TWI407963B - Contains the composition of riboflavin and sesamin - Google Patents
Contains the composition of riboflavin and sesamin Download PDFInfo
- Publication number
- TWI407963B TWI407963B TW096109040A TW96109040A TWI407963B TW I407963 B TWI407963 B TW I407963B TW 096109040 A TW096109040 A TW 096109040A TW 96109040 A TW96109040 A TW 96109040A TW I407963 B TWI407963 B TW I407963B
- Authority
- TW
- Taiwan
- Prior art keywords
- sesamin
- riboflavin
- fatigue
- analgesic
- composition
- Prior art date
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- AUNGANRZJHBGPY-UHFFFAOYSA-N D-Lyxoflavin Natural products OCC(O)C(O)C(O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-UHFFFAOYSA-N 0.000 title claims abstract description 107
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- PEYUIKBAABKQKQ-AFHBHXEDSA-N (+)-sesamin Chemical compound C1=C2OCOC2=CC([C@H]2OC[C@H]3[C@@H]2CO[C@@H]3C2=CC=C3OCOC3=C2)=C1 PEYUIKBAABKQKQ-AFHBHXEDSA-N 0.000 title claims description 133
- PEYUIKBAABKQKQ-UHFFFAOYSA-N epiasarinin Natural products C1=C2OCOC2=CC(C2OCC3C2COC3C2=CC=C3OCOC3=C2)=C1 PEYUIKBAABKQKQ-UHFFFAOYSA-N 0.000 title claims description 125
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Description
本發明係關於能增強核黃素生理活性之組成物,含有核黃素與芝麻素類之組成物,進一步說,具有可預防及/或減低各種疾患及外傷引起之疼痛之鎮痛作用組成物,或具有可預防及/或減低肉體及/或精神之疲勞之抗疲勞作用組成物,及含此之飲食品。
核黃素(Riboflavin)亦稱為維生素B2(Vitamin B2),係被分類為維生素中之水溶性維生素之生理活性物質。此核黃素在預防及治療包含白內障之多種眼睛疾病有助益,也能改善眼充血、乾燥、癢、眼睛疲勞等症狀(免費百科事典『維基(Wikipedia)』:網址http://ja.wikipedia.org/)。又,核黃素之生理活性方面,報告指出核黃素類化合物有活化免疫機能作用(專利文獻1)及核黃素類化合物作為毒性休克之預防、治療劑係有效的(專利文獻2)。
另外,也有關於核黃素生理活性之鎮痛作用方面的報告。如,高量攝取核黃素可預防偏頭痛(非專利文獻1)及,顯示在發炎性疼痛上於腹腔內以3~100mg/kg濃度投與時,有與用量相關之鎮痛作用,但對於神經痛無效(非專利文獻2),有報告指出以1~50mg/kg之濃度經口投與時,於福馬林試驗之鎮痛效果在25mg到頂點,就算增加至75mg效果也不會再增加等(非專利文獻2、3)。
