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Polyethylene glycol-polyvinyl alcohol copolymer-metaxalone prodrug and synthesis method thereof

A technology of polyvinyl alcohol copolymer and polyethylene glycol, which is applied in the field of metaxalone prodrug and its synthesis, can solve the problems of slow dissolution rate, low loading capacity, and difficulty in obtaining it, so as to prolong half-life and increase water solubility. sexual effect

Inactive Publication Date: 2013-01-30
NORTHWEST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although polyethylene glycol has obvious advantages as a macromolecular carrier for prodrugs, since there are only 1 or 2 active hydroxyl groups at the molecular chain end of polyethylene glycol, its loading capacity is low, and the active drug molecules connected to the polymer chain less, it is often difficult to get a high loading rate
Polyvinyl alcohol has many activating groups, and each structural unit has a hydroxyl group, which can be connected with drugs. The drug loading can be changed according to the conditions, but its dissolution rate in water is relatively slow, and it needs proper heating to achieve fast dissolve

Method used

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  • Polyethylene glycol-polyvinyl alcohol copolymer-metaxalone prodrug and synthesis method thereof
  • Polyethylene glycol-polyvinyl alcohol copolymer-metaxalone prodrug and synthesis method thereof
  • Polyethylene glycol-polyvinyl alcohol copolymer-metaxalone prodrug and synthesis method thereof

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Abstract

The invention discloses a polyethylene glycol-polyvinyl alcohol copolymer-metaxalone prodrug represented by the general structural formula (I), wherein R is an integer of 10-100 and X is an integer of 3-10. The PEG-PVA-Met macromolecule prodrug synthesized by the present invention can not only increase the water solubility of the small molecule drug metaxalone and extend its half-life, but can also effectively control the release of the drug in the human body. This is undoubtedly good news for many patients with chronic diseases.

Description

technical field [0001] The invention relates to a metaxalone prodrug with a polyethylene glycol-polyvinyl alcohol copolymer as a carrier and a synthesis method thereof, belonging to the technical field of drug synthesis. Background technique [0002] With the development of polymer science and modern medicine, polymer drug controlled release system (PDDS) has become a hot research field. According to the mode of interaction between drugs and polymer carriers, PDDS can be divided into two categories, one is drug A drug slow release system that is physically embedded in a polymer carrier, that is, a drug slow release system obtained by encapsulation or compounding technology. The other is a macromolecule prodrug obtained by linking a polymer carrier with a small molecule drug through a covalent bond connection technology, also called a polymer prodrug. A prodrug is a special form of drug that remains inactive until transported to the site of action, and releases the active dr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/421A61P29/00A61P21/02
Inventor 张娟刘毅锋张亚洲周永柱
Owner NORTHWEST UNIV
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