艾叶挥发油-β环糊精包合物的制备及其稳定性的研究
详细信息    本馆镜像全文|  推荐本文 |  |   获取CNKI官网全文
摘要
艾叶为菊科植物艾草(Artemisia argyi Levl.Et Vant)的干燥叶,其味苦、辛、性温,归肝、脾、肾经。具有理气血、温经脉、逐寒湿、止冷痛,、安胎止痒等功效。挥发油为其主要药用成分,具有平喘、镇咳、祛痰及抗菌消炎等功效。但由于挥发油具有较强的挥发性、刺激性、遇光和热不稳定、水溶性差等原因,严重影响了其在生产中的应用。采用环糊精包合技术,将其制成挥发油包合物,意在提高艾叶挥发油的稳定性和可用性,进而提高艾叶挥发油的应用。本课题从艾叶中提取挥发油,采用了三种包合技术进行包合,筛选优化得到较佳的包合工艺,并对其包合物的稳定性等方面进行了比较,研究如下:
     (1)艾叶挥发油β-环糊精的包合研究:以挥发油包合率,包合物收得率和包合物含油率为评价指标,采用正交实验进行工艺优化,对研磨法、饱和水溶液法、超声法制备的包合物进行了综合评价。按三种方法的最佳包合工艺条件制备3批样品,测定超声法、饱和水溶液法和研磨法的平均包合率分别为50%、93%、55%。由结果可知,饱和水溶液法包合率较高,且更适于大生产,所以选用饱和水溶液搅拌法包合挥发油。
     (2)艾叶挥发油β-环糊精包合物的物相鉴别:采用显微镜观察、薄层色谱法、紫外分光光度法进行了物相鉴别,结果证实,显微镜观察与紫外图谱显示艾叶挥发油经β-环糊精包封后,形成了新的物相,包合物已形成;艾叶挥发油在包合前后及包合物的薄层色谱鉴别表明艾叶挥发油与β-CD形成稳定的环糊精包合物,且在挥发油在包合前后性质没有发生变化;紫外图谱与显微镜观察显示包合物的形成。
     (3)艾叶挥发油β-环糊精包合物的稳定性研究:采用抗光解性实验、热稳定性实验、湿稳定性试验对包合物的稳定进行测定,所得的数据可以看出:包合物中艾叶挥发油的含量百分比明显的要比混合物中的艾叶挥发油的含量百分比高,而在挥发性试验中,包合物中艾叶挥发油的失重百分比也明显比混合物中的失重百分比低,因此,我们可以推断出当艾叶挥发油与β-CD形成包合物以后能明显提高挥发油的稳定性,降低挥发性。
     综上所述,采用饱和水溶液法制备的艾叶挥发油β-CD包合物操作简便,成本低,对设备要求不高,且稳定性好,具有一定推广应用价值。
Artemisia vulgaris was the dried leaves of Artemisia argyi Levl.Et Vant, which was bitter, acrid, warm and went through the spleen, liver and kidney. It have many functions, such as warm blood, dispel cold, release pain, cure cough and asthma, Stop-leak tocolysis, dampness itching etc. The main medicinal components was volatile oil, having smooth over asthma, antitussive, expectorant and anti-bacterial inflammatory effects. However, volatile oil has a strong volatility and pungent, unstable in case of light and heat, poor solubility, that seriously affected its application. Volatile oil will be more stability and availability as well as improving the application, by using of cyclodextrin technology. The purpose of this project is to extract oil from the leaves, by using three different techniques to get a better optimized technology. Then compare the stability of the complex extracted. The results of the studies are as follows:
     (1) Volatile oilβ-cyclodextrin complex:The utilization ratio of the volatile oil from Artemisia argyi, the content of volatile oil in inelusion compound and the recovery ratio of inclusion counpound were as criteria. The three processes were studied by orthogonal experimental design using orthogonal form (L9(43)) and compare the methed of trituration,the methoed of saturation water solution, supersound method.By three methods best preparation conditions inclusion 3 batches of samples, determination of ultrasonic, saturated aqueous solution method and grinding method average inclusion rate was 50% and 93% and 55%. From the results, the method of saturation water solution was confirmed as the better technology for preparing the aetherolea P-CD clathrate, with higher inclusion rate and more suitable for large-scale production.
