Mechanochemical Assisted Extraction Of Activegardenia And Preparation Of Genipin Solid Dispersion And Complex

In this paper,with mechanical chemical technology as the main content,mechanical chemical technology was applied in extraction separation of effective components of gardenia and development of preparations of genipin of derivative of gardenoside,an effective component of gardenia.Mechanochemical application was adopted through the extraction separation of gardenia and the development of subsequent preparation.According to the work content,this paper is divided into two parts:1.Usage of mechanochemical method in assisted extraction and separation of effective components of gardenia;2.usage of mechanochemical method in the development of stable genipin solid dispersions and inclusion complexes.The first part is divided into three chapters,in which the first chapter,firstly,summarized the pharmacological activity,application and main components of economic plants and traditional Chinese herb,gardenia,and briefly introduced the known extraction method of various active components.Secondly,it elaborated the principles of mechanochemical method and the differences between mechanochemistry and traditional solution chemistry in detail.It focused on the elaboration of the principle of using mechanochemical method in assisted extraction of effective components of plants and process of research at home and abroad.The second chapter,based on the disadvantages in the extraction of effective components of gardenia mentioned in the previous chapter,and combining with the idea of using mechanochemical method in assisted extraction,the assisted extraction technology of effective components of gardenia with mechanochemical method was finally confirmed.Through mechanochemical treatment,effective components of gardenia,like gardenia oil,geniposide,gardenia yellow and pectin as well as triterpenes,can be fully extracted and utilized under the condition of not increasing the extra technological process,which not only can weed out the use of ethyl alcohol,but also significantly improve the extraction efficiency of the product and relatively traditional handicraft for quality.The yield of gardenia yellow,geniposide,gardenia oil and pectin was 3.24%?E=420?,2.55%,19.67%and 18.16%respectively.unsaturated fat in gardenia oil was increased 2%than product extracted by traditional methods,Signature compound Saffron aldehyde contended in volatile oil was unchanged during milling;Color value of gardenia yellow was up to 420after purification,the quality of gardenia yellow,geniposide and pectin were as same as the product extracted by traditional method in content,In allusion to the problem of difficulty in extraction and separation of gardenia yellow and geniposide from gardenia due to a similar nature and in combination with the solid adsorption capacity of mechanochemistry,the third chapter mainly explored the research on the method for selective extraction of gardenia yellow and successfully developed a two-step method of mechanochemical assisted selective extraction of gardenia yellow and geniposide.After adopting this method,geniposide and gardenia yellow can be separated directly via solvent.The content of geniposide in gardenia yellow after separation accorded with the national standard,solving the problem of long segregated time and big solvent consumption.The color value of extracted gardenia yellow was 150,and the content of geniposide was less than 5%,meeting the national standard.Possible mechanism of selective extraction could be summarized as deformation of adjuvant during milling,structure changes in active carbon led to changes in ability of adsorption and desorption.The second part,firstly,summarized the pharmacological activity and application of genipin:a derivative form geniposide.Aiming at the problem existing when using genipin as medicine and in combination with the idea of preparation of stable drug preparations with mechanochemical method,genipin and a variety of drug carriers were formed into solid dispersion and inclusion complexes,and according to the water solubility and stability of prepared drug preparations hydroxypropyl-?-cyclodextrin was finally selected as the optimal carrier,solubility of genipin in hydroxypropyl-?-cyclodextrin inclusion complex was up to 62.40g/L,which was increased 6.14 times when compared with the raw material,this complex also had good stability in water solution,solid states and PBS solution.It could be dissolve in water within 5minutes.Meanwhile,¹H-NMR,XRD,DCS,IR and phase-solubility method was adopted to analyze the causes of solubilization and stability of hydroxypropyl-?-cyclodextrin towards genipin.Inclusion ratio and stability constant at 30^oC of this complex were determined as 1:1 and1155 M^-1?Complex made by mechanochemical method own greater entrapment rate than complex made by traditional method.At last,through the test of hepatotoxicity in vitro of drug delivery system,results show that hepatotoxicity in vitro of drug delivery system prepared through mechanochemical method was significantly decreased.Obstacles blocked usage of genipin in clinical trials were preliminary solved.