Views:0 Author:Site Editor Publish Time: 2021-03-30 Origin:Site
Acyclovir has a strong inhibitory effect on herpes virus DNA polymerase, but the drug is poorly water-soluble and its oral absorption rate is about 15%, which seriously affects its clinical application. Hydroxypropyl-β-cyclodextrin (HP-β-CD) is a kind of hydroxyalkylated derivative of β-cyclodextrin, the solubility in aqueous solution is >50% (W/V) and it is soluble in alcohol In the aqueous solution. The inclusion of HP-β-CD on acyclovir increases the solubility of acyclovir, which is 4.4 times the original solubility on average, and solves the problems of poor water solubility and poor oral absorption of acyclovir. Selecting HP-β-CD as the inclusion substance of acyclovir, the preparation process is simple, the quality control method is reliable, the preparation stability is good, and it can meet the needs of clinical ophthalmology.
HP-β-CD is a non-crystalline white powder, stable to light, alkali and heat. It can withstand 80℃ and 4 500xl light for 10 d. It is easy to absorb moisture under high humidity conditions (humidity 92.5%) and is unstable to strong acids. . Hydroxypropyl-β-cyclodextrin is easily soluble in water, and its solubility at room temperature is greater than 50% (m/V), even as high as 75% (m/V). And can be dissolved in alcoholic water solution.
Compared with β-CD, HP-β-CD has the following characteristics:
①HP-β-CD has low nephrotoxicity and can be used parenterally. The route of administration is better than β-CD;
②HP-β-CD is not hydrolyzed by gastric acid and α-amylase, hardly participates in the metabolism of organisms, and does not accumulate;
③HP-β-CD and the drug form a complex to promote the release of the drug, while the β-CD and the drug form a complex to have a slow-release effect on the drug;
④HP-β-CD has low surface activity, basically no hemolysis and irritation, while β-CD has hemolytic effect, and parenteral administration also has a certain irritation effect.