Sitafloxacin tablet and preparation method thereof

Abstract

The invention discloses a sitafloxacin tablet, which comprises (i) a medicated micropill with 34-40 mesh grain size and (ii) a tabletting auxiliary material, wherein the medicated micropill is composed of sitafloxacin / pharmaceutically acceptable salt, a micropill auxiliary material, and an ethanol aqueous solution, and the weight ratio between the medicated micropill and the tabletting auxiliary material is 1: (2-5). The invention further relates to the preparation method of the sitafloxacin tablet, which comprises the following steps: using the sitafloxacin / pharmaceutically acceptable salt, the micropill auxiliary material, and the ethanol aqueous solution to prepare a softwood, squeezing out the prepared spheronization medicated micropill, and then, adding the tabletting auxiliary material to the prepared micropill containing sitafloxacin / pharmaceutically acceptable salt and obtaining the sitafloxacin tablet. According to the sitafloxacin tablet, the preparation process is simple and environmentally-friendly, and the prepared tablet is stable and safe. Therefore, safe and effective clinical medicine is ensured.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a sitafloxacin tablet and a preparation method thereof. Background technique [0002] Sitafloxacin (Sitafloxacin) is a broad-spectrum quinolone antibacterial drug developed by Daiichi Sankyo Pharmaceutical Co., Ltd. (Daiichi Sankyo). Quinolones, mycoplasma, and chlamydia all have strong antibacterial activity, and have the advantages of good absorption, high bioavailability, and wide tissue distribution. [0003] Japanese patent JP2231475A first disclosed the chemical structure, pharmaceutical use and preparation method of sitafloxacin. The chemical name of sitafloxacin is 7-[4(S)-amino-6-azaspiro[2,4]heptan-6-yl]-8-chloro-6-fluoro-1-[(1R, 2S)-2-fluorocyclopropyl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, Cas No.: 127254-12-0, has the chemical structure shown in the following formula. Since the compound has a cis (1R,5R)-2-fluorocyclopropylamine group in its chemical stru...

AI Technical Summary

Problems solved by technology

[0005] Studies have found that sitafloxacin is unstable to light, easily decomposes under light, and produces a variety of photodegradation products, which may lead to a decrease in antibacterial activity and adverse reactions. Therefore, it is often necessary to add titanium dioxide, Iron oxide, silicon dioxide and other opacifying agents are used for coating treatment. The sitafloxacin tablets (GRACEVITTABLETS) listed by the original research company Daiichi Sankyo Pharmaceutical Co., Ltd. in Japan have added coating materials such as opacifying agent titanium dioxide to prevent sitafloxacin The photodegradation of Floxacin, this method of preparation through the final coating of the tablet can only alleviate its photodegradation to a certain extent, and increase the production cost and operation difficulty

Ye Hong and others also added 0.1 to 5% sunscreen in the prescription disclosed in Chinese patent application CN 1013732277A, and tried to reduce the exposure of sitafloxacin to light in the pharmaceutical process, so as to enhance the stability of sitafloxacin tablets agent, but the chance of reducing exposure to light during the pharmaceutical process is uncontrollable, so the effect is not obvious

[0006] In addition, Daiichi Sankyo Pharmaceutical Co., Ltd. issued a summary instruction sheet for sitafloxacin ( http: / / www.info.pmda.go.jp ) records that sitafloxacin is almost insoluble in water, releases very slowly in neutral media, and has high solubility under acid or alkaline conditions, but slow release will produce acid and alkali degradation products

And the release rate of sitafloxacin tablets disclosed in the prior art is not ideal, so it is necessary to improve the release rate of sitafloxacin solid preparation

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