另一方面,包含維生素B2之維生素B群之抗疲勞作用,也就是維生素B群之疲勞恢復及疲勞預防作用已為人知(專利文獻3)。而市面上也有販賣於疲勞時及肌膚乾燥時服用之含維生素B1及維生素B2及維生素B6之營養補充劑及飲用品。
[專利文獻1]特開平5-201864號公報[專利文獻2]特開平10-29941號公報[專利文獻3]特開2005-23008號公報
[非專利文獻1]Schoenen,J.,NEUROLOGY,50,466-470,1998[非專利文獻2]European Journal of Pharmacology,421,157-164,2001[非專利文獻3]European Journal of Pharmacology,492,35-40,2004
如上所述,有各種關於核黃素之生理活性之報告,而其效果並不完備,核黃素主要用於補助其他化合物之生理活性為目的而搭配使用,現今並未有關於揭示核黃素本身生理活性增強方面的報告。又,如上所述,雖然維生素B群之抗疲勞作用已為人知,但關於具體之核黃素(維生素B2
)之抗疲勞作用並未有任何之揭示。
本發明,係對於人及動物等是安全的,而能長期食用,且係能增強核黃素生理活性之組成物,特別以提供飲食品為目的。
本發明者們,為解決上述課題努力研究之成果,發現令人驚訝之結果,同時攝取核黃素及芝麻素類,可增強核黃素之生理活性。具體上,如上所述,核黃素單獨經口投與之鎮痛效果有上限,但與芝麻素類同時攝取可增強核黃素之效果,得到單獨使用核黃素所沒有之鎮痛效果。又,本發明者們,為做疲勞度之評估使用水浸負荷之動物模式,以游泳試驗評估之結果,發現核黃素有抗疲勞之作用。接著,發現其抗疲勞作用藉由與芝麻素類併用得到單獨使用核黃素所沒有之效果,發現核黃素及芝麻素類可發揮優異之相乘作用,完成本發明。
另外,本發明係關於含有下述之飲食品之組成物。
1.一種組成物,其特徵係含有核黃素及芝麻素類。
2.上述第1項之組成物,其中,對於核黃素總量1而言,芝麻素類之總量比例(重量比)為4.5以下。
3.如上述第1或2項之組成物,其中,芝麻素類係含1重量%以上之芝麻素類之芝麻素類濃縮物。
4.如上述第1~3項中任一項之組成物,其中,芝麻素類為芝麻素及/或表芝麻素。
5.如上述第1~4項中任一項之組成物,其中,核黃素為磷酸核黃素鈉或酪酸核黃素之任一者。
6.如上述第1~5項中任一項之組成物,其係為經口用。
7.一種鎮痛劑,其特徵為含有核黃素及芝麻素類作為有效成分。
8.一種抗疲勞劑,其特徵為含有核黃素及芝麻素類作為有效成分。
9.一種芝麻素類之使用,其係為了增進核黃素之生理活性。
本發明之核黃素(本說明書中,也表示為「維生素B2
」),係包含核黃素之衍生物、或此等之藥理學可容許之鹽類。核黃素之衍生物或其藥理學可容許之鹽類方面,具體上有黃素單核苷酸(FMN)、黃素腺嘌呤二核苷酸(FAD)、核黃素四丁酸酯、磷酸核黃素鈉(維生素B2
磷酸酯)、磷酸核黃素單二乙醇胺鹽、酪酸核黃素(維生素B2
酪酸酯)、無色核黃素、單氫化黃素、無色核黃素磷酸酯、無色核黃素單核苷酸、或無色核黃素腺嘌呤二核苷酸等,但其中,以使用吸收性高之磷酸核黃素鈉及安定性佳之酪酸核黃素為佳。本發明中,前述之核黃素中任一者皆可單獨使用或複數併用。另外,此等之製造方式並未限定,天然萃取物、微生物發酵品、合成品之任一皆可使用。
本發明之芝麻素類,包含芝麻素及其類似物。該芝麻素之類似物方面,除表芝麻素外,有如特開平4-9331號公報中之二噁烷環[3.3.0]辛烷衍生物。芝麻素類之具體例方面有芝麻素、芝麻醇、表芝麻醇、芝麻素酚等、此等之立體異構物或消旋物,可單獨使用或混和使用,但本發明中,以使用芝麻素及/或表芝麻素為佳。另,芝麻素類之代謝物(如特開2001-139579號公報記載)也有本發明之效果,係包含於本發明之芝麻素類類似物,可用於本發明。
