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Preparation method of gemifloxacin mesylate medicinal composition

A technology of gemifloxacin mesylate and a composition, which is applied in the field of preparation of pharmaceutical compositions, can solve the problems of uneven granulation, many fine powders and the like, and achieves uniform particles, large drug loading, and difference in tablet weight. stable effect

Active Publication Date: 2013-03-06
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In view of the problems of the technologies described above, the purpose of this invention is to provide a method for preparing gemifloxacin mesylate granules in combination with wet pre-granulation and fluidized bed granulation. The uneven granulation caused by the wall, the technical difficulties of uneven granulation and excessive fine powder due to electrostatic adsorption of materials in the fluidized bed granulation process; A preparation method of gemifloxacin acid preparation, the gemifloxacin particles prepared by the method are uniform, and the tablet weight difference is stable

Method used

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  • Preparation method of gemifloxacin mesylate medicinal composition
  • Preparation method of gemifloxacin mesylate medicinal composition
  • Preparation method of gemifloxacin mesylate medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The three methods of wet granulation, fluidized bed granulation and wet pre-granulation combined with fluidized bed granulation were compared, as follows:

[0046] Scheme A: wet granulation steps:

[0047]Add 426.39g of gemifloxacin mesylate to the