Ubenimex fat emulsion injection and preparation method thereof

Abstract

The invention discloses a ubenimex fat emulsion injection, comprising ubenimex, oil for injection, emulsifier, stabilizer, isoosmotic adjusting agent and water, wherein, the concentration of the ubenimex is 0.05-10g / ml, the concentration of the oil for injection is 5-30g / ml, the concentration of the emulsifier is 0.8-3.0g / ml, the concentration of the stabilizer is 0.1-2.0g / ml, and the concentration of the isoosmotic adjusting agent is 2-3g / ml. Through measuring, the quality and the appearance of the fat emulsion injection of the invention are uniform, the average particle diameter is about 300nm, and the pH value is 5.0-9.0, thus, the fat emulsion injection can be used for injection. The ubenimex fat emulsion injection has obvious anti-tumor function. According to the characteristics of common fat emulsion injection, the ubenimex fat emulsion injection as an anti-tumor medicine also has the functions of slow releasing, targeting, providing organisms with energy and the like.

Description

technical field [0001] The invention relates to an ubenimex fat emulsion injection and a preparation method thereof, belonging to the field of medical biotechnology. Background technique [0002] At present, effective measures to conquer cancer include surgery, radiotherapy, chemotherapy, etc., but they all have their limitations. For example, radiotherapy and chemotherapy generally have toxic side effects such as killing healthy red and white blood cells, liver and kidney toxicity, and nervous system damage. Therefore, the development of effective anticancer drugs has become a long-term key research topic in the world's medical circles. When the fourth treatment mode of cancer - biological therapy received attention, Ubenimex API and capsules (trade name Baishixin) made a major breakthrough in this field. As a biological response modifier, Ubenimex has It has the characteristics of definite curative effect, clear mechanism of action, extremely low toxicity and convenient a...

AI Technical Summary

Problems solved by technology

[0005] The currently marketed Ubenimex product only has its capsule (Baishixin). As an oral preparation, there are certain limitations because: (1) After the drug is swallowed orally, it must be dissolved in the gastrointestinal tract, It disintegrates, dissolves, absorbs, and then distributes to the whole body with the blood circulation, and finally acts on the affected part to exert a therapeutic effect. However, the water solubility of Ubenimex is very poor. For insoluble drugs, the dissolution rate of the drug is very slow. The absorption process is often limited. Although Ubenimex is well absorbed orally, the adverse reactions of the digestive system caused by chemotherapy increase the difficulty of oral administration, and nausea and vomiting make patients reluctant to take the drug directly

(2) The drug is easily affected by food and needs to be absorbed after the stomach is emptied into the small intestine, and its effect is slow. However, there are various digestive enzymes and enzymes produced by the intestinal flora in the digestive tract, which can make the drug not yet absorbed metabolic inactivation

(3) Ubenimex also has some gastrointestinal adverse reactions

These have caused a lot of inconvenience to patients and doctors, and increased the suffering of patients and medical costs.

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