Albendazole chitosan microsphere composition and preparation method thereof

A technology of albendazole shell and albendazole, which is applied in the field of bendazole chitosan microspheres, can solve the problems of low drug encapsulation efficiency and drug loading capacity of nanoparticles, and can not meet the requirements of clinical treatment, etc. , to achieve the effects of prolonging the action time of the drug, prolonging the action time in the body, and simple preparation method

Inactive Publication Date: 2012-07-04
石河子大学医学院第一附属医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Lian Wenyuan and others published the research content of preparing albendazole chitosan nanoparticles with chitosan in China Tissue Engineering Research and Clinical Rehabilitation, 2011, 15(47): 8847-8850, but the method prepared The highly toxic organic solvent dichloromethane was used in the process, and the drug encapsulation efficiency and drug loading capacity of nanoparticles were low, which could not meet the requirements of clinical treatment.

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  • Albendazole chitosan microsphere composition and preparation method thereof
  • Albendazole chitosan microsphere composition and preparation method thereof
  • Albendazole chitosan microsphere composition and preparation method thereof

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Embodiment 1

[0038]Embodiment 1: the albendazole chitosan microsphere composition comprises the chitosan that the weight portion is 10 parts of albendazole and the weight portion; The deacetylation degree of chitosan is 100%, and viscosity is 99 cps.

[0039] The preparation method of the albendazole-chitosan microsphere composition comprises the following processes: dissolving albendazole and chitosan in 8% acetic acid aqueous solution to form a water phase; dissolving 1% Span-80 in liquid paraffin The oil phase is formed in the water phase, and the volume ratio of the water phase and the oil phase is 1:4; the water phase is injected into the oil phase and stirred, the stirring speed is 500 rpm, and the stirring time is 3 hours to obtain an emulsion; then under stirring, the concentration is 20% glutaraldehyde was dropped into the emulsion, the stirring speed was 400 rpm, and the stirring time was 120 minutes. After the microspheres were cross-linked and solidified, centrifuged at 2000rpm...

Embodiment 2

[0040] Embodiment 2: the albendazole chitosan microsphere composition comprises the chitosan that the weight portion is 20 parts of albendazole and the weight portion; The deacetylation degree of chitosan is 100%, and viscosity is 10 cps.

[0041] The preparation method of the albendazole-chitosan microsphere composition comprises the following processes: dissolving albendazole and chitosan in 8% acetic acid aqueous solution to form a water phase; dissolving 8% Span-80 in liquid paraffin The oil phase is formed in the water phase, and the volume ratio of the water phase and the oil phase is 1:5; the water phase is injected into the oil phase and stirred, the stirring speed is 400 rpm, and the stirring time is 2.5 hours to obtain an emulsion; then under stirring, the concentration is 15% formaldehyde was dropped into the emulsion, the stirring speed was 500 rpm, and the stirring time was 160 minutes. After the microspheres were cross-linked and solidified, centrifuged at 2500 r...

Embodiment 3

[0042] Embodiment 3: the albendazole chitosan microsphere composition comprises the chitosan that the weight portion is 20 parts of albendazole and the weight portion; The deacetylation degree of chitosan is 100%, and viscosity is 1cps.

[0043] The preparation method of the albendazole-chitosan microsphere composition comprises the following processes: dissolving albendazole and chitosan in 6% acetic acid aqueous solution to form a water phase; dissolving 2.0% Span-80 in liquid paraffin The oil phase is formed in the medium, and the volume ratio of the water phase and the oil phase is 1:6; the water phase is injected into the oil phase and stirred, the stirring speed is 600 rpm, and the stirring time is 5 hours to obtain an emulsion; then under stirring, the concentration is 35% glutaraldehyde was dropped into the emulsion, the stirring speed was 500 rpm, and the stirring time was 100 minutes. After the microspheres were cross-linked and solidified; 3000rpm was centrifuged fo...

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Abstract

The invention relates to an albendazole chitosan microsphere composition and a preparation method thereof. The albendazole chitosan microsphere composition consists of albendazole and chitosan. The preparation method comprises the following steps of: dissolving albendazole and chitosan in a dilute acetic acid solution to form an aqueous phase, and dissolving a surfactant in oil to form an oil phase, wherein the volume ratio of the aqueous phase to the oil phase is (1:2)-(1:8); injecting the aqueous phase into the oil phase and stirring to obtain an emulsion; adding a crosslinking curing agent into the emulsion while stirring; after the crosslinking curing of microspheres is finished, performing centrifugal separation; washing with petroleum ether; and drying to obtain the albendazole chitosan microspheres. The albendazole chitosan microspheres provided by the invention have the characteristics of narrow particle size distribution, high encapsulation efficiency and simple preparation method; and compared with albendazole tablets, the albendazole chitosan microsphere composition has the advantages that the bioavailability is obviously improved to reach about 500% of the bioavailability of the albendazole tablets, the action time of the medicine can be prolonged, and the in-vivo medicine release time is increased to 48 hours.

Description

technical field [0001] The invention relates to an albendazole chitosan microsphere with higher bioavailability. Background technique [0002] Hepatic echinococcosis, also known as hepatic echinococcosis, is a chronic parasitic disease caused by the cystic larvae (Echinococcus) of Echinococcus parasitizing in the human liver. It is a zoonosis that seriously endangers the human body. Healthy endemic parasitosis. Albendazole (ABZ) is currently the first-choice therapeutic drug at home and abroad. It has been clinically proven that ABZ has a good anti-hydatid effect for more than ten years. 30-60% of patients can improve their symptoms after chemotherapy. Long-term treatment of patients can significantly prolong life. However, due to the low solubility and poor gastrointestinal absorption of albendazole tablets currently on the market, there is a problem of low bioavailability, which limits the effective application of albendazole in clinical practice. [0003] Therefore, th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4184A61K47/36A61P33/00
Inventor 王新春彭心宇
Owner 石河子大学医学院第一附属医院
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