Hydrooxypropyl Beta Cyclodextrin(HP-β-CD)
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.