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Crystal Geniposide



Crystal Geniposide is a kind of product with high purity, high-tech and high value, and it is a kind of monomer raw material medicine, intermediate of food additive, a standard product of medicinal plant with international advanced level, which to be developed by adopting modern separating technology, modern detecting technology, modern biotechnology. With Crystal Geniposide, We can develop a series of monomer new medicine, new compound medicine and high-tech foodstuff colorant. Crystal Geniposide will make a great contribution to the aspects of perfecting the human life, in proving human health, promoting the modernization of traditional Chinese medicine and the international economic development.

1. Introduction to raw material
Crystal Geniposide is made by separation, purification and crystallization from Gardenia, a kind of traditional Chinese medicine.
Gardenia is the ripe fruit of Gardenia jasminoides Eills, and its original plant is an evergreen shrub with a height of 60-200cm. It is with twig and downy green leaves at first and smooth later. With short stem, the leaves are growing in pairs; Two pieces of stipules with film material, are growing in the inner side of the leaves’stem; The luster oval or inverse ovate leaves belong to leather material with a length of 6 - 12cm, width of 3 - 4cm. The flower is big and very fragrant with short peduncle, green calyces, white corolla (later become pale yellow). The inverse ovate or long oval fruits are big with sarcocarp, red and yellow color, and the husks with 6 to 8 pieces of fleshy wing vertical ridge. The bar shape persistent calyces are growing on the top. There are some yellow seeds in oval or ovate shape. The inflorescence is from May to July, and the fruit growing period is from Aug. to Nov. It’s growing in the hillside shaw in warm regions and distributes in those provinces, such as Hunan, Hubei, Guangxi, Guangdong, Jiangxi, Fujian, Taiwan, Jiangsu, Zhejiang, Anhui, Henan, Yunnan, Guizhou, Sichuan etc. Since it enjoys high medicinal value and economical value, in recent years, artificial gardening of Crystal Geniposide has been adopted in some areas. Some large-scale green planting bases have been established in areas of Hubei, such as Changyang(是崇阳还是宜昌的长阳?), Xianning, Huanggang, Xiaogan etc.
After the first frost in autumn, harvest the fruit when the fruit is ripe with deep red yellow color. Scald the fruit in boiling water, then filter the water and exposed in the sun till the fruit is dry and hard, or steam in the steamer for a while, then dry it in the sun or by rire in order to destroy its inherent enzymatic system and keep the effective ingredients in the ripe fruits. If the Genipin need to be extracted, then it is inappropriate to steam, scald or insolate in order to keep the high activity of its β-glucoside enzyme, hydrolyze Geniposide to Genipin and Glucose in order to gain higher yield.
The Gardenia raw material used in the products is produced in Hubei green planting base. At present, with acreage of 30,000 mu, the annual output of the base is 1,000,000 kg. According to the plan of No.128EZBF[2004] document, the base shall develop to 200,000 mu during the period of the Eleventh Five-Year Plan, which will meet the demands of raw material for the industrialization and scale production of Gardenia industrial chain in quantity. Thus, it can satisfy the conditions of non-pollution and no fertilizer during the planting period in quality, thereby ensures the high quality from the beginning.

