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Series of polymers with acid-sensitive degradation and temperature-sensitive properties and drug-loading composition thereof

A polymer and property technology, applied in the fields of biomedicine and polymer medical materials, can solve the problems of chemical cross-linking monomer toxicity, high water content increases the risk of deterioration, unstable drug release properties, etc., and achieves good drug release properties , controllable degradation, and convenient administration

Pending Publication Date: 2022-01-28
FANTAI INST OF CHEM MEDICINES NANJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned traditional in-situ gel materials more or less have the following problems: poor biocompatibility and difficulty in metabolism; chemical cross-linking monomers have certain toxic effects; drug release properties are unstable; high water content in the system increases the risk of deterioration; Positively injecting temperature-sensitive materials with high temperature will bring pain to patients, and even cause local necrosis, etc.
However, the unique degradation pathway of this new polyorthoester makes it have a higher safety risk than traditional polyorthoesters
During its degradation process, one of the final products of the degradation of the five-membered ring of orthoester is formic acid. This degradation product with optic neurotoxicity greatly limits its clinical application prospects.

Method used

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  • Series of polymers with acid-sensitive degradation and temperature-sensitive properties and drug-loading composition thereof
  • Series of polymers with acid-sensitive degradation and temperature-sensitive properties and drug-loading composition thereof
  • Series of polymers with acid-sensitive degradation and temperature-sensitive properties and drug-loading composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] Embodiment 1 A kind of preparation method of oligomer monomer

[0112] The oligomer monomers of this example were prepared from glyceryl monostearate (GMS) and glycolide (GA). The molar ratio of the two components is 1:1.

[0113] as attached figure 1 As shown, weigh glyceryl monostearate (GMS) (17.928g, 0.05mol) and glycolide (GA) (5.8035g, 0.05mol) in a pressure-resistant reaction tube, under the protection of an inert gas, at 180 ℃ airtight heating and stirring for 24h, the product obtained is glyceryl monostearate diglycolide (GMS-diGL).

Embodiment 2

[0114] Example 2 A method for preparing a polymer with acid-sensitive degradation and positive temperature-sensitive properties

[0115] The polymer with acid-sensitive degradation and positive temperature-sensitive properties in this example was prepared from 3,9-bis(ethylene)-2,4,8,10-tetraoxaspiro[5,5]undecane (DETOSU), triethylene glycol (TEG) and glyceryl monostearate diglycolide (GMS-diGL). The molar ratio of the three components (DETOSU:TEG:GMS-diGL) was 90:80:20.

[0116] as attached figure 2 As shown, under strict anhydrous conditions, DETOSU (1.910 g, 0.009 mol) was dissolved in 15 ml of anhydrous tetrahydrofuran (THF) and TEG (1.2014 g, 0.008 mol) in a 50 ml flask, and GMS-diGL (0.9493 g , 0.002mol) was dissolved in 5ml of anhydrous THF. The GMS-diGL solution was added to the solution of DETOSU and TEG to initiate polymerization. Within minutes, the solution reached boiling point. The solution was allowed to cool to room temperature, then concentrated by rotar...

Embodiment 3

[0117] Example 3 A method for preparing a polymer with acid-sensitive degradation and positive temperature-sensitive properties

[0118] The polymer with acid-sensitive degradation and positive temperature-sensitive properties in this example was prepared from 3,9-bis(ethylene)-2,4,8,10-tetraoxaspiro[5,5]undecane (DETOSU), triethylene glycol (TEG) and glyceryl monolaurate diglycolide (GML-diGL). The molar ratio of the three components (DETOSU:TEG:GML-diGL) was 95:80:20.

[0119] Under strict anhydrous conditions, DETOSU (2.0164 g, 0.0095 mol) was dissolved in 15 ml of anhydrous (tetrahydrofuran) THF and TEG (1.2014 g, 0.008 mol) in a 50 ml flask, and GML-diGL (0.7807 g, 0.002 mol ) was dissolved in 5 ml dry THF. The GML-diGL solution was added to the solution of DETOSU and TEG to initiate polymerization. Within minutes, the solution reached boiling point. The solution was allowed to cool to room temperature, then concentrated by rotary evaporation at 50°C, followed by rota...

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Abstract

The invention discloses a series of polymers with acid-sensitive degradation and temperature-sensitive properties and a drug-loading composition thereof, the polymers have a structure represented by a formula (1), and have degradation and temperature-sensitive properties in a physiological environment, the polymers are in a solid state below a phase-transition temperature, are in a liquid state above the phase-transition temperature, and are in a stable state in a low-temperature environment of a storage condition. The polymer has a good fluidity state in a use environment, good drug release property and degradability are maintained, stability during storage and needle passing performance during injection are taken into consideration, and the invention also discloses a preparation method of the polymer and a pharmaceutical composition containing the polymer.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and polymer medical materials, and specifically relates to a series of polymers with acid-sensitive degradation and positive temperature-sensitive properties, a preparation method thereof, and a pharmaceutical composition. [0002] technical background [0003] In the field of drug sustained and controlled release research, the properties of sustained-release materials are one of the important factors that determine the success or failure of formulation design. An ideal sustained-release injection material should take into account good biocompatibility, effective control of drug release, and good injectability. In the field of drug delivery, the commonly used in situ gels include natural gel materials and synthetic gel materials according to their sources. Gel generation), high temperature positive thermosensitivity (sol at higher temperature, gel after injection temperature drop), pH sensitiv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/664C08G63/78A61K9/00A61K9/06A61K31/428A61K31/439A61K45/00A61K47/34A61P1/08A61P25/16
CPCA61K47/34C08G65/002A61K31/428A61P25/16Y02A50/30
Inventor 何东升涂家生冯作勋孙春萌
Owner FANTAI INST OF CHEM MEDICINES NANJING
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