Sulfonation modification process of thio chitosan

Abstract

The invention discloses a sulfonation modification process of thio chitosan, which comprises: firstly, obtaining sulfonic aldehyde by using diethoxy methyl bromide and thiourea as initial raw materials and by a series of processes including addition, hydrolysis, enzyme-induced oxidation, Dowwex-50 column purification; and secondly, modifying the thio chitosan by using the sulfonic aldehyde under an alkaline condition to obtain sulfo thio chitosan of which 60 to 70 percent of the N atom positions is modified by the sulfo. In the invention, based on the large functional amino content of the chitosan, a novel and better high polymer material is provided by sulfonating the aminos for loading medicaments through electrostatic attraction. When the sulfo thio chitosan of the invention is used asa medicament carrier, the carrying capacity is high, the medicament release is smooth, and the release time is long. In addition, no toxic compound is adopted in the whole synthesis process, and the final product is adhesive and can carrier a large amount of ionic medicaments by an ionic exchange mechanism. The product can be used in developing novel sustained-release, controlled-release and targeting medicament administration systems and is a safe and biodegradable novel functional high polymer material.

Description

technical field [0001] The invention relates to a N-atom position sulfonation modification process of mercapto chitosan, which belongs to the technical field of compound synthesis process. Background technique [0002] As a biocompatible and degradable polymer material, mercaptochitosan is often used as a drug carrier to load therapeutic drugs through microencapsulation. Due to the swelling of chitosan, the drug diffuses into the surrounding environment through the gel layer and microsphere erosion. It can achieve a certain purpose of slow and controlled release of drugs, but this slow and controlled release effect is not ideal, the kinetic characteristics of the released drugs are often unstable, and the drug concentration fluctuates greatly; in addition, the drug release time is short (often several hours, most drugs are released), can not achieve the purpose of long-term treatment, especially for treatment methods such as arterial embolization chemotherapy with drug-loade...

AI Technical Summary

Problems solved by technology

[0002] As a biocompatible and degradable polymer material, mercaptochitosan is often used as a drug carrier to load therapeutic drugs through microencapsulation. Due to the swelling of chitosan, the drug diffuses into the surrounding environment through the gel layer and microsphere erosion. It can achieve a certain purpose of slow and controlled release of drugs, but this slow and controlled release effect is not ideal, the kinetic characteristics of the released drugs are often unstable, and the drug concentration fluctuates greatly; in addition, the drug release time is short (often several hours most of the time Drugs are released), and the purpose of long-term treatment cannot be achieved, especially for treatment methods such as arterial embolization chemotherapy with drug-loaded microspheres (delivery of drug-loaded microspheres to the target site through femoral artery catheterization), ordinary microspheres are often Loading a fixed amount of drugs in advance cannot meet the changing requirements of clinical drug dosage, and due to the short sustained release time, repeated femoral artery cannulation is required to deliver microspheres, causing pain to patients, which requires the development of clinically available drugs. The microspheres used by doctors are simple to load drugs, and can flexibly control the amount of drugs loaded, and one-time administration can achieve long-term (about one week) sustained release effect

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