Sitafloxacin tablet and preparation method thereof

A technology of sitafloxacin and tablets, which is applied in the field of pharmacy, can solve problems such as unsatisfactory release rate of sitafloxacin tablets, increase of production cost and operation difficulty, instability of sitafloxacin to light, etc., to avoid Release unqualified, improve bioavailability, avoid photo-instability effects

Inactive Publication Date: 2013-05-01
YANGTZE RIVER PHARM GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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  • Sitafloxacin tablet and preparation method thereof
  • Sitafloxacin tablet and preparation method thereof
  • Sitafloxacin tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 sitafloxacin tablet

[0030] Prescription 1:

[0031] (1) Pill core prescription:

[0032] Names of raw materials and auxiliary materials

Dosage

Sitafloxacin hydrochloride

50g (calculated as sitafloxacin)

sucrose

35g

Sodium carboxymethyl starch

5g

Povidone

10g

20% ethanol solution

100g

Make 1000 capsules

[0033] (2) Tablet core prescription

[0034] material name

Dosage

microcrystalline cellulose

250g

lactose

150g

Made into 1000 pieces

[0035] Preparation Process

[0036] (1) Preparation of sitafloxacin pellets: Weigh the prescribed amount of sitafloxacin main drug and auxiliary materials and mix them uniformly according to the principle of equal increase, add the prescribed amount of 20% ethanol solution, stir well and put into double Screw extruder, the orifice diameter is 0.4-0.5mm; the extruded strip-shaped m...

Embodiment 2

[0038] Embodiment 2 sitafloxacin tablet

[0039] Prescription 2:

[0040] (1) Pill core prescription:

[0041] Names of raw materials and auxiliary materials

Dosage

Sitafloxacin anhydrous

50g (calculated as sitafloxacin)

lactose

35g

Croscarmellose Sodium

5g

Povidone

10g

30% ethanol solution

100g

Make 1000 capsules

[0042] (2) Tablet core prescription

[0043] material name

Dosage

microcrystalline cellulose

500g

Made into 1000 pieces

[0044] Preparation Process

[0045](1) Preparation of sitafloxacin pellets: Weigh the prescribed amount of sitafloxacin main drug and auxiliary materials and mix evenly according to the principle of equal increase, add the prescribed amount of 30% ethanol solution, stir well and put into double Screw extruder, the orifice diameter is 0.4-0.5mm; the extruded strip-shaped material is collected in the spheronizer, an...

Embodiment 3

[0047] Embodiment 3 sitafloxacin tablet

[0048] Prescription 3:

[0049] (1) Pill core prescription:

[0050] Names of raw materials and auxiliary materials

Dosage

Sitafloxacin anhydrous

50g (calculated as sitafloxacin)

Mannitol

35g

Sodium carboxymethyl starch

5g

Hypromellose

10g

25% ethanol solution

100g

Make 1000 capsules

[0051] (2) Tablet core prescription

[0052] material name

Dosage

microcrystalline cellulose

350g

lactose

100g

Made into 1000 pieces

[0053] Preparation Process

[0054] (1) Preparation of sitafloxacin pellets: Weigh the prescribed amount of sitafloxacin main drug and auxiliary materials and mix them uniformly according to the principle of equal increase, add the prescribed amount of 25% ethanol solution, stir well and put into double Screw extruder, the orifice diameter is 0.4-0.5mm; the extruded strip-shaped ...

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4709A61K47/38A61K47/36A61K47/32A61P31/04
Inventor 陈令武包玉胜张海波梁慧兴路显锋李浩冬尹必喜
Owner YANGTZE RIVER PHARM GRP CO LTD
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