Method for preparing amino acid and lactic acid copolymer

A technology of lactic acid copolymerization and amino acid, applied in the field of preparation of biodegradable materials, can solve the problems of large amount of reagents, time-consuming, complex process, etc., and achieve the effect of reducing synthesis cost, rapid synthesis and easy product

Inactive Publication Date: 2007-08-29
SOUTH CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the rather cumbersome preparation and purification process of cyclic monomers such as morpholine-2,5-dione and lactide makes the entire preparation route of amino acid and lactic acid copolymer tedious, and the amount of solvent and reagent used is large, resulting in the overall existence of Unfavorable economic factors such as complex process, time-consuming, and high consumption

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Using D, L-LA and glycine as raw materials, mix them evenly according to the mass ratio m(D, L-LA):m(glycine) = 98:2, and obtain the intermediate Body I, adding catalyst zinc oxide (mass percentage is 0.6% of Intermediate I), melt polycondensation at a temperature of 165° C. and a pressure of 70 Pa for 10 h. After the reaction, the product was purified by dissolving in chloroform at room temperature, precipitated by methanol, and dried in vacuum to obtain a white powdery amino acid and lactic acid copolymer. The structure of the copolymer was confirmed by polymer characterization methods such as infrared spectroscopy, hydrogen nuclear magnetic resonance spectroscopy, and gel permeation chromatography. , Intrinsic viscosity [η] 0.8458dL / g, amino acid and lactic acid copolymer synthesized by this method can successfully prepare Fuliping slow-release microspheres.

Embodiment 2

[0022] Use D, L-LA, and alanine as raw materials, mix them evenly according to the mass ratio m(D, L-LA):m(alanine)=90:10, and remove water after prepolymerization at 130°C, 4000Pa, and 12h Intermediate I was obtained after treatment, adding catalyst zinc lactate (0.5% by mass of Intermediate I), controlled temperature 160°C and pressure 80Pa, and reacted for 20h. After the reaction, the product was dissolved in chloroform, purified by methanol precipitation, and vacuum-dried to obtain a white powdery amino acid and lactic acid copolymer. The structure of the copolymer was confirmed by polymer characterization methods such as infrared spectroscopy, hydrogen nuclear magnetic resonance spectroscopy, and gel permeation chromatography. The characteristics Viscosity [η] 0.5236dL / g, amino acid and lactic acid copolymer synthesized by this method successfully prepared 5-fluorouracil sustained-release microspheres.

Embodiment 3

[0024] Using L-LA and tyrosine as raw materials, mix them uniformly according to the mass ratio m(L-LA):m(tyrosine)=50:50, and obtain intermediate Body I, adding catalyst ferrous lactate (mass percentage is 0.1% of Intermediate I) at a temperature of 165 ° C and a pressure of 90 Pa, melt polycondensation for 3 hours. After the reaction, the product was dissolved, precipitated and purified, and vacuum-dried to obtain a white powdery amino acid and lactic acid copolymer. The structure of the copolymer was confirmed by polymer characterization methods such as infrared spectroscopy, hydrogen nuclear magnetic resonance spectroscopy, and gel permeation chromatography. The intrinsic viscosity [ η] 0.3085dL / g, can be applied to the preparation of ciprofloxacin drug microspheres.

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Abstract

The invention relates to a manufacture method for amino acid and lactic acid copolymer used for medicine slow release that uses alpha-amino acid and lactic acid as raw material. It adopts the method of fusion copolymerization condensation to shorten compounding time. And is easy to operate and is benefit to decrease the compound cost of the biology degradation.

Description

technical field [0001] The invention relates to a preparation method of a biodegradable material used for drug sustained release, in particular to a preparation method of amino acid and lactic acid copolymer. technical background [0002] Amino acid and lactic acid copolymers are one of the biodegradable materials, which can be applied to drug sustained release, tissue engineering, etc. In the traditional synthesis method of amino acid and lactic acid copolymers, ring-opening homopolymerization of morpholine-2,5-dione is usually performed, or morpholine-2,5-dione and cyclic monomer lactide Preparation by ring-opening copolymerization [Int'Veld P J A, Dilstra P J, Vanlochem J H, Feijen J.Synthesis of alternate polydepsipeptides by ring-opening polymerization of morpholine-2,5-dione derivatives[J]. Makromol Chem, 1990, 191(8) : 1813~1825; Zhang Guodong, Yang Jiyuan, Feng Xinde. Research Progress of Polylactic Acid [J]. Progress in Chemistry, 2000, 12(1): 89~102; Tang Zhirong,...

Claims

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Application Information

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IPC IPC(8): C08G63/08C08G63/78C08G63/685
Inventor 汪朝阳侯晓娜
Owner SOUTH CHINA NORMAL UNIVERSITY
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