TWI243685B - Acidic composition for oral administration and its uses - Google Patents
Acidic composition for oral administration and its uses Download PDFInfo
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- TWI243685B TWI243685B TW088115457A TW88115457A TWI243685B TW I243685 B TWI243685 B TW I243685B TW 088115457 A TW088115457 A TW 088115457A TW 88115457 A TW88115457 A TW 88115457A TW I243685 B TWI243685 B TW I243685B
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Preparation or treatment thereof
- A23L2/385—Concentrates of non-alcoholic beverages
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Preparation or treatment thereof
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Preparation or treatment thereof
- A23L2/52—Adding ingredients
- A23L2/62—Clouding agents; Agents to improve the cloud-stability
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- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
- A23L29/206—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin
- A23L29/231—Pectin; Derivatives thereof
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- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
- A23L29/206—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin
- A23L29/238—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin from seeds, e.g. locust bean gum or guar gum
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
- A23L29/206—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin
- A23L29/256—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin from seaweeds, e.g. alginates, agar or carrageenan
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
- A23L29/206—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin
- A23L29/262—Cellulose; Derivatives thereof, e.g. ethers
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- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
- A23L29/269—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of microbial origin, e.g. xanthan or dextran
- A23L29/27—Xanthan not combined with other microbial gums
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
