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Preparation of Artesunate Fat Emulsion for Injection and Its Pharmaceutical Application

A technology of artesunate and fat, applied in the field of pharmacy, can solve the problems of inability to be used for injection and cannot play a role, and achieve the effects of increasing stability, reducing toxic and side effects, and having good stability

Inactive Publication Date: 2015-12-09
福州欣瑞普医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This preparation is an oral dosage form and is also not intended for injection
However, for some patients with acute malaria, oral medication often does not work, and injection preparations must be used. Therefore, it is necessary to develop a new formulation of artesunate for the defects of oral and powder injection preparations of artesunate and the lack of technology.

Method used

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  • Preparation of Artesunate Fat Emulsion for Injection and Its Pharmaceutical Application
  • Preparation of Artesunate Fat Emulsion for Injection and Its Pharmaceutical Application
  • Preparation of Artesunate Fat Emulsion for Injection and Its Pharmaceutical Application

Examples

Experimental program
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Effect test

Embodiment 1

[0029] prescription:

[0030]

[0031] Put 50mg of artesunate into 1mL of absolute ethanol to fully dissolve into a solution, mix this solution with 10g of soybean oil for injection, evaporate and remove the absolute ethanol, add 1.2g of egg yolk lecithin for injection, 0.02g of egg yolk lecithin under nitrogen protection The antioxidant vitamin E was mixed at 60°C to form an oil phase mixture. Mix 50 mL of water for injection, 0.4 g of sodium oleate and 2.5 g of glycerin at 60° C. to form an aqueous phase mixture. Mix the water phase mixture and the oil phase mixture under the protection of nitrogen, and add water to 100mL. At 60°C, disperse at a high speed of 6500r / min and then mechanically stir for 20min to make colostrum. After adjusting the pH to 7.0, under the condition of a pressure of 105MPa Homogenize 8 times to obtain a homogeneous milky solution; filter the milky solution, seal it with nitrogen gas, sterilize at 115°C for 15 minutes, and store it below 25°C.

Embodiment 2

[0033] prescription:

[0034]

[0035]Put 500mg of artesunate into 5mL of chloroform and fully dissolve into a solution, mix this solution with 10g of olive oil for injection, evaporate and remove the chloroform, add 1.2g of lecithin for injection and 0.02g of antioxidant vitamin E under nitrogen protection , mixed at 70°C to form an oil phase mixture. Mix 70mL of water for injection, 2.5g of xylitol, and 0.2g of F68 at 70°C to form an aqueous phase mixture. Mix the water phase mixture and the oil phase mixture under the protection of nitrogen, add water to 100mL, at 70°C, 7000r / min high-speed dispersion and then mechanically stir for 20min to make colostrum, adjust the pH to 7.5, and carry out under the condition of 90MPa pressure Homogenize 9 times to obtain a homogeneous milky solution; filter the milky solution, seal it with nitrogen gas, sterilize at 120°C for 25 minutes, and store it below 25°C.

[0036] 2. Artesunate fat emulsion injection prepared with different e...

Embodiment 3

[0038] prescription:

[0039]

[0040] Put 300mg of artesunate into 3mL of acetone to fully dissolve into a solution, mix this solution with 20g of sesame oil for injection, evaporate the acetone, add 2.4g of egg yolk lecithin for injection, 0.02g of antioxidant vitamin E under nitrogen protection , mixed at 70°C to form an oil phase mixture. Mix 150mL of water for injection, 5g of glycerin, and 0.02g of oleic acid at 70°C to form an aqueous phase mixture. Mix the water phase mixture and the oil phase mixture under the protection of nitrogen, add water to 200mL, at 70°C, 7500r / min high-speed dispersion, then mechanically stir for 20min to make colostrum, adjust the pH to 8.0, and carry out under the condition of 95MPa pressure Homogenize 6 times to obtain a uniform milky solution; filter the above milky solution, seal it with nitrogen gas, sterilize at 125°C for 10 minutes, and store it below 25°C.

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Abstract

The invention discloses an artesunate fat emulsion injection preparation which contains 0.01 to 30 wt% of artesunate, 10.0 to 30.0 wt% of oil for injection, 0.6 to 30.0 wt% of an emulsifier, 0 to 10 wt% of a solubilizer, 0 to 5 wt% of a co-emulsifier, 2.25 to 7 wt% of an isotonic agent and 0.002 to 0.075 wt% of an anti-oxidant, with the balance being injection water. The invention also discloses a preparation method and pharmacodynamic and safety evaluation for the artesunate fat emulsion injection preparation. The artesunate fat emulsion provided by the invention has the characteristics of good biocompatibility, high physical stability, convenient preparation, good security, high drug loading capacity and the like, has a particle size of less than 200 mu m and is suitable for injection, e.g, intravenous injection and intramuscular injection. According to the invention, the characteristic that a soybean oil fat emulsion inhibits growth of plasmodium falciparum is utilized to enhance anti-malarial effects of drugs, to improve bioavailability of the drugs and to reduce toxic and side effects of the drugs; nutrients needed by the body of a patient with malaria can be provided, the activity of lymphocytes of the patient is improved, which assists the patient in resisting malaria and recovering.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a fat emulsion injection, in particular to an artesunate fat emulsion injection. Background technique [0002] Artemisinin is an effective antimalarial monomer isolated and purified from Artemisia annua by Chinese scholars in the early 1970s. It is a new type of sesquiterpene lactone compound containing a peroxide bridge structure. The characteristics of no drug resistance and low toxicity are called "the greatest hope for the treatment of malaria" by the World Health Organization, and can be regarded as the greatest contribution of Chinese pharmaceutical workers to human society. Its discovery has become another important milestone in the world's antimalarial history after quinine. However, studies have shown that taking artemisinin preparations alone for a long time can easily lead to drug resistance of pathogens, and artemisinin is water-soluble and has low bioavailability. Therefore, a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/357A61P33/06
CPCY02A50/30
Inventor 马玉樊陈涛王汝涛王惟娇卢婷利赵雯王荧
Owner 福州欣瑞普医药科技有限公司
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