本發明所用之芝麻素類,型態及製造方法並未有任何限制。選擇芝麻素類之芝麻素時,通常,亦可使用由芝麻油以公知之方法(如,特開平4-9331號公報所記載)萃取出之芝麻素(芝麻素萃取物或純化物),亦可直接使用市售之芝麻油(液狀)。但直接使用芝麻油時,因芝麻油之特殊氣味於官能上有不好之評價,以使用芝麻油萃取之無味無臭之芝麻素萃取物(或芝麻素純化物)為佳。又,使用芝麻油時,因芝麻素含量低,為得到適當之芝麻素搭配量,處方之含核黃素(維生素B2
)組成物之單位投與之體積變的過大,不適宜投與。特別是經口投與用製劑之情況,製劑(錠劑、膠囊劑等)過大,則攝取有困難。所以,以攝取量少之觀點來看,也以使用芝麻油所得之芝麻素萃取物(或芝麻素純化物)為佳。
如此,以使用芝麻素類之芝麻素類之濃縮物為佳。濃縮程度方面,依使用之芝麻素類種類及搭配之組成物型態可做適合之設計,一般,以使用芝麻素類濃縮為1重量%以上之芝麻素類濃縮物為佳。芝麻素類濃縮物之芝麻素類含量,以20重量%以上為佳,以50重量%以上更佳,以70重量%以上最佳,而以90重量%以上濃縮(純化)之者最為合適。
本發明所使用之芝麻素類,如上所述,因其為傳統食品中所發現之化合物或其類似物,在安全性方面極優異。將此於7週齡之ICR雄性小鼠,以芝麻素2.14g/day/kg連續投與2週(經口投與),未發現任何之異常。
本發明所使用之芝麻素類,特別是芝麻素及/或表芝麻素,本發明之申請人們發現其有自律神經調節作用(國際公開WO2004-105749),但於本發明之增強鎮痛及抗疲勞作用並無所知,且無推測或揭示關於增強核黃素生理活性方面的事。
本發明作為人及動物,特別是作為人之預防及/或減低疼痛之鎮痛劑是有效的。於此,動物係指經濟動物、寵物及實驗動物,具體上,經濟動物係指牛、馬、豬、山羊、羊等之家畜、雞、鴨、鵪鶉、火雞、鴕鳥等家禽、青魽、紅魽、鯛、竹夾魚、鯉魚、鱒魚、鰻魚等經濟上飼養之動物,寵物方面有狗、貓、猴、鳥、倉鼠、金魚等寵物、伴侶動物,實驗動物方面有小鼠、大鼠、豚鼠、米格魯、迷你豬、紅毛猩猩、食蟹猿等於醫學、生物學、農學、藥學等領域之研究用動物。
本發明之鎮痛劑,以一時之輕度疼痛到慢性難以忍受之劇痛為對象。對於疼痛,一般,藉由使用鎮痛劑來控制疼痛,但其效果不足,說其對於關節痛、神經痛、腰痛等之慢性疼痛只有一時之鎮痛效果也不為過,而鎮痛劑之持續使用,常會造成胃腸障礙、腎傷害及肝傷害等副作用。另外,關節痛、神經痛、腰痛等之疼痛,有隨年齡增加的傾向,近年來伴隨著急速高齡化,不單是單純地改善除去疼痛,其預防之社會需要也日益增加。
本發明之鎮痛劑對於上述之種種疼痛及伴隨此等之疾患係有用的。本發明之鎮痛劑,藉由併用芝麻素類,使核黃素之鎮痛作用相乘地增強,與傳統鎮痛劑相較發揮優異之鎮痛效果。又,以長期食用的飲食品所攝取之核黃素及芝麻素作為有效成分,無副作用,可持續使用。另外,不單期望可日常攝取以減低慢性疼痛,亦可預防伴隨疼痛之疾病(經痛等),為新穎之鎮痛劑。而,痛的感覺,有感受性強與弱的人之分別,無客觀的尺度,無法判定正常或有疾病之情況為多,不像傳統鎮痛劑般藉由藥物之投與進行醫療行為,而可說是可以日常攝取之飲食品型態有效之者。
本發明之組成物,除該鎮痛作用外,亦可用作人及動物之抗疲勞劑。動物係指該鎮痛劑之對象動物,其中本發明之抗疲勞劑用於能有疲勞感之人、經濟動物、寵物及實驗動物,特別適用於人。在此,經濟動物係指牛、馬、豬、山羊、羊等之家畜及賽馬、獵犬等,寵物方面有狗、貓等,實驗動物方面有小鼠、大鼠、豚鼠、米格魯、迷你豬、紅毛猩猩、食蟹猿等於醫學、生物學、農學、藥學等領域之研究用動物。
所謂疲勞,係連續給予身體或精神上之負荷時所見到的一時性身體或精神之表現低下之現象,所謂表現低下係指,身體或精神上的作業能力在質或量上的低下。又本發明之『疲勞』,亦包含慢性疲勞症候群及過勞死。
本發明之抗疲勞劑,有減弱該疲勞之作用與疲勞恢復之作用,具體上可提高運動及作用部位(含腦)之運作之持續時間,及抑制同運動量及作用量之疲勞物質的增加(持久力增加、體力增強)、改善運動及作用部位雖未疲勞而腦及神經等已感到疲勞的狀態、及促進運動及作用部位之由疲勞狀態回復到正常狀態之效果。
