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 Hydrooxypropyl Beta Cyclodextrin(HP-β-CD)

HP-β-CD Properties:

HP-β-CD retains the properties of β-CD on the whole. But HP-β-CD still has some different properties, for example:

1
HP-β-CD is in normal temperature water-soluble is very high, about over 50%, so it can't crystalize in alcohol.
2
The selectivity of held matter of HP-β-CD is different from β-CD, it probably is changed for some matter holding molecular proportion.
3
HP-B-CD neither is resolved and metabolized nor accumulate on the whole, HP-B-CD is taked orally that the majority excrete to outside the body with the excretion, the majority will be excrete to outside the body with the urine if the medicine is not absorbed by bowels.
4
HP-B-CD can promote held matter to release quickly in organism.

5
The suerface activation and haemolysis activation of HP-B-CD are low than B-CD or other derivative,the usage is more safety.

HP-B-CD contains above-mentioned pioperties, therefore it suffers the extensive concern in the medicine field more and more. In order to strengthen people understanding the application aspect of HP-B-CD, and below illustrate with example:
1
In the aspect of increasing water-soluble of insoluble medicine. For example, Dihydroartemisinin and Artemether are all insoluble in water. After holding by HP it's solubility can reach to the standard of Injection power. The solubility of Digoxinum which in the 50% HP solution increases from 0.07mg/ml to 68mg/ml.
2
In the aspect of increasing medicinal stablity. For example, after  estradiol is hold by HP-β-CD, taking it in room temperature, its degradable half-life extends from 1.2 years to 4 years.
3
In the aspect of dropping medicinal harmful side effect. For example, We can use HP-β-CD to make the injection, and then make intramuscular injection, this way can make the absorption of living thing for medicine to obviously increase, and alleviate the harm for stomach and intestines or muscle.
4
In strengthening medicine untilization ratio respect.
5
In the safety of HP-β-CD respect. According to systermatic subacute and chronic toxicity research certificate, HP-β-CD neither leads to disease nor leads to death for samll mouse. After the rabbit is intravenous injection, HP-β-CD is runned off from the blood at once, and it will be excrete to outside the body with the urine, continuous injection hasn't bad symptoms too. For mouses and monkeys intravenous inject 200mg/kg of HP-β-CD, it will hasn't clinical influence. The dosage of oral taken or intravenous injection HP-β-CD is 15g/kg or 10g/kg respectively, it doesn't lead to death for monkeys, too. Humen beings' clinical research makes known to oral taken, intravenous infusion, intravenous injection, nasal cavity, under the tougue and eyes for HP-β-CD, doesn't show bad reaction and irritant for eyes and muscle. Thus it can be proved that HP-β-CD is very safety for living thing.

It will be safe absolutely if accords to following method to use HP-β-CD:
The applicative method and dosage of HP-β-CD for human body:
1
Intravenous infusion Total weight of application: 30g Medthod of application: 5% continuous uses 4 days
2
Intravenous injection Total weight of application: 3g Dosage: 150mg/kg Medthod of application: 5% continuous uses 4 days
3
Oral taken (percent) Total weight of application: 0.2g/kg Dosage: 0.2mg/kg Medthod of application: pill
4
Nasal cavity Total weight of application: 600mg/day Dosage: 40mg/day Medthod of application: 10% aqueous solution
5
Oral cavity under the tough Total weight of application: 120mg/kg Dosage: 120mg/kg Medthod of application: pill
6
Skin Medthod of application: 45% aqueous solution
HP-β-CD hemolysis actived and surface actived is low, it isn't irritant for skin and muscle, even if the consistency of HP-β-CD get 100mg/ml, to inject for muscle,it is irritant, too. In these aspect, HP-β-CD is better than other solutizers.
To sum up HP-β-CD is the best medicine carrier certainly in the present.

   
 

Hydroxypropyl beta cyclodextrin 

Description: Hydroxypropyl beta cyclodextrin (HPBCD)is  the hydroxypropyl derivative of B-cyclodextrin.It has the best balance of enhanced aqueous solubility, the wide range of drugs with which it forms stable complexes, and the most extensive collection of safety data with no adverse reactions reported. HPBCD is itself very soluble in water (greater than 500 mg/ml at room temperature compared to 18 mg/ml for B-CD)

  Appearance white powder
  Specific Rotation +120~+145˚
  Degree of substitution 4--8
  Loss on drying <=6%
  Residue on ignition <=0.1%
  Heavy Metal(Pb) <10ppm
  Arsenic <5ppm
  Purity >=97%

 

   
       
