Dihydroartemisinin emulsion for injection, freeze-dried emulsion and preparation method thereof

A technology for dihydroartemisinin and injections, which is applied in the fields of emulsion delivery, anti-infective drugs, oil/fat/wax non-active ingredients, etc. It can solve problems such as unsuitable use, unsafe hidden dangers, and nephrotoxicity, and achieves Good long-term stability, avoid delamination effect

Inactive Publication Date: 2010-01-13
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Part of the drug in the emulsion prepared by using such a solubilizer will be dispersed in the water phase through solubilization instead of being encapsulated in the oil phase. At the same time, there are some problems in the emulsion when it is administered intravenously. Solubilizer for injection preparations; povidone can hinder the coagulation process during intravenous injection, and there are unsafe risks, so it is not suitable for use in injections; hydroxypropyl-β-cyclodextrin may cause hemolysis during intravenous injection At the same time, it has nephrotoxicity, and it has been reported in the literature that it is carcinogenic. So far, we do not have a deep understanding of the safety of hydroxypropyl-β-cyclodextrin, so its use should be cautious
In addition, the highest drug loading amount of the drug in the example can reach 4.6 mg / ml, but only 0.1 mg / ml of the preparation was used in the in vivo anti-tumor experiment, and the reason is unknown

Method used

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  • Dihydroartemisinin emulsion for injection, freeze-dried emulsion and preparation method thereof
  • Dihydroartemisinin emulsion for injection, freeze-dried emulsion and preparation method thereof
  • Dihydroartemisinin emulsion for injection, freeze-dried emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032]Take 0.05g of dihydroartemisinin, 0.25g of soybean lecithin, 0.10g of oleic acid, dissolve and mix evenly with an appropriate amount of ethanol at room temperature, evaporate to dryness under reduced pressure to remove ethanol, add 5g of soybean oil for injection, 0.05g of glycerol monostearate Mix the esters uniformly at 40°C to form oil phase A; take 80ml of water for injection, add 2.2g glycerin to it, stir and dissolve 0.25g F68 at room temperature to form water phase B; mix the above oil phase A with water phase B at 40°C , stirred by a high-speed homogenizer at the same temperature for 5 minutes to make colostrum, add water for injection to a final volume of 100ml, and adjust the pH value to 6-7.5; transfer the prepared colostrum into a micro-jet high-pressure homogenizer, and adjust it evenly Treat the pressure to 5000psi for 2 cycles, then adjust the homogenization pressure to 15000psi for 8 cycles to obtain the emulsion, pass the emulsion through a 0.22μm micropo...

Embodiment 2

[0034] Take 0.20g of dihydroartemisinin, 1.2g of soybean lecithin, 0.18g of oleic acid, dissolve and mix evenly with an appropriate amount of ethanol at room temperature, evaporate to dryness under reduced pressure to remove the ethanol, add 10g of soybean oil for injection, 0.10g of glycerol monostearate Mix the esters uniformly at 55°C to form oil phase A; take 80ml of water for injection, add 2.2g glycerin to it, and stir and dissolve 1.2g F68 at room temperature to form water phase B; mix the above oil phase A with water phase B at 55°C Mix and stir for 10 minutes with a high-speed homogenizer at the same temperature to make colostrum, add water for injection to a final volume of 100ml, and adjust the pH value to 6-7.5; transfer the prepared colostrum into a micro-jet high-pressure homogenizer, adjust Homogenize the pressure to 5000psi for 4 cycles, then adjust the homogenize pressure to 15000psi for 8 cycles to prepare the emulsion, pass the emulsion through a 0.22μm micro...

Embodiment 3

[0036] Take 0.25g of dihydroartemisinin, 1.8g of soybean lecithin, 0.8g of cholesterol, dissolve and mix evenly with an appropriate amount of ethanol at room temperature, evaporate to dryness under reduced pressure to remove ethanol, add 10g of soybean oil for injection, 0.10g of glyceryl monostearate in Mix well at 80°C to form oil phase A; take 80ml of water for injection, add 2.2g glycerin to it, and stir and dissolve 1.8g F68 at room temperature to form water phase B; mix the above oil phase A with water phase B at 80°C, Stir with a high-speed homogenizer at the same temperature for 5 minutes to make colostrum, add water for injection to a final volume of 100ml, and adjust the pH value to 6-7.5; transfer the prepared colostrum into a micro-jet high-pressure homogenizer to adjust the homogenization Treat the pressure to 5000psi for 4 cycles, and then adjust the homogenization pressure to 15000psi for 8 cycles to obtain the emulsion, pass the emulsion through a 0.22μm micropo...

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Abstract

The invention discloses an injection dihydroartemisinin emulsion, which is prepared by adjusting the pH value of the mixture consisting of the following raw materials with weight / volume percent based on the total volume of the emulsion: 0.05-0.3 percent of dihydroartemisinin, 5-30 percent of injection oil, 0.5-10 percent of emulsion, 0.1-3 percent of stabilizing agent, 0.5-5 percent of isoosmotic adjustment agent and the rest of injection water; the stabilizing agent consists of one or more of sodium taurocholate, sodium deoxycholate, oleic acid, sodium oleate and cholesterin and glycerol stearate. Freeze-dried emulsion can be made through freeze drying after adding freeze-dried protecting agent into the emulsion. The invention also discloses a method for preparing the emulsion as well as the freeze-dried emulsion. The injection dihydroartemisinin emulsion prepared by the method leads to the stable existence of dihydroartemisinin in the oil phase of the emulsion and has the advantages of good long term stability and curative effect, high bioavailability and accordance with the standards of intravenous injection; and the freeze-dried emulsion is convenient for carrying and storage and can further increase the stability of drugs.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a dihydroartemisinin emulsion for injection, a freeze-dried emulsion and a preparation method thereof. Background technique [0002] In the 1860s, malaria parasites became resistant to the long-used antimalarial drugs such as chloroquine, and spread rapidly around the world. Finding drugs that could treat drug-resistant malaria became an urgent medical problem that needed to be solved at that time. In 1972, Chinese researchers isolated an effective antimalarial monomer from the traditional Chinese medicine Artemisia annua, and named it artemisinin. Artemisinin is a new type of sesquiterpene lactone compound with a unique peroxide bridge structure in the molecule. It is used for the treatment of malaria. It has the characteristics of fast onset of action, good antimalarial effect and low toxicity. Chloroquine-resistant Plasmodium has special effects on drug-resistant ce...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61K9/107A61K31/357A61K47/44A61K47/14A61K47/12A61P35/00A61P33/06
Inventor 梁文权王硕叶祖光梁秉文
Owner ZHEJIANG UNIV
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