另外,本發明之抗疲勞劑目標之慢性疲勞症候群係指,造成日常生活障礙之長期全身疲勞感、倦怠感、微熱、淋巴節腫脹、肌肉痛、關節痛、精神神經症狀等基本症狀。本發明之抗疲勞劑可處理此慢性疲勞症候群,也就是能緩和慢性疲勞症候群之各種症狀,使其回到正常狀態。又,本發明之抗疲勞劑目標之過勞死,係指於重度之過勞狀態,就算無法保持身體之活力,無法完全地感受到疲勞,結果,發生腦血管疾病及心疾病而到永久無法勞動及死亡之狀態。本發明之抗疲勞劑係能處理慢性疲勞症候群,藉此能預防過勞死。
本發明之抗疲勞作用,也就是作為『抗疲勞劑』之效果,可利用接下來的實驗確認。也就是於水浸斷眠試驗中游泳時間的測定。使用水浸飼育般無法得到充足之睡眠及休息的姿勢,在肉體及精神上皆無法休息的環境下飼育的小鼠,於負重狀態使其游泳,藉由測定10秒以上鼻子沉於水下為止之時間,確定其疲勞度。此動物模式係為肉體上及精神上疲勞之模式,所以如藉由投與被試驗物質而能延長游泳時間的話,可確認可預防或改善肉體及精神疲勞及其伴隨之肌肉痛等苦痛、增強體力延長至疲勞的時間、回復疲勞保持身體之活力等對於疲勞之耐受性。
本發明之抗疲勞劑,藉由攝取此而不易疲勞,或有疲勞恢復之效果。也就是說,不止於運動等肌肉運動時感受到肉體疲勞時、計算作業等連續作業時感受到精神疲勞時,攝取以期由疲勞恢復,預先攝取再從事勞動、運動等也有預防效果。又,藉由運動前及中攝取,可期待其持久性增加。另外,藉由日常的攝取,也可預防精神上的疲勞及伴隨之疾病。
本發明藉由含核黃素及芝麻素類,相乘地增強核黃素之生理活性,如鎮痛作用及抗疲勞作用,用作健康食品,因各成分之生理作用,達到增進健康之期望。
於本發明之含核黃素及芝麻素類之組成物中,期待其各自之生理作用,其搭配量並未設限。一般,核黃素以厚生勞動省所定之日本人營養所需量搭配即可,具體上,1天,成人男子為1.2mg、成人女子為1.0mg。又,核黃素並無關於引起健康障礙之上限方面之報告,其搭配量並無上限,但是一般,成人一日份量在100mg以下,以50mg以下為佳。又,芝麻素類之搭配量一般成人一日份量在1~200mg,以5~100mg為佳。
另一方面,期待增強核黃素之生理活性,而於核黃素搭配芝麻素類時,以核黃素換算的情況(本說明書中,亦表記為『核黃素當量』),相對於核黃素之總量1而言,芝麻素類之總量的比例以重量比4.5以下,又以4.0以下為佳,以3.5以下搭配更佳。雖然預想搭配之芝麻素類比例愈多,愈能增強核黃素之作用,但不在該比例之範圍內,則無法獲得優異之相乘效果。搭配之芝麻素類的下限值,只要能得到所求之作用,如鎮痛作用及抗疲勞作用之相乘效果之量即可,並未設限,參考該日常用量搭配使用即可。一般,以核黃素換算時,相對於核黃素之總量1而言,芝麻素類之總量的比例為重量比為0.01以上,以0.5以上為佳,以0.1以上更佳,以1以上特佳。
在核黃素之生理活性之一的鎮痛作用中,將核黃素當量30mg之磷酸核黃素鈉與50mg或100mg之芝麻素類經口攝取時,即重量比為核黃素:芝麻素類=1:1.67或1:3.33時,確認磷酸核黃素鈉之鎮痛作用有提升(實施例1、2)。又,本發明者們確認在核黃素之生理活性之一的抗疲勞作用中,將核黃素當量25mg或50mg之磷酸核黃素鈉與50mg之芝麻素類經口攝取時,即重量比為核黃素:芝麻素類=1:2或1:1時,確認磷酸核黃素鈉之抗疲勞作用有提升,但核黃素當量10mg之磷酸核黃素鈉與50mg之芝麻素類經口攝取時,即重量比為核黃素:芝麻素類=1:5時,確認磷酸核黃素鈉之抗疲勞作用並無提升(實施例3、4)。
本發明之組成物以醫藥組成物利用時,其投與型態可以液劑、錠劑、顆粒劑、散劑、膠囊劑、乾糖漿劑、丸劑等型態經口投與,亦可以注射劑型態投與,其型態可依病況及其進行情況、其他條件而做合適選擇。又,因本發明之有效成分核黃素(除酪酸核黃素外)為水溶性,芝麻素類為脂溶性,個別以不同型態攝取亦可。具體上,有將核黃素顆粒與水同時攝取時,同時攝取充填有溶於油脂的芝麻素類軟膠囊之方法,及藉由依各自吸收速度設置時間差之攝取方式,可得到鎮痛效果。
