TW482685B - Lipophilic carrier preparations comprising digalactosyldiacylglycerols - Google Patents
Lipophilic carrier preparations comprising digalactosyldiacylglycerols Download PDFInfo
- Publication number
- TW482685B TW482685B TW084101256A TW84101256A TW482685B TW 482685 B TW482685 B TW 482685B TW 084101256 A TW084101256 A TW 084101256A TW 84101256 A TW84101256 A TW 84101256A TW 482685 B TW482685 B TW 482685B
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- Prior art keywords
- polar
- galactolipid
- scope
- composition
- lipids
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- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
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- A—HUMAN NECESSITIES
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- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
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- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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Landscapes
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Description
經濟部中央標準局員工消費合作社印製 482685 A7 __^_ B7___ 五、發明説明(1 ) 技術範圍 本發明關於有連續脂相的親脂性載體製劑,含有與非極 性脂合併的極性脂物質,視需要也含極溶劑。該載體製劑 適用作醫藥組合物中活性劑的載體,及化妝、食物及農業 產物中活性劑之載體。 發明背景 在翳藥工業上,將藥物與生物相容性的並具人類良好耐 受性的親脂載體合用,是普遍的問題。其原因在,第一, 所合用的活性成分的化學結構的範圍廣大,及因此而導致 的性質的各異;第二,按各成分所選用的載體須是與具廣 範圍結構的各活性成分有充分適用性的。 為要製成充分適用性的親脂載體,需使用極性脂,為生 物相容性及安全起見,較佳是用天然的膜脂,與非極性脂 如植物油或固醇酯合用。琨在唯一可用的膜脂是磷脂質物 質,多油大豆或卵磷脂輸衍生而來,或經合成製得。磷脂 質是兩性離子的,如磷脂醯膽鹼及磷脂醯乙醇胺,或是帶 有負電荷的,如磷脂醯肌醇或磷脂醯甘油。 親脂性載體可Μ是有機化溶液,如微乳液或反相膠束溶 液,反相泡或水包油乳液。 人造奶油及塗抹食品為油包水乳液,可含多達75¾重量 比的水相。此水相分散於三酸甘油酯的油内,典形的是植 物油,如菜子油。此水相一般含增稠劑,如明膠,K使多 水的油連續性乳液安定。乳化劑一般是磷脂質,如大豆磷 一 4 - 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再頁) 、>τ % 經濟部中央標準局員工消費合作社印製 482685 -A7 ____B7____ 五、發明説明(2 ) 脂質(大豆卵磷脂)。此等乳化劑由磷脂質類混合物所構 成,如兩性離子的磷脂醯膽鹼及磷脂醯乙醇胺,及離子性 的磷脂醯肌醇。通常都知道此等卵磷脂乳化劑是工業尺度 上製造安定的食物乳液的最常使用的天然脂。也都知道, 此等乳液具與卵磷脂乳化劑有關的缺點和問題。 先前技藝 現在只有少數具連續脂相親脂性製劑的例報告過。 W0 92/05771敘述至少有二脂成分的形成脂顆粒的基質 •,之一是非極性的,另一是兩親的及極性的。此一可含生 物活性物質的形成顆粒的基質,在與水性糸統互相作用時 同時也形成分散的脂顆粒。據說此兩親的及極性的脂成分 可形成雙層,係選自磷脂質,如磷脂藤膽鹼;而此非極性 脂為單-,二-或三酸甘油酯。 P · L · L n i s i曾就含卵磷脂(即磷脂醯膽鹼)的微乳液 凝膠作過敘述並說明其特徵,見,例如,D. Cap it an i et al·, Langmuir, 1993,V o1. 9,頁 685 - 689° 除鱗脂 質外,此等凝膠遷含少量的水及有機溶劑,如烷類,脂肪 酸酯及胺類。這些也稱為有機凝膠。此等凝膠可用作經皮 吸收的藥物的基質。 油體内與正常泡相反構造的反相泡的存在,係Η . Kunieda 首先報告,見,例如,H. Kunieda et al·, advanced Materials, 1992, Vol. 4,頁 291- 293。反相 泡為層狀液體结晶的分散液,可使油體的量增加,亦即此 -5 - 本紙張尺度適用中國國家標準(CNS ) A4規格(210'〆297公釐) (請先聞讀背面之注意事項再本頁) 甘
