JP2004035516A - Lipolysis-promoting agent and skin cosmetic for slimming - Google Patents

Lipolysis-promoting agent and skin cosmetic for slimming Download PDF

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JP2004035516A
JP2004035516A JP2002198139A JP2002198139A JP2004035516A JP 2004035516 A JP2004035516 A JP 2004035516A JP 2002198139 A JP2002198139 A JP 2002198139A JP 2002198139 A JP2002198139 A JP 2002198139A JP 2004035516 A JP2004035516 A JP 2004035516A
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extract
lipolysis
slimming
larrea
present
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JP3755819B2 (en
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Tomohiro Terauchi
寺内友広
Mikito Ihara
伊原幹人
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Naris Cosmetics Co Ltd
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Naris Cosmetics Co Ltd
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Abstract

<P>PROBLEM TO BE SOLVED: To obtain a lipolysis-promoting agent effective in improvement of inclination to obesty constitution by promoting decrease in systemic or topical adipose tissues, suppression or prevention of obesity by preventing increase in the tissues, and to prepare a skin cosmetic for slimming containing the lipolysis-promoting agent. <P>SOLUTION: The lipolysis-promoting agent comprises an extract of a plant of the genus Larrea of the family Zygophyllaceae. The skin cosmetic for slimming is obtained by formulating the extract as an active ingredient. Particularly, the skin cosmetic for slimming is obtained by formulating the extract of the plant of the genus Larrea of the family Zygophyllaceae with other specific ingredient as active ingredients. <P>COPYRIGHT: (C)2004,JPO

Description

【0001】
【産業上の利用分野】本発明は、脂肪分解促進剤に関し、詳しくはハマビシ科(Zygophyllaceae)ラレア属(Larrea)植物の抽出物を有効成分として含有することを特徴とした痩身用皮膚化粧料に関する。
【0002】
【従来の技術】体内の脂肪は消費エネルギーに対し、過剰分の摂取エネルギーが、白色脂肪細胞の中性脂肪として蓄積して生じる物である。体脂肪としての蓄積が大きい肥満は、美容上好ましくないばかりでなく、動脈硬化等の様々な疾病を引き起こす。最近は、過食、運動不足、及びストレス等による肥満が増加しており、特に女性は外見上からもスリムな引き締まった体を切望する傾向にある。
【0003】従来、顔や体の余分な脂肪を減らし、引き締まった体を保つために、各種運動や食事制限に加え、体内の新陳代謝を促すようなマッサージ用ジェルやクリーム等の化粧料を用いることが知られている。このような化粧料には、脂肪を構成している脂肪細胞の脂質分解を促進し、痩身効果を有しめることを目的としてカフェインのような脂質分解促進剤を配合しているものもある。脂肪分解を促す物質としてはカフェインの他、植物抽出液として、茶抽出物、コラ抽出物等が知られているが、いずれも充分な効果を有するものではなく、より一層効果の高い脂質分解促進物質の開発が望まれていた。また、皮下脂肪等の蓄積は、健康上も好ましくなく、皮下脂肪等の減少、あるいは蓄積の防止が重要な問題となっている。このため、食欲抑制剤等の経口薬、食事制限および運動等によるアプローチが種々なされているが、皮下脂肪等を抑制または減少させる満足な効果を有する脂肪分解促進剤および痩身用皮膚化粧料は見出されてはいなかった。
【0004】
【発明が解決しようとする課題】従って、本発明の目的は、脂肪細胞の脂肪分解を促進し、優れた痩身効果を与える脂質分解促進剤を提供することにある。
【0005】
【課題を解決するための手段】本発明者らは上記課題を達成するために鋭意研究した結果、ハマビシ科(Zygophyllaceae)ラレア属(Larrea)植物より抽出された抽出物に脂肪細胞の脂質分解を促進する効果を見い出し、特定の成分とを組み合わせるとにより脂質分解促進効果さらに高まることを発見し、本発明を完成するに至った。