2. Research progress
The Gardenia as a medicament can date back to thousands of years, which was first recorded in Shennong’s Classic of Materia Medica. The historical documents show that it is widely used in clinical recipes with functions of cooling the internal heat and detoxifying the body, promoting gallbladder function and protecting liver, anti-inflammatory and easing pain, such as Gardenia Husk Soap, Gardenia Magnolia Bark Soap, Gardenia Ginger Soap, Gardenia Bean-pod Soap, Coptis Detoxicating Soap etc, and the descriptions including high Gardenia content, so it shows that the Gardenia plays an important role in treating the diseases related to liver, gaooboadder etc. In recent years, in China, incidences of those diseases are high, such as acute and chronic hepatitis, pancreatitis, cholecystitis, cardiovascular diseases, but there are no ideal medicines, the pharmacological function of Gardenia in this aspect attracts great attention of scholars both from home and abroad.
The modern pharmacology and pharmacodynamics research indicates that Gardenia and its leaching liquor has the following functions:
1) Antibacterial and antiviral function:
Gardenia has inhibition to staphylococcus aureus, meningococcus, gonporrhea diplococcus, Catarrhalcoccus; its leaching liquid has inhibition to many kinds of dermomycosis; its decoction can kill the leptospira and schistosome imago, and Gardenia has inhibition to HBV-DNA as well.
2) Anti-inflammation function:
All the Gardenia extraction, Ethyl Acetate and Geniposide have anti-inflammation functions, and inflammation and pain relieving functions to soft tissue injury.
3) Cholagogic function:
Both Gardenia and its internal iridoid have the cholagogic function.
The experiment improved that its decoction(1g/kg)can shrink the mouse gallbladder; its lixivivium can inhibit the bilirubin in ligation bile duct of rabbit, and reduce the content of bilirubin in blood, all the Geniposide, crocin, crocetin and Gardenia Extraction can promote the gall excretion, and its cholagogic fumction is the same with dehydrocholic acid sodium.
4) Promote the pancreas excretion:
Gardenia and its several extractions have the obvious functions to promote the pancreas excretion and reduce the activity of Steapsin. Geniposide enjoys the best effects in reducing the activity of Steapsin and increasing the pancreas excretion. All these functions may be directly related to keeping the structure and function of pancreas cell film.
5) Blood pressure reduction function:
Take Gardenia decoction and extraction orally or inject through abdominal cavity, which has functions of persistent blood pressure reduction to anaesthesia and normal sober animals(rabbit and cat ). Its function has nothing to do with the histamine, afferent nerve and neuroganglion. Soti was thought that its oressure reduction function in the center was mainly caused by deepening the intensity of medullary parasympathetin nerves center.
6) Treatment of jaundice, persisting hepatitis and chronic hepatitis: Yinzhihuang injection is a specific medicine to treat hepatitis and its main element extracted from Baicalin, Gardenia and Cp]apillanol. Tt is proved through large clinical observation in the whole country, that this medicine have those functions, such as inhibiting pathological changes of liver cells, promoting liver cells regeneration, activating inner liver circulation, benefiting to gall and reducing jaundice, enhancing hepatic glycogen and inducing to generate the endogenous interferon.
7) Inhibiting tumour function:
The Gardenia extract has some inhibiting function to S-180 carjncle cells and ascites liver cancer cells.

3. Preparation process
Column layer analysis method is adopted to separate and purify the Crystal Geniposide. The multi-solvent system to crystallize, stationary phase, moving phase and crystallized solvent all belong to medical grade, food grade and sub-purified grade respectively, which has assured safety, high purity and high benefit of the products. The main technology process is as follows: Gardenia Extract Resin absorption Eluent A Refine Crocin.

                   ProductA
       EluentB   Ultrafiltration    Cold  concentrate

       Column analysis     Separate in enzyme technology
       Refine
       UVIRHPLC    Crystallize     Crystal     Geniposide
                  ProductB
Crystallize    Enzyme split
Genipin        ProductC(不太懂这个地方)

4. Product features
1) Appearance: White needle crystals
2) Molecular structure:这里是不是差点什么
3) Molecular weight: 388
4) Dissolubility: Easy to dissolve in water, methanol, ethanol etc, difficult to dissolve in the aether, chloroform etc.
5) Stability: The dry crystal is stable in the normal temperature(-10 - 35), and hard to absorb moisture.
6) It is relatively stable in the condition or weai acid.
7) Enzymolysis: Its water liquid ezsy to be hydrolyzed to Geniposide and glucose in the effect of emulsion and β-glueoside with the temperature 40 - 60.
8) Melting degree: 163.5 - 164

5. Product standard:
Chapter 4 is the compulsory content in Medicinal plant and preparation imports and exports green pioneering standard that announced and managed by Cooperation Ministry of Foreign Economic of the People’s Republic of China.
4)Limited index
4.1 Heavy metal and arsenic salt
4.1.1 Total heavy metal 20.0mg/kg
4.1.2 Lead(Pb) 5mg/kg
4.1.3 Cadmium(Cd) 0.3mg/kg
4.1.4 Mercury(Hg) 0.2mg/kg
4.1.5 Copper(Cu) 20.0mg/kg
4.1.6 Arenic(As) 2.0mg/kg
4.2 Aflatoxin content
4.2.1 Aflatoxin content B1 5mg/kg
4.3 Pesticide residual amount
4.3.1 Benzene hezachoride(BHC) 0.1mg/kg
4.3.2 DDT                0.1mg/kg
4.3.3 Pentachloronitrobenzene  0.1mg/kg
4.4 Microbial limitpc/g   pc/ml
Carry out accordint to the regjlations of Pharmacopoeia of People’s  Republic of China(2000 edition).
4.5 Inaddition to above standardsother quality should be in accord with Pharmacopoeia of People’s  Republic of Chian(2000 edition).
     This product should be fully carried out not only strictly according to above standarsbut also put forward more strict requirements in the following projects.
              