- A61K8/733—Alginic acid; Salts thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
- A61K8/817—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen; Compositions or derivatives of such polymers, e.g. vinylimidazol, vinylcaprolactame, allylamines (Polyquaternium 6)
- A61K8/8176—Homopolymers of N-vinyl-pyrrolidones. Compositions of derivatives of such polymers
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- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
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Description
1243685
$較佳在2.5至4.以圍内,尤佳使用於含有水果酸之飲料 福:ί Ϊ =明之適合黏度調整聚合物材料包括食品級 ΐ:ΐ= 增稠劑,例如,藻酸鹽,刺槐木豆樹 二少唐’瓜耳樹膠,阿拉伯樹膠(gum打以丄㈧,黃蓍 =,=叉土膠,阿拉伯樹膠(acacia gum},黃酸樹膠,果 膠,纖維素衍生物及在食品範圍與口腔用途之其它組合物 中所使用之其它此種天然或半合成聚合物材料,其包括其 一或多種之混合物。適合之合成,非多醣黏性調整聚合物 為聚乙烯吡咯酮(PVP)。 本發明使用之較佳複合多醣物質包括藻酸鹽,黃酸樹膠 與果膠’尤其南曱氧基果膠,低酯果膝及醯胺化或剖份醯 胺化果膠。適合之藻酸鹽包括商業上可得之低,中^高黏 性藻酸鹽產ί勿。例如,由Μ ο n s a n t 〇製造,品名為 Kelcoloid LVF及Manucol LF之低黏度丙二醇藻酯及藻酸 鈉;由Monsanto製造,品名為Manucol之中黏度藻酸鈉; 由Monsanto製造,品名為Kelcoloid之高黏度丙二醇藻酸 酯。適合之黃酸樹膠包括一些得自Monsanto。品名為
Keltrol T , Keltrol RD ,Keltrol TF ,Keltrol SF 及 Keltrol BT。適合之果膠包括高曱氧基果膠,例如,得自 SKW Biosystems 之Unipectin QC40 ;低醋果膠,例如,以 品名GENU LM 22 CG與GENU LM 12 CG販售之產物;部份醯 胺化低酯果膠,例如,以品名GENU LM 101 AS及GENU LM 1 02 AS販售之產物;及醯胺化低酯果膠,例如,品名為
O:\60\60228.PTD 第6頁 1243685 五、發明說明(4) GENU LM 104 AS FS 販售之產
Hercules公司。 王邓該果膠產物皆得自 已顯不該齒質腐損之抑制 — 加而增加。然而,黏度並非景t塑二:二物材料濃度增 素;比較於相同黏度下,損可能性之主要因 尤其於飲料調配物特有之低勒 之〜響顯示 至不同程度。@此,可以】以抑制命質腐損 (範圍自涪栌方从,m 夠仔到付合所要產物種類 產物)黏度之遭度選擇並使用適於= = 性 例如…般㈣度產物(例如,_ 能得到約i 0厘泊(c P )以下(較佳約6厘泊以 之、聚辰人又 物材料。可知’雖然黏度值並非 ;黏度之水口 測定之條件…之正確值丄U:係取決於其被 你々沒灿·· 你取决於所使用設備及其被操 作之條仵。 因此,本發明適用於所有經口食用或利用之酸性產物。 其—包括酸性飲料,食用醋,調咮料,醃潰物,貯藏食品, 糖菓類與各式各樣的酸性產物(例如,酸性乳製品),以及 其它欲經口食用之較佳呈液體或半固體型式之其它物質, 例如,口腔保健產品(如漱口液,及藥物)。 八 本發明可適用各種固體,半固體或液體食品,尤其酸性 飲料。這些包括不起泡與碳酸酒精及非酒精飲料(例如, 水果飲料)’及尤其健康飲料(例如,黑醋栗果汁飲料或添 加維生素飲料)。本發明亦係關於用以製備酸性飲料之濃 縮物及粉末狀型式。在一項較佳具體實例中,該酸組合物