【0006】すなわち本発明は、ハマビシ科(Zygophyllaceae)ラレア属(Larrea)植物の抽出物よりなることを特徴とする脂質分解促進剤、および前記抽出物を有効成分として配合することを特徴とする痩身用皮膚外用剤である。本発明の脂肪分解促進剤には、外用剤、注入剤、経口薬等の他、一般食品としてそのまま用いるものや、添加物として用いるものも含まれる。
【0007】以下、本発明の構成について詳述する。本発明で用いられるハマビシ科(Zygophyllaceae)ラレア属(Larrea)植物の抽出物は、座瘡による丘疹形成や膿疱形成の防止作用があることはすでに知られている(特表平5−507069号公報)、しかしながら、ハマビシ科(Zygophyllaceae)ラレア属(Larrea)植物の抽出物の有する脂肪細胞の脂質分解促進作用については今までに知られてはいなかった。
【0008】
【発明の実施の形態】
以下、本発明の構成について詳述する。本発明に述べるハマビシ科(Zygophyllaceae)ラレア属(Larrea)植物は、米国南部から中米にかけて見られる常緑の小低木で、開花期には黄色の花を咲かせる。また、クレオソート樹(Creosote Bush)あるいは Desert Shrubとも称され、その葉や小枝を煎じたものはチャパラ茶(chapparal)として知られる。このラレア属(Larrea)植物には、Larrea tridentata,L. divaricata,L. mexicanaなどが知られ、このうち特に好ましいものは、メキシコにおいて生薬 Gobernadoraとして重用されている Larrea tridentataである。
【0009】本発明の抽出物にはラレア属(Larrea)植物の枝、葉、花、根、種子などいずれの部位を用いても構わないが、簡便に利用するには全草を用いると良い。本発明のラレア属植物抽出物としては、ラレア属植物を溶媒、例えば水、低級アルコール、含水低級アルコール、プロピレングリコール、1,3−ブチレングリコール、ブタノール等の極性溶媒またはクロロホルム、ジクロルエタン、四塩化炭素、酢酸エチルエステル、エーテル等あるいはこれらの混合物の有機溶媒で抽出して得た抽出液をそのままあるいは濃縮したエキスを用いるか、エキスを吸着法、例えばイオン交換樹脂を用いて不純物を除去したものやポーラスポリマーのカラムにて吸着させた後メタノールまたはエタノールで溶出し、濃縮したエキスも使用できる。また分配法、例えば水/酢酸エチルで抽出した抽出物等も用いられる。
【0010】本発明におけるラレア属植物の抽出物の配合量は、乾燥物として0.000001〜10.0重量%。好ましくは、0.00001〜5.0重量%である。
【0011】本発明においてはハマビシ科(Zygophyllaceae)ラレア属(Larrea)から抽出された抽出物と、他の特定の成分とを併用することにより、脂質分解促進効果はより高められる。かかる成分としては、キサンチン誘導体、βアドレナリン作用興奮薬、α2アドレナリン作用抑制薬、海藻抽出物、茶抽出物、ツボクサ抽出物、ショウブ抽出物、サイコ抽出物から選ばれる一種または二種以上が好ましい。
【0012】本発明で用いられるキサンチン誘導体としては、例えば、キサンチン、アミノフィリン、テオフィリン、コリンテオフィリン、カフェイン、テオブロミン、1,7−ジメチルキサンチン、オクストリフィン、ジプロフィリン、プロキシフィリン等が挙げられる。これらは1種を単独で、または2種以上を組み合わせて用いることができる。これらのキサンチン誘導体は、合成または茶葉等の植物から実質的に単離されたものを使用することができる。
【0013】本発明で用いられる海藻抽出物は褐藻類、紅藻類、緑藻類の全藻から抽出されるものであり、抽出方法は特に限定されるものではなく、例えば水、アルコール等の親水性有機溶剤、あるいはそれらの混合液、またはグリセリン、1,3−ブチレングリコール等の多価アルコール、あるいは水と多価アルコールとの混合液により抽出される。
【0014】本発明で用いられるβアドレナリン作用興奮剤は特に限定されず、例えばイソプロテレノール、エピネフリン、ノルエピネフリン、ドブタミン、ドパミン、ブトパミン、サルブタモール、テルブタリン、イソエタリン、プロトキロール、フェノテロール、メタプロテレノール、クロルプレナリン、ヘキソプレナリン、トリメトキノール、塩酸プロカテロール、プレナルテロール、フォルスコリン、ジソジウム(R,R)−5−〔2−〔〔2−(3−クロロフェニル)−2−ヒドロキシエチル〕−アミノ〕プロピル〕−1,3−ベンゾジオキソール−2,2−ジカルボキシレート、(R,R)−4−〔2−({2−〔(3−クロロフェニル)−2−ヒドロキシエチル〕アミノ}プロピル)フェニル〕フェノキシ酢酸、{2−ヒドロキシ−5−〔2−({2−ヒドロキシ−3−〔4−(1−メチル−4−トリフルオロメチル)−1H−イミダゾール−2−イル〕フェノキシ}プロピル)アミノ〕エトキシ}−ベンズアミドモノメタンスルフォネート、エリスロ−DL−1−(7−メチルインダン−4−イロキシ)−3−イソプロピルアミノブタン−2−オールおよびこれらの薬理的に許容される塩等が挙げられる。薬理的に許容される塩としては、薬理的に許容される酸付加塩、金属塩、アンモニウム塩、有機アミン付加塩、アミノ酸付加塩等が挙げられる。本発明においては、イソプロテレノール、ドブタミン、サルブタモールおよびこれらの薬理的に許容される塩からなる群から選ばれる一種または二種以上を用いることが好ましく、この場合の塩としては塩酸塩や硫酸塩が好ましい。
【0015】本発明で用いられるα2アドレナリン作用抑制剤は特に限定されず、例えばヨヒンビン、フェントラミン、フェノキシベンザミン、トラゾリン、エルゴタミン、エルゴトキシン、ジヒドロエルゴタミン、エルゴメトリン、メチルエルゴメトリン、ジヒドロエルゴトキシン、ラウオルシン、ピペロキサンおよびこれらの薬理的に許容される塩等が挙げられる。薬理的に許容される塩としては、上記と同様のものが挙げられる。本発明においては、ヨヒンビン、フェントラミン、エルゴタミンおよびこれらの薬理的に許容される塩からなる群から選ばれる一種または二種以上を用いることが好ましく、この場合の塩としてはメシル酸塩や酒石酸塩、塩酸塩が好ましい。
