The safety of Hydroxypropyl Beta Cyclodextrin
Hydroxypropyl Beta Cyclodextrin (HPBCD) has a lower haemolysis than erb-cd. Compared with other derivatives, the order of hemolysis is dm-bbcd > sbe1-cd.However, 0.1ml of 45% water solution of some HPBCD caused 2% erythrocyte suspension hemolysis in rabbits, proving that the hemolysis of HPBCD cannot be ignored.J&j itraconazole intravenous injection contains 40% of hpbcd4, which can alleviate the hemolysis of HPBCD by controlling the drip rate (1ml/min) in clinical use.
About 3% of the radioactivity was detected in the urine of rats after oral HPBCD isotope labeling.However, no HPBCD prototype was detected in blood and urine after oral administration of HPBCD, indicating that the oral absorption of HPBCD is low and it is easy to be degraded in the gastrointestinal tract.In rats, HPBCD500, 2000 or 5000mg•kg-1•d-1 were taken orally for 25 months, and exocrine glandular hyperplasia was found.However, no similar results were observed in mice taking 500, 2000 or 5000•kg-1•d-1 for 22 to 23 months. Pancreatic hyperplasia may be a specific side effect of rats.Volunteers oral 16 g a day for 14 d, and non-toxic reaction, but more than 16 g can cause diarrhea, soft and static note 0.5 ~ 3 g, did not cause the change of the human body all tested parameters, volunteers can tolerate.Animal experiments showed that according to the different dose and method, in mice, rats, rabbits, dogs, horses, monkeys for experimental animals, such as the highest dose within the peritoneal and intravenous drug 10g•kg-1, oral 15g•kg-1 dosing after observing the behavior of animals, eating habits, and organs of animals for histological examination had no adverse effect. 20%, 40%, 50% (w/v) HPBCD solution, no irritation to skin, eyes, muscles.
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