1243685 五、發明說明(5) 是一種隨時可飲用之飲料或自天然果汁(例如,黑錯栗汁) 製成可經稀釋之飲料濃縮物。 本發明可有利地適用於含有天然及/或附加酸化劑之酸 性組合物中,尤其適用於食品,且特別適用於飲料。該酸 組合物可含有有機及/或無機酸,且可以添加維生素,例 如,抗壞血酸。較佳之酸化劑包括飲用酸,例如,檸樣 酸,蘋果酸,乳酸,磷酸,醋酸與酒石酸及其混合物。 根據本發明之組合物中該酸化劑濃度由該產物種類,所 要有效pH,所要官能性質及所選擇酸源之酸度決定。組合 物之酸度可以根據滴定酸度表示,滴定酸度是一種經由計 算中和所存在之酸種類所需之氫氧化鈉體積以測定存在於 溶液中之酸重量%之方法。實際上,滴定酸度是一種於 °C溫度下,使用已知濃度之標準氫氧化鈉溶液電勢滴定之 方法。一般叙料之滴定酸度範圍為〇· 〇丨至4% w/w,且一般 以水果為主之隨時可飲用飲料之滴定酸度範圍為〇 . i至2% w/w。一般而言,本發明組合物中該酸濃度(例如,以水果 ,主之產物中該酸濃度)範圍為〇.〇1% w/w至4% w/w,適合 摩巳圍為0· 1% w/w至2· 5% w/w。主要含檸檬酸及/或蘋果酸 作為該酸化劑之一般隨時可飲用之水果飲料之酸濃度佔該 飲料組合物之〇 · 〇 1至丨· 0 % w / w。在稀釋用之濃縮物中,一 般擰檬酸/蘋果酸濃度範圍佔該組合物之〇1至4% w/w。可 以使用飲用酸之混合物,例如,選自檸檬酸,蘋果酸,磷 酸及礼酸與本技藝中已知之其它食品級賦形劑之混合物。 可以使食品(例如,飲料)去甜味,或使用天然糖或合成 !243685
甜味劑(例如,糖 藝中已知之其它糾月,天冬胺醯苯基丙胺醯甲酯),或本技 習用添加物,例如味2使其具甜味。組合物亦可含有其它 及二氧化碳。 ,苯甲酸鈉,山梨酸,調味劑,著色劑 本發明文中使用
式時,該組合物^該名詞“有效PH,,係、意指當呈液體变 相中間物製成之P ’或固化(其中該組合物係為經由液 體或半固體組合物f或半固體)前該組合物之PH,或當固 PH。該名詞固^ =或溶解在液體(例如,水)中時之 或半固姊 匕括處理或補充液相中間物,以形成固體 六f t優點得自使用低含量鈣(其適合呈鹼鹽型式)。當鈣 "It* 8rt~ 5 rb jol. . % 田於該酸進行部份中和反應(其可以使唾液更決 迷中和口中棄丨丨nr u τ①下之酸殘留物)致使該調配物之缓衝能力減 於田4弓f在時’絕對濃度I不重要,因為其會根據該存在 夂之性貝及農度而不同。可以以任何適合型式添加鈣,其 1便之巧或為可溶性鹽(例如,碳酸鈣,氫氧化鈣,檸檬 酸妈’顏果酸鈣,擰檬酸蘋果酸鈣,乳酸鈣,氯化鈣,磷 酸躬’甘油磷酸鈣或曱酸鈣)或可以使該組合物得到不良 味道之機會減至最低之任何其它鹽。鈣含量適合以相對於 該酸化劑莫耳濃度之莫耳基礎計算。鈣存在量至高為每莫 耳酸化劑之0· 8莫耳。該鈣與酸之莫耳比可以自〇· 01至 0·75 ’適合自〇·〇5至0.6,且就以水果為主之飲料產物而 言’ 一般自0.1至〇.5。
第9頁 1243685 五、發明說明(7) 本發明另一方面係提供一種減少口腔用途之酸性組合 腐損牙齒之方法,其包括添加黏度調整聚合物材料, 而要每莫耳之0至0.8莫耳#5至酸性口服組合物中,若恭 要,可控制声有效pH,使其小於或等於a. 5。 為了避免疑慮,“若需要或希望(ifnecessary〇r desired)”係包括使pH達至所定義範圍内,並控制邱於所 定義範圍内。可以經由添加鹼(例如,可溶性鹼鹽,如氫 氧化鈉或檸檬酸鈉,蘋果酸鈉或乳酸鈉)並必要時添加= 以調整該調&物有效pH至所要值。 本發明亦係關於一種經由口服含有黏度調整聚合物材料 與酸化劑,及視需要每莫耳酸含有〇至〇· 8莫耳鈣之組合物 以減少經由口服組合物中之酸所引起之齒質腐損之方法, 其中該組合物之有效pH小於或等於4. 5。 本發明進一步係關於含有黏度調整聚合物材料與酸化 劑,並視需要每莫耳酸含有〇至〇 · 8莫耳鈣之組合物(其pH 小於或等於4 · 5)在製造用以減少由口服組合物中之酸引起 之齒質腐損之藥物之用途。 口服組合物可含有儀或其它離子作為補充礦質反應之輔 助劑。其亦可含有有效量之蘋果酸或其飲用鹽以維持所存 在躬之溶解性,以便防止不溶性鈣鹽之沉澱或使其沉澱反 應減至最低。附加之蘋果酸有助於該飲料之總酸度,該酸 度之剩餘物係由其它(較佳天然存在)酸(例如,檸檬酸, 乳酸及酒石酸)提供。 叮以根據·自用方法合各成份以製成口服組合物。可以
第10頁 1243685
五、發明說明(8) 使固體成份溶解在水性介質(例如,&〜γ 加其它組份前進行加熱。通常在添加^ 了 :=高要 黏度調整聚合物材料(例如,複合多醣類剪切混合使 水合。一般而言,在裝填入瓶内或罐内或其 肉二 使飲料及其它液體產物經巴斯德滅菌,^ ^ ς 2 經“包裝内巴斯德滅菌”。 -戈在褒填後,使其 全部實驗中所使用之食 以下實例為本發明之例證說明 品級聚合物之商業來源如下: 得自 Monsanto,Tadworth,Surrey,UK 以品名Keitrol
T ,Keltrol RD ,Keltrol TF ,Keltr〇l SF ,Keltr〇1 BT 販售之黃酸樹膠;得自IFF,Haverhill,Suff〇lk,UK之 黃酸樹膠聚合物;得自Thew Arnott & Co. Ltd. Wallington,Surrey,UK之黃酸樹膠,瓜耳樹膠及黃蓍 膠;得自SKW Biosystems , Newbury , Berkshire , UK 以品 名Satiaxane販售之黃酸樹膠,及以品名Lygomme MM391販 售之黃酸樹膠/瓜耳樹膠混合物;得自Dan i sco Ingredients Ltd,Bury St Edmunds,UK 以品名