【0016】サイコ抽出物としては、ミシマサイコ、マンシュウミシマサイコ、ダフリカサイコ等の抽出物が挙げられ、茶抽出物としては、緑茶、烏龍茶等の抽出物が挙げられる。その他の抽出物についても、抽出方法は特に限定されるものではなく、例えば水、アルコール等の親水性有機溶剤、あるいはそれらの混合液、またはグリセリン、1,3−ブチレングリコール等の多価アルコール、あるいは水と多価アルコールとの混合液により抽出される。これらは適宜濃縮、精製、滅菌、乾燥等を施して使用される。
【0017】上記成分の配合量は、乾燥物換算で0.001〜30.0重量%、好ましくは0.01〜10.0重量%である。
【0018】この発明にかかる脂肪分解促進剤および痩身用皮膚外用剤の各種有効成分の配合量(含有量)は、前記有効成分の種類および/またはその組合せ、ならびにその使用目的、態様、使用形態、使用回数等々に応じて変動させることができるので、特に限定されない。原則的には、有効量存在すればよいことになる。この発明にかかる有効成分は1種類でも作用効果を発揮することができるが、2種類以上の有効成分を適宜組み合わせて利用することより、優れた相乗効果を奏することができる。
【0019】また、本発明の脂肪分解促進剤および皮膚外用剤組成物には、外用剤として用いる場合、上記成分の他に医薬品や化粧品の各種製剤において使用されている界面活性剤、油性成分、保湿剤、高分子化合物、紫外線吸収剤、抗炎症剤、殺菌剤、酸化防止剤、金属イオン封鎖剤、防腐剤、ビタミン類、色素、香料等を配合することができる。外用剤以外に用いる場合でも、効果を損なわない範囲であれば抗炎症剤、酸化防止剤、防腐剤、ビタミン類、色素、香料等を配合することができる。
【0020】本発明の脂肪分解促進剤は、例えば、食品、経口投与薬、皮膚化粧料等に配合することができ、また痩身用皮膚化粧料の剤型は特に限定されるものではなく、皮膚塗布用、浴用、洗浄用等のクリーム、乳液、ジェル、スティック、シート、パップ、軟膏、オイル、ワックス、ゾル、ゲル、パウダー、スプレー、液体、顆粒等とすることができる。食品、経口投与薬等に用いる場合では、液体、錠剤、顆粒、粉末、カプセル等にすることや、一般の食品に添加物として用いることも出来る。
【0021】
【実施例】次に、実施例により本発明を更に詳細に説明するが、本発明は、これらの実施例により制限されるものではない。なお、実施例中の部は、特に断りのない限り重量部を示す。
【0022】1.抽出物の調製例
(1)調製例1(水抽出物)
前記各植物の原体2〜5gを円筒濾紙に入れ、イオン交換水50〜100mLに浸し、60℃で8時間加熱抽出してロ液を得た。この操作を3回繰り返し、全てのロ液を合せて凍結乾燥して各植物の水抽出物を得た。
【0023】
(2)調製例2(各種低級アルコール抽出物)
抽出溶媒に各種低級アルコールを用い、ソックスレー抽出器を用いて8時間抽出した後、溶媒を留去、抽出物を粉末にして各植物の各種低級アルコール抽出物を得た。
【0024】(3)調製例3(各種有機溶媒または有機溶媒水溶液抽出物)
前記水抽出物における抽出操作において、水の代わりに各種有機溶媒または有機溶媒水溶液を使用した。全ての抽出液を合せて可能な限り溶媒を留去、濃縮した後、凍結乾燥して各植物の各種有機溶媒または有機溶媒水溶液抽出物を得た。
【0025】2.脂肪合成促進効果の測定方法
まず、(1)10容量%CS含有DMEM培地、(2)分化誘導培地を調製する。
(1)10 容量% CS 含有 DMEM 培地:DMEM培地(ICN Biomedicals 社製)13.48gに蒸留水1L加え、それぞれ終濃度10容量%CS (CALF BOVINE SERUM)、0.1重量%炭酸水素ナトリウム、70mg/Lストレプトマイシン硫酸塩および70mg/Lベンジルペニシリンカリウムを添加して調製する。
【0026】(2)分化誘導培地:DMEM培地(ICN Biomedicals 社製)13.48gに蒸留水1L加え、それぞれ終濃度10容量%CS (CALF BOVINE SERUM)、10μg/mLインシュリン、0.5mM 1−メチル−3−イソブチルキサンチン(MIX)、0.25μM デキサメサゾン、0.1重量%炭酸水素ナトリウム、100mg/Lストレプトマイシン硫酸塩および70mg/Lベンジルペニシリンカリウムを添加して調製する。
【0027】マウス由来の前駆脂肪細胞3T3−L1を6穴マルチプレートを用いて10%牛胎児血清を含むDME培地(ダルベッコ変法イーグル培地)で37℃で培養した。なお、培地は2〜3日毎に交換した。Confluent後、培養液を吸引除去し、PBS(−)で細胞を1回洗浄した後、分化誘導培地を加え、2日間分化誘導/培養し、脂肪細胞へと分化させた。その後は元の培地で培養を続けた。約1週間後、脂肪細胞へ分化した3T3−L1細胞に各供試料添加溶液2mLを加え、培養し、1日(24時間)後に培地中のグリセロール量を脂肪分解の指標として定量した。培地中に遊離したグリセロール量を酵素法(ベーリンガー・マンハイム社製
F−キット;グリセロール)にて測定する。尚、測定は5回行いその平均値で示す。
【0028】各植物試料(純分約1重量%)を、10容量%CS含有DMEM培地で希釈して1容量%供試料添加溶液(純分約0.1mg/mL)とした。また、有効成分の併用においては1容量%供試料添加溶液(純分約0.1mg/mL)を1:1で混合し、2mlとし添加した。なお、ブランクとして10容量%CS含有DMEM培地、陽性対照としてカフェイン、エピネフリン、ヨヒンビン(純分約0.01mg/mL)を試験に供した。
【0029】この発明にかかる各種抽出物の脂肪分解促進効果は、数1により脂肪分解促進率(%)を算出して表した。結果は表1に示した。
【0035】
【数1】

Figure 2004035516
【0036】
【表1】
Figure 2004035516
【0037】表1からハマビシ科(Zygophyllaceae)ラレア属(Larrea)植物には脂質分解を促進する効果があり、さらに本抽出物と特定成分を組み合わせにより飛躍的に脂質分解が促進されることがわかる。
【0038】3.化粧料の処方例
次に、この発明にかかる各植物の各種抽出物を用いて、本発明にかかる化粧料を作製した。なお、配合割合は重量部である。
【0039】(1)処方例1(化粧水)
<組成>(重量%)
larrea divaricata抽出物…0.2
グリセリン…5.0
ポリオキシエチレンソルビタンモノラウレート(20E.O)…1.5
精製水…残部
エタノール…10.0
