Delafloxacin meglumine freeze-dried preparation used for injection, and preparation method thereof

Abstract

The invention belongs to the technical field of medicine, and more specifically relates to a delafloxacin meglumine freeze-dried preparation used for injection, and a preparation method thereof. The delafloxacin meglumine freeze-dried preparation used for injection is mainly composed of delafloxacin meglumine, meglumine, absolute ethyl alcohol, polyoxyl 15 hydroxystearate, and a pH conditioning agent. According to the preparation method, ethyl alcohol is removed in freezing drying process; the using amount of polyoxyl 15 hydroxystearate is relatively small, so that the safety is high, the potential safety problems of delafloxacin meglumine for injection caused by polyoxyl 15 hydroxystearate are avoided, and clinical application range is widened. The delafloxacin meglumine freeze-dried preparation is a loosened block substance, is rapidly dissolved in water, and is high in redissolving performance, and the quality is stable after long term of storage.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a freeze-dried preparation of delafloxacin meglumine for injection and a preparation method thereof. Background technique [0002] Delafloxacin (English name: delafloxacin) is a new generation of broad-spectrum fluoroquinolone antibacterial drug developed by Rib-X Pharmaceuticals. The results of a double-blind phase II clinical study on 150 cSSSIs hospitalized patients showed that: every 12 hours Intravenous injection of 300 mg and 450 mg of this product for consecutive 5-14 days can cure 97.2% and 92.5% of patients with cSSSIs, and 91.2% in the tigecycline group. The antibacterial activity of this product against quinolone-resistant MRSA bacteria is at least 32 times that of levofloxacin, ciprofloxacin, gatifloxacin, and moxifloxacin (MIC90 of this product≤0.5ug / mL, MIC90 of the above-mentioned other drugs are all greater than 16ug / mL); while the antibacterial act...

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Problems solved by technology

[0003] Chinese patent publication number CN 103705942 A and publication number CN 104958296 A have announced the antimicrobial composition of delafloxacin meglumine for injection, which all utilize the inclusion technology of sulfobutyl ether-β-cyclodextrin to improve the The solubility of lafloxacin in aqueous solution. At present, there are few safety data on the auxiliary material cyclodextrin. This type of auxiliary material has certain hemolytic and carcinogenic properties, and there may be unknown and more serious toxic side effects

[0004] Therefore, if the auxiliary materials commonly used in injections can be used, and the dosage is as small as possible, and the safety cannot be guaranteed such as cyclodextrin, the application range of delafloxacin meglumine for injection can be enlarged. At the same time, the inventor In the actual test, it was found that when the delafloxacin meglumine for injection was diluted with 0.9% sodium chloride solution, its related substances changed significantly, which brought troubles to the clinical preparation of medical staff and brought problems to the use of patients. Security risks

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