Propofol medium/long-chain injection emulsion and production method thereof

Abstract

The invention relates to a propofol medium / long-chain injection emulsion and a production method thereof. Every 100 ml of the injection emulsion contains 0.7-1.2 g of propofol, 3-7g of refined olive oil, 3-7 g of medium-chain triglyceride, 0.8-1.2 g of egg yolk lecithin, 1.85-2.65 g of glycerol, 0.006-0.02 g of oleic acid, 2-5g of sodium hydroxide and the balance of water for injection. The production method comprises the following steps of 1, vacuumizing production equipment, and introducing nitrogen; 2, preparing a water phase; 3, preparing an oil phase; 4, preparing a primary emulsion; 5, performing homogenization: carrying out high-pressure homogenization for multiple times; and 6, performing emulsion filling and sterilization. According to the invention, soybean oil in a traditional injection emulsion is replaced with the refined olive oil, and many unsaturated acids in the refined olive oil improve the oxidation resistance of the propofol, so that impurities in the injection emulsion have no obvious increase trend, and the drug stability is improved; and the amount of the oleic acid in the injection emulsion is adjusted to be 0.1-0.4 mg, so that the possibility of hemolysis caused by excessive use of the oleic acid or sodium oleate is prevented.

Description

technical field [0001] The invention relates to the field of pharmaceutical production, in particular to a medium / long chain injection emulsion of propofol and a production method thereof. Background technique [0002] Propofol, whose chemical name is 2,6 diisopropylphenol, is a new type of alkylbenzene intravenous anesthetic, which can be used for rapid induction of anesthesia or maintenance of anesthesia, induction of anesthesia is fast and smooth, and can also be used as a surgical and diagnostic procedure sedative effect in. [0003] In 1995, a new type of medium / long chain fat emulsion containing 1% propofol produced by B. Braun Melsungen AG, Melsungen, Germany was applied clinically in Europe and Japan. Its oil phase was composed of 50% medium Chain triglyceride (MCT) and 50% LCT composition, studies have shown that LCT / MCT-propofol fat emulsion does not change the pharmacokinetics and efficacy of propofol in vivo, but significantly reduces the occurrence of injection...

AI Technical Summary

Problems solved by technology

No stabilizers are added to the prescription, and within 24 months of validity, blood levels of phosphatidylcholine, lysophosphatidylethanolamine, impurity I (4,4-bis(2,6-diisopropylphenol)), impurity II (2,6-diisopropyl-1,4-benzoquinone) and total impurities tend to increase significantly, and adverse drug reactions will also increase significantly

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