又,本發明之組成物的投與量方面,依對象、病況及進行狀況、其他條件而做合適選擇即可,但以得到以人(成人)為對象之鎮痛作用及/或抗疲勞作用為目的之經口投與時,一般,係為1~200mg,以2~100mg為佳,以一日1~3次頻率連續投與為佳。
於本發明中,在不損及其效果時,核黃素及芝麻素類可與其他之任意所希望之成分搭配。如,維生素E、維生素C等維生素類,礦物質類、賀爾蒙、營養成分、香料等之生理活性成分外,於製劑時可搭配乳化劑、等張化劑、緩衝劑、溶解輔助劑、防腐劑、安定劑、抗氧化劑等。本發明之組成物,如上所述,可作為鎮痛劑及或抗疲勞劑之者,但推想核黃素(維生素B2
)能與芝麻素類所具有之其他種種之生理作用有相加或相乘的作用,故不單作為醫藥組成物,用作健康食品亦相當合適。
這裡所說之健康食品,如,膠囊劑及錠劑般含有本發明之核黃素及芝麻素類組成物作為有效成分之製劑或食品,及於一般食品中搭配本發明組成物做為其中一種成分,附加對身體有鎮痛作用及抗疲勞作用等種種機能之機能性食品(包含特定保健用食品及有條件之特定保健用食品)。更包含以預防及減低身體疼痛及減輕身體疲勞或促進疲勞恢復為宗旨之鎮痛作用及/或抗疲勞作用之食品等。
含核黃素及芝麻素類之健康食品方面,其型態並未特別限制,可以粉末狀、顆粒狀、錠劑狀等之固體狀;溶液狀、乳液狀、分散液狀等之液狀;或膏狀等之半固體狀等之任意之型態調製。
以下,由試驗例及實施例,更具體地說明本發明,但本發明並不為其所限制。
無關於芝麻素類鎮痛作用之報告。在此,討論芝麻素類之鎮痛作用。
鎮痛作用試驗方面,以改變部分Moon們之醋酸Writhing試驗(Biol.Pharm.Bull.(2005))方法進行。具體之試驗方法如下。由Clea Japan,Inc購入Wistar品系雄性大鼠(5週齡),以1週時間在試驗環境下馴化後,將順利發育之動物供給實驗。於醋酸Writhing試驗3日前,將大鼠一群6隻分成3群,在對照組以5ml/kg之橄欖油用量,其餘2群用將芝麻素類(芝麻素/表芝麻素混合物;芝麻素:表芝麻素(重量比)=5:5)各自以50、100mg/kg之用量溶解於橄欖油,以餵食器經口投與。接著試驗之2日前也進行同樣地投與,更於試驗前日,進行早、晚2回,共4回之投與。試驗當日,給前日晚開始禁食之大鼠經口投與生理食鹽水5ml/kg,再於1小時後於腹腔投與含1%醋酸之生理食鹽水1ml/170g,測量投用後之30分鐘內Writhing次數。
其結果如圖1所示。芝麻素類投與群(Sesamin50mg,Sesamin100mg)與對照組(Olive)相比,多少有Writhing次數增加之傾向,明顯地發現芝麻素類在醋酸Writhing試驗中無鎮痛作用。
證明芝麻素類可提升核黃素(維生素B2
)之鎮痛作用。由Clea Japan,Inc購入Wistar品系雄性大鼠(7週齡),以1週時間在試驗環境下馴化後,將順利發育之動物供給實驗。於醋酸Writhing試驗3日前,將大鼠一群6隻分成4群,其中2群以5ml/kg之橄欖油用量,其餘2群用與試驗例1相同芝麻素類各自以50、100mg/kg之用量溶解於橄欖油(5ml/kg),以餵食器經口投與。與試驗例1同樣進行4次投與。試驗當日,給前日晚開始禁食之大鼠於對照組經口投與生理食鹽水5ml/kg,其餘3組以維生素B2
(磷酸核黃素鈉;Nacalai Tesque,Inc.)以核黃素當量30mg/kg用量溶於生理食鹽水經口投與,用試驗例1之基準測量Writhing次數。
其結果如圖2所示。相對於對照組(Olive+Saline)之Writhing次數,顯示維生素B2
單獨群(Olive+VB2)有降低傾向,確認了維生素B2
之鎮痛作用。與此維生素B2
單獨群(Olive+VB2)相比,芝麻素與維生素B2
組合之群(Sesamin50mg+VB2
,Sesamin100mg+VB2
)中芝麻素類100mg/kg、50mg/kg任一中,Writhing次數皆有減少。確認與芝麻素類之搭配可增強維生素B2