經濟部中央標準局員工消費合作社印製 482685 A7 ____B7___ 五、發明説明(5 ) 泡由反相雙層構造構成。此反相雙層一般含有親水及親脂 兩親物的混合物。 糖基甘油酯為糖脂的一型,是植物綑胞膜的普遍知道的 成分。常見的是K半乳糖為基本構造的二種類型,單半乳 糖基二醯基甘油(MGDG)及二半乳糖基二釀基甘油(DGDG) ’ 佔類囊體膜的乾重量的達40¾ 。 植物糖脂含碳水化合物單位,主為半乳糖,聯於甘油上 。於MGDG中,半乳糖環的1-位上有聯於甘油的冷-鏈,而 在DGDG中在各糖間有a,1巧6鐽。較少的成分是植物硫苷 脂,更正確的名稱是磺異鼠李糖基二醯基甘油,SQDG,於 脫氧葡萄糖殘基末端第6個碳上含磺酸脂而非羥基。多數 楂物糖脂可以下式說明
Ri-〇-CH2
I
R2-0-CH
I H2C斗0-碳水化合物-ch2 + n-r3 其中1及R2各獨立是飽和的或不飽和的2-24個碳原子的有 0 - 6個雙鐽的脂肪酸殘基,進一步酯化的羥基酸,即酯脂 (estolides),或氫;此碳水化合物為單糖單位;η = 1 -5 ;而R3是羥基或磺酸酯基團。 SE 9400368-8揭示可供工業使用的藉萃取及色層分析分 離方法由植物製備糖基甘油酯的製法。 在研究糖基甘油酯與非極性脂,如單-,二-及三酸甘 -6 - 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閲讀背面之注意事項再^^本頁) 訂 % 482685 A7 B7 經濟部中央標準局員工消費合作社印製 五、發明説明(4 ) 油酯,脂肪醇酸,固醇及固醇酯,視需要與其他極性脂( 如磷脂及神經鞘脂類),在水內或少量水内的交互作用時 ,發明人驚奇地發現,此類製劑可用作藥物的親脂性載體 ,也可用作皮虜保養、營養劑及食物的調配物。 本發明說明 本發明提供Μ極性脂物質半乳糖脂為基礎的與非極性脂 合併使用的脂載體。此半乳糖脂的極性頭為半乳糖單位, 與磷脂質相比,有不同的物理化學性質。此結合機制係Μ 極性頭(即半乳糖單位)的羥基與半乳糖基醯基甘油的親 脂鏈及非極性成分,與要結合的化合物的交互作用為基礎 〇 本發明關於有連續脂相的親脂性載體製劑,含有與非極 性脂合併的極性脂物質,視需要也含極溶劑,其特點在此 極性脂是半乳糖脂物質,含至少50%的二半乳糖基二醯基 甘油,其餘為其他極性脂。 於較佳的製劑中,此半乳糖脂物質含約70-80¾的二半乳 糖基二醯基甘油,及20-30¾的其他極性脂。 於另一較佳的製劑中,此半乳糖脂物質含達100¾的二半 乳糖基二醯基甘油。 此二半乳糖基二醯基甘油可K如下通式說明 一 7 - 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閲讀背面之注意事項再本頁) Μ 翁 482685 Α7 Β7 經濟部中央標準局員工消費合作社印製 五、發明説明(5 )
RrO-〒 H2
R2-0-CH I H2C+0 -半乳糖單位 -CH2 - R3 其中^及^各獨立是飽和的或不飽和的10 - 22個碳原子的 有0 - 4個雙鐽的脂肪酸殘基;而R3是羥基或磺酸酯基團。 作為較佳的脂肪酸殘基,R α及1^2可以說是天然的脂肪釀 基基團,如由飽和酸棕櫚酸(C15H3:tCO; 16:0)及硬脂酸 (C^HsKO; 18:0)得來的殘基;由單未飽和酸油酸 (ClvH33CO; 18:1)得來的殘基;由多未飽和的酸亞油酸 (C17H31CO; 18:2)及亞麻酸(C17H2QCO; 18:3)得來的殘 基。此等脂肪酸殘基也可含K其由其他脂肪酸酯化的羥基 聯於甘油基上的羥基酸,即所謂酯脂。 為半乳糖脂物質一部分的其他極性脂為不同葡糖酯及磷 脂的混合物,如MGDG及磷脂醯基膽鹼。組合物取決於用Μ 製備半乳糖脂的起始物質及方法。 半乳糖脂物質各成分的特定比例對本發明並不重要,只 要DGDG的含量至少是50%即可。但在多數使用情形下,高 含量DGDG (最重要的形成雙層的成分)可達最佳優點。 半乳糖脂物質可由幾乎所有植物材料萃取。較佳的植物 材料是穀類的種子及仁,如小麥,裸麥,燕麥,玉米,大 米,粟及芝麻。燕麥粗穀及小麥麵筋的脂濃度較高,有用 於製備方法的優點。 Κ半乳糖或其他單糖單位(如葡萄糖)為基礎的合成的 -8 一 本紙張尺度適用中國國家標準(CNS ) Α4規格(210><297公釐) (請先閲讀背面之注意事項再頁) Μ 482685 A 7 __^___ B7___ 五、發明説明(6 ) 二糖基二醯基甘油,及從任何來源分離出來的M其他碳水 化合物單位而非半乳糖為基礎的天然的糖基甘油,根據本 發明都可使用。 非極性脂方面並無特別限制。植物油,動物油,合成油 ,脂肪酸,天然的及合成的甘油酯,固醇酯,脂肪醇,等 等,可例舉說明。 使用半乳糖脂可製得所有形式的親脂有機化溶液。結合 的活性物質可為有機化的溶液的一部分*也可Κ,例如, 懸浮液的形式安定化。 舉例說,親脂性載體製劑可藉混合半乳糖脂與非極性脂 ,如三釀基甘油,製得。三釀基甘油可選自棕櫚油或其他 相似的有較高固體脂肪含量或熔點的天然油。較佳的合適 的三醯基甘油是棕櫚油分餾物,由分餾商業棕櫊袖成三藤 基甘油特定混合物製得,視甘油的主為棕櫚酸、油酸及硬 脂酸的酯的合併而定。 親脂性載體製劑也可藉混合半乳糖基甘油脂與液體三酸 甘油酯(如中等鏈的三醯基甘油(MCT)及大豆油)製得。 此外,非極性脂-半乳糖脂混合物可含導致形成反相泡 、反相囊及油包水的含量增加的水或水溶液。 反相泡係藉Κ 4 : 1重量比加半乳糖脂及更極性的兩親物 (如溶血磷脂醯膽鹼)的混合物至三酸甘油酯油(較佳是 MCT油)内製備。兩親物的總濃度小於3% (重量/重量) 。然後再加少量(小於總製劑的1!« (重量/重量)水或水 溶液。