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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.
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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% |
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Applications |
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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 |
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HP-β-CD
Caution:
1、HP-β-CD is easy dissolved in water oneself. In room temperature,
solubility>50g/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.
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The
commonly used medthod for HP-β-CD helding medicine (or other matter): |
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1、Ingredient
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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Packing
&loading |
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This data is only for your information purposes and does not imply
guarantee for a certain application.
Please note:
We do not deliver the product to private users! |
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If you need an indicative price to your country, please kindly advise
the annual quantity needed, destination port and we will send you
our soonest CNF(Cost + Freight) price. Your indication for a workable
price level will sure speed up our fastest service for you |
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We really need to get
feed back from our customers in order to improve our performances.
Any information about quotations from competitors will be welcomed
since we hope to work as a team with you.
Your kind help will be very much appreciated.
Best regards from SHENZHEN
, China
Mr. JEFFERY TSUI
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Material
Safety Data Sheet |
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Related Materials and
Informations |
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Dextrin(Dt)
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Alpha Cyclodextrin |
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Beta-Cyclodextrin |
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Hydroxyethyl
Beta Cyclodextrin |
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Methyl-Beta-Cyclodextrin |
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Glucose-Beta-Cyclodextrine |
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If the above information
doesn't cover |
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