之鎮痛作用。
確認實施例1之再現性。由Clea Japan,Inc購入Wistar品系雄性大鼠(5週齡),以1週時間在試驗環境下馴化後,將順利發育之動物供給實驗。於醋酸Writhing試驗3日前,將大鼠以每群10~18隻分成3群,其中2群(1群、2群)以5ml/kg之橄欖油,其餘2群(3群、4群)用與實施例1相同芝麻素類以100mg/kg之用量溶解於橄欖油,以餵食器經口投與。與實施例1同樣進行4次投與。試驗當日,給前日晚開始禁食之大鼠,於4群中之2群(1群、3群)經口投與生理食鹽水5ml/kg,其餘2群(2群、4群)以維生素B2
(磷酸核黃素鈉;Nacalai Tesque,Inc.)以核黃素當量30mg/kg用量溶於生理食鹽水經口投與,再用試驗例1之基準測量Writhing次數。
其結果如圖3所示。相對於對照組(Olive+Saline)之Writhing次數,顯示維生素B2
單獨群(Olive+VB2)有降低傾向(抑制率10.5%),但芝麻素類單獨群(Sesamin+Saline)無法有如試驗例1般相同之鎮痛作用。但是,芝麻素類與維生素B2
組合之群(Sesamin+VB2
)則大幅減少(抑制率26.6%),確認維生素B2與芝麻素類之搭配有相乘之鎮痛作用(Tukey多重比較檢定結果,維生素B2
與芝麻素類之組合群與對照組之間p<0.05,芝麻素類單獨群間p<0.01)。
被試驗物質之核黃素及芝麻素類與實施例1為相同之者,也就是,使用芝麻素/表芝麻素混合物(芝麻素:表芝麻素(重量比)=5:5)及核黃素(磷酸核黃素鈉;Nacalai Tesque,Inc.)。
藉由水浸斷眠試驗,評估其對疲勞之效果。評估為以部分改良之Tanaka們之方法(Neurosience,Let.352,159-162,2003)進行。也就是,試驗動物使用8週齡之雄性Balb/c小鼠,使平均體重均等以1群9隻將小鼠分為7群。表1所示之核黃素值係將所用之磷酸核黃素鈉換算為核黃素之值。其中,6群為水浸試驗之壓力群,以水溫23℃、深7mm之自來水取代床墊(紙墊)在飼育籠中飼育,小鼠以水浸來阻斷睡眠。2日之水浸斷眠試驗中,1日1次、2日強制經口投與各被試驗樣本。被試驗樣品中,芝麻素類溶於橄欖油、核黃素類溶於蒸餾水。投與順序為核黃素、芝麻素類之順序,對照組則用蒸餾水、橄欖油做強制經口投與。
水浸飼育2日後,於小鼠尾部加上體重8%之重物使其游泳,測量到10秒以上沉於水中為止所需時間。水浸飼育群(水浸斷眠壓力群)之小鼠之游泳時間較一般飼育群來的縮短,藉由被試驗樣本投與群小鼠,可抑制多少之游泳時間縮短,來判定對疲勞之效果。
結果如圖4所示。由圖可明顯瞭解,水浸飼育對照群之游泳時間較一般飼育對照群縮短。另外,投與芝麻素及核黃素之群,各自之游泳時間縮短被抑制,但將彼等同時投與可相乘地增加其效果。
如表2將小鼠分為6群外,與實施例3同樣地,測定核黃素及芝麻素類之抗疲勞作用。表2中之核黃素之值,係表示將所用之磷酸核黃素鈉換算為核黃素之值。
結果如圖5所示。由圖可知,芝麻素及核黃素中相乘效果,於芝麻素50mg/kg、核黃素10mg/kg時,無法發揮。要有相乘效果,以核黃素換算,核黃素之總量為1時,芝麻素類之總量以重量比5.0以下是必須的。
芝麻素 0.01g維生素B2
0.01g醋酸生育醇 0.25g無水矽酸 20.5g玉米澱粉 179.0g
將以上粉末混和均勻後,加入10%羥丙基纖維素.乙醇溶液100ml,以常法混和、壓出、乾燥,得到顆粒劑。
明膠 60.0%甘油 30.0%對羥基苯甲酸甲酯 0.15%對羥基苯甲酸丙酯 0.51%水 適量
於上述成分所成軟膠囊劑之皮中,以常法填充以下之組成物,得到一粒200mg之軟膠囊劑。
芝麻素 10.0mg維生素B2
1.0mg甘油脂肪酸酯 15.0mg蜜蠟 15.0mg小麥胚芽油 250mg
芝麻素 0.01g維生素B2
0.1g澱粉 282g蔗糖脂肪酸酯 9.0g氧化矽 9.0g
將此等混和,以單發式打錠機打錠,製造直徑9mm、重300mg之錠劑。