                Quality  index
      
Content(HPLC)
≥98%
Lead(Pb)
≤2mg/kg
Arsenic(AS)
≤1mg/kg
Total bacteria
100u/g
Pathogenic Bacteria
Shoulen’t  be round

6.Application and develobment
Presently,the application of Geniposide focuses on three aspects
8) Develop new medicine
Mainly included
National first class new medicine of Chnese traditional medicine(sole effect monomer Geniposide)
  Oral new medicine treating acute and cyronic hepatitis
  Oral new medicine treating pancreatitis
  Oral new medicine treating cholecystitis
  National first class chemical new medicine(sole effect monomer Genipin)

  Oral new medicine treating acute and chronic hepatitis
  Oral new medicine treating pancreatitis
  Oral new medicine treating cholecystitis
  National first class monomer compound new medicine(Geniposide(90%)plus Crocin(10%))
  Oral new medicine treating cardiovascular diseases
  Oral new medicine treating acute and chronic hepatitis
  Oral new medicine treating myocardium ischemia
  National monomer compound new medicine(Geniposide plus ginkgolic flavone glycoside)New medicine treating cardiovascular diseases
  National compound injection new medicine of Cinese traditional medicine(Geniposide plus crocin plus baicalin plus capillanol effective part)
  New medicine treating heauy hepatitis,acute and chronic hepatitis,baby jaundice
  New medicine treating kidney stone,ureter stone
  National first class monomer injection iew medicine(Geniposide 99%,or Genipin 99%)New medicine treating liver,gallblaeedr and kidney diseases
  National compound new medicine of Chinese traditional medicine(Geniposide plus the rffective part of Chinese traditional medicine)
  New medicine treating cardiovascular and cerebrovascular disease
  New medicine treating hypertension
  New medicine resisting infantile convulsion and lowering temperature
  New medicine resisting bacterium and virus

  National new medicine of Chinese traditional medicine for external application(Geniposide plus the rffective elements of Chinese traditional medicine)
  New medicine diminishing inflammation and killing pain
  New medicine resisting epiphyte infection
  New medicine treating red and swelling due to sprain
2)Making colorants of high puritymainly including:
High purity communal natural pigmentgardeniablue
High purity communal natural pigmentgardenia-red
High purity communal natural pigmentgardenia-green
High purity communal natural pigmentgardenia-black
   The above products made with crystal gardenia have the characteristics of high color valuestrong coloring power and acid-proof and cedrol-proof.
3)Standard product of medicinal plants
The waster liquid and liquor produced due to the separation and purification of Geniposide contain crocin and Iridoid Glycoside that has a similar structure witheniposide with Geniposide with lower content and higher valuewhich can be made with similar method into standard plant productsmainly including
Genipin
Geniposidic-1-β-Gentiobioside
Gardenoside
Geniposidic acid
Shanzhiside
Aoperuloside
Deacetylasperuloside acid methylesl
Gardoside
Scandoside methylesler
10-Acetyl Geiposide
These standard products of plant extracts have a wide usage in the fields of confirming the plant elements, distinguishing the unknown plant elements, research on toxicology, pharmacology and pharmacodynamics, and metabolic regulation of animalcule, etc.
最后由 eyeviviyou 于 2009-07-02 02:10:09编辑
^_^欢迎大家去我的博客看看
楼主 Date: 2009-07-02 02:06:47
Crystal Geniposide is made by separation, purification and crystallization from Gardenia, a kind of traditional Chinese medicine.
crystal Geniposide is made from a traditional chinese medecine, Gardenia,through the techniques of sepration, purification and crystallization
你这里的意思是说一种传统的中药材栀子通过分离,净化和结晶技术从而获得crystal geniposide吗? 明白了一些 但是像后面的at first and smooth later就不是很懂了  没有帮上忙憨笑
Date: 2009-07-02 10:32:55
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