防腐剤…適量
〔製法〕前記原料を精製水に加え均一に混合する。
【0040】(2)処方例2(化粧用クリーム)
<組成>(重量%)
[油相]
ミツロウ…2.0
ステアリルアルコール…5.0
ステアリン酸…8.0
スクワラン…10.0
自己乳化型グリセリルモノステアレート…3.0
ポリオコシエチレンセトリエーテル(20E.0)…1.0
[水相]
Larrea tridentata抽出物…0.2
精製水…残部
1,3−ブチレングリコール…5.0
防腐剤…適量
〔製法〕前記水相の原料を混合し、加熱して70℃に保ち水相部とする。一方、油相の原料を混合し、加熱溶解して70℃として油相部とする。この油相部を前述の水相部に加えて予備乳化を行ない、ホモミキサー均一に乳化し、30℃まで冷却し化粧用クリームを得る。
【0041】(3)処方例3(化粧用乳液)
<組成>(重量%)
[油相]
スクワラン…8.0
ワセリン…2.0
ミツロウ…0.5
ソルビタンセスキオレート…0.8
ポリオキシエチレンセチルエーテル(20E.O)…1.2
[水相]
Larrea
divaricata抽出物…0.1
カフェイン…2.0
ミシマサイコ抽出物…0.2
カルボキシビニルポリマー…0.5
1,3−ブチレングリコール…0.5
水酸化カリウム…0.1
精製水…残部
エタノール…7.0
防腐剤…適量
〔製法〕前記水相の原料を混合し、加熱して70℃に保ち水相部とする。一方、他の原料を混合し、加熱溶解して70℃として油相部とする。この油相部を前述の水相部に加えて乳化し、30℃まで冷却し化粧用乳液を得る。
【0042】(4)処方例4(パック剤)
<組成> (重量%)
[粉体]
酸化チタン…8.0
カオリン…7.0
[油相]
オリーブ油…3.0
[水相]
Larrea
divaricata抽出物…0.5
酢酸ビニル樹脂エマルジョン…15.0
ポリビニルアルコール…10.0
精製水…残部
グリセリン…5.0
エタノール…5.0
防腐剤…適量
〔製法〕水相の原料を混合し、均一にする。さらに他の原料を混合し、均一になるまで攪拌してパック剤を得る。
【0043】(5)処方例5(クリーム状ファンデーション)
<組成>             (重量部)
[粉体]
タルク…5.0
セリサイト…8.0
酸化チタン…5.0
色顔料…1.5
[油相]
モノイソステアリン酸ポリグリセリル…3.0
ポリオキシエチレン硬化ヒマシ油…1.5
イソノナン酸イソトリデシル…10.0
[水相]
Larrea
tridentata抽出物…0.3
精製水…残部
1,3−ブチレングリコール…5.0
防腐剤…適量
〔製法〕油相の一部と粉体を3本ロールミルにかけ、残りの油相を加え加熱溶解させ、80℃に保つ。次に、加熱溶解した水相を徐々に加えて80℃で乳化し、これを攪拌しながら室温まで冷却して、クリーム状ファンデーションを得る。
【0044】4.化粧料の効果試験例
さらに、この発明にかかる化粧料を用いて、実際に使用した場合の効果について検討を行った。
【0045】処方例3の効果試験を実施した。処方例3を実施例12とする。対照としてLarrea divaricata抽出物、カフェイン、ミシマサイコ抽出物を除いたプラセボ乳液を同様な方法にて処方したものを比較例10として用いた。
【0046】ヒトによる効果試験[評価方法]20〜40代女性20人ずつに前記実施例12および比較例10の処方の乳液を全身に朝晩塗布してもらい、1ヵ月連用してもらった。連用前後の体重および体脂肪率(体全体に対する脂肪の割合)を生体インピーダンス測定を原理とする測定器(体重計付き体脂肪計、タニタ社製)により測定した。使用前、使用後の体重および体脂肪率の平均値を求めた。その結果を表2に示す。
【0047】
【表2】
Figure 2004035516
【0048】上記の結果より明らかなように、本発明品である実施例12を用いた場合は、使用前に比べて体重は微減少であったが体脂肪率の減少は顕著であった。比較例10ではほとんど減少がみられなかった。
【0049】次に、この発明にかかる各植物の各種抽出物を用いて、本発明にかかる食品・経口投与薬への処方を作製した。なお、配合割合は重量部である。
【0050】処方例6(錠剤)
Larrea
divaricata抽出物(乾燥物)…0.1
結晶セルロース…20.0
乳糖…76.9
ショ糖脂肪酸エステル…3.0
[製法]前記原料を混合して打錠する。
【0051】処方例7(カプセル)
Larrea
divaricata抽出物…0.5
カフェイン…1.0
ミシマサイコ抽出物…0.5
グルコース…残部
[製法]前記原料を混合してカプセルに成形する。
【0052】処方例8(ドリンク剤)
Larrea
divaricata抽出物…10.0
グルコース…5.0
酸化防止剤…適量
精製水…残部
【0053】処方例8のドリンクを用いて効果試験を実施した。処方例8を実施例13とする。対照としてLarrea divaricata抽出物を除いて精製水に置き換えたものを比較例11として用いた。
【0054】ヒトによる効果試験[評価方法]20〜40代女性20人ずつに前記実施例13および比較例11の処方のドリンクを朝晩服用してもらい、1ヵ月連用してもらった。連用前後の体重および体脂肪率(体全体に対する脂肪の割合)を生体インピーダンス測定を原理とする測定器(体重計付き体脂肪計、タニタ社製)により測定した。使用前、使用後の体重および体脂肪率の平均値を求めた。その結果を表3に示す。
【0055】
【表3】
Figure 2004035516
【0056】
【発明の効果】以上記載したように、本発明が、全身もしくは局所の脂肪組織を減少させ、肥満の抑制または防止、肥満体質の改善に有効な脂肪分解促進剤、および該効果を有する痩身用皮膚化粧料を提供できることは明らかである。[0001]
BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a lipolysis accelerator, and more particularly, to a skin cosmetic for slimming, which comprises an extract of a plant belonging to the genus Zygophyllaceae (Larrea) as an active ingredient. .
