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Biodegradation polymer and its preparing process and application

A biodegradable polymer technology, applied in pharmaceutical formulation, transportation and packaging, packaging items, etc., can solve the problems of lower glass transition temperature and shortened storage period of polymers at room temperature, so as to reduce demand, speed up degradation time, The effect of increasing Tg

Active Publication Date: 2008-02-20
TIANDA PHARMA ZHUHAI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, biological evaluations have shown that the glass transition temperature (Tg) of the polymer is lower than that of polylactide, resulting in a shorter shelf life of the polymer at room temperature

Method used

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  • Biodegradation polymer and its preparing process and application
  • Biodegradation polymer and its preparing process and application
  • Biodegradation polymer and its preparing process and application

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0129] (a) step In the preparation of polyglycol ester, the most commonly used general reaction is according to the ring-opening esterification polymerization reaction between the diol of following formula and lactide:

[0130]

[0131] The advantage of the melt polycondensation reaction is that it avoids the use of solvents and a large number of other additives, which results in more convenient purification. It also yields reasonably high molecular weight polymers. However, more severe conditions are usually required to make the chain acidolyzable (or hydrolyzable in the presence of water). If the polymer backbone is susceptible to deprivation of hydrogen atoms or oxidation due to subsequent recombination of large free radicals, undesired, thermally induced side reactions, such as crosslinking reactions, may occur.

[0132] The function of the first step reaction (a) is to use an initiator to open the ring of the heterocyclic compound of structural formula III, IV or V. ...

Embodiment 1

[0187] Embodiment 1: Taking 1,4-cyclohexanedimethanol (CHDM) as starting material synthesis poly(L-lactide-cyclohexanedimethanol-ethyl phosphate LAEG-CHDM-EOP) polymer

[0188] 20 g (0.139 mol) of (3S)-cis-3,6-dimethyl-1,4-dioxane-2,5-dione (L-lactide LAEG) (purchased from Aldrich Chemical Company , recrystallized from ethyl acetate, sublimed and recrystallized again from ethyl acetate) and 2.0 g (13.9 mmol) of 1,4-cyclohexanedimethanol were placed in a 250 ml round-bottomed flask filled with dry argon. The flask was sealed under vacuum and placed in an oven heated to 140°C. The flask was maintained at this temperature for about 48 hours with intermittent shaking.

[0189] Then take out the flask and lower it to room temperature, add 200ml of chloroform and stir to dissolve, put it into an ice-salt bath to cool down, and add 4ml of triethylamine. Under argon flow and stirring, 2.26 g of ethyl dichlorophosphate was slowly added while maintaining 20-30°C. After stirring f...

Embodiment 2

[0190] Example 2: Properties of PolyLAEG-CHDM-EOP Prepared as Described in Example 1

[0191] A polymer prepared as described in Example 1, wherein (x or y) / n=10:1. The resulting poly( LAEG-CHDM-EOP ) The polymer was analyzed by GPC using polystyrene as a standard, and the resulting figure showed that Mw was 38341 and Mn was 18856, as shown in Figure 2.

[0192] The Tg measured by DSC is 37.67° C., as shown in FIG. 3 .

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Abstract

The invention relates to a polylactic polymer with organic phosphate bond in the main chain of biological degradation, which can change into innocuity residue by internal degradation. The solidity and hydrophobicity of lactic acid or glycollic acid prepolymer are strengthened by adding a circularity compound that potentially improves the final polymer Tg containing phosphorus, redudeces the need of high molecular weight prepolymer, and the internal degradation time is quickened by using low molecular weight preolymer and improving organic phosphate contents, which improves the encapsulating ratio between polymer and a plurality of aquosity medicines (such as paclixtel or docetaxel). Finally, practical matrices formed by medicine and polymer have much better mixing compatibleness without phenomena of medical phasic demixing and independent crystallization.

Description

technical field [0001] The present invention relates to biodegradable polylactic acid polymers containing phosphate linkages in the backbone which degrade in vivo to nontoxic residues. The polymer provided by the invention can be used for medical devices implanted in patients, drug release systems for sustained and controlled release, etc., and can also be used for engineering materials such as medical sutures, fabric fibers, foams, and plastics. Background technique [0002] Biocompatible polymeric materials have been widely used in applications for the release of therapeutic drugs and medical implant devices. But at the end of the course of treatment, medical staff still need to remove the biocompatible polymers that have completed drug delivery or have no medical value from the patient's body. Therefore, the most ideal polymer material is a biodegradable polymer material. [0003] Often frequent periodic dosing regimens are undesirable in many situations. For example, w...

Claims

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Application Information

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IPC IPC(8): C08G63/692C08G63/78C08L67/04A61K47/34A61L33/06A61L15/62
Inventor 赵中郭茂军刘华伟梁土观
Owner TIANDA PHARMA ZHUHAI
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