の実施例に 制限されるものではない。  Hereinafter, the present invention will be described specifically with reference to Examples, but the present invention is not limited to the following Examples.

実施例 1 Example 1

鹿糖 6 0 g  60 g of cane sugar

卵白 2 0 g  20 g of egg white

大豆油 6 g  6 g soybean oil

無機塩混合物 6 g  6 g of inorganic salt mixture

ビタミン混合物 2 g  2 g of vitamin mixture

結晶セルロース 6 g  Crystalline cellulose 6 g

ピオチン 2 0 0 g  Piotin 200 g

全量 1 0 0 g  100 g

結晶セルロースとピオチンを予め均一に混合した後、 その他の成分を追加混合, 造粒して高カロリー型顆粒剤を調製した。  After preliminarily mixing crystalline cellulose and biotin, the other components were additionally mixed and granulated to prepare a high calorie granule.

実施例 2 Example 2

鹿糖 6 0 g  60 g of cane sugar

卵白 2 0 g  20 g of egg white

大豆油 6 g  6 g soybean oil

無機塩混合物 6 g  6 g of inorganic salt mixture

ビタミン混合物 2 g  2 g of vitamin mixture

結晶セルロース 6 g ピオチン 7 5 0 g Crystalline cellulose 6 g Piotin 7 500 g

全量 1 0 0 g  100 g

結晶セルロースとピオチンを予め均一に混合した後、 その他の成分を追加混合、 造粒して高カロリー型顆粒剤を調製した。  After microcrystalline cellulose and biotin were uniformly mixed in advance, other components were additionally mixed and granulated to prepare a high calorie granule.

比較例 Comparative example

蔗糖 6 0 g  60 g sucrose

卵白 2 0 g  20 g of egg white

大豆油 6 g  6 g soybean oil

無機塩混合物 6 g  6 g of inorganic salt mixture

ビタミン混合物 2 g  2 g of vitamin mixture

結晶セルロース 6 g  Crystalline cellulose 6 g

ピオチン 1 5 0 g  Piotin 150 g

全量 1 0 0 g  100 g

結晶セルロースとピオチンを予め均一に混合した後、 その他の成分を追加混合、 造粒して高カロリー型顆粒剤を調製した。  After microcrystalline cellulose and biotin were uniformly mixed in advance, other components were additionally mixed and granulated to prepare a high calorie granule.

試験例 Test example

S Dラッ卜 (ォス) 体重 4 0 0 gを用いて以下の試験を行った。 各 6頭ずつ 3 群に分け、 実施例 1、 実施例 2、 および比較例 1の餌をそれぞれ 1 0 g Z日摂餌 させた。 各餌に配合される蛋白源である卵白はピオチンを吸着する性質を有して いるため、 卵白 2 O m gに吸着されるピオチン 1 5 0 gを添加した比較例を、 ピオチン量のブランクとした。 従って、 各実施例に含まれる有効ピオチン量は、 実施例 1が 5 0 g / 1 0 0 g餌、 実施例 2では 6 0 0 z g / 1 0 0 g餌にそれ ぞれ相当する。  The following test was performed using an SD rat (oss) body weight of 400 g. The animals of Example 1, Example 2, and Comparative Example 1 were each fed 10 g Z days each in three groups of six animals each. Since egg white, which is a protein source in each diet, has the property of adsorbing biotin, the comparative example in which 150 g of biotin adsorbed on 2 O mg of egg white was added was used as a blank for the amount of biotin. . Therefore, the amount of effective biotin contained in each example is equivalent to 50 g / 100 g of the bait in Example 1 and to 600 g / 100 g of the bait in Example 2.