[0002]
2. Description of the Related Art Fat in the body is produced by storing excess energy as neutral fat in white adipocytes with respect to consumed energy. Obesity, which has a large accumulation as body fat, is not only cosmetically undesirable, but also causes various diseases such as arteriosclerosis. In recent years, obesity due to overeating, lack of exercise, stress, and the like has been increasing, and in particular, women tend to crave a slim and lean body from the appearance.
[0003] Conventionally, in order to reduce excess fat on the face and body and maintain a firm body, in addition to various exercises and dietary restrictions, the use of cosmetics such as massage gels and creams that promote metabolism in the body has been used. It has been known. Some of such cosmetics contain a lipolysis accelerator such as caffeine for the purpose of promoting lipolysis of fat cells constituting fat and having a slimming effect. In addition to caffeine as a substance that promotes lipolysis, tea extracts and kola extracts are known as plant extracts, but none of them have a sufficient effect, and more effective lipolysis. The development of accelerators was desired. In addition, accumulation of subcutaneous fat and the like is not preferable from the viewpoint of health, and reduction of subcutaneous fat and the prevention of accumulation are important issues. For this reason, there have been various approaches using oral drugs such as appetite suppressants, dietary restrictions, and exercise. It was not served.
[0004]
SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide a lipolysis promoter which promotes lipolysis of fat cells and provides an excellent slimming effect.
[0005]
Means for Solving the Problems The present inventors have made intensive studies to achieve the above object, and as a result, the extract extracted from plants of the genus Zygophyllaceae Larrea (Larrea) is subjected to lipid decomposition of adipocytes. The present inventors have found an effect of promoting the effect, and found that a combination with a specific component further enhances the effect of promoting lipid degradation, thereby completing the present invention.
That is, the present invention provides a lipolysis accelerator characterized by comprising an extract of a plant belonging to the genus Zygophyllaceae (Larrea), and a slimming composition comprising the extract as an active ingredient. An external preparation for skin. The lipolysis promoter of the present invention includes those used as a general food as well as those used as additives, in addition to external preparations, injections, oral drugs, and the like.
Hereinafter, the configuration of the present invention will be described in detail. It is already known that the extract of the plant belonging to the genus Zygophyllaceae (Larrea) used in the present invention has an effect of preventing the formation of papules and pustules due to acne (Japanese Unexamined Patent Application Publication No. 5-50769). However, the effect of the extract of the plant belonging to the genus Zygophyllaceae Larrea (Larrea) on the lipolysis of fat cells has not been known so far.
[0008]
BEST MODE FOR CARRYING OUT THE INVENTION
Hereinafter, the configuration of the present invention will be described in detail. The Zygophyllaceae (Larrea) plant described in the present invention is an evergreen small shrub found from the southern United States to Central America, and blooms yellow flowers during flowering. It is also called Creosote Bush or Desert Shrub, and its leaves and twigs are known as chapara tea. The Larrea plant includes Larrea tridentata, L. et al. divaricata, L .; mexicana and the like, among which particularly preferred is Larrea tridentata, which is used heavily as a crude drug Gobernadora in Mexico.
The extract of the present invention may use any part such as branches, leaves, flowers, roots and seeds of a plant of the genus Larrea, but whole plants may be used for simple use. . As the extract of the plant belonging to the genus Larea of the present invention, a plant belonging to the genus Lalea in a solvent, for example, a polar solvent such as water, lower alcohol, hydrated lower alcohol, propylene glycol, 1,3-butylene glycol, butanol or chloroform, dichloroethane, carbon tetrachloride Extracts obtained by extracting an extract obtained by extracting an organic solvent of ethyl acetate, ether, ether, or the like or a mixture thereof as is or using an extract, or an extract obtained by removing impurities using an adsorption method, for example, an ion exchange resin, An extract which is adsorbed on a porous polymer column, eluted with methanol or ethanol, and then concentrated can also be used. In addition, a partitioning method, for example, an extract extracted with water / ethyl acetate and the like are also used.
The amount of the extract of the plant belonging to the genus Larea in the present invention is 0.000001 to 10.0% by weight as a dry matter. Preferably, it is 0.00001 to 5.0% by weight.
In the present invention, the combined use of an extract extracted from the genus Larrea (Zygophyllaceae) and other specific components further enhances the effect of promoting lipid degradation. As such a component, one or more selected from a xanthine derivative, a β-adrenergic stimulant, an α2-adrenergic inhibitor, a seaweed extract, a tea extract, a boxweed extract, a shobu extract, and a psycho extract are preferable.
The xanthine derivatives used in the present invention include, for example, xanthine, aminophylline, theophylline, choline theophylline, caffeine, theobromine, 1,7-dimethylxanthine, oxtrifin, diprofylline, proxyphilin and the like. These can be used alone or in combination of two or more. As these xanthine derivatives, those substantially synthesized or isolated from plants such as tea leaves can be used.