     (2.) Volatile oilβ-cyclodextrin phase identification:Microscopy, thin layer chromatography, UV spectrophotometry were the methods of identification. The results confirmed that a new phase was formed inβ-essential oil Cyclodextrin encapsulation through the microscope and UV spectrum, after that inclusion complexes have been formed; volatile oil in the inclusion TLC before and after are consistent with, because that there are no spots in same condition. It showed that volatile oil has been with theβ-CD to form a stable inclusion complex, and in the nature of inclusion did not change before and after. The UV spectrum and Microscopy can give the formation of inclusion complexes
     (3) Volatile oilβ-cyclodextrin complex stability:The stability of inclusion complexes were determined by anti-photolysis experiments, thermal stability test, wet test. The result shows that the content of volatilize oil in inclusion compound did not change. In the mixtrue, however, the content of volatilize oil decreased. It showed that volatile oil in inclusion compound was much more stable under light,heat and humidity. In the volatility test, loss on drying of the compound was smaller than that of the mixture, indicating that inclusion compound could lower volatilization of volatile oil. Therefore, we can infer that when the volatile oil andβ-CD inclusion complex can significantly improve the stability and reduce volatile.
     In summary, essential oilβ-CD inclusion complex prepared by saturated aqueous solution was simple, low cost and less demanding on equipment, and good stability, with a certain application value.
引文
[1]中华人民共和国药基委员会.中国药典(一部)[S]广州:广东科技出版社,1995:68.
    [2]江苏新医学院编.中药大辞典(上册)[M].上海:上海科学技术出版社,1986:559-599.
    [3]任仁安主编.中药鉴定学[M].上海:上海科学技术出版社,1986:333.
    [4]邱洁芬,胡遵荣.试述艾叶的药理作用及临床应用[J].实用中医药杂志,2003,19(8):446.
    [5]蔡平.艾叶的药理作用及应用[J].时珍国医国药,2001,12(12):1137.
    [6]和生,王建华.中药方剂的药理与临床研究进展,第1版[M].广州:华南理工大学出版社,1991:197,198.
    [7]潘炯光,徐植灵,吉力,等.艾叶挥发油的化学研究[J].中国中药杂志,1992,17(12):741.
    [8]刘国声.艾叶挥发油成分的研究[J].中草药,1990,21(9):8.
    [9]周峰,秦路平,连佳芳,等.艾叶的化学成分、生物活性和植物资源[J].药学实践杂志,2000,18(2):96.
    [10]龚志锦,詹铭洲.病理组织制片与染色技术[J].上海:上海科学出版社,1994:48-49.
    [11]张哲,陈辉,实用病理组织染色技术[M].沈阳:辽宁科技出版社,1988:30-31.
    [12]何疆,邓丽,胡之德,等.苏木精荧光共振光散射法测定DNA[J],兰州大学学报(自然科学版),2008,44(2):69-73.
    [13]T.Iijima, Y.Karube, The Interaction of Acid Azo Dyes With Chemieally Modifiedβ-Cyelodextrins, Dyes and Pigments,1998, (36):305-311.
    [14]K.M.Twarah, S.J.Khouri, Determination of the Stability and Stoiehiometry of β-Methyl Red Inclusion Complexes withy-Cyclodextrin, Dyes and Pigments,2000, (45):229-233.
    [15]Y.J Liu, C.C.You, T.Wada, et.al., Moleeular Recognition of Fluorescent Dyes with Novel Triethylenetetraamine-tetheredbis(β-Cyelodextrin) and its CoPPer (Ⅱ)ComPlex:Enhanced Binding and Selectivity by Tether Ligation, Tetrahedron Lett.,2000, (41):6869-6873.
    [16]GM.Zhang, S.M.Shuang, C.Dong, et.al., Study on the Interaction of Methylene Blue with Cyelodextrin Derivatives by Absorption and Fluoreseence Speetroseopy, SPeetrochimi.ActaA,2003, (59):2935-2941.
    [17]Y.J.Guo, J.H.Pan, X.M.Li, et.al., Eleetroanalytieal Method of Acid Red 1 and its Supramolecular System with Cyelodextrins, Dyes and Pigments,2006, (70):27-30.
    [18]Y.J.Guo, J.H.Pan, W.J.Jing, Determination of Orange Ⅱ and the Supramolecular System of Orange Ⅱ with Cyelodextrins by Polarography, Dyes and Pigments,2004, (63):65-70.
    [19]Loftsson T, Fridrisdotir H,O lafsdoB et al.Acta pharm.Nord.1991. (3):215-217
    [20]黎洪珊,王培玉.β-环糊精衍生物的研究进展及在药剂学上的应用[J].中国药学杂志,1999,34(4):220-223
    [21]AllanR H,wen J S, ChristopherT S.A CSS ymp.Se t,1995,590:60-71
    [22]Amstrong DW.In Huber O.and Sze jtli J.(eds), proceedings of Fourth Intenrational symposium on cyclodextrims,kluwerA Cademic,Dordrech,Holland,1998:437-449
    [23]唐有棋主编.当代化学前沿.北京:中国致公出版社,1997:78
    [24]吴金龙.夏秀华.β-环状糊精毒性和致变性研究[J].卫生研究,1989,18(4):36
    [25]P agintonJ set al.Beta-cyclodextrin.Perfuner and Flavorist.1986,(11):49-58
    [26]Gerloc zy et al. Alsorption and metabolism of β-cyclodextrin by rats.I.Int.symp on cyclodextrins.1981,2(4):101-108
    [27]林桂涛,徐淑国.β-环糊精包封中药挥发油新方法的探讨[J].中国中药杂志,1992,17(5):283-285.
