Neostigmine mesylate injection and preparation method thereof

Abstract

The invention discloses a neostigmine mesylate injection and a preparation method thereof. The neostigmine mesylate injection comprises 0.05%-0.08% of neostigmine mesylate, 0.7%-0.9% of an isoosmoticadjusting agent, 0.095%-0.25% of a pH adjusting agent and the balance of water for injection. According to the invention, specific auxiliary materials are selected and process steps are reasonably controlled; according to the neostigmine mesylate injection, the product is isotonic, the sterile guarantee level is extremely high; the preparation method is simple, safe, effective and controllable inquality, F0 is larger than 15, the sterile guarantee level SAL is smaller than or equal to 10 <-6 >, the prepared injection is low in impurity level content, the osmotic pressure ratio of the productis 0.9-1.1, the injection still has high stability after being accelerated for 6 months at the temperature of 40 DEG C, all impurities are not obviously increased, and newly-added impurities are not generated.

Description

technical field [0001] The invention relates to the technical field of medicine. More specifically, it relates to a neostigmine methylsulfate injection and a preparation method thereof. Background technique [0002] Neostigmine is a reversible cholinesterase inhibitor, which was first successfully synthesized by Roche Pharmaceuticals in 1931. It mainly exerts a complete cholinergic effect by inhibiting the activity of cholinesterase. , Cardiovascular and bronchial smooth muscle is weak, it can promote gastric contraction and increase gastric acid secretion for gastrointestinal smooth muscle, and promote the peristalsis of small and large intestines, especially colon, so as to prevent intestinal flaccidity and promote intestinal contents to push down. It has a strong excitatory effect on skeletal muscle, but a weaker effect on the central nervous system. Neostigmine bromide is commonly used clinically for oral administration, and neostigmine methosulfate is for injection ad...

AI Technical Summary

Problems solved by technology

Patent CN201610105070.2 discloses a neostigmine methosulfate injection and its preparation method, which is prepared by adding neostigmine methosulfate to water for injection, sterilizing and filtering, and sterilizing at 100°C for 30 minutes, but the method The probability of contamination under the 95% confidence limit of the sterility assurance level is only <0.1%, and the probability of microbial contamination is high

It can be seen that the existing neostigmine methosulfate injection products still have certain deficiencies in controlling the level of impurities to ensure product stability, and in ensuring the level of sterility

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