The seaweed extract used in the present invention is extracted from all algae of brown algae, red algae and green algae, and the extraction method is not particularly limited. Extraction is carried out with a solvent or a mixture thereof, a polyhydric alcohol such as glycerin or 1,3-butylene glycol, or a mixture of water and a polyhydric alcohol.
The β-adrenergic stimulant used in the present invention is not particularly limited. Chlorprenaline, hexoprenaline, trimethoquinol, procaterol hydrochloride, prenalterol, forskolin, disodium (R, R) -5- [2-[[2- (3-chlorophenyl) -2-hydroxyethyl] -amino] Propyl] -1,3-benzodioxole-2,2-dicarboxylate, (R, R) -4- [2-({2-[(3-chlorophenyl) -2-hydroxyethyl] amino} propyl ) Phenyl] phenoxyacetic acid, {2-hydro C-5- [2-({2-hydroxy-3- [4- (1-methyl-4-trifluoromethyl) -1H-imidazol-2-yl] phenoxy} propyl) amino] ethoxy} -benzamide monomethane Sulfonate, erythro-DL-1- (7-methylindan-4-yloxy) -3-isopropylaminobutan-2-ol, and pharmaceutically acceptable salts thereof. Pharmaceutically acceptable salts include pharmaceutically acceptable acid addition salts, metal salts, ammonium salts, organic amine addition salts, amino acid addition salts and the like. In the present invention, it is preferable to use one or two or more selected from the group consisting of isoproterenol, dobutamine, salbutamol and a pharmaceutically acceptable salt thereof, and in this case, the salt may be a hydrochloride or a sulfate. Is preferred.
The α2 adrenergic inhibitor used in the present invention is not particularly limited. And piperoxane and pharmaceutically acceptable salts thereof. Examples of the pharmacologically acceptable salt include the same as described above. In the present invention, it is preferable to use one or two or more selected from the group consisting of yohimbine, phentolamine, ergotamine and a pharmaceutically acceptable salt thereof, and in this case, the salt may be a mesylate salt or a tartrate salt. Hydrochloride is preferred.
Examples of the psycho extract include extracts of Mishima saiko, Manshu mishima saiko, dafurika saiko and the like, and tea extracts include extracts of green tea, oolong tea and the like. For other extracts, the extraction method is not particularly limited. For example, water, a hydrophilic organic solvent such as alcohol, or a mixture thereof, or glycerin, a polyhydric alcohol such as 1,3-butylene glycol, Alternatively, it is extracted with a mixture of water and a polyhydric alcohol. These are used after appropriately concentrating, purifying, sterilizing, drying and the like.
The amount of the above components is 0.001 to 30.0% by weight, preferably 0.01 to 10.0% by weight in terms of dry matter.
The amounts (contents) of the various active ingredients of the lipolysis promoter and slimming skin external preparation according to the present invention are determined according to the kind of the active ingredients and / or the combination thereof, and the purpose, mode and mode of use thereof. , Can be varied according to the number of times of use, etc., and is not particularly limited. In principle, an effective amount only needs to be present. Although the active ingredient according to the present invention can exert its function and effect even if it is one kind, an excellent synergistic effect can be exhibited by using two or more kinds of active ingredients in appropriate combination.
When used as an external preparation, the lipolysis accelerator and the external preparation for skin of the present invention, when used as an external preparation, include surfactants, oily components used in various pharmaceutical and cosmetic preparations, Moisturizers, polymer compounds, ultraviolet absorbers, anti-inflammatory agents, bactericides, antioxidants, sequestering agents, preservatives, vitamins, pigments, fragrances, and the like can be added. Even when used other than external preparations, anti-inflammatory agents, antioxidants, preservatives, vitamins, pigments, fragrances, and the like can be added as long as the effects are not impaired.
The lipolysis-promoting agent of the present invention can be incorporated, for example, into foods, orally administered drugs, skin cosmetics, etc. The form of skin cosmetics for slimming is not particularly limited. Creams, emulsions, gels, sticks, sheets, cataplasms, ointments, oils, waxes, sols, gels, powders, sprays, liquids, granules and the like for application, bathing, washing and the like can be used. When used in foods, orally administered drugs, etc., they can be made into liquids, tablets, granules, powders, capsules and the like, and can also be used as additives to general foods.
[0021]
EXAMPLES Next, the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples. In addition, the part in an Example shows a weight part unless there is particular notice.
1. Preparation Example of Extract (1) Preparation Example 1 (Water Extract)
2 to 5 g of the original substance of each plant was placed in a thimble filter paper, immersed in 50 to 100 mL of ion-exchanged water, and heated and extracted at 60 ° C. for 8 hours to obtain a filtrate. This operation was repeated three times, and all the liquids were combined and freeze-dried to obtain an aqueous extract of each plant.
[0023]
(2) Preparation example 2 (various lower alcohol extracts)
After extracting with various Soxhlet extractors using various lower alcohols as the extraction solvent, the solvent was distilled off, and the extract was powdered to obtain various lower alcohol extracts of each plant.
(3) Preparation Example 3 (Extracts of various organic solvents or aqueous solutions of organic solvents)
In the extraction operation of the water extract, various organic solvents or organic solvent aqueous solutions were used instead of water. All extracts were combined, the solvent was distilled off as much as possible, concentrated, and then freeze-dried to obtain various organic solvents or organic solvent aqueous extracts of each plant.
2. First, a (1) DMEM medium containing 10% by volume of CS and a (2) differentiation-inducing medium are prepared.
(1) DMEM medium containing 10 % by volume of CS : 1 L of distilled water was added to 13.48 g of DMEM medium (manufactured by ICN Biomedicals), and the final concentration was 10% by volume of CS (CALF BOVINE SERUM), 0.1% by weight of sodium hydrogen carbonate, Prepared by adding 70 mg / L streptomycin sulfate and 70 mg / L potassium benzylpenicillin.