Grinstead JU543販售之黃酸樹膠/羧甲基纖維素鈉 ( 35/6 5 % w/w)混合物;得自Red Carnation gums Ltd, Laindon,Essex,UK之阿拉伯樹膠,丙二醇藻酸鹽及緩甲 基纖維素納;得自Hercules Ltd ’Reigate ’Surrey ’UK 之 Blanose 纖維素樹膠(9M31XF);得自Monsanto ’ Tadworth,Surrey,UK 以品名Kelocoloid LVF ’ Kelcoloid HVF,Manucol DH 及 Manucol LF 販售之藻酸鹽
O:\60\60228.PTD 第11頁 1243685
1243685 五、發明說明(10) 增稠劑之該對照物飲料產生1 6微米琺瑯質損失,而該含黃 酸樹膠之飲料產生1微米5法瑯質損失。 測定活體外琺瑯質損失之方法 以由Davis & Winter (Davis WB, Winter PJ,
Dental Journal, 1 977,143,116- 119)及West 等人(West NX 等人,J Dentistry, 1 99 8,26(4),32 9-335 )所述之方
法’以4小時測定該活體外琺瑯質損失,以測定該試驗溶 液之腐損可能性。將最近才拔出的無齲蛀智齒製成切片, 並安裝在具有頰形態在最上面之環氧樹脂墊中。將該琺瑯 質試樣磨碎,移除極少量琺瑯質以製造一種平坦水平墊。 經由surfometiry記錄基線測定,且經由塗敷pvc膠帶記述 之區域,於37 t下使6個遮蓋琺瑯質標本暴露於2〇〇 =成驗溶液下4 X H、時,並使用高架授拌。每小時 換該試驗溶液,。接著以去離子水洗濯該琺瑯質試樣, 該PVC膠帶,並經由surf ometry評估、’ 承 實例2 /、,且織^貝失。 混合以下成份以製成1 成份 右旋糖單水合物 麥芽糊精 π队徜千運動飲料 數量(公斤) 400
538 〇· 6 〇. 38 17· 〇 38. 〇 阿斯巴甜 合成糖精 样椒酸納 檸檬酸
1243685
五、發明說明(11) 抗壞血酸 1.2 檸檬酸卸 2.4 維生素預混合物 〇4 (B2,B6,B12,於鹼酸,泛酸) 橘子調味劑 3.0 β-胡蘿蔔素(1%) 6.0 布雷諾斯(Blanose)纖維素樹膠 1. 〇 (9M31XF)
經由使該粉末(5 〇克)在水(5 〇 〇毫升)中經稀釋以製成供 消費之飲料(pH 3· 4)。 八 實例3 在去離子水中製備擰檬酸溶液,並經0 · 1莫耳濃度氫氧 化納溶液調整至pH 3· 8。以碳酸鈣型式添加鈣及/或以 Ke 1 tro 1 τ型式添加黃酸樹膠。如實例1所述,以4小時之 活體外測定法測試全部溶液。 結果 檸檬酸 單水合物 (CAMH)(%w/v) 黃酸樹膠 (% w/v) Ca/CAMH 莫耳比 4小時琺瑯質損失 (微米) 0.3 0 0 7.6 0.3 0.034 0 5.3 0.3 0 0.3 5.4 0.3 0.034 0.3 2.8
實例4 4選適於抑制齒質腐損之食品級增稠劑 於s π 、υ rPm (剪切速率61· 2 s-1),37 °C下使用配備有UL接
第14頁 1243685 五、發明說明(12) 頭之Br ookf i e 1 d L VDV I I +黏度計,使用足量增稠劑以得到 5-6厘泊之溶液。在去離子水中使用檸檬酸單水合物(AR 級,BDH Merck Ltd)以製成檸檬酸緩衝劑,其並經苯甲酸 納(0.16克/升,AR級,BDH Merck Ltd)保存。除了瓜耳樹 膠於1 0 0 0 rpm下使用磁性攪拌器攪拌一液不同外,使全部 增稠劑在緩衝劑中使用S i 1 v e r s ο η高剪切授拌器滲合2分鐘 以進行水合反應。在水合反應前經由乾滲合以製成增稠劑 混合物。所製成全部溶液之pH為3. 4 0,而可滴定酸度為 0· 3% w/v CAMH (檸檬酸單水合物)。使用緩衝性檸檬酸 (0· 3% w/v CAMH,pH 3. 40)溶液作為對照物。如實例1所 述,以4小時之活體外測定法測試溶液。