実施例 1、 実施例 2、 および比較例に示した餌を与えつつ、 8 0日間3 0ラッ トを飼育し、 その間の体重増加量ならびに摂取量を測定した。 その結果、 摂取量 は実施例 2の餌を与えた群で有意に増加した (第 1図) にもかかわらず、 体重増 加量はピオチン摂餌量の増加に伴い、 抑制されることが示された (第 2図) 。 図面の簡単な説明 第 1図は、 試験開始後 6 0日目から 7 0日目における、 各 S Dラッ卜群の実施 例および比較例の顆粒剤の平均食餌量を示す。 グラフ上の縦線は標準偏差を示し ている。 While feeding the diets shown in Example 1, Example 2, and Comparative Example, 30 rats were bred for 80 days, and weight gain and intake during that period were measured. As a result, although the intake was significantly increased in the group fed the diet of Example 2 (Fig. 1), it was shown that the weight gain was suppressed with an increase in the amount of biotin consumed. (Figure 2). BRIEF DESCRIPTION OF THE FIGURES FIG. 1 shows the average food consumption of the granules of Examples and Comparative Examples in each SD rat group from day 60 to day 70 after the start of the test. The vertical line on the graph indicates the standard deviation.

第 2図は、 ピオチンを摂食させた S Dラッ卜の 7 0日間の平均体重の増加量を 示したグラフであり、 縦軸は体重増加量、 横軸は実験期間 (週) である。 また、 〇は比較例 1、 △は実施例 1、 口は実施例 2の各顆粒剤を用いたときの結果であ る。  FIG. 2 is a graph showing the average weight gain of the SD rats fed with biotin for 70 days, in which the vertical axis represents the weight gain and the horizontal axis represents the experimental period (weeks). In addition, 〇 indicates the results when the granules of Comparative Example 1 were used, Δ indicates the results when the granules of Example 1 were used, and 口 indicates the results when the granules of Example 2 were used.

Claims

請 求 の 範 囲 The scope of the claims 1. ピオチンを有効成分とすることを特徴とする肥満防止剤 1. An anti-obesity agent characterized by using biotin as an active ingredient
PCT/JP1999/001748 1997-10-08 1999-04-02 Obesity preventives Ceased WO2000059507A1 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP9276089A JPH11116478A (en) 1997-10-08 1997-10-08 Antiobesity agent
AU29614/99A AU2961499A (en) 1997-10-08 1999-04-02 Obesity preventives
PCT/JP1999/001748 WO2000059507A1 (en) 1997-10-08 1999-04-02 Obesity preventives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP9276089A JPH11116478A (en) 1997-10-08 1997-10-08 Antiobesity agent
PCT/JP1999/001748 WO2000059507A1 (en) 1997-10-08 1999-04-02 Obesity preventives

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US8962015B2 (en) 2007-09-28 2015-02-24 Sdg, Inc. Orally bioavailable lipid-based constructs
US9145453B2 (en) * 2007-09-28 2015-09-29 Sdg, Inc. Orally bioavailable lipid-based constructs
US20100080773A1 (en) 2008-09-26 2010-04-01 Sdg, Inc. Orally Bioavailable Lipid-Based Constructs
US8846053B2 (en) * 2008-09-26 2014-09-30 Sdg, Inc. Orally bioavailable lipid-based constructs
AU2018236190B2 (en) 2017-03-13 2025-02-20 Sdg, Inc. Lipid-based nanoparticles with enhanced stability
US11077173B2 (en) 2017-03-13 2021-08-03 Sdg, Inc. Lipid-based nanoparticles and methods using same

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JPH05192090A (en) * 1991-12-04 1993-08-03 Norin Suisansyo Kyushu Nogyo Shikenjo Method for feeding vitamin b group to monogastric animals
JPH0995448A (en) * 1995-09-29 1997-04-08 Calpis Food Ind Co Ltd:The Method for increasing blood biotin concentration and biotin-containing food and drink

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
JPH05192090A (en) * 1991-12-04 1993-08-03 Norin Suisansyo Kyushu Nogyo Shikenjo Method for feeding vitamin b group to monogastric animals
JPH0995448A (en) * 1995-09-29 1997-04-08 Calpis Food Ind Co Ltd:The Method for increasing blood biotin concentration and biotin-containing food and drink

Non-Patent Citations (1)

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Title
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AU2961499A (en) 2000-10-23

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