(2) Differentiation induction medium : 1 L of distilled water was added to 13.48 g of DMEM medium (manufactured by ICN Biomedicals), and the final concentration was 10% by volume CS (CALF BOVINE SERUM), 10 µg / mL insulin, 0.5 mM 1- It is prepared by adding methyl-3-isobutylxanthine (MIX), 0.25 μM dexamethasone, 0.1% by weight sodium bicarbonate, 100 mg / L streptomycin sulfate and 70 mg / L potassium benzylpenicillin.
The mouse preadipocyte 3T3-L1 was cultured at 37 ° C. in a DME medium (Dulbecco's modified Eagle medium) containing 10% fetal bovine serum using a 6-well multiplate. The medium was changed every two to three days. After confluent, the culture solution was removed by suction, and the cells were washed once with PBS (-). After that, a differentiation-inducing medium was added, and differentiation induction / culture was performed for 2 days to differentiate into adipocytes. Thereafter, the culture was continued in the original medium. About one week later, 2 mL of each sample addition solution was added to the 3T3-L1 cells differentiated into adipocytes, cultured, and after one day (24 hours), the amount of glycerol in the medium was quantified as an indicator of lipolysis. The amount of glycerol released in the medium is measured by an enzymatic method (F-kit manufactured by Boehringer Mannheim; glycerol). The measurement was performed five times and the average value is shown.
Each plant sample (about 1% by weight in pure content) was diluted with a DMEM medium containing 10% by volume of CS to obtain a 1% by volume sample-added solution (about 0.1 mg / mL in pure content). When the active ingredients were used in combination, 1% by volume of a sample addition solution (about 0.1 mg / mL in pure content) was mixed at a ratio of 1: 1 and added to 2 ml. A DMEM medium containing 10% by volume of CS was used as a blank, and caffeine, epinephrine, and yohimbine (pure content: about 0.01 mg / mL) were used as positive controls in the test.
The lipolysis-promoting effect of the various extracts according to the present invention was expressed by calculating the lipolysis-promoting rate (%) according to Equation 1. The results are shown in Table 1.
[0035]
(Equation 1)
Figure 2004035516
[0036]
[Table 1]
Figure 2004035516
From Table 1, it can be seen that the Zygophyllaceae plant of the genus Larrea has the effect of promoting lipid degradation, and that the combination of the present extract with a specific component dramatically accelerates the lipid degradation. .
3. Example of Formulation of Cosmetic Next, the cosmetic according to the present invention was prepared using various extracts of each plant according to the present invention. The mixing ratio is part by weight.
(1) Formulation Example 1 (Lotion)
<Composition> (% by weight)
larrea divaricata extract ... 0.2
Glycerin ... 5.0
Polyoxyethylene sorbitan monolaurate (20EO) 1.5
Purified water ... residual ethanol ... 10.0
Preservative: Appropriate amount [Production method] The raw materials are added to purified water and mixed uniformly.
(2) Formulation example 2 (cosmetic cream)
<Composition> (% by weight)
[Oil phase]
Beeswax ... 2.0
Stearyl alcohol ... 5.0
Stearic acid ... 8.0
Squalane ... 10.0
Self-emulsifying glyceryl monostearate ... 3.0
Polyoxyethylene setriether (20E.0) ... 1.0
[Aqueous phase]
Larrea tridentata extract ... 0.2
Purified water ... balance 1,3-butylene glycol ... 5.0
Preservative: proper amount [Production method] The raw materials for the aqueous phase are mixed and heated to 70 ° C. to make the aqueous phase. On the other hand, the raw materials of the oil phase are mixed and dissolved by heating to 70 ° C. to obtain an oil phase portion. This oil phase is added to the above-mentioned aqueous phase to carry out preliminary emulsification, homogenize uniformly with a homomixer, and cool to 30 ° C. to obtain a cosmetic cream.
(3) Formulation example 3 (cosmetic emulsion)
<Composition> (% by weight)
[Oil phase]
Squalane ... 8.0
Vaseline ... 2.0
Beeswax ... 0.5
Sorbitan sesquiolate… 0.8
Polyoxyethylene cetyl ether (20EO) 1.2
[Aqueous phase]
Larrea
divaricata extract 0.1
Caffeine… 2.0
Mishima saiko extract ... 0.2
Carboxyvinyl polymer ... 0.5
1,3-butylene glycol ... 0.5
Potassium hydroxide 0.1
Purified water ... residual ethanol ... 7.0
Preservative: proper amount [Production method] The raw materials for the aqueous phase are mixed and heated to 70 ° C. to make the aqueous phase. On the other hand, other raw materials are mixed and dissolved by heating to 70 ° C. to obtain an oil phase. This oil phase is added to the above-mentioned aqueous phase and emulsified, and cooled to 30 ° C. to obtain a cosmetic emulsion.
(4) Formulation Example 4 (Packing agent)
<Composition> (% by weight)
[powder]
Titanium oxide 8.0
Kaolin ... 7.0
[Oil phase]
Olive oil ... 3.0
[Aqueous phase]
Larrea
divaricata extract ... 0.5
Vinyl acetate resin emulsion 15.0
Polyvinyl alcohol ... 10.0
Purified water ... balance glycerin ... 5.0
Ethanol ... 5.0
Preservative: Proper amount [Production method] Mix the raw materials of the aqueous phase and make them uniform. Further, other raw materials are mixed and stirred until the mixture becomes uniform to obtain a pack.