經超音波振動後即製成反相泡的细分散液。 本紙張尺度適用中國國家標準(CNS ) Α4規格(210 X 297公釐) I·: - · (請先閱讀背面之注意事項再本頁) 、1-τ 經濟部中央標準局員工消費合作社印製 482685 Α7 Β7 經濟部中央標準局員工消費合作社印製 五、發明説明(7 ) 可製成較高糖基脂濃度(但水含量仍低)(總製劑的 0· 2 4¾ (重量/重量)的反相囊。反相囊也稱作微乳液, 由油內的水聚集體構成。聚集體的形狀及構造可形成黏性 系統,即、、微乳液凝膠"。 可形成更高水含量(大於總製劑的5¾ (重量/重量)) 的油包水乳液。此類乳液有二相系統,由油内的細分散的 水構成。油包水乳液為熱動力學上不安定的,但可為動力 學上安定的。 水溶液可含純水,緩衝液,生理鹽水,葡萄糖、半乳糖 、丙烯二醇、聚乙烯二醇、甘油等的溶液。此外也可使用 增稠劑,如明膠,瓊脂糖,鹿角菜,甲基纖維素,及乙羥 乙基纖維素。 本發明遷關於使用上述親脂性載體製劑作為醫藥、化妝 品、食物或農業產物中活性劑的載體。 本發明選關於含上述親脂性載體製劑的醫藥組合物,其 中非極性脂為MCT油,夜櫻草油,棕櫊油分餾物,或生物 活性物質。 此生物活性物質可為親脂性藥物,如抗癌劑,抗微生物 劑特別是抗黴菌劑,免疫抑制藥物如環孢素,皮虜學藥物 ,如止痛劑及消炎劑*止癢劑,消毒劑,收斂劑,洗劑, 及激素,影響精神的藥物,麻醉藥物及其他親脂性藥物, Μ及使用半乳糖脂才能解決調配物製造上的問題的藥物。 選有多種脂如自由態的脂肪酸,單-、二-及三醯基甘油 ,磷脂,膽固醇酯及其他本身有治療活性的脂與利於製成 一 10 - 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) JI— · (請先閲讀背面之注意事項再?本頁) 訂
482685 A7 B7 五、發明説明(8 ) (請先閲讀背面之注意事項再本頁) 親脂性載劑的脂,都Μ半乳糖脂為基礎。如係此情形,生 物活性物質是非極性脂。 翳藥及化妝製劑可由在開放水浴内於40 - 70 °C熔化棕櫚 油部分製備。稱出有效成分及糖甘油酯的重量加於小瓶内 。將熔化的棕櫚油分餾物移入小瓶,此混合物K高剪混合 器於近1000轉/分鐘於40 - 70 °C分散2 - 4分鐘。再加形成 典形的可使用的調配物所需的水或水溶液,再用棒小心將 調配物混合。 醫藥組合物可調配成供動物,特別是哺乳動物(包括人 ),經口、經腸、非經口、經直腸、經陰道、局部、眼、 鼻、或耳給予。 局部皮虜保養製備,K其使用方式可粗分為醫藥局部皮 膚保養製劑及化妝製劑。 醫藥局部皮膚保養製劑的例有各種含一或多種有效成分 的罾劑。膏劑包括含油基的及含水包油或油包水乳液型基 的。 在用作化妝品製劑時,可將主要的成分與一般常規使用 的化妝品成分,如油性物質,紫外線吸收劑,醇,螯合劑 ,出調整劑,防腐劑,增稠劑,色素,香料等按所需混合 經濟部中央標準局員工消費合作社印製 〇 作為化妝品*可調配成各種形式的皮虜化妝品製劑,例 如油包水或水包油形式的乳化化妝品,霜,化妝品乳液* 化妝水,油性化妝品,口紅,粉底,皮虜清潔製劑,養髮 劑,頭髮成形製劑,頭髮光澤製劑,頭髮生長刺激劑,等 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 482685 A7 B7 五、發明説明(9 ) 等。 油包水乳液,例如人造奶油及食品塗抹,係K傳統方法 製備。 半乳糖脂物質 如下所述,半乳糖脂物質係由各種榖類製備,並用於製 造本發明實例所述之載體製劑及醫藥組合物。除非另有說 明,說明中所用%指重量%。然溶劑混合物中各溶劑的比 則指容積比。 由燕麥製得半乳鑛脂物皙 將200公斤燕麥仁(Kungsornen AB, Sweden)磨碎,用 1 000公升95¾的乙醇於70 1C在萃取桶内在攪拌下萃取3小 時。趁熱將此泥樣物離心,並從固體顆粒中分出。液體部 分於60 °C蒸發,得約10公斤淺棕色油體。 將此油體加於含6.25公斤二氧化矽膠(Matrix Silica ^,顆粒大小20- 45毫米,孔直徑60义,購自^1(:(^ Corp.,USA)之不銹鋼柱上。柱溫為50°C。然後用30公升 己烷:異丙醇混合物,90 : 1 0,洗,除去所有非極性脂。 經濟部中央標準局員工消費合作社印製 再用20公升己烷:異丙醇混合物,60 ·· 40,從柱上洗離 半乳糖脂物質,製得半乳糖基二釀基甘油分餾物。將此分 餾物蒸發,得約700克DGDG,為主要的脂類。再將半乳糖 脂物質溶於水内,凍乾,即形成自由流動的粉。 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 482685 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(10 )
由半乳鑛脂增冬DGDG 將5 0克由燕麥製得之半乳糖脂,含DGDG約70% ,溶於 250毫升己烷:異丙醇,70: 30,内,使總容積為300毫 升。將所得溶液載於二氧化矽膠(110克)柱上,Μ 1公 升己烷··異丙醇混合物,70 : 30,洗離。此增多DGDG的部 分再用2公升丙酮洗離。將丙酮部分蒸發並凍乾。17克總 產出物幾為純DGDG產物。 糖脂之舅化... 將200克上述自燕麥製得之半乳糖脂溶於2公升溫異丙 醇内。將15克鈀/碳催化劑(Pd 15%,水分53%,
Engelhard Rome s.r.i·, Italy)置於壓力反應器(
Model No. 4552M; Parr Instrument Co·, USA)底部,此 反應器攪拌器軸上裝有二葉輪。將溶液在氮封下移入反應 器,減少著火危險。將反應器封閉,先K氮氣加壓三次Μ 排除空氣,再Μ氫氣(Plus 4. 5,購自AG A Gas ΑΒ,
