A kind of injection of dezocine and preparation method thereof

Abstract

The invention discloses an injection of dezocine, which comprises per milliliter: 10.1-25 mg of dezocine, 1-15 mg of sodium chloride, 5-20 mg of lactic acid, 300-450 mg of propylene glycol, sodium hydroxide and the rest The nitrogen saturated water for injection, the consumption of sodium hydroxide is to adopt 30~70 volume % nitrogen saturated water for injection to dissolve dezocine, sodium chloride, lactic acid and propanol to obtain solution 1, then use this sodium hydroxide aqueous solution to adjust the content of solution 1 Dosage for pH to 3.5‑5.0. The injection has good stability and stable quality, and is suitable for long-term storage.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an injection of dezocine and a preparation method thereof. Background technique [0002] Dezocine belongs to a typical opioid alkaloid analgesic, developed by Astra, Sweden. These drugs work by stimulating opioid receptors. Dezocine is less addictive and is suitable for the treatment of moderate to severe pain after surgery, visceral colic and pain in patients with advanced cancer. Due to its good tolerance and safety, dezocine has become a drug with good development prospects in clinical practice. [0003] Dezocine is white or off-white crystalline powder, odorless, soluble in methanol, ethanol or glacial acetic acid, slightly soluble in acetone, ethyl acetate or chloroform, almost insoluble in water, sensitive to high temperature, oxidation and other environments. [0004] The specification of dezocine on the market in China is 1mL: 5mg, and its instruction usag...

AI Technical Summary

Problems solved by technology

Sodium metabisulfite was added to the prescription as an antioxidant, which delayed the degradation of dezocine to a certain extent (degradation product A, RRT=0.4, effectively controlled), but in the study, the inventors found that according to Physicians'desk Reference 1997 published the prescription, low concentration (5mg / ml) dezocine injection can be well prepared, while high concentration dezocine injection (10mg / ml~25mg / ml) can be sterilized by autoclave The high temperature in the process will cause another degradation product B (RRT=1.8) in the preparation product to increase significantly and the increase degree is uncontrollable. The model of the sterilizer, the position of the sample in the sterilizer, the sterilization temperature, Sterilization time has an impact on the increase of degradant B, which can easily cause excessive degradant B in the injection (exceeding the impurity limit stipulated in the drug quality standard of dezocine injection), so it is often used in the preparation process. Sterilization temperature or sterilization time to ensure that the degradation product B of the preparation does not exceed the standard, so that the level of sterility assurance is reduced

Visible, F 0 The increase of the value will inevitably lead to a significant increase in the degradation product B

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