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研究生:彭寬嘉
研究生(外文):Kuan-Chia Peng
論文名稱:環糊精包覆中藥牡丹皮之研究與應用
論文名稱(外文):The inclusion complexes of Moutan Cortex extract with cyclodextrin: preparation and application
指導教授:蔡育勳
指導教授(外文):Yu-hsin Tsai
學位類別:碩士
校院名稱:中國醫藥大學
系所名稱:中國醫學研究所碩士班
學門:醫藥衛生學門
學類:醫學學類
論文種類:學術論文
論文出版年:2009
畢業學年度:97
語文別:中文
論文頁數:61
中文關鍵詞:牡丹皮酚環糊精黑色素包覆作用
外文關鍵詞:Moutan Cortexpaeonolcyclodextrinsmelanininclusion
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中藥牡丹皮在傳統中醫上具有清熱涼血、活血化瘀、降壓及抗菌美白功效。主要成分為丹皮酚,酚類化合物易揮發也因為親油性、不會水溶,易影響中藥成品穩定。因此尋找適當材料將丹皮酚轉換成不易揮發形式,材料須兼顧不破壞活性成分及不產生副產物。環糊精是澱粉水解後的寡糖分子,特殊的疏水環狀圓桶分子結構,包覆客分子於中間孔洞,形成主客一體複合物質,改變所包覆客體化合物之化學性質、物理性質及生物可利用性。本研究擬利用環糊精包覆技術,來提昇牡丹皮脂溶性成份對水的溶解度,達到奈米水性化之目的。以牡丹皮美白功效作測試,本研究分兩部分探討環糊精包覆的新型中藥製劑之影響。先行牡丹皮粗萃物及丹皮酚的美白測試,再進行牡丹皮粗萃物的環糊精包覆和包覆物分析鑑定及美白測試。本研究實驗證實牡丹皮粗萃包覆奈米藥物已成功製備,並獲得UV及NMR分析儀器鑑定證實其成份,並將粗萃包覆奈米藥物置入水中時,呈現透明水溶液態,證明粗萃包覆奈米藥物具有良好的水溶性。最後將兩組對照,從DPPH test及Tyrosinase inhibition test中且在特定條件下,看到環糊精並未導致牡丹皮粗萃物活性消失。證實環糊精確實可將脂溶性成分包覆並轉換其化學性質,且不影響原本成分的活性與功效。
Moutan Cortex (Cortex moutan radicis), a widely used traditional Chinese medicine for the treatment of various diseases. A variety of compounds in Mouton Cortex that Paeonol, a major phenolic component. A phenolic extract of Moutan Cortex has been reported to exhibit DPPH radical-scavenging activity. Cyclodextrins (CDs) are a family of cyclic oligosaccharides that are composed of α-1,4-linked glucopyranose subunits. Cyclodextrins are most important. Because of their inclusion complex forming capability, the properties of the materials with which they complex can be modified significantly . The aim of this study was to prepare inclusion complexes of the paeonol that extraction of Moutan Cortex with CD in order to improve their water-solubility, and studied antioxidant activity and tyrosinase inhibition for drug and CD complex. CD complex analied by UV spectrometer and 1H-NMR (Nuclear magnetic resonance). Modified L-Tyrosine method was used to determine tyrosinase inhibition activity. 1,1-diphenyl-2-pricrylhydrazyl (DPPH) radical-scavenging method was used to determine the antioxidant activities ability.
目錄
第一章 前言...............1
第二章 文獻探討..................................5
一、 實驗植物介紹...................................5
1. 植物介紹...........................................5
2. 牡丹皮的中醫臨床應用........................7
二、黑色素形成機制......................................8
1. 黑色素的形成和位置..............................8
2. 紫外線及自由基對黑色素形成的影響.........11
3. 酪胺酸?◇?論............................11
三、環糊精.................................15
1. 環糊精介紹..............................15
2. 環糊精結構.........................15
3. 環糊精特性.................17
4. 環糊精應用........................17
5. 環糊精物理及化學性質影響在中藥製劑上的應用………………18
6. 環糊精的釋放控制機制............................20
7. HP-β-環糊精概述.................................21
第三章 實驗材料與方法..................................23
一、 實驗材料、藥品與儀器設備....................24
1. 中藥材料之來源............................24