Sweden)加壓三次。然後將氫壓維持於6巴,將攪拌器定 於600轉/分鐘,將混合物加熱至7〇 °C。反應混合物加熱 至所定溫度費時1 4分鐘。氫化反應進行6小時後,將反應 產物用0.45微米的過濾器過濾,排除碳顆粒及鈀。於迴旋 蒸發器上蒸發去溶劑,再將殘餘固體物質番散於1600毫升 去離子水内,凍乾。 經過濾及凍乾後得氫化半乳糖脂155克。此氫化程度K 氣體色層分析評估;氫化產物中只能測定出飽和脂肪酸。 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閲讀背面之注意事項再本頁) 討
482685 A7 B7 五、發明説明(n ) 由小麥麵筋製诰半乳糖脂 將1公斤小麥麵筋粉(AB Skanebranner丨er, Sweden)用 4公升95¾的乙醇於70 °C在燒杯内萃取3小時。在400 -5 00千帕壓力下過濾此泥樣物,所得濾過物用1公升95¾ 的乙醇洗。合併之乙醇溶液於最高溫60 1C下蒸發,得約 60克黃色油體。 將此油體加於含45克二氧化矽膠(Mat rex Si 1 lea Si ,顆 粒大小20- 45毫米,孔大小60义購自&1!1丨〇〇110〇1^·, USA)之不銹鋼柱上。再用700毫升己烷:異丙醇混合物, 90 : 10,洗此柱,除去中性脂。 此柱再用1000毫升己烷:異丙醇混合物,70 ·· 30,洗, K除去MGDG及其他極性脂。再用1000毫升純丙酮洗離 DGDG。蒸發後製得約4克幾為純DGDG^i物。 Λ 由裸麥製诰半乳糖脂 將100克裸麥片(Kungsornen AB, Sweden)於工業用己 烷及異丙醇混合物,90 : 10,内攪拌60分鐘。此泥樣物經 過濾及蒸發後製得〇 . 5克極性脂。將此殘餘物溶於1 〇毫升 * 己烷:異丙醇混合物,70 : 30,内,載於三相聯成一系列 的 Sep-pak sillica plus柱(Millipore Corp·,USA)上, 用20毫升同樣的溶劑混合物洗,再用15毫升丙酮洗離。將 洗離物蒸發,凍乾,製得47毫克半乳糖脂。 不同半乳糖脂物質的化學及物理定性。 一 14 - 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再本頁) 1r
經濟部中央標準局員工消費合作社印製 482685 Α7 Β7 五、發明説明(12 ) 賠分析 脂類分析係用高效液體色曆分析(HPLC)完成’使用裝有 二醇修改的(d ί 〇 liolified)二氧化矽膠(Lichrosphere 100 DIOL, 5微米,250毫米x4毫米内直徑;Ε·
Merck,GerroarTy)的柱。此柱於水浴内於75°C封閉。分析 系統由 HPLC泵 CM 4000 (LDC/Milton roy, USA) ’ 及注射 器,model 7125,具一 20 微升的注射環(Rhe o dyne Inc·, USA),構成。所用蒸發光散射測定儀為Sedex 45 (S.E.D.E.R.E·, France),分別裝有 Sedex 55霧化室,上 有漂移管溫度及97 °C與2 · 0巴的空氣入口壓。 分析過程中移動相的流速為1毫升/分鐘。使用二元溶 劑梯度,線性超過25分鐘,^100¾ A開始,M 100¾ B結束 ,此處A =己烷:異丙醇:正丁醇:四氫呋喃:異辛烷··水 ,64: 20: 6: 4·5: 4·5: 1,而B =異丙醇:正丁醇:四氫 呋喃:異辛烷:水,7 5 : 6 : 4 · 5 : 4 · 5 : 10 。所有溶劑都 含醋酸銨180毫克/公升。 經濟部中央標準局員工消費合作社印製 (請先閲讀背面之注意事項再本頁) 數據收集及處理使用GynkoSoft Data system version 4.22 (Softtron Grobh, Germany)。分析標準注射量為 100 微克。Μ 與確認的標準(karlshamns LipidTeknik AB, Sweden)比較滯留時確定。此系統未測出揮發性化合 物。定量分析Μ峰面積計算作基準。 電勢係用 Zetasizer 4 儀(Malvern Instruments L t d . , I丨K)於半乳糖脂稀水分散液測定。 本紙張尺度適用中國國家標準(CNS ) Α4規格(21〇Χ297公釐) 482685 A7 _____B7 五、發明説明(15) 表 1 不同半乳糖脂物質的定性 〇 一 GL o-h-GL 〇-DGDG w - G L w - D G D G — 卜GL DGDG含量, 面積% 73 70 72 100 80 100 67 Z-電勢, 毫伏特 -74 - 76 - 30 -51 -75 - 38 - 37 ----- (請先閲讀背面之注意事項再本頁} £ 訂 於此表1及下表2中使用如下的縮寫: o-GL =由燕麥製得之半乳糖脂 〇-h-GL =氫化的由燕麥製得之半乳糖脂 〇-DGDG =加強的由燕麥製得之半乳糖脂 w-GL =由小麥製得之半乳糖脂 w-DGDG =加強的由小麥製得之半乳糖脂 r-GL =由裸麥製得之半乳糖脂
_防S#分析 經濟部中央標隼局員工消費合作社印製 脂肪酸分析係於脂轉脂化成脂肪酸甲酯後用氣體色層# 析完成。此等脂肪酸係於裝配有毛细管柱30米X 〇· 25毫# 内直徑(DB-WAX; J&W Scientific, USA),柱上注射器及 燄離子化測定器的Varian 3500毛細管氣體色層分析儀分 離出並作定性分析。使用氦作載體氣。使用GynkoSof t -16 一 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 482685 A7 ____B7_____ 五、發明説明(14 )