O:\60\60228.PTD 增稠劑 品名(供應商) 增稠劑 濃度· (%w/v) 4小時进瑯質 損失(微米) SD (微来) 黃酸樹膠(澄清狀) Keltrol T 0.07 9.8 2.2 黃酸樹膠.. (IFF) 0.07 14.7 1.2 黃酸樹膠 (澄清狀可分散性) Keltrol RD 0.07 6.6 0.8 黃酸樹膠 (Thew Arnott Co. Ltd) 0.07 9.7 1.2 黃酸樹膠(微細篩目) Keltrol TF 0.07 8.3 0.8 黃酸樹膠 Satiaxane 0.07 14.1 1.6 黃酸樹膠(平滑流動) Keltrol SF 0.1 7.2 1.3 黃酸樹膠 (澄清狀/耐鹽性) Keltrol BT 0.07 10.7 2.4 黃酸樹膠/瓜耳樹膠 Lygomme MM3 91 0.22 丨 14.7 1.7 黃酸樹膠/ 羧曱基纖維素鈉 Grinstead JU543 0.12 13.6 2.1 阿拉伯樹膠 (Red Carnation Gums) 10.5 13.7 1.5 丙二醇藻酸鹽 (低黏度) Kelcoloid LVF 0.59 4.8 0.3 丙二醇藻酸鹽 (Red Carnation Gums) 0.45 < 6.9 1.8 丙二醇藻酸鹽 (高黏度) Kelcoloid HVF 0.39 6.3 1.0 藻酸鈉(中黏度) Manucol DH 0.55 2.6 0.9 藻酸鈉(低黏度) Manucol LF 0.75 2.9 0.5 第15頁 1243685 五、發明說明(13) 增稠劑 品名(供應商) 增稠劑 濃度·(%w/v) 4小時琺瑯質 損失(微米) SD (微米) 瓜耳樹膠 (Thew Arnott Co. Ltd) 0.18 11.1 1.2 黃蓍膠 (Thew Arnott Co. Ltd) 0.22 11.0 1.8 Iota鹿角菜脊 Genuvisco type J 0.375 2.7 0.6 高甲氧基果膠 Unipectin QC40 1 9.9 1.1 部份醯胺化低酯杲膠 (柑橘皮) GENU LM 102 AS 1 1.6 0.3 醯胺化低酯果膠 (柑橘皮) GENU LM 104 AS 1 0.7 0.4 部份醯胺化低酯果膠 (柑橘皮) GENU LM 101 AS 1.1 2.0 0.8 低酯果膠(甜橘皮) GENU LM 22 CG 1.2 5.7 0.6 低酯果膠(柑橘皮) GENULM12CG 1.1 1.4 0.6 丙二醇藻酸鹽/低甲氧 基醯胺化果膠(50:50) Kelcoloid LVF & GENU LM 102 AS 0.54 1.53 0.58 丙二醇藻酸鹽/ 黃酸樹膠(66.6:33.3) Kelcoloid LVF & Keltrol RD 0.15 7.57 0.45 對照物 .. - - 24.5 1.9 對照物 - - 20.8 2.0 對照物 - - 24.1 3.8 對照物 - - 30.5 3.17 對照物 - - 19.9 1.53 對照物 - - 29.9 1.53 實例5 在一些p Η及酸度值範圍内添加增铜劑對於抑制齒質腐損之 影響 製備具有通常可在清涼飲料中找到之pH及酸度值之溶 液。溶液之製法為在擰檬酸缓衝劑中,使用S i 1 v e r s ο η高 剪切混合器剪切所需用量之增稠劑2分鐘,並經苯曱酸鈉
O:\60\60228.PTD 第16頁 1243685 五、發明說明(14) -------- 6克/升)保存。經由添加1莫耳濃度NaOH調整該pH至所 王口 ^ /合液得到5至6厘泊黏度值(Brookfield LVD VII + UL接頭,50 rpm,37。〇。如實例i所述,以4小時之活 體1卜測定法測試溶液。該結果證明該科技在-些pH值及黏 度犯圍内減少ί法螂質損失之效力。 增稠^«1 增稠劑濃度 (%w/v) pH 酸度 (%w/w CAMH) 4小時琺瑯質 損失(微米) SD (微米) 對照物\ - 2.5 0.1 63.4 4.4 Keltroi RD __α〇7 2.5 0.1 8.7 12 Keltrol RD __α〇7 2.5 1 0.3 9.7 1.2 Kelcoloid LVF 2.5 0.3 11.5 3.6 對照物 , 2.5 0.3 41.04 0.2 對照物 - 2.5 0.3 30.4 6.1 Keltrol RD __α〇7 3.0 0.7 13.5 1.6 對照物 - 3.0 0.7 34.2 3.8 Kelcoloid LVF __〇55 3.0 0.3 11.6 3.0 Keltrol RD 0.07 3.0 0.3 7.84 1.1 對照物 - 3.0 0.3 23.2 0.4 對照物 - 3.0 0.3 26.3 2.5 Keltrol RD 0.07 4.5 1.0 7.1 1.3 Kelcoloid LVF 0.59 4.5 1.0 11.4 1.0 對照物 - 4.5 1.0 21.2 1.8 實例6 . — 增稠劑之黏度及種類對於活體外琺瑯質損失之影響之測定 測定兩種商業上可得之優良樹膠,高酯柑橘屬果膠 (GENUVIS)及微細緻磨碎黃酸樹膠(KeHr〇i 之黏度對漢 度之圖。在〇· 3% w/v檸檬酸單水合物缓衝劑中使樹膠水 合,並使用1莫耳濃度1〇1{調整至ρΗ 3· 4。於37它下操作 可控制應變之Rhe〇metrix RFSII黏度計(具cuette體形),
