Conjugate of Polyethylene Gylcol and Naloxone and Pharmaceutical Composition and Use Thereof

a technology of polyethylene gylcol and naloxone, which is applied in the field of hydrophilic polymernaloxone conjugate, can solve the problems of side effects that affect the quality of life of patients, ineffective orally administered in the form of tablets, and side effects
US20150045555A1Active Publication Date: 2015-02-12JENKEM TECH CO LTD TIANJIN
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Patent Information

Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
JENKEM TECH CO LTD TIANJIN
Publication Date
2015-02-12

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Abstract

Provided are a PEG-naloxone conjugate of general formula (II) and a pharmaceutical composition comprising the conjugate. In the conjugate, n is an integer in the range of 1-20. Also provided is a three-branched or four-branched conjugate of PEG and naloxone. Structural modification of naloxone with a hydrophilic polymer improves the pharmacokinetic properties of the drug, increase the water solubility of naloxone, improve the in vivo distribution of the drug, reduce the side effects of naloxone on central nervous system, and relieve bowel dysfunction and constipation caused by chronic administration of opioids. Also provided are a pharmaceutical composition comprising the conjugate of the invention and use of the conjugate.
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Description

TECHNICAL FIELD

[0001] The present invention relates to a hydrophilic polymer-naloxone conjugate, in particular, a conjugate of a small molecular oligomeric ethylene glycol and naloxone, and to a pharmaceutical composition thereofBACKGROUND OF THE INVENTION

[0002] Opioid analgesics, such as morphine, are irreplaceable strong analgesics which have been widely used in clinical practice. Data shows that a total of 230 million prescriptions of opioids were written out just in the year 2007 in the US. Opioids mainly act on opioid receptors. Opioid receptors include three types, μ-, δ- and κ-receptors, each includes various subtypes. Opioid receptors exist in central nervous system such as spinal cord as well as peripheral nerves in stomach, small intestine, exocrine glands and the like. Therefore, opioid analgesics, having strong analgesic effects on central nervous system, lead to side effects by acting on peripheral opioid receptors. Primary side effects include opioid-induced bowel dysfun...

Claims

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