Data system version 4.22 (Softtron GmbH, Germany) 完成資料整理。轉酯化係由加1毫克脂樣品至2毫升碳酸 二甲酯:異辛烷,1 : 1,内完成。加1毫升2 . 3克納溶於 200毫升甲醇内的溶液,將試管強烈搖動30秒,並於室溫 置15分鐘K確保反應完全。加3毫升水,再搖動試管,然 後Μ 2x重力離心。將0 . 5微升有機層注射於據下述分離條 件的色層分析儀上。爐K溫度控制操作,從130 °C ( 2分 鐘)起始,增加至150°C (30。/分鐘)及220 °C (3.2°C/ 分鐘 > ,每一階段維持10分鐘。注射器溫度為13〇υ ,測 定器溫度為250它。開使時氣流為2.7毫升/分鐘。使用 外標準方法Μ正常化的重量百分比表示結果。校正因子未 用於少量成分,因尚缺乏標準或可接受的純度。 (請先閱讀背面之注意事項再本頁) 討
經濟部中央標準局員工消費合作社印製 -17 - 本紙張尺度適用中國國家標準(CNS ) Α4規格(210 X 297公釐) 482685 A7 B7 五、發明説明(15) 表 2 脂肪酸組合物定性 脂 肪 酸 姐 合 〇 -GL 0-h-GL o-DGDG w ~ G L w-DGDG r-GL 物 重 量 % C 14 :0 1 C 16 ··0 20 21 21 16 15 13 12 C 18 :0 1 1 74 2 1 1 C 18 ·· 1 η -9 17 17 19 6 5 8 C 18 :1 η 1 1 1 1 1 1 C 18 :2 η -6 53 52 58 71 68 69 C 18 :3 η -3 2 2 3 3 3 5 少 量 物 質 6 6 5 1 3 8 5 <1% 及 未 確 定 者 (請先閱讀背面之注意事項再本頁) Μ 經濟部中央標準局員工消費合作社印製 二半乳糖某二_基甘油之NMR光譜 MBruker AM-400 光譜儀(Bruker Analysische Messtechnik GmbH, Germany)於 100.614 MHz 13C 頻率記 錄一向量去偶合質子的天然存在的13C H MR光譜。脈衝角 為36。,脈衝重複時為1 . 0秒,每數據點解析為1 . 526 Hz。過程中使用3 Hz線擴大。樣品(10 - 40毫克)K 730 微升 DMS〇-de (Aldrich Chemical Comp., Inc·, USA)及 20微升 D2O (Aldrich Chemical Comp·,Inc·,USA)混合 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 482685 A7 B7 五、發明説明(16 ) 物稀釋,並移至NMR管(5毫米內直徑)。 表 3 由小麥及燕麥製得之二半乳糖基二醯基甘油之1 3C化學 位移(P P 1B ) 經濟部中央標準局員工消費合作社印製 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 482685
A B 五、發明説明(17 ) 經濟部中央標準局員工消費合作社印製 信號 w-DGDG o-DGDG 脂肪酸部分 C (η ) 13.8 13.7 C(η- 1 ) 21.9 21.9 C (η-2) 30 . 8 30,8 C,伸甲基 28,3-28.9 28 . 4-29·0 C ,烯丙基 26 . 5 26,5 C ,雙烯丙基 25 . 1 25 . 1 C,烯屬 127.6-129.6 127.6-129.5 C3 24. 3 24.3 C2 33.3, 33.5 33.3, 33.5 C1 172.2,172.5 172.1, 172.4 甘油部分 s η - 1 62,3 62,4 s η - 2 69 . 8 69 . 8 s η - 3 66,6 66.6 二半乳糖基部分 C1 (内) 103.6 103.6 C f (外) 99,4 99.4 其他 60.4, 66.3, 60.4, 66.3, 67.7, 68.2, 67.7, 68.2, 68.6, 69,3, 68.6, 69.3, 70 ♦ 1 , 71♦1, 70.1, 71.1, 72· 8, 72·8 72.8,72· 9 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 482685 A7 _B7______ 五、發明説明(18 ) 實例1 . 親脂性載體之製劑(加強夜櫻草油’含20%的7 -亞麻酸(G L A )) 以下列成分製備親脂性載體 50 . 50 . 請 閲 讀 背 之 注 意 事 項 成—分…
半乳糖脂物質 加強夜櫻草油,20% GLA 將半乳糖脂物質於3分鐘22, 000轉/分鐘高剪混合下分 散於油内。然後將油相於50 置40分鐘。製得澄清高黏度 的親脂性載體,此載體冷至室溫時仍為澄清的。 實例2 . 含5%環孢素A之親脂性載體之製備(加強夜櫻草 油,含20¾的GLA) 含醫藥活性化合物的親脂性載體K下列成分製備: 經濟部中央標準局員工消費合作社印製 分 成 ¾ 質油 物草 脂櫻 A 糖夜素 乳強孢 半加環 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 482685 Α7 Β7 五、發明説明(19 ) 將半乳糖脂物質於2分鐘22, 〇〇〇轉/分鐘高剪混合下分 散於油内。將親脂性載體加熱至50 °C,變成澄清。此澄清 油相内加環孢素A 。將環孢素/油混合物維持5 0 °C,不時 搖動,至成澄清液體。 實例3. 含抗壞血酸基刊-GL A之親脂性載體之製備 Μ下列成分製成凝膠: (請先閱讀背面之注意事項再本頁)