O:\60\60228.PTD 苐17頁 1243685 五、發明說明(15) 並使用125 s-i剪切速率製成濃度對黏度之圖形。於所使用 條件下’測定這兩種樹膠之濃度,得到2 · 5厘泊,5 · 〇厘 泊,10厘泊及20厘泊黏度值。使用Br〇〇kf ield LVDVI1 +黏 度計(於60 rpm (104 S—1)及37〇C下,配備UL接頭)測定羧 曱基纖維素納树膝(Red Carnation gums Ltd)之黏度對濃 度分佈圖。經由自該分佈圖使用外延法估計於這些條件下 得到20厘泊黏度所需之大約濃度。使用實例丨所述之筛選 測定法以測試溶液之活體外琺螂質損失。 結果 黏度 (厘泊) %w/v 黃酸樹膠 %w/v 果膠 %w/v CMC 4小時琺瑯質 損失-黃酸樹膠 (微米) 4小時琺瑯質 損失-果膠 (微米) 4小時琺瑯質 損失-CMC (微米) 2.5 0.05 0.67 - 8.7 11.5 5 0.08 0.9 0.17 7.8 12.0 31.0 10 0.14 '1.20 - 2.3 9.0 20 0.24. 1.6 0.39 2.5 1 2.7 13.5 於不同濃度下測試低曱氧基醯胺化果膠(GENU LM 1 0 2 AS)及低黏度丙二醇藻酸鹽(Kelcoloid LVF)之腐損可能 性。於pH 3. 40下使用0· 3% w/v擰檬酸單水合物緩衝劑使 各樹膠溶液進行水合反應。於50 rpm (剪切速率61 2 s—1) 及37 C下使用Brookfield LVDVII +黏度計(配備ul承接器) 測定黏度。 GENU LM 102 AS (%w/v) (厘泊) 4小時珠鄉質損失 (微米、 1.0 5.7 Τδ~~— 0.75 「3.8 Χ4~- 0.5 2.3 -
1243685 ----—, 五、發明說明(16)
Kelcoloid LVF (%w/v) (厘泊、 0.59 0.45
結果證實黏度並非影響該模式 ^ 已發現琺瑯質損失隨著各測試材知可能性之主要因素。 少,但是琺瑯質損失量並不相等黏度增加而普遍性減 定產物種類,尤其於1 〇厘泊或更/、表不腐損可能性為特 具低腐損可能性之酸性組合物。之黏度值最適於調製 實例7 增稠劑及#5對於齒質腐損之影響 使用择樣酸緩衝劑(300克/升9)及苯甲酸納防腐劑⑴克/ 升)製備方便飲用之水果飲料之具—般pH及酸度之試驗調 配物。使用Silver son高剪切混合器摻合該溶液2分鐘。於 50 rpm (剪切速率 61.2 f)及 37。〇下,使用 Br〇〇kfield LVDV I I +黏度計(配備UL承接器)測定黏度。使用實例1所述 之篩選測定法測試溶液之活體外珠螂質損失。該結果顯示 添加增稠劑及約至酸組合物中可以於比不含增稠劑之酸組 合物所需還低之鈣含量及pH值下提供低腐損可能性。 成份 試驗溶液A 試驗溶液B ( 去離子水 800毫升 800毫升 苯曱酸酯儲備溶液 20毫升 20毫升 黃酸樹膠(Keltrol RD) 1.8克 2.0克 檸檬酸健備溶液 20毫升 20毫升 碳酸鈣 0.28 克 0.157 克 去離子水 至1800毫升 至1800毫升 1莫耳濃度NaOH 至 pH 3.40 至 pH 3.20 去離子水 至2升(體積) 至2升(體積)
O:\60\60228.PTD 第19頁 1243685 發明說明(17) 试驗浴液 黏度 (厘泊) pH 可滴定酸度 (%w/w CAMH) 鈣/酸比率 - τ * 4小時琺瑯質 損失(微米) A 8 3.4 0.3 0.1 1.4 B 9 --------------- 3.2 0,3 0.05 3.3 實例8 方便飲用之黑醋栗果汁飲料 一種基劑糖漿之製法如下: 使>苯甲酸鈉(〇 · 8 〇克)溶解在淨水中,並經淨水稀釋至約 2〇〇毫升。先後添加黑醋栗濃縮物(88·2毫升),抗壞血酸 (2.55克)與阿斯巴甜(16〇克),合成糖精(〇〇5克),及山 梨酸鉀(1 · 5 2克)之淨水溶液。添加黑醋栗調味劑(丨·丨4毫 升)至該混合物中,並使該體積經淨水修正為1升。 兩種方便飲用之飲料調配物之製法如下: 抑添加增稠劑至水(2· 5升)中,使用高剪切Silvers〇n混合 器攪拌,並持續混合以形成溶液。使碳酸鈣(若存在)溶解 在淨水中,並緩慢添加至該溶液中。攪拌添加基劑糖漿(i 升)以开》成均勻溶液,然後使體積經水調整至5升。該p H經 1莫耳)辰度氲氧化納修正為3.4。於50 rpm及37°C下使用具 有UL承接器iBrookfiekd LVDII +黏度計測定黏度。這兩 種調配物之可滴定酸度(%w/w CAMH)為〇. 4。使用實例1所 述之篩選測定法測試各調配物之活體外斑瑯質損失。 增稠劑(克) CaC03 鈣/酸. 莫耳比 黏度 (厘泊) 4小時琺瑯質損失 (微米) Kelcoloid LVF (29.5) - - 6.7 3.6 Keltrol RD (4.5) 0.7 0.1 1 7.6 6.2
1243685 五、發明說明(18) 實例9 方便飲用之有泡沬木莓調味飲料
