A kind of injection containing oily medicine and preparation method thereof

Abstract

The invention provides an injection containing oiliness drugs, which essentially comprises oiliness drugs, a solubilizing agent and water and is characterized in that the solubilizing agent is Tween-80 and poloxamer with the mass ratio of the Tween-80 and the poloxamer ranging from 1:4 to 4:1 and the concentration sum of the Tween-80 and the poloxamer in the injection being 0.5 percent to 1.5 percent, wherein, the concentration of the Tween-80 in the injection ranges from 0.2 percent to 0.6 percent; the poloxamer is one or two of poloxamer 68 (F68) and poloxamer 188 (F188) which are used for injection. Meanwhile, the injection of the invention uses the Tween-80 and the poloxamer at the same time as the solubilizing agent, thus the dosage of the Tween-80 can be reduced on the basis of clarifying the injection so as to further reduce the risk of hemolysis caused by the Tween-80.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to injections, especially injections containing oily medicines. Background technique [0002] Many oil-based drugs have poor water solubility, and the injections made of them are often cloudy and unstable in quality. Tween-80, also known as polysorbate-80, is a commonly used solubilizer for injections containing oily drugs to improve the solubility of oily drugs in water, and the usual dosage is 0.5% to 1%. Tween-80 has antihypertensive and slight hemolytic effects, and is often used in intramuscular injections, but should be used with caution in intravenous injections. Studies have shown that when the Tween-80 content in the injection exceeds 0.5%, hemolysis may occur when it is used for intravenous injection, such as Xingnaojing injection containing 0.8% Tween-80. The study by Zhou Yanwen and others found that among 11 kinds of traditional Chinese medicine injections, Xinnaojing ha...

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Problems solved by technology

And adding Tween-80 0.4% concentration just has slight hemolysis, 1.6% hemolysis effect strengthens, and reaches 2% and then causes complete hemolysis (Ma Kongchen, Huang Yongjun, Wang Min, etc. new auxiliary material---poloxamer 108 toxicity and general pharmacology research .Journal of Shenyang Pharmaceutical College, 1993, 10(2): 105); Poloxamer 188 is used as intravenous emulsifier and stabilizer in the concentration range of 0.001 to 10%, using human blood cells to observe at 25°C for more than 18 hours without hemolysis Very safe (Luo Mingsheng, Gao Tianhui. Encyclopedia of Pharmaceutical Excipients. Sichuan Science and Technology Press. 1993: 544); In addition, Poloxamer 188 is also commonly used as an emulsifier for intravenous fat emulsion, but it is solubilized by F68 alone, and the solution is milky white

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