成分 1 抗壞血酸基-6 ~ G L A 6.25 半乳糖脂物質 40.72 MCT油 53.03 、τ 將抗壞血酸基-6-GU ,抗壞血酸的7 -亞麻酸酯(購 自Callanish Ltd., Scotland)分散於油內。再將半乳糖 脂物質加於分散液内,然後將混合物加熱至約50 °C,再作 高剪混合。冷至室溫後,製得黏性稍渾濁的安定的分散液 〇 實例4. 無水硫蘭姆調配物之製備 硫蘭姆之非經口給予調配物,抗乙醇藥,Μ下列成分製 本紙張尺度適用中國國家標準(CNS ) A4規格(210x297公釐)
經濟部中央標準局員工消費合作社印製 482685 A7 B7 五、發明説明(20 ) 備: 由燕麥製得之半乳糖脂 硫蘭姆 MCT油 20 . 32· 48· 使用ultraturrax均質器以2000轉/分鐘使各成分混合 15分鐘,再以3000轉/分鐘混合5分鐘。 形成懸浮液,含高量细分散的硫蘭姆顆粒,稠度一致。 此懸浮液有極佳物理安定性,於室溫下儲存不見有沉澱。 懸浮液的黏度較低,此調配物可用細針注射筒(:内直徑 1 . 0毫米)遞送。 此調配物可滴注於人十二指腸,於此處發揮硫蘭姆的長 效抗乙醇作用。
訂 經濟部中央標準局員工消費合作社印製
本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 482685 A7 __B7 五、發明説明(21 ) 實例5 . 反相泡之製備 Μ下列成分製成反相泡:
組合物Α 組合物B 成分 由燕麥製得之半乳糖脂 1.65 1 . 56 溶血磷脂醯基膽鹼,由 0.40 -- 大豆製得 磷脂醴基肌醇,由大豆製得 一 0.38 水 0 · 5 6 0,64 MCT 油 97·39 97.42 稱出各成分後,於超音波振盪浴内在30 - 40 °C作超音波 振盪1小時。所形成的綑分散液安定性超過一星期。其内 之大反相泡Μ有錄影增強糸統(A r g u s 1 0 ; H a m a m a t s u Photonics Co., Japan)的示差干擾相對比顯微鏡 (X2F-NTF-21; Nikon, Japan)評估。 經濟部中央標準局員工消費合作社印製 此實例之反相泡係K脂成分作基礎,適用於醫藥及化妝 品給予。過去係用磷脂或合成界面活性劑於烴屬油内製備 ,後面二種成分一般對人毒性太強,不宜使用。而且,根 據本發明的反相泡較過去Μ合成界面活性劑及烴屬油所製 成者有較佳安定性。 -2 4 - 本紙張尺度適用中國國家標準(CNS ) Α4規格(21〇Χ:297公釐) 482685 A7 ___ B7_ _ 五、發明説明(22 ) 請 先 閱 讀 背 之 注 意 事 項 再 反相泡分散液是有機化溶液的一例,此分散液可結合生 物活性物質,例如蛋白質藥物如干擾素,肽激素如降鈣素 或胰島素。藉反相泡手段使溶於水的蛋白質藥物或激素結 合於三酸甘油酯油內,可使藥物易於通過親脂性細胞膜。 藥物分子位於反相泡之雙層内,也對藥物有安定作用。特 定地說,藥物經口給予後可免於在腸内降解。 實例6 , 反相囊之製備 高黏性的反相囊凝膠(有機凝膠,微乳液凝膠)係如下 製備: 訂 經濟部中央標準局員工消費合作社印製 成分 由燕麥製得之半乳糖脂 17 . 9 MCT油 81.3 水 0.8 將半乳糖脂物質與MCT 油混合成均質分散液 。在連續攪 下於分散液内滴加水。 立即形成澄清凝膠, 高黏度維持 一個月Μ上。 實例7 . 微乳液之製備 微乳液Μ下列成分製備: 25 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) 482685 A7 B7 五、發明説明(25 ) 成 分 1 抗 壞 血 酸 基-6 - G L A 7 · 49 半 乳 糖 脂 物質 17 ♦ 66 MCT 油 63. 53 水 11 · 32 請 閲 讀 背 面 之 注 意 事 項 經濟部中央標準局員工消費合作社印製 將抗壞血酸基-6 - G L A分散於油內。分散液内加半乳糖脂 物質。於此油相內在高剪混合下加溫膜濾過的水。即製成 澄清的淺黃色的液體。 實例8 . 油包水乳液之製備 油包水乳液以下列成分製備 成分 由燕麥製得之半乳糖脂 20 , M C T油 49 ‘ 1.0¾的水性鹿角菜凝膠 3 0 , 將半乳糖脂物質與MCT油混合成均質澄清分散液。再將 於60 1C熔化的鹿角菜凝膠在高剪混合下緩慢加於油相内。 冷至室溫後,即形成高黏度的牛奶樣油連續性乳液。 26 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐)
Claims (1)
- 482685 第84101256號專利申請案 中文申請專利範圍修正本(8 7年4月) A8 B8 C8 D8 修正 申請專利範圍 3 . 經濟部中央梂準局只工消費合作社印装 一種具連 質與非極 性脂基質 半乳糖二 之其他極 其中該親 半乳糖脂 根據申請 乳糖脂基 2 0 - 3 0尤的 根據申請 合物,其 油。 根據申請 物,呈反 - 一半乳 -二水溶 -一非極 根據申請 物,呈反 - 一半乳 --水溶 -一非極 根據申請 續脂相的親脂性載體 性脂合併,視需要含 為由5 0 - 1 0 0 % Μ亞麻 醯基甘油所組成且其 性脂之半乳糖脂基質 脂性載體組合物包含 基質及補足1 0 0 Si!的非 專利範圍第1項之親 質含約70 -80¾的二半 其他極性脂。 專利範圍第1或2項 中半乳糖脂基質含達 組合物,其含有極性脂基 極性溶劑,其特徵在此極 脂酸、油酸與棕櫚酸之二 f余為具有不同糖脂或磷脂 總組合物重量之'1 - 50¾的 極性脂。 