(5) Formulation Example 5 (creamy foundation)
<Composition> (parts by weight)
[powder]
Talc ... 5.0
Sericite ... 8.0
Titanium oxide 5.0
Color pigment: 1.5
[Oil phase]
Polyglyceryl monoisostearate ... 3.0
Polyoxyethylene hydrogenated castor oil… 1.5
Isotridecyl isononanoate 10.0
[Aqueous phase]
Larrea
Tridentata extract ... 0.3
Purified water ... balance 1,3-butylene glycol ... 5.0
Preservative: Appropriate amount [Preparation method] A part of the oil phase and the powder are put on a three-roll mill, and the remaining oil phase is added and dissolved by heating, and kept at 80 ° C. Next, the aqueous phase dissolved by heating is gradually added, and the mixture is emulsified at 80 ° C., and cooled to room temperature with stirring to obtain a creamy foundation.
4. Example of Effect Test of Cosmetic Further, the effect of the cosmetic according to the present invention when actually used was examined.
An effect test of Formulation Example 3 was conducted. Formulation Example 3 is Example 12. As a control, a placebo emulsion excluding the Larrea divaricata extract, caffeine, and the mishima saiko extract was formulated in the same manner and used as Comparative Example 10.
Effect test by humans [Evaluation method] Emulsions of the formulations of Example 12 and Comparative Example 10 were applied to the whole body in the morning and evening by 20 women in their 20s and 40s, and were continuously used for one month. The body weight and the body fat percentage (the ratio of fat to the whole body) before and after continuous use were measured by a measuring device (body fat meter with a weight scale, manufactured by Tanita) based on bioimpedance measurement. Average values of body weight and body fat percentage before and after use were determined. Table 2 shows the results.
[0047]
[Table 2]
Figure 2004035516
As is clear from the above results, when the product of the present invention, Example 12, was used, the body weight was slightly reduced as compared to before use, but the body fat percentage was significantly reduced. In Comparative Example 10, almost no decrease was observed.
Next, using the various extracts of each plant according to the present invention, a formulation for a food / orally administered drug according to the present invention was prepared. The mixing ratio is part by weight.
Formulation Example 6 (tablets)
Larrea
divaricata extract (dry matter) 0.1
Crystalline cellulose ... 20.0
Lactose ... 76.9
Sucrose fatty acid ester 3.0
[Production method] The above raw materials are mixed and tableted.
Formulation Example 7 (Capsule)
Larrea
divaricata extract ... 0.5
Caffeine ... 1.0
Mishima saiko extract ... 0.5
Glucose: balance [Preparation method] The raw materials are mixed and molded into capsules.
Formulation Example 8 (drink)
Larrea
divaricata extract ... 10.0
Glucose ... 5.0
Antioxidant: Appropriate amount of purified water: balance An effect test was conducted using the drink of Formulation Example 8. Formulation Example 8 is Example 13. As a control, one obtained by removing the Larrea divaricata extract and replacing it with purified water was used as Comparative Example 11.
Effect test by human [Evaluation method] Twenty women in their 20s and 40s were asked to take the drinks of the formulations of Example 13 and Comparative Example 11 in the morning and evening, and to use them continuously for one month. The body weight and the body fat percentage (the ratio of fat to the whole body) before and after continuous use were measured by a measuring instrument (body fat meter with a weight scale, manufactured by Tanita) based on bioimpedance measurement. Average values of body weight and body fat percentage before and after use were determined. Table 3 shows the results.
[0055]
[Table 3]
Figure 2004035516
[0056]
As described above, the present invention provides a lipolysis promoter effective for reducing systemic or local adipose tissue, suppressing or preventing obesity, and improving obesity, and a slimming agent having the effect. It is clear that skin cosmetics can be provided.

Claims (4)

ハマビシ科(Zygophyllaceae)ラレア属(Larrea)植物の抽出物を有効成分として含有することを特徴とする脂肪分解促進剤。A lipolysis accelerator comprising an extract of a plant belonging to the genus Zygophyllaceae (Larrea) as an active ingredient. 請求項1記載の脂肪分解促進剤を含有する痩身用皮膚外用剤。An external preparation for slimming skin, comprising the lipolysis promoter according to claim 1. ハマビシ科(Zygophyllaceae)ラレア属(Larrea)植物の抽出物と、キサンチン誘導体、βアドレナリン作用興奮薬、α2アドレナリン作用抑制薬、海藻抽出物、茶抽出物、ツボクサ抽出物、ショウブ抽出物、サイコ抽出物から選ばれる一種又は二種以上を配合することを特徴とする脂肪分解促進剤。An extract of a plant belonging to the genus Zygophyllaceae (Larrea), a xanthine derivative, a β-adrenergic stimulant, an α2-adrenergic inhibitor, a seaweed extract, a tea extract, a camellia extract, a shobu extract, a psycho extract A lipolysis accelerator comprising one or more selected from the group consisting of: 請求項3記載の脂肪分解促進剤を配合することを特徴とする痩身用皮膚外用剤。An external preparation for slimming skin, comprising the lipolysis promoter according to claim 3.
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7407674B2 (en) 2006-03-16 2008-08-05 Lotte Co., Ltd. Lipolysis promoter and food-and-drink and feed containing the same
KR101348471B1 (en) 2011-10-05 2014-02-13 숙명여자대학교산학협력단 A composition comprising Larrea cuneifolia Cav. for the prevention and treatment of menopausal symptom

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7407674B2 (en) 2006-03-16 2008-08-05 Lotte Co., Ltd. Lipolysis promoter and food-and-drink and feed containing the same
KR101348471B1 (en) 2011-10-05 2014-02-13 숙명여자대학교산학협력단 A composition comprising Larrea cuneifolia Cav. for the prevention and treatment of menopausal symptom

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