    [28]富志军,周志新.胶体磨应用于肉桂油-β-环糊精包合物制备工艺条件的实验筛选.中成药,1994,16(12):6-7.
    [29]张勇,黄贤智.荧光光谱法研究α-溴代萘与β-环糊精2:2重叠包络物的形成[J].化学学报,1997,(55):69-75.
    [30]江云宝,黄贤智,陈国珍.荧光光谱和吸收光谱研究醇与β-环糊精的相互作用[J].化学物理学报,1991,7(3):289-293.
    [32]朱晓峰,许旭,林炳承.β-环糊精和十二烷基硫酸钠包合作用的微量热法研究[J].高等学校化学学报,1998,19(9):1504-1506.
    [32]刘淑琴,刘志敏,潘景浩.环糊精及其包合物的电化学研究及应用[J].电化学,1996,2(4):430-434.
    [33]李培芝,毛敏媛,朱婷婷.循环伏安法研究硝基药物的β-环糊精包络物[J].分析化学,1994,22(1):58-60.
    [34]王烈群,景舒,张宏宇.包合物的研制及溶出速率测定[J].中国中药杂志,1994,25(12):540-543.
    [35]江云宝,黄贤智,陈国珍.荧光光谱和吸收光谱研究醇与β-环糊精的相互作用[J].化学物理学报,1991,7(3):289-293.
    [36]张有明,魏太保.β-环糊精对D/L-酪氨酸对映体的手性识别及超分子包合物的合成[J].应用化学,1998,15(6):45-48.
    [37]侯曙光,王培玉.盐酸雷尼替丁-β-环糊精包合物的研制[J].中国药学杂志,1996,31(8): 479-481.
    [38]张勇,黄贤智.荧光光谱法研究α-溴代萘与β-环糊精2:2重叠包络物的形成[J].化学学报,1997,(55):69-75.
    [39]雍国平,李光水,郑飞,周会舜.β-环糊精包合物的结构研究[J].高等学校化学学报,2000,21(7):1124-1126.
    [40]缪振春.核磁共振技术在药物与环糊精包合物的结构分析中的应用[J].药物分析杂志,1985,5(5):316-319.
    [41]Wood,D.J.;Hruska,F.E.;Saenger,W.1H NMR study of the inclusion of aromatic moleculesina-cyclodextrin[J].Amer. Chem. Soc.1977,99(6):1735-1740.
    [42]刘东红,李蕾.Bragg方程和X光的折射率[J].山东工业大学学报,2000,30(6):525-527.
    [43]郭瑞云,常俊标,林素凤.β-环糊精包结几种萘衍生物的圆二色性的研究[J].光谱学与光谱分析,1996,16(2):38-41.
    [44]秦雪梅,王严冰,漆晓梅,等.β-环糊精包结宫必康冲剂中两种中药挥发油成分的研究[J].山西医学院学报,1996,27(4):257
    [45]张纯,郭澄,高杰.丹皮酚-β-环糊精的理化性质[J].第二军医大学学报,1997;18(1):95
    [46]蔡漆,钟贵陵,高申用.正交实验法研究β-环糊精对陈皮挥发油的包合作用[J].中国医院药学杂志,1995,15(7):291
    [47]李光华,张建军,肖春.环糊精的包合作用—烈香杜鹃挥发油的包合实验[J].中成药研究,1986,(8):11
    [48]刘树芬,杨晓红,李晓红,等.苍术挥发油—β—环糊精包合物的研究[J].中国药学杂志,1992,27(11):658
    [49]蔡漆,钟贵陵,高申.用正交实验法研究β-环糊精对陈皮挥发油的包合作用.中国医院药学杂志,1995,15(7):291
    [50]张雁冰,卢建莎,赵清治,等.毛叶香茶菜醇-p-环糊精包合物的制备中药材[J].1998,21(5):250.
