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Preparation technology of micro emulsion containing artemisic methyl ether (or artemisic ethyl ether or artemisic succinate)

A technology of artemether and arteether, which is applied in the field of preparation technology of microemulsion containing artemether (or arteether or artesunate), can solve the problems of poor curative effect, difficult absorption, poor water solubility of tablets, etc. Effectiveness, reducing gastrointestinal irritation, thermodynamically stable effect

Inactive Publication Date: 2005-08-10
广州中生生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, the dosage forms of artemisinin mainly include artemisinin suppositories or oral preparations, oral preparations and parenteral preparations of artesunate, artemether intramuscular injection preparations, etc. The tablets made have the disadvantages of poor curative effect and difficulty in absorbing

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 (microemulsion): Take 20 grams of glycerin, 8 grams of artemether, arteether or 10 grams of artesunate and caprylic triglyceride and mix them evenly, stir to dissolve, and add an appropriate amount of ethanol to obtain a clear and transparent solution; Add 15 grams of soybean phospholipids and dissolve in a constant temperature water bath at 80°C to obtain a clear solution; add an equal volume of water for injection, mix well, fill with nitrogen, and distribute. Sterilize at 105°C for 45 minutes.

Embodiment 2

[0025] Example 2 (Sub-nanoemulsion): Place 100 grams of medium-chain triglycerides, 12 grams of soybean phospholipids for injection, 22 grams of glycerol for injection and appropriate amount of water for injection in a high-speed tissue masher, disperse under nitrogen flow, and then pour Into the two-part milk homogenizer, slowly add 50 grams of refined soybean oil at 90°C and 20 grams of artemether (or arteether or artesunate), emulsify under nitrogen flow until the droplet size is less than 0.8 μm, and then add water to 1000 Milliliters, filtered, filled, filled with nitrogen, capped, autoclaved (115°C, 25 minutes). Store below 25°C (avoid freezing).

Embodiment 3

[0026] Example 3 (Solid Lipid Nanoparticles): Take 10 grams of artemether (or artemether or artesunate), 10 grams of soybean phospholipids and 30 grams of stearic acid, and heat to 80°C ± 5°C under nitrogen , Add 30 grams of glycerin and 5 grams of poloxamer 188 at the same temperature under stirring to make colostrum. Under the condition of 80℃±5℃ and nitrogen flow, homogenize the milk 5 times with a high-pressure milk homogenizer, fill it with nitrogen, and quickly cool to form Artemether (or artemether or artesunate) suspension.

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Abstract

An artemether microemulsion as novel antimalaria contains artemether, arteether or artesunate, emulsifier, emulsifying aid and plant oil. It can be applied by intravenous injection, oral taking, percutaneous absorption, and spray. Its preparing process is also disclosed.

Description

Technical field: [0001] The invention relates to a preparation process, formula and application of a novel antimalarial drug artemether microemulsion. [0002] It can be prepared into emulsions, powder injections, ointments, creams, solid lipid nanoparticles, and the route of administration is intravenous injection, oral administration, skin massage, spray administration and the like. Background technique: [0003] In the 1970s, Chinese scholars isolated the antimalarial drug artemisinin from the Chinese herbal medicine Artemisia annua. In the 1980s and 1990s, my country developed a new second-generation antimalarial drug-artemisinin, a derivative of artemisinin. The advent of similar drugs is a new milestone in the history of antimalarial drug research. There are 300 million cases of malaria every year around the world, and artemisinin-based drugs have significant curative effects and have little toxic and side effects on the human body. So far, no drug-resistant cases have been...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/35A61P33/06
Inventor 李校堃姚崇舜
Owner 广州中生生物技术有限公司
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