呈味:DL-酒石酸鈉 0.1g琥珀酸 0.009g甜味:糖漿 800g酸味:檸檬酸 12g維生素:維生素C 10g芝麻素 1g維生素B2 3g維生素E 3g環糊精 5g香料 15ml氯化鉀 1g硫酸鎂 0.5g
將上述成分搭配,添加水使成為10L。此飲劑1次可飲用約100ml。
本發明之含有核黃素及芝麻素類之組成物,核黃素所具有之生理活性,如鎮痛作用及抗疲勞作用可藉由與芝麻素類合併攝取而發揮相乘效果,對人及動物為安全的,所以,本發明可持續攝取。
[圖1]芝麻素類之鎮痛作用及影響之示意圖。
[圖2]藉由核黃素(維生素B2
)及芝麻素類組合之鎮痛作用示意圖。
[圖3]藉由核黃素(維生素B2
)及芝麻素類組合之鎮痛作之相乘效果示意圖。
[圖4]藉由核黃素及芝麻素類組合之抗疲勞作用示意圖。
[圖5]藉由核黃素及芝麻素類組合之抗疲勞作用示意圖。
Claims (8)
- 一種組成物,其特徵係含有核黃素及芝麻素類,且對於核黃素總量1而言,芝麻素類之總量比例(重量比)為4.5以下,而前述芝麻素類係選自芝麻素、表芝麻素、芝麻醇、表芝麻醇、及芝麻素酚所成組群中之一種以上的化合物。
- 如申請專利範圍第1項之組成物,其中,芝麻素類係含1重量%以上之芝麻素類之芝麻素類濃縮物。
- 如申請專利範圍第1或2項之組成物,其中,芝麻素類為芝麻素及/或表芝麻素。
- 如申請專利範圍第1或2項之組成物,其中,核黃素為磷酸核黃素鈉或酪酸核黃素之任一者。
- 如申請專利範圍第1或2項之組成物,其係為經口用。
- 一種鎮痛劑,其特徵為含有核黃素及芝麻素類作為有效成分,且對於核黃素總量1而言,芝麻素類之總量比例(重量比)為4.5以下,而前述芝麻素類係選自芝麻素、表芝麻素、芝麻醇、表芝麻醇、及芝麻素酚所成組群中之一種以上的化合物。
- 一種抗疲勞劑,其特徵為含有核黃素及芝麻素類作為有效成分,且對於核黃素總量1而言,芝麻素類之總量比例(重量比)為4.5以下,而前述芝麻素類係選自芝麻素、表芝麻素、芝麻醇、表芝麻醇、及芝麻素酚所成組群中之一種以上的化合物。
- 一種含有核黃素之鎮痛劑或抗疲勞劑之製造方法,其係包含藉由添加芝麻素、表芝麻素、芝麻醇、表芝麻醇、及芝麻素酚所成組群中之一種以上的化合物於鎮痛劑或抗疲勞劑中,以增進核黃素之鎮痛作用或抗疲勞作用。
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US (2) | US20090054443A1 (zh) |
EP (2) | EP1997496B1 (zh) |
JP (2) | JP5430927B2 (zh) |
KR (1) | KR101451438B1 (zh) |
CN (1) | CN101410115B (zh) |
AU (1) | AU2007237685B2 (zh) |
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HK (2) | HK1126663A1 (zh) |
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AU2007237685B2 (en) | 2006-03-15 | 2012-08-09 | Suntory Holdings Limited | Compositions containing riboflavin and sesamin-class compounds |
JP5069416B2 (ja) * | 2006-03-15 | 2012-11-07 | サントリーホールディングス株式会社 | 吸湿性の改善された飲食品用組成物 |
WO2008126587A1 (ja) * | 2007-03-15 | 2008-10-23 | Suntory Holdings Limited | 抗疲労剤 |