將果膝增稠劑(GENU LM 102 AS)(37.5克)、✓主入溫熱(1 升)中,並使用S i 1 v e r s ο η混合器進行高剪切混合。分別製 成山梨酸鉀(1.28克),合成糖精(0.27克),檸檬酸(14〇 克)與阿斯巴甜(1 · 2 0克)之溶液及抗壞血酸與檸檬酸钟之 溶液,然後添加至該果膠物中,並經混合。添加木每調味 料(2 · 5 1毫升)及胭脂紅紅色顏料(〇 · 5 0毫升)之分散水溶液 至該混合物中以形成一種基劑糖聚,其並經水稀釋至1 6 7 升。該基劑糖漿經碟酸水稀釋(1份糖漿比2份水)以形成泡 沫飲料。於50 r pm及37 °C下使用具有UL承接器之 Brookfield LVDII +黏度計測定黏度。使用實例^斤述之篩 選測定法測試該產物之活體外琺瑯質損失。 該產物具有以下參數: pH ·· 3. 5 酸度(%w/w CAMH ) : 〇· 4 黏度(c P) : 0 2 ί法瑯質損失(m ) . 3 67
實例1 0 方便飲用之可樂調味泡沫飲料 經由混合以下成份製成可樂濃縮物: 磷酸85% : , ^ 130克
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第21頁 1243685 可樂乳液 : 0 · 7 5升 焦糖雙倍濃度 : 3.125# 添加水至 : 10升 經由混合以下成份以製成可半糖裝: 糖漿67 Br ix : 70升 (或阿斯巴甜 :300克) 可樂濃縮物 :2.5升 可樂調味加強劑 ·· 〇 · 0 6升 黃酸樹膠(Keltrol RD) : 420克 添加水至 :1 〇 〇升 該可樂糖漿經碳酸水稀釋(1份糖喈士 5、 U之泡綠料。 禪糖水心水)以形成 實例11 聚乙烯吡咯知I對於抑制齒質腐損之影響 •添加苯甲酸納(0· 16克/升)作為防腐劑,在去離子水中 製備檸檬酸緩衝劑(〇.3%w/v檸檬酸單水合物)。使該溶液 經1莫耳濃度NaOH調整至ρΗ 3·4。以攪拌添加聚乙咯 酮(PVP-K30,125克/升)至該溶液中,並攪拌所形成溶液 20刀鐘。得到pH 3·4,可滴定酸度0.3% w/w CAMH,黏度 4·7 厘泊(37 C ’50 rpm,Brookfield LVDVII+,UL 承接 裔)之溶液。當以4小時使用該活體外腐損篩選測定法測試 時’該溶液之J法瑯質損失1 3 · 8微米,而對照物缓衝劑溶液 之ί法瑯質損失25微米。 實例1 2
O:\60\60228.PTD 第22頁 1243685 五、發明說明(20) 漱口液調配物 使用以下成份製備漱口 液·· 成份 %w/W 乙醇96% BP 8 可溶性糖 0. 06 氣化錄堪基卩比鍵 0. 05 Tego Betain CK-KB5 0. 2 調味料 0. 1 2 醋酸鈉三水合物 0. 05 醋酸8 0 % 0.1575 PVP-K30 12. 5 氣化約二水合物 0.123 去離子水 78· 74 一起混合讀乙醇,氯化錄蝶基D比鍵,T e g ο B e ΐ a i η CK-KB5 (柯卡醯胺基丙基甜菜驗)及調味料以形成一種透 明溶液。在分離容器中, 使各成份剩餘物一起混合並攪拌 20分鐘。然後添加該乙醇系溶液至該水溶液中以製造pH為 4 · 5,且鈣與酸之莫耳比為0 . 4之漱口液。
O:\60\60228.PTD 第23頁 申請日期.孫、之} 1案號:88115457 ” 干 侦尤 發明專利說明書 Λ 發明名稱 中文 自口施用之酸性組合物及其用途 英文 ACIDIC COMPOSITION FOR ORAL ADMINISTRATION AND ITS USES 發明人 姓名 (中文) 1.尼克拉珍貝克 2·大衛梅雅特帕克 姓名 (英文) 1. NICOLA JANE BAKER ............... _ 2. DAVID MYATT PARKER 國稭 1·英國2.英國 …- 住、居所 ? SS i 1 iSSI:ftf市皇家森林工廠 2·夬國葛势桊西轉召起桃★市皇家森林工廠 姓名 (名稱) (中文) 丄,英商史密斯克林貝克曼公司 ----- 姓名 、(名稱) (英文) —國籍— l.iiMITHKLINE BEECHAM PLC------- 1 ϋ 1^! 一 __________________ 申請人 住、居所 (事務所) 代表人 姓名 (中文) 代表人 姓名 (英文)
2001.04. 20.001 1243685 案號 88115457 年&月 五、發明說明(1) Λ ,金.· 曰