脂性載體姐合物,其中半 乳糖二_基甘油及 中任一項之親脂性載體組 1 〇 〇 %的二半乳糖二_基甘 專利範圍第1或2項中任一項之親脂性載體組合 相泡形式,含有總組合物重量計: 糖脂物質,及視需要其他兩性物,0 . 5 - 3 . 0 5K ; 液,0 . 1 - 1 . 0 % ;及 性脂,達1 0 0 %。 專利範圍第1或2項中任一項之親脂性載體組合 相囊形式,含有總組合物重量計: 糖脂基質,1-50¾ 厂 液,0 . 1 - 5 . 0 % ;及 性脂,達1 0 0 %。 專利範圍第1或2項中任一項之親脂性載體組合 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) (請先閲讀背面之注意事項再填寫本頁) 482685 A8 B8 C8六、申請專利範圍 經濟部中央揉準局月工消費合作社印製 物,圼油包水乳液形式,含有總組合物重量計: —一半乳糖脂基質,1-30¾ ; --水溶液,1 - 8 0 % ;及 -一非極性脂,達1 0 0 %。 7 ♦ 根據申請專利範圍第1或2項中# 一項之親脂性載體組合 物,其係用作醫藥、化妝品及食物產品中活性物質的載 體。 8· 根據申請專利範圍第1或2項中任一項之親脂性載體組合 物,其用於製備醫藥組合物,該醫藥組合物進一步含有 生物活性物質。 9 · 根據申請專利範圍第8項之親脂性載體組合物,其中非 極性脂為三_基甘油,較佳是中等鐽的三醯基甘油 (MCT),夜櫻草油,棕櫚油分餾物或生物活性物質。 I 〇 ·根據申請專利範圍第8項之親脂性載體組合物,其中該 醫藥組合物係經口、經腸、非經口、經直腸、經陰道、 局部、經眼、經鼻、或經耳给予。 II · 一種半乳糖脂基質組合物,其係用作極性脂Μ製備具連 續脂枏並含有非極性脂及極性脂基質的親脂性載體製劑 ,該半乳糖脂基質由至少5 0 %之二半乳糖二醯基甘油所 組成,其餘為其他極性脂。 1 2 .根據申請專利範圍第11項之半乳糖脂基質組合物,其含 約7 0 - 8 0 %二半乳糖二薩基甘油及2 0 - 3 0 %其他極性脂。 1 3 .根據申請專利範圍第11或1 2項之半乳糖脂基質組合物, 其由達1 0 0 %之二半乳糖二醯基甘油所姐成。 本紙張尺度適用中國國家橾準(CNS ) Α4規格(210 X 297公釐) (請先閲讀背面之注意事項再填寫本頁) 訂 #1 482685 A8 B8 C8 D8 六、申請專利範圍 14. 一種用Μ製備反相泡之半乳糖脂基質組合物,其由至少 5 0 %之二半乳糖二醯基甘油所組成,其餘為其他極性脂 ,視需要組合磷脂或其他兩性物。 1 5 .根據申請專利範圍第1 4項之半乳糖脂基質組合物,其由 約7 0 - 8 0 %之二半乳糖二醯基甘丨油及2 0 - 3 0 %之其他極性 脂所組成。 1 6 .根據申請專利範圍第1 4或1 5項之半乳糖脂基質組合物, 其由達100¾之二半乳糖二醯基甘油所姐成。 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局身工消費合作社印裝 本紙張尺度適用中國國家標準(CNS > A4规格(210X297公釐〉
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SE9400368A SE9400368D0 (sv) | 1994-02-04 | 1994-02-04 | Glycolipid material |
SE9402456A SE517678C2 (sv) | 1994-07-12 | 1994-07-12 | Lipofila bärarpreparat med en kontinuerlig lipidfas |
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TW084101256A TW482685B (en) | 1994-02-04 | 1995-02-13 | Lipophilic carrier preparations comprising digalactosyldiacylglycerols |
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US (1) | US5716639A (zh) |
EP (1) | EP0743851B1 (zh) |
JP (1) | JP3203359B2 (zh) |
KR (1) | KR100220546B1 (zh) |
CN (1) | CN1091591C (zh) |
AT (1) | ATE201980T1 (zh) |
AU (1) | AU691250B2 (zh) |
CA (1) | CA2182577C (zh) |
DE (1) | DE69521300T2 (zh) |
DK (1) | DK0743851T3 (zh) |
ES (1) | ES2158084T3 (zh) |
FI (1) | FI963066A (zh) |
HU (1) | HU221432B (zh) |
MY (1) | MY112435A (zh) |
NO (1) | NO312495B1 (zh) |
NZ (1) | NZ279954A (zh) |
PL (1) | PL178394B1 (zh) |
TW (1) | TW482685B (zh) |
WO (1) | WO1995020945A1 (zh) |
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1995
