低分子量聚谷氨酸的制备及其在眼科靶向药物中的应用研究

摘要

Large molecular weight drugs cannot be absorbed by human corneas. In order to minimize the side effects caused by absorption into eyeball trough cornea in the application of the highly toxic Mitomycin C in ocular surface diseases, PGA derivative macromolecule prodrug PGA-MMC was designed. To reduce the package wrapping effect on MMC using the chain-like macromolecules modifying such as PGA, which can make the pesticide effect reduce, PGA was first quantitative hydrolyzed to get lower molecular weight PGA(1~5 k).And then series of low molecular weight PGA-MMC was synthesized .%人体角膜难以吸收分子量较大的药物分子，为了减少高毒药物治疗眼表疾病时经角膜吸收导致的眼内副作用，设计了丝裂霉素C的L-聚谷氨酸衍生物高分子前药。为了减少市售链状大分子聚谷氨酸修饰后，丝裂霉素C被其包缠导致的药效降低，将市售的L-聚谷氨酸先进行定量水解，获得了一系列较低分子量的L-聚谷氨酸（1~5 k），通过电泳法确证其分子量，并将其应用制备了系列低分子量L-聚谷氨酸衍生物高分子丝裂霉素C前药。