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Tetrandrine nanoemulsion injection and method of preparing the same

A technology of tetrandrine and nanoemulsion, which is applied in the direction of pharmaceutical formula, emulsion delivery, medical preparations of non-active ingredients, etc., can solve the problems of affecting the drug release effect and unsatisfactory stability, and achieve the improvement of drug bioavailability Low density, easy industrial production, and increased dispersion

Inactive Publication Date: 2008-10-08
ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The formula and preparation method used in this method generally produce emulsions with a particle size of more than 100mn, which is not a transparent solution and has unsatisfactory stability, which in turn affects the drug release effect.

Method used

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  • Tetrandrine nanoemulsion injection and method of preparing the same
  • Tetrandrine nanoemulsion injection and method of preparing the same
  • Tetrandrine nanoemulsion injection and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] a. Take tetrandrine 0.6g, Tween-80 15.5g, polyethylene glycol 400 7.8g, ethyl oleate 5g, glycerin 1.5g, oleic acid 0.5g and water for injection 70g, set aside;

[0066] b. Dissolve tetrandrine in a mixture of Tween-80 and polyethylene glycol 400, add ethyl oleate, glycerin and oleic acid, mix well, and set aside;

[0067] c. Stir at normal temperature and pressure, and at the same time slowly add the amount of water for injection dropwise until the system forms a clear liquid, and the tetrandrine nanoemulsion with a transparent appearance is obtained.

[0068] d. Filling and sterilizing the tetrandrine nanoemulsion to prepare the tetrandrine nanoemulsion injection.

[0069] After testing, the average particle diameter of the tetrandrine nanoemulsion is 16.8nm.

Embodiment 2

[0071] a. Take Tetrandrine 1.2g, polyethylene glycol-vitamin E succinate 15.0g, propylene glycol 8.0g, soybean oil for injection 10.0g, glycerin 2.0g, oleic acid 2.0g and water for injection 62g, set aside;

[0072] b. Dissolve tetrandrine in a mixture of polyethylene glycol-vitamin E succinate and propylene glycol, add soybean oil for injection, glycerin and oleic acid, mix well, and set aside;

[0073] c. Stir at normal temperature and pressure, and at the same time slowly add the amount of water for injection dropwise until the system forms a clear liquid to obtain a transparent tetrandrine nanoemulsion with a particle size of 10-100 nm.

[0074] d. Filling and sterilizing the tetrandrine nanoemulsion to prepare the tetrandrine nanoemulsion injection.

[0075] After testing, the average particle diameter of the tetrandrine nanoemulsion is 21.5nm.

Embodiment 3

[0077] a. Take Tetrandrine 1.8g, polyethylene glycol-vitamin E succinate 19.5g, propylene glycol 7.0g, soybean oil 15.0g, glycerin 1.2g, oleic acid 2.5g and water for injection 50.5g, set aside;

[0078] b. Mix polyethylene glycol-vitamin E succinate, propylene glycol, ethyl oleate, glycerin, and oleic acid, stir at normal temperature and pressure, and slowly add water for injection dropwise until the system forms a clear liquid;

[0079] c. Add tetrandrine, stir and dissolve to obtain tetrandrine nanoemulsion with a particle size of 10-100 nm and a transparent appearance.

[0080] d. Filling and sterilizing the tetrandrine nanoemulsion to prepare the tetrandrine nanoemulsion injection.

[0081] After testing, the average particle diameter of the tetrandrine nanoemulsion is 18.3nm.

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Abstract

The invention discloses a hanfangchin a nanoemulsion injection and a preparation method thereof, containing the hanfangchin a, surfactant, cosurfactant, oil phase and water phase. The nanoemulsion of the invention has the advantages of simple preparation method, transparent appearance, 10-100nm of particle diameter and good stability, thereby remarkably improving solubility of the hanfangchin a, so as to improve bioavailability of drugs, and changing intracorporal process of drugs, so as to increase targeting to liver, reduce toxic and side effect and improve treatment effect.

Description

technical field [0001] The invention relates to a tetrandrine injection and a preparation method thereof, more specifically a tetrandrine nanoemulsion injection and a preparation method thereof. Background technique [0002] Nanoemulsion is a transparent, thermodynamically stable and isotropic oil-water mixing system, generally composed of oil phase, water phase, surfactant and co-surfactant. Nanoemulsion can be formed spontaneously, and the preparation process is simple. Most of the dispersed phase particles are spherical and uniform in size, and the particle size is usually 10-100nm. As a new drug delivery system, it is stable, slow-release, can improve drug bioavailability and exert targeting effects. After intravenous injection, it is phagocytosed by the reticuloendothelial system in the body and passively enters the liver and spleen to achieve liver targeting. [0003] Tetrandrine (tetrandrine, TET), also known as tetrandrine, is a bisbenzylisoquinoline alkaloid extra...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/4748A61K47/34A61K47/44A61P1/16A61K47/10A61K47/22A61K47/24A61K47/26
Inventor 桂双英吴蕾
Owner ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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