- 1995-02-06 US US08/676,137 patent/US5716639A/en not_active Expired - Lifetime
- 1995-02-06 WO PCT/SE1995/000117 patent/WO1995020945A1/en active IP Right Grant
- 1995-02-06 JP JP52055795A patent/JP3203359B2/ja not_active Expired - Lifetime
- 1995-02-06 PL PL95315780A patent/PL178394B1/pl not_active IP Right Cessation
- 1995-02-06 AU AU17235/95A patent/AU691250B2/en not_active Ceased
- 1995-02-06 DK DK95909185T patent/DK0743851T3/da active
- 1995-02-06 KR KR1019960704239A patent/KR100220546B1/ko not_active IP Right Cessation
- 1995-02-06 AT AT95909185T patent/ATE201980T1/de not_active IP Right Cessation
- 1995-02-06 CN CN95191484A patent/CN1091591C/zh not_active Expired - Fee Related
- 1995-02-06 EP EP95909185A patent/EP0743851B1/en not_active Expired - Lifetime
- 1995-02-06 ES ES95909185T patent/ES2158084T3/es not_active Expired - Lifetime
- 1995-02-06 DE DE69521300T patent/DE69521300T2/de not_active Expired - Lifetime
- 1995-02-06 CA CA002182577A patent/CA2182577C/en not_active Expired - Fee Related
- 1995-02-06 NZ NZ279954A patent/NZ279954A/en unknown
- 1995-02-06 HU HU9602142A patent/HU221432B/hu not_active IP Right Cessation
- 1995-02-09 MY MYPI95000299A patent/MY112435A/en unknown
- 1995-02-13 TW TW084101256A patent/TW482685B/zh not_active IP Right Cessation
-
1996
- 1996-08-02 FI FI963066A patent/FI963066A/fi not_active IP Right Cessation
- 1996-08-02 NO NO19963242A patent/NO312495B1/no not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
NO312495B1 (no) | 2002-05-21 |
NO963242L (no) | 1996-08-02 |
FI963066A0 (fi) | 1996-08-02 |
JPH09508415A (ja) | 1997-08-26 |
WO1995020945A1 (en) | 1995-08-10 |
NO963242D0 (no) | 1996-08-02 |
HU9602142D0 (en) | 1996-09-30 |
CN1140405A (zh) | 1997-01-15 |
AU1723595A (en) | 1995-08-21 |
KR100220546B1 (ko) | 1999-09-15 |
US5716639A (en) | 1998-02-10 |
FI963066A (fi) | 1996-09-30 |
MY112435A (en) | 2001-06-30 |
JP3203359B2 (ja) | 2001-08-27 |
DK0743851T3 (da) | 2001-09-03 |
HUT75470A (en) | 1997-05-28 |
EP0743851A1 (en) | 1996-11-27 |
PL315780A1 (en) | 1996-12-09 |
DE69521300T2 (de) | 2002-05-02 |
PL178394B1 (pl) | 2000-04-28 |
EP0743851B1 (en) | 2001-06-13 |
AU691250B2 (en) | 1998-05-14 |
ATE201980T1 (de) | 2001-06-15 |
ES2158084T3 (es) | 2001-09-01 |
CA2182577A1 (en) | 1995-08-10 |
HU221432B (en) | 2002-10-28 |
CN1091591C (zh) | 2002-10-02 |
NZ279954A (en) | 1998-02-26 |
DE69521300D1 (de) | 2001-07-19 |
CA2182577C (en) | 2002-08-20 |
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