CONJUGATE OF POLYGLYCOL AND NALOXONE AND PHARMACEUTICAL COMPOSITION AND USE THEREOF

摘要

Provided are a polyglycol - naloxone conjugate of general formula (II) and a pharmaceutical composition containing the conjugate. In the conjugate, n is an integer of 1 - 20. Also provided is a conjugate of three - branched or four - branched polyglycol and naloxone. Structural modification is performed on naloxone via hydrophilic polymers to improve the pharmacokinetic properties of the drug, increase the water solubility of naloxone itself, improve the distribution of the drug in the body, reduce the side effects of naloxone on the central nervous system, and relieve bowel dysfunction and constipation due to the long-term use of opioid medicines. Also provided are a pharmaceutical composition containing the conjugate of the present invention and use of the conjugate.