    [51]关家彦,孙殿甲,吴光雷,等.岩白菜素包结物的研制[J].中成药,1991;13(1):4
    [52]颜耀东,冯波,黄晓洁,等.齐墩果酸-p-环糊精包合物的研究.中成药[J].1995;,1 7(6):2
    [53]于莲,张丽华,高萍,等.β-环糊精包结羚羊感冒片中三种挥发油成分的研究[J].中成药,1991,13(9):4
    [54]陈宁,石庭森,赵守孝,等.救心油-β-环糊精包合物的研究[J].中国中药杂志,1995,20(7):411
    [55]邵伟,王大庆,米广太,等.芦丁-β-环糊精包合物的研究[J].中药材,1998,21(1):31
    [56]黄桂花,梁洪华,王德风,等.β-环糊精对羲术醇的包合作用探讨[J].西北药学杂志,1997,12(5):219
    [57]丁燕飞,姚瑶,周彦彬,等.尼群地平β一环糊精包合物的研制[J].中国医院药学杂志,2003,23(8):461
    [58]姚广演,崔殿波,刑少峰,等.硝酸甘油β—环糊精包合物的研究[J].中国医药工业杂志,1993,24(10):45
    [59]何进,毕殿洲,刘宝庆.大蒜油β—环糊精包合物的稳定性考察[J].中国药学杂志,1997,32(4):216
    [60]唐跃年,李方,卜书红.地高辛环糊精包合物的制备与鉴定[J].中国新药杂志,1999,8(12):12.
    [61]陈亮,何凤慈,蓝永烨.维生素E-β-环糊精包合物的制备研究[J].中国新药杂志,1999,8(2):33
    [62]宋洪涛,郭涛,赵明宏,等.肉桂油β-环糊精包合物的理化性质[J].中国医院药学杂志,2003,23(1):12
    [63]奚念朱主编,药剂学(第三版).北京:人民卫生出版社,1995:363
    [64]刘书堂,锥文栋,张雪荣,等.川芍茶调冲剂工艺改进的实验研究[J].中草药,1996,27(11):663
    [65]日本公开特许.1978,56:313
    [66]李树珍,官士杰.生姜挥发油β-CD包结物的稳定性考察[J].中国中药杂志,1992,17(8):481
    [67]刘西瑛,刘云清.磷酸苯丙呱林β—环糊精包合物的性质及制备开发[J].中国药学杂志,1997,32(4):21 8
    [68]侯曙光,王培玉.盐酸雷尼替丁β—环糊精包合物的研制[J].中国药学杂志,1998,15(2):26
    [69]袁淑兰,石庭森,阮金秀.氟安定-β-环糊精包结物的生物利用度研究[J].中国医院药学杂志,1988,8(4):1
    [70]吕万良,屠锡德,郑奋秀,等.β-环糊精包合物中酮洛芬吸收及其生物膜限速理论研究[J].中国药科大学学报,1997,28(4):214-214
    [71]Otero Espinar,F.J; et al.Minutes Int.symp.cyclodextri-ns,1990,15(5):460
    [72]徐治,姚颂华,李方,等.双氯芬酸β-环糊精包合物滴眼液的制备[J].中国药房,2002,(12):722
    [73]夏开元,包如才.环状糊精在中药冲剂中的应用[J].中成药研究,1985:(8):3
    [74]庞志功,汪宝琪,朱慧勤.用β-环糊精单分子胶囊荧光法测定秦九中龙胆苦试的含量研究.药物分析杂志,1994,14(4):50
    [75]汪宝琪,庞志功,李生有.β-环糊精单分子胶囊荧光法测定大黄素、大黄酚、大黄酸的含量[J]中国药科大学学报,1991,22(6):375
    [76 J杨造萍.环糊精及其衍生物在药物分析中的应用.国外医学药学分册.1994,2 1(5):257
    [77]高晓旭,杜风国,高志光.p—环糊精包合长白木挥发油的工艺研究[J].北华大学报(自然科学版).2005,(10):66
    [78]蔡平.艾叶的药理作用及应用[J].时珍国医国药,2001,12(12):1137
    [79]白云蛾,漆小梅.β-CD在中药方面的运用[J].中国医药学院杂志,2000.20(4):237-238
    [80]传隆,黄泰康.中药辞海,第1卷,第1版[M].北京:中国医药科技出版社,1993:1384
    [81]周莉玲,苏子仁,陈若筠,等.脑力宝丸中挥发油的稳定性研究[J]中成药,1992,4(3):6-6
    [82]宋洪涛,郭涛,颜秀涛,等.苏合香β-环糊精包合物与混合物的稳定性比较[J].解放军药学学报,2000,16(3):163
    [83]卞加花,陈听.挥发油β-环糊精包合物的制备研究[J].时针国医国药杂志.2005,16(3):192
    [84]陆彬.药物新剂型与新技术[M].北京:人民卫生出版社,1998:28-28

© 2004-2018 中国地质图书馆版权所有 京ICP备05064691号 京公网安备11010802017129号

地址:北京市海淀区学院路29号 邮编:100083

电话:办公室:(+86 10)66554848;文献借阅、咨询服务、科技查新:66554700