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It receives more and more widespread attention in the pharmaceutical field due to the special structure and properties of hydroxypropyl-β-cyclodextrin (HP-β-CD). Examexample the application characteristics of hydroxypropyl-β-cyclodextrin:
1, Increasing the water solubility of insoluble drugs. For example, dihydroartemisinin and Artemisia methyl ether themselves are not soluble in the HP-β -CD envelope after its solubility can meet the requirements of powder injection. The solubility of Digoxin in 50% HP-β -CD solution increased from 0.07mg/ml to 68mg/ml.
2, Increasing drug stability. For example, after estradiol envelopes with HP-β -CD, the half-life of placing its degradation at room temperature can be extended from 1.2 years to 4 years.
3, Reducing drug side effects. For example, the vasodilator drug Nimodipine is not soluble in water, and oral administration is susceptible to the first effect of the liver. Muscular administration using HP-β -CD for injection significantly increases biological absorption of drugs and reduces damage to the gastrointestinal or muscle tissue.
4, Improving drug availability.For example, after steroid hormones are surrounded by HP-β -CD, they can not only have high solubility and fast release, but also about 2 times higher drug levels in the blood compared with unenvelope hormones.
5, Security side of HP-β -CD. According to systematic subacute and chronic toxicity studies, HP-β -CD does not cause mouse disease and leads not to death. After intravenous injection of rabbits, HP-β -CD was quickly removed from the blood, excreted with urine, and was injected continuously without adverse symptoms. No clinical effect on 200mg
,HP-β -CD for intravenous administration in rats and monkeys. monkeys were also not administered orally or intravenous HP-β -CD up to 15g or 10g,, respectively. Human clinical studies showed that HP-β -CD received oral, intravenous infusion, intravenous injection, nasal, subtongue, and eye administration, showing no adverse reactions and irritation to the skin, eyes, and muscles. This shows that HP-β -CD is very safe for organisms.
1, Increasing the water solubility of insoluble drugs. For example, dihydroartemisinin and Artemisia methyl ether themselves are not soluble in the HP-β -CD envelope after its solubility can meet the requirements of powder injection. The solubility of Digoxin in 50% HP-β -CD solution increased from 0.07mg/ml to 68mg/ml.
2, Increasing drug stability. For example, after estradiol envelopes with HP-β -CD, the half-life of placing its degradation at room temperature can be extended from 1.2 years to 4 years.
3, Reducing drug side effects. For example, the vasodilator drug Nimodipine is not soluble in water, and oral administration is susceptible to the first effect of the liver. Muscular administration using HP-β -CD for injection significantly increases biological absorption of drugs and reduces damage to the gastrointestinal or muscle tissue.
4, Improving drug availability.For example, after steroid hormones are surrounded by HP-β -CD, they can not only have high solubility and fast release, but also about 2 times higher drug levels in the blood compared with unenvelope hormones.
5, Security side of HP-β -CD. According to systematic subacute and chronic toxicity studies, HP-β -CD does not cause mouse disease and leads not to death. After intravenous injection of rabbits, HP-β -CD was quickly removed from the blood, excreted with urine, and was injected continuously without adverse symptoms. No clinical effect on 200mg
,HP-β -CD for intravenous administration in rats and monkeys. monkeys were also not administered orally or intravenous HP-β -CD up to 15g or 10g,, respectively. Human clinical studies showed that HP-β -CD received oral, intravenous infusion, intravenous injection, nasal, subtongue, and eye administration, showing no adverse reactions and irritation to the skin, eyes, and muscles. This shows that HP-β -CD is very safe for organisms.Zhiyuan Biotechnologyl production of hydroxypropyl-β-cyclodextrin, properties, production process, stability, pharmacology, toxicology, distortion, mutation, cancer, hemolysis and irritation, have done thorough research, preparation of compounds can significantly improve drug stability, increase the solubility and biological utilization of insoluble drugs, reduce drug side effects, cover up bad drug odor, etc.
