Ornidazole injection and preparation method thereof

Abstract

The invention discloses an ornidazole injection and a preparation method thereof. Mixed liquid of absolute ethyl alcohol and polyethylene glycol-15-hydroxystearate serves as a solvent of the ornidazole injection, wherein the polyethylene glycol-15-hydroxystearate accounts for 6-14% in terms of the mass percentage of the injection. The use of a propylene glycol solvent can be prevented, and the preparation (the injection) is good in stability and good in clinical safety. The invention also discloses a preparation method of the injection; and the preparation process (the preparation method) is simple and easy to implement.

Description

technical field [0001] The invention relates to an ornidazole injection and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Ornidazole (Omidazole) is a drug against anaerobic bacteria and antiprotozoal infection. It is a nitroimidazole derivative without disulfiram-like effect. The antimicrobial effect of ornidazole is through the reduction of the nitro group in its molecule to amino in an anaerobic environment or through the interaction of free radicals with microbial cell components, resulting in the death of microorganisms. It is used for the treatment of anaerobic bacteria, amoeba Various diseases caused by protozoa, giardia, trichomonas, etc., have the advantages of high curative effect, good tolerance, good tissue penetration, wide distribution in the body, etc. It is a substitute for metronidazole and tinidazole. Ornidazole's good anti-oxidative bacteria and anti-protozoal (such as trichomonas, etc.) ...

AI Technical Summary

Problems solved by technology

[0004] (1) The original preparation Tiberal contains a large amount of propylene glycol to keep ornidazole injection stable, and the safe range of propylene glycol is that the dosage does not exceed 25mg / kg per day. Each tube of Tiberal contains about 1.4g of propylene glycol, which is the first in clinical use. Ornidazole is 1g for a single dose, and the specification of Tiberal is 0.5g / cartridge, so two cartridges are needed, that is, propylene glycol is about 2.8g, which is 40mg / kg for a 70kg person, which exceeds the safe range of the human body and has potential safety hazards

[0005] (2) Most of the domestic generic drug preparations use water for injection as the solvent, but the water solubility of ornidazole is not good under neutral conditions. It is basically stable during storage, and the related substances do not exceed the quality standard limit (single impurity does not exceed 0.5%, total impurity does not exceed 1.0%), but ornidazole injection with a pH value of 1.8~2.3 is more irritating to blood vessels. It improves the tolerance of the human body, and at the same time increases the incidence of infusion pain and phlebitis. According to statistics, about 59% of patients with pain and various degrees of phlebitis caused by ornidazole injection (Wang Bo, China Medical Frontiers, 2009, 4(24): 69)

However, the study found that the storage stability of the above-mentioned ornidazole injection at a lower temperature (-10°C to 20°C) is poor, and it is prone to the defect that the visible insoluble particles exceed the standard

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