  Applications    
       
  The application directions of Hydroxypropyl-beta-cyclodextrin:
Hydroxypropyl-beta-cycoldextrin is abbreviated to HP-β-CD or HPB,it is hydrogen atom which is in the remains of glucose in β-CD 2-, 3- and 6-hydroxl, is replaced hydroxyproply-oxygen by HP.
HP-β-CD, as β-CD, to many other chemical compounds, not only has fine holding action, which develop dissolubility of held matter, also has the advantages of high water-soluble, improvement the release speed of held medicine in the organism and high biological atilizablity. HP-β-CD not only getting to safety properties is wide-ranging but also is a medicine subsidiary metrial what it hasn't harmful side effects
   
  HP-β-CD Caution:


1
HP-β-CD is easy dissolved in water oneself. In room temperature, solubility50g/100ml, even to get over 80g/100ml. When its consistency is 40%, it flows verywell, not sticking. After medicine and HP-β-CD form compound matter, medical consistency of raise and HP-β-CD of consistency of raise are linear relationship. 
2
When HP-β-CD or HP-β-CD of medicial compound matter was made aqueous solution, produced a volume expansion obviously, their volume expansion are about 1ml/g below low consistency (50% w/v). When the consistency 20% (w/v), the volume expansion is about 0.7ml/g. 
3
HP-β-CD is soluble in methanol and ethanol, this sistuation for raising medical helding provided extensive chance. Usually HP-β-CD and medical helding is in a ratio (w/w) of 10-20 to 1 (their ratio can enlarge 30-40 to 1 under some situation), useing above-metioned the technology of raising solubility, HP-β-CD of dosage reduced 7-8 to 1 obviously (or 20-30 to 1). 
4
HP-β-CD aqueous solution is steady for high pressure sterilization temperature and pressure of influence, and 45% (w/v) of HP-β-CD aqueous solution can be filtrated by 0.2μ of filter to kill germs below low temperature. 
5
HP-β-CD is idea medicine that it conquers to universally existent questions in biology products. 
In the aspect of HP-β-CD increasing medical stability, raising the medicine (cann't soluble in water) of solubility, reducing medical irritability for people, raising medical biology utilization ratio as so on, it will bring about important effect. So HP-β-CD has a vast range of prospects of development. 
   
  The commonly used medthod for HP-β-CD helding medicine (or other matter):    
 
1Ingredient

a) If the holding matter is water-soluble matter, you will can according fixed proportion to solubilize in walter.
b) If the holding matter isn't water-soluble matter, you will can solubilize holding matter in ethanol
methanol or soluble solvent for holding matter. In addition, when HP-β-CD solubilizes in water or alcohol, according to fixed proportion to solubilize each other or mix.
2
Promoting the method of helding reaction (the following handling method, you'd better adjust the temperature higher, it's gradually getting low temperature in the course of the handling.)

a) Taking above-mentioned mixed solution, to stir high speed in room temperature or low temperature.
b) Given above-mentioned condition to treat by ultrasonic wave.
c) Given above-mentioned to grind by coloid.
d) Using above-mentioned high pressure (or low pressure) starch.
3
Helding compound matter of drying

The specimens which are after holding and handling can adopt, reduce pressure to dry beside then shatter.
4
Helding compound matter of examination

You can adopt fluorescent light spectrum law to test helding matter how to form normal number, in addition, you can also adopt NMR law to analyze HP-β-CD for certain matter of helding information.
5
Helding matter of releasing and picking up.

a) Under the normal situation, helding compound matter is basic steady. In water solution, it usual isn't released by insoluble helding matter in water. But there are some helding matter are fit for HP-α-CD or HP-γ-CD, their stable constants are lower after they and HP-β-CD formal helding compound matter, so if they are taken in aqueous solution for long time, helding matter is released of its own accord from HP-β-CD, too, and it will form some sediment in water.
b) When helding compound matter is in water solution, it makes helding water-soluble matter enlarge released speed and released measure with the tempurature of going up, under the suitable condition making released matter consistency and helding matter consistancy by HP-β-CD get to balance.
c) Helding compound matter can be extract again and again by some organic solvent (it will be best solvent which is HP-β-CD can't be dissolve.) the method can mdke helding matter to be extrant.
All kind of above-mentioned helding principle, helding compound matter of character, just for HP-β-CD reference. You can choose different handling methods to different quality of matter. Even if the same handling method, they still get different helding effect possibly for handling temperature, solution consistency, long or short handling times, handling intensity.
We hope that the users can according to helding matter of quality to choose suit handling method and helding condition, so that it make to get the best helding effect. If you need to help for useage technology, our company of technology department will assist to solve with all our strength.
   
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  Material Safety Data Sheet    
       
  Related Materials and Informations    
 
Dextrin(Dt) 
   
  Alpha Cyclodextrin    
  Beta-Cyclodextrin    
  Hydroxyethyl Beta Cyclodextrin    
  Methyl-Beta-Cyclodextrin    
  Glucose-Beta-Cyclodextrine    
       
     
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