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Method for preparing tetrandrine lung-targeted controlled-release microspheres

A tetrandrine, lung-targeting technology, applied in the field of medicine and health, can solve the problems of low drug loading, failure to obtain pharmacodynamic effect and controlled release effect at the same time, and large particle size of microspheres, and achieve drug loading rate. The effect of high and low blood drug concentration, distribution in non-affected tissue, and stable quality

Inactive Publication Date: 2011-11-16
GUANGZHOU MEDICAL COLLEGE ATTACHED CANCER HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these methods have the following defects: (1) the prepared microspheres are still relatively large in size; (2) the drug loading is relatively low.
This makes the application of these methods still have certain limitations, and fails to obtain the desired drug effect and controlled release effect at the same time.

Method used

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  • Method for preparing tetrandrine lung-targeted controlled-release microspheres
  • Method for preparing tetrandrine lung-targeted controlled-release microspheres
  • Method for preparing tetrandrine lung-targeted controlled-release microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] (1) Tetrandrine is used as the drug and polylactic acid is used as the polymer excipient, and the drug and the polymer excipient are dissolved respectively to form a drug solution and a polymer excipient solution; wherein the concentration of the polylactic acid solution is 5%.

[0025] (2) Mix the drug solution and the polymer auxiliary material solution according to the volume ratio of 8:100, and stir evenly; the weight ratio of tetrandrine and polylactic acid in the mixed solution is 5:7.

[0026] (3) Ultrasonic emulsification: put the mixed liquid in a glass container, turn on the ultrasonic generator, the power is 5 kilowatts, and the emulsification time is 20 minutes.

[0027] (4) Coagulation: the liquid is stirred at a stirring speed of 600 rpm for 1 hour.

[0028] (5) Solidification: Add glutaraldehyde to the liquid to solidify the microspheres, and stir continuously at a stirring speed of 500 rpm for 1 hour.

[0029] (6) Sedimentation: The prepared microsphere...

Embodiment 2

[0033] (1) Tetrandrine is used as a drug and polylactic acid is used as a polymer excipient, and the drug and the polymer excipient are dissolved respectively to form a drug solution and a polymer excipient solution; wherein the concentration of the polylactic acid solution is 2%.

[0034] (2) Mix the drug solution and the polymer auxiliary material solution according to the volume ratio of 8:100, and stir evenly; the weight ratio of tetrandrine and polylactic acid in the mixed solution is 5:8.

[0035] (3) Ultrasonic emulsification: put the mixed liquid in a glass container, turn on the ultrasonic generator, the power is 5 kW, and the emulsification time is 10 minutes.

[0036] (4) Coagulation: the liquid is stirred at a stirring speed of 600 rpm for 1 hour.

[0037] (5) Solidification: Add glutaraldehyde to the liquid to solidify the microspheres, and stir continuously at a stirring speed of 500 rpm for 1 hour.

[0038] (6) Sedimentation: The prepared microspheres are settl...

Embodiment 3

[0042] (1) Tetrandrine is used as a drug, and chitosan is used as a polymer auxiliary material, and the drug and the polymer auxiliary material are dissolved respectively to form a drug solution and a polymer auxiliary material solution; wherein the concentration of the chitosan solution is 3.5%.

[0043] (2) Mix the drug solution and the polymer auxiliary material solution according to a volume ratio of 12:100, and stir evenly; the weight ratio of tetrandrine and polylactic acid in the mixed solution is 5:9.

[0044] (3) Ultrasonic emulsification: put the mixed liquid in a glass container, turn on the ultrasonic generator, the power is 5 kilowatts, and the emulsification time is 20 minutes.

[0045] (4) Coagulation: the liquid is stirred at a stirring speed of 600 rpm for 1 hour.

[0046] (5) Solidification: Add glutaraldehyde to the liquid to solidify the microspheres, and stir continuously at a stirring speed of 500 rpm for 1 hour.

[0047] (6) Sedimentation: The prepared ...

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Abstract

The invention belongs to the field of medicaments and hygiene and relates to a method for preparing tetrandrine lung-targeted controlled-release microspheres. The method comprises the following steps of: preparing tetrandrine serving as a medicament into solution; and preparing one of polylactic acid, chitosan and gelatin serving as a high-polymer auxiliary material into solution; mixing the solution according to a certain proportion; and performing ultrasonic emulsification, coagulation, solidification, centrifugal separation and drying under a specific condition to obtain the tetrandrine microspheres. The method can obtain lung-targeted controlled-release microspheres. The microspheres have the advantages of small particle size, high medicament carrying rate, medicament application effect superior to that of microspheres prepared by the conventional method, high chemical stability and microorganism stability, controllable method and process and stable quality.

Description

technical field [0001] The invention belongs to the field of medicine and health, and relates to a preparation method of tetrandrine lung-targeted controlled-release microspheres. Background technique [0002] Lung cancer is the most common malignant tumor and the main cause of human cancer death. According to statistics, about 80% of lung cancer patients are in the middle and advanced stages when they are discovered, and they lose the opportunity for surgery. The main treatment is radiotherapy and chemotherapy. However, chemotherapy is limited by the side effects of chemotherapy. Although some patients can see the short-term curative effect, the remission period is short, the toxic and side effects are large, and the curative effect is not good. In recent years, many scholars have carried out in-depth research on the treatment of advanced lung cancer with traditional Chinese medicine, and have made some progress. [0003] Tetrandrine, also known as tetrandrine, is a bisb...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/4748A61K47/34A61K47/36A61K47/42A61P35/00A61P11/00
Inventor 程国华胡泽丽
Owner GUANGZHOU MEDICAL COLLEGE ATTACHED CANCER HOSPITAL
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