本發明係關於增叙劑與〜安定劊在自口施用之酸性組合物 (例如,食物)及口腔衛生護理組合物中減少或抑制與酸消 耗有關之牙齒損害(亦即,齒質腐損)之用途。 齒質腐損之定義為“經由酸及/或螯合作用(不包括細 菌)化學性腐蝕牙齒表面,使牙齒硬組織產生病理學慢性 局部化無痛損失”(I m f e 1 d,1 9 9 6 )。引起該腐損之酸衍生 自飲食,職業性或内源性來源,且並非口内微生物之產 物。由於各年齡層飲食頻率增加之傾向,齒質腐損發生的 機會增加。 國際專利公告(W0 9 7 / 3 0 6 0 1 )描述具有減少牙齒腐損性 質之以酸為主之液體組合物,其中鈣之存在量為每莫耳酸 之0.3至0.8莫耳,且其pH在3.5至4.5範圍内。 通常添加複合多醣樹膠或其它具有黏度調整性質之天然 或合成聚合物至飲料,其它食品及口服產物中作為增稠 劑,安定劑,乳化劑及增構劑。這些聚合物包括天然與半 合成聚合物,例如,藻酸鹽,刺槐木豆樹膠,膠凝糖樹 膠,瓜耳樹膠,阿拉伯樹膠,黃酸樹膠,果膠,纖維素, 及其衍生物;合成聚合物,例如,聚乙烯吡咯酮(PVP)及 其它在本技藝中已知之此種物質。·
Van der Reijden 等人(Caries Res·, 1997, 3 1, 2 1 6 - 2 3 )描述使用含有增稠劑之唾液替代組合物進行一些 活體外實驗以調查其齲齒防護性質,其包括對於活體外琺 瑯質之脫礦質作用及補充礦質作用之影響。亦描述於pH 5 . 0下一些聚合物材料對於羥基磷灰石晶體在5 0毫莫耳濃
O:\60\60228.ptc 第4頁 2001.04. 20.004 1243685 4·妁
案號 88115451、 :车 ----ΓΤΧ:~ 五、發明說明(2) 丨% & \ 度-曰&L中之溶解作用之影響,並描述pH循環實驗,直 使牛的綠瑯質曝露於脫礦質作用緩衝劑(pH 4 · 8 )下^並曝 露於含有一些已溶解聚合物之補充礦質作用緩衝劑(* 7 . 0 )下。 目前頃發現添加具有安定化,乳化及/或增稠性質之天 然及合成聚合物材料至酸性食物與口腔衛生護理組人物中 可減少由於自牙齒琺瑯質損失鈣與磷酸(其通常與此"種產 物有關)所產生之牙齒腐損。 而且,頃驚訝地發現添加一或多種此種聚合物材料及好 至口腔用途之酸性組合物中比單獨添加聚合物或約更能夠 大大地減少牙齒琺瑯質中之鈣及磷酸鹽損失。因此 == 此W0 9 7 / 3 0 6 0 1中所揭示還低之"值下,以每莫耳較,丨、於 鈣調配既可口又具貯藏安定性且能夠有效減少由於之 之齒質腐損之口腔用途之酸性組合物。 、文所致 因此,本發明係提供一種黏性調整聚合物材料 施用之酸性組合物中之牙齒腐損抑制劑之用途,其:口部 合物之有效pH小於或等於4 . 5。 ’、节該級 本發明另一方面係提供一種自口施用之組合物,复 酸化劑,黏度調整聚合物材料及詞化合物,其中該^包含 中妈之存在量至高每莫耳酸之〇·8莫耳,且該組合物且合物 效pH小於或等於4. 5。 〈有 根據本發明之自口施用之組合物有效pH根據產物 酸含量及所要器官感覺性質而不同。供使用於本發 =、, 合組合物之有效pH在2· 0至4· 5範圍内,更佳自2· 5至4適
O:\60\60228-940817.ptc 第24頁
Claims (1)
- I 1243685 前 六、申請專利範圍 1 . 一種自口施用之酸性組合物,其含有黏度調整聚合物 材料作為牙齒腐損抑制劑,該黏度調整聚合物材料為複合 多醣物質,其中該組合物之有效pH範圍為2. 0至4. 5。 2 .根據申請專利範圍第1項之酸性組合物,其中該複合 多醣物質為一種藻酸鹽,黃酸樹膠或果膠。 3 .根據申請專利範圍第1至2項中任一項之酸性組合物, 其中該酸化劑包括檸檬酸,蘋果酸,乳酸,酒石酸,磷 酸,醋酸或其混合物。 4 ·根據申請專利範圍第1至2項中任一項之酸性組合物, 其中該酸性組合物含有一種#5化合物,致使#5係以每莫耳 酸最高0.8莫耳含量存在於該組合物中。 5 .根據申請專利範圍第4項之酸性組合物,其中該鈣源 為一種可溶性妈鹽。 6 .根據申請專利範圍第1至2項中任一項之酸性組合物, 其中該酸性組合物為一種飲料,或用以製備飲料之液體或 固體濃縮物。 7.根據申請專利範圍第6項之酸性組合物,其中該飲料 為一種健康飲料。 8 .根據申請專利範圍第1至2項中任一項之酸性組合物, 其中該酸性組合物為一種口腔保健產品。 9.根據申請專利範圍第6項之酸性組合物,其中該飲料 之pH在2. 5至4. 0範圍内。 1 0 .根據申請專利範圍第6項之酸性組合物,其中該飲料 之可滴定酸度在0.01至4% w/w範圍内。O:\60\60228-940817.ptc 第25頁
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1998
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- 1999-08-31 DK DK99946084.3T patent/DK1112003T4/da active
- 1999-08-31 CN CN99813090A patent/CN1108110C/zh not_active Expired - Fee Related
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