2. 藥品………………………………………………………..24
3. 儀器設備………………………………………………..25
二、 實驗方法………………………………….…………………..26
1. 牡丹皮粗萃物之製備與分析……………………………………..26
1.1牡丹皮粗萃膠之製備…………………………………………..26
1.2牡丹皮粗萃物之分析…………………………………………….27
2. 環糊精包合物的製備…………………………………..27
2.1含牡丹皮粗萃物之環糊精奈米包覆藥物的製備………………….27
2.2含丹皮酚環糊精奈米包覆藥物的製備………………………29
3. 清除自由基能力……………………………………............30
3.1 DPPH測試樣品溶液配製……………………………………………30
3.2 對照組與實驗組樣品溶液配製………………………………..30
3.3 清除 α,α-diphenyl-β-pricrylhydrazyl ( DPPH ) 自由基之實驗方法…30
4. 中藥萃取物對酪胺酸抑制能力評估……………………………31
4.1體外抑制酪胺酸?′〝妐桲蝷妥?試樣品溶液配製…………31
4.2對照組與實驗組樣品溶液配製………………………………31
4.3 體外抑制酪胺酸?′〝妐桲蝷完篘蝷隤k…………………………32
第四章 結果..................................33
一、牡丹皮粗萃物之製備與分析……………………………………..33
1.1牡丹皮粗萃膠………………………………………………33
1.2牡丹皮粗萃物之分析……………………………………33
1.3丹皮酚乙醇溶液標準曲線………………………………………….34
二、環糊精奈米包覆藥物實驗結果…………………………35
2.1粗萃牡丹皮奈米包覆藥物…………………………………………35
2.2丹皮酚奈米包覆藥物……………………………………………36
2.3奈米包覆藥物之水溶特性………………………………………...37
三、奈米包覆藥物的鑑定……………………………..38
3.1 UV 分析鑑定奈米包覆藥物………………………...38
3.2 NMR分析鑑定奈米包覆藥物……………………………………….39
四、藥物及奈米包覆藥物抗氧化能力………………40
4.1 HQ、丹皮酚及粗萃牡丹皮對α,α-diphenyl-β-pricrylhydrazyl ( DPPH )自由基清除能力………………40
4.2奈米包覆藥物對α,α-diphenyl-β-pricrylhydrazyl ( DPPH )自由基清除能力………41
4.3藥物及奈米包覆藥物對α,α-diphenyl-β-pricrylhydrazyl ( DPPH )自由基清除能力之比較…42
五、中藥萃取物對美白的有效能力………………………43
5.1 HQ、丹皮酚及粗萃牡丹皮對Tyrosinase inhibition 的美白有效能力………43
5.2奈米包覆藥物對Tyrosinase inhibition 的美白有效能力評估…44
5.3藥物及奈米包覆藥物對Tyrosinase inhibition 的美白有效能力比較……………45
5.4粗萃及標準品的HP-β-環糊精奈米包覆藥物對Tyrosinase inhibition的美白有效能力比較……………………46
第五章 討論...................................47
第六章 結論.......................................53
參考文獻………………………………………………………54
圖目錄
圖2.1牡丹皮(Moutan Cortex).............................. 5
圖2.2 牡丹皮飲片…...………………………..5
圖2.3丹皮酚(paeonol)之結構圖…..…………………..7
圖2.4 人體皮膚結構圖…………………….......9
圖2.5黑色素細胞位置與酪胺酸機轉…………………………………10
圖2.6黑色素形成路徑機轉.....................10
圖2.7 不同型態之環糊精……………………………………………..15
圖2.8 β-環糊精結構圖…………………………….16
圖2.9環糊精奈米技術包覆示意圖………………………………..21
圖4.1牡丹皮粗萃膠…………………………………..............33
圖4.2牡丹皮粗萃膠之分析……………………34
圖4.3丹皮酚乙醇溶液標準曲線………………………………35
圖4.4粗萃牡丹皮奈米包覆藥物……………………………...36
圖4.5丹皮酚奈米包覆藥物…………………………………...36
圖4.6奈米包覆藥物之水溶特性………………………………37
圖4.7 UV分析鑑定奈米包覆藥物…………………………..38
圖 4.8 NMR分析鑑定奈米包覆藥物………………………39
圖 4.9 HQ、丹皮酚及粗萃牡丹皮對α,α-diphenyl-β-pricrylhydrazyl (DPPH )自由基清除能力 40
圖 4.10奈米包覆藥物對α,α-diphenyl-β-pricrylhydrazyl ( DPPH )自由基清除能力…………………………41
圖 4.11藥物及奈米包覆藥物對α,α-diphenyl-β-pricrylhydrazyl ( DPPH )自由基清除能力之比較.........................42
圖 4.12 HQ、丹皮酚及粗萃牡丹皮對Tyrosinase inhibition 的美白有效能力................................43
圖4.13奈米包覆藥物對 Tyrosinase inhibition 的美白有效能力....44
圖 4.14藥物及奈米包覆藥物對Tyrosinase inhibition 的美白有效能力之比較...45
圖4.15粗萃及標準品的HP-β-環糊精奈米包覆藥物對Tyrosinase inhibition 的美白有效能力比較…………46
表目錄
表 2.1 衛生署公布美白成分及濃度限制列表……….14
表 2.2 各國環糊精應用許可情形………….22
表 2.3 環糊精安全性一覽………………………22
表 3.1 實驗流程大綱…………………………23
表 3.2 β-環糊精包覆製程…………………………..28
表 3.3 HP-β-環糊精包覆製程……………………………….29
表 3.4丹皮酚HP-β-環糊精包覆製程………………….29
表 3.5丹皮酚β-環糊精包覆製程…………………29
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