Application of cleavable polyethylene glycol (PEG) lipid derivative in preparation

• Main Authors: ZHANG LING, HONG WEIWEI, DENG YIHUI, SONG YANG, XU HUAN, ZOU JIA, WANG LONG
• Format: Patent
• Language: Chinese; English
• Published: 07.11.2012
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; COMPOSITIONS BASED THEREON; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONSONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; ORGANIC MACROMOLECULAR COMPOUNDS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; STEROIDS; THEIR PREPARATION OR CHEMICAL WORKING-UP

The invention belongs to the technical field of medicaments, and provides application of a cleavable polyethylene glycol (PEG) lipid derivative to preparation of a PEGylated preparation for relieving or avoiding accelerated blood clearance. In the application, liquid microparticle preparations such as liposome, vesicles, emulsions, microemulsion, micelles, nanoparticles and the like are modified by the cleavable PEG lipid derivative such as PEG-cholesteryl hemisuccinate, PEG-cholesteryl methyl carbonate, PEG-alpha tocopheryl hemisuccinate and the like; and the measurement of variation of preparation elimination in tissues such as animal blood plasma, liver, spleen and the like after a cleavable PEG lipid derivative-modified medicinal preparation is repeatedly injected proves that repeatedinjection of cleavable PEG lipid derivative-modified microparticle preparations only causes light accelerated blood clearance or avoids the accelerated blood clearance, namely the accelerated blood clearance can be relieved o