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Preparing method for suspensoid of complete trans vitamin A acid

An all-trans retinoic acid and nano-suspension technology, which can be used in emulsion delivery, sensory disease, drug combination, etc. Maintaining effective drug concentration and other issues to achieve the effects of high repeatability, simple and convenient preparation process, and improved stability

Inactive Publication Date: 2004-11-17
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although some results have been obtained in animal experiments, there are still obvious deficiencies: 1, the drug loading is low (such as all-trans retinoic acid silicone oil, generally less than 15mg / L); 2, it is difficult to maintain the effective drug concentration during the treatment period ( All-trans retinoic acid is photothermally unstable and prone to chemical changes)
The existence of these problems greatly limits the practical application of all-trans retinoic acid in clinical treatment.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] 6. Prepare 1.0 mg / ml all-trans retinoic acid in acetone;

[0029] 7. Add 2.0 ml of the above-mentioned all-trans retinoic acid acetone solution into 100 ml of triple distilled water and perform ultrasonic treatment for 1 hour;

[0030] 8. Use a circulating water pump to vacuumize for 3 hours to remove the organic solvent;

[0031] 9. After filtration, store at 4°C in the dark.

Embodiment 2

[0033] 1. Prepare 5.0 mg / ml all-trans retinoic acid in acetone;

[0034] 2. Add 2.0 ml of the above-mentioned all-trans retinoic acid acetone solution into 150 ml of triple distilled water and perform ultrasonic treatment for 2 hours;

[0035] 3. Use a circulating water pump to vacuumize for 6 hours to remove the organic solvent;

[0036] 4. After filtration, store at 4°C in the dark.

Embodiment 3

[0038] 1. Prepare 10 mg / ml retinoic acid acetone solution;

[0039] 2. Add 2.0 ml of the above retinoic acid acetone solution into 200 ml of triple distilled water for 3 hours of ultrasonic treatment;

[0040] 3. Vacuum treatment with a circulating water pump for 6 hours to remove organic solvents; filter and store in the dark at 4°C.

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Abstract

The preparation method of all-trans retinoic acid nano-suspension is a preparation method of nano-medicine, and the preparation method is as follows: prepare an acetone solution of all-trans retinoic acid, and the concentration of retinoic acid is 1-10 mg / ml; The acetone solution of all-trans retinoic acid is added to water to obtain mixed solution A. The volume ratio of the two liquids mixed is: acetone solution of all-trans retinoic acid: water = 1:50~1:100, when the two liquids are mixed Use an ultrasonic instrument for ultrasonic treatment; use an ultrasonic instrument to perform ultrasonic treatment on the mixed solution A for 1-5 hours; use a vacuum device to vacuum the mixed solution A after ultrasonic treatment for 2-8 hours to remove the organic solvent; A nanosuspension loaded with all-trans retinoic acid was obtained. The invention can reduce the toxic reaction of the medicine, increase the safe dose, and prolong the residence time of the medicine in the eye, thereby effectively exerting the anti-proliferation effect of the medicine.

Description

1. Technical field: [0001] The invention relates to a preparation method of nano-medicine, in particular to a preparation method of all-trans retinoic acid nano-suspension nano-medicine. 2. Background technology: [0002] The development of new drugs is not enough to guarantee the progress of drug therapy: the high toxicity of drugs, low absorption, rapid metabolism, and difficult injection of water-insoluble drugs may be the main reasons for treatment failure. The development of nano-medicine may overcome the above problems. The bioavailability of drugs can be significantly improved after nanotechnology. Controlling the size and particle size distribution of nanoparticles can control the release rate of drugs and improve the efficacy and effective utilization of drugs. [0003] At present, in the field of nanomedicine research, the screening of drug carriers and the optimization of preparation processes are the research focus. Current carriers include nanoparticles, nano...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/192A61P27/02
Inventor 夏强顾宁段磊
Owner SOUTHEAST UNIV