Composite microsphere prepn of lactic acid-hydroxyacetic acid copolymer and its prepn process

A technology of composite microspheres and copolymers, which is applied in the field of pharmacy, can solve the problems of large particle size and complicated preparation methods, and achieve the effect of simple preparation method, simple preparation and delayed release

Active Publication Date: 2007-06-06
ZHEJIANG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug in this composite microsphere is completely encapsulated into the bilayer alginate-chitosan microsphere, so that the protein drug is protected by double hydrophilic polymers, not only has a suitable hydrophilic microenvironment, It is expected to improve the stability of the protein, and the co

Method used

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Example Embodiment

[0026] Example 1 A method for preparing PLGA microspheres modified by alginic acid and chitosan according to the present invention

[0027] Weigh about 0.33g PLGA (50:50), dissolved in 4ml of dichloromethane as the organic phase; also weighed 30mg of BSA model drug, dissolved in 100μl of distilled water and 100μl of 1% sodium alginate as the internal water phase, and the two phases were mixed Ultrasound with posterior probe (50w, 1s×20 times), fully emulsified and injected into 40ml mixed solution (50ml 2% PVA+50ml 2% chitosan solution+1g CaCl 2 The continuous filtrate of the mixed solution), high-speed stirring at 12000 rpm for 5 minutes, rotary evaporation under reduced pressure for 1 hour, centrifugation, washing with water 3 times, and freeze-drying. Alginic acid and chitosan modified PLGA microspheres with a size of 5 μm, a uniform particle size and a round shape were obtained.

[0028] The composite microspheres prepared by the method of the present invention can significant...

Example Embodiment

[0032] Example 2

[0033] Same as Example 1, but with a ratio of PLGA of 70:30, PLGA (70:30) microspheres modified with alginic acid and chitosan were obtained.

Example Embodiment

[0034] Example 3

[0035] Same as Example 1, but weighed 0.2g of PLGA, dissolved in 2ml of dichloromethane as the organic phase, mixed with the water phase and placed on a probe ultrasonic instrument, sonicated at 200w, 40s, formed colostrum and injected 20ml of the mixed solution PLGA microspheres modified with alginic acid and chitosan were homogenized for 3 minutes under stirring at 800 rpm, and the encapsulation efficiency and particle size of PLGA microspheres modified with alginic acid and chitosan were not statistically different.

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Abstract

The composite microsphere preparation of lactic acid-hydroxyacetic acid copolymer consists of medicine, calcium alginate, chitosan, glycolide-lactide copolymer, emulsifier and medicine supplementary material. It is prepared through adding low concentration sodium alginate solution to inner water phase containing medicine, forming initial emulsion with PLGA-containing organic phase, injecting PVA solution with chitosan and calcium chloride to form complex emulsion, decompression rotary evaporation to cure, water washing and freeze drying. The process is simple and feasible, and has no influence on the size of microsphere and no change in protein encapsulating rate, capacity of forming one hydrophilic micro environment to protect protein medicine, and capacity of reducing the release of medicine.

Description

technical field [0001] The invention belongs to the field of pharmacy, relates to a biodegradable microsphere preparation and a preparation method thereof, in particular to a hydrophobic biodegradable lactic acid-glycolic acid copolymer modified with natural hydrophilic biodegradable materials alginic acid and chitosan ( PLGA) composite microsphere preparation and preparation method thereof. This new type of compound preparation is of great significance for solving the phenomenon of sudden release of drugs encapsulated in sustained-release PLGA microspheres, especially for those drugs with strong potency, whose effective dose is close to the toxic dose, that is, with a small therapeutic window. Background technique [0002] Lactic acid-glycolic acid copolymer (PLGA) is also known as lactide-glycolide copolymer, polyethylene lactide, etc. It is polymerized from glycolic acid (or glycolic acid) and lactic acid, and is a biodegradable polymer material. Due to its easy synthes...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K47/34A61K9/00
Inventor 郑彩虹梁文权
Owner ZHEJIANG UNIV
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