US8703789B2 (en) * | 2007-09-19 | 2014-04-22 | Suntory Holdings Limited | Compositions incorporating sesamin-class compounds and vitamin B1 class compounds |
WO2009038090A1 (ja) * | 2007-09-19 | 2009-03-26 | Suntory Holdings Limited | セサミン類とアラキドン酸類を含有する組成物 |
JP5794761B2 (ja) * | 2007-09-19 | 2015-10-14 | サントリーホールディングス株式会社 | セサミン類及びビタミンeを含有する抗疲労剤 |
CN103446197B (zh) * | 2013-09-11 | 2016-04-13 | 白心亮 | 一种保肝制品 |
WO2016152846A1 (ja) * | 2015-03-23 | 2016-09-29 | サントリーホールディングス株式会社 | 概日リズム改善用組成物 |
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- 2007-03-15 EP EP07738720.7A patent/EP1997496B1/en not_active Not-in-force
- 2007-03-15 US US12/282,707 patent/US20090054443A1/en not_active Abandoned
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- 2007-03-15 CN CN2007800087982A patent/CN101410115B/zh active Active
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JPWO2007119378A1 (ja) | 2009-08-27 |
TW200803865A (en) | 2008-01-16 |
EP1997496B1 (en) | 2015-07-29 |
KR101451438B1 (ko) | 2014-10-15 |
EP1997496A1 (en) | 2008-12-03 |
AU2007237685A1 (en) | 2007-10-25 |
CA2645833C (en) | 2014-12-30 |
WO2007119378A1 (ja) | 2007-10-25 |
KR20080110814A (ko) | 2008-12-19 |
AU2007237685B2 (en) | 2012-08-09 |
SG170120A1 (en) | 2011-04-29 |
US9895375B2 (en) | 2018-02-20 |
US20150080407A1 (en) | 2015-03-19 |
CA2645833A1 (en) | 2007-10-25 |
JP2014040463A (ja) | 2014-03-06 |
MY163134A (en) | 2017-08-15 |
HK1201754A1 (zh) | 2015-09-11 |
CN101410115B (zh) | 2012-01-04 |
HK1126663A1 (en) | 2009-09-11 |
JP5430927B2 (ja) | 2014-03-05 |
EP1997496A4 (en) | 2012-05-16 |
CN101410115A (zh) | 2009-04-15 |
JP6095549B2 (ja) | 2017-03-15 |
EP2826481A1 (en) | 2015-01-21 |
US20090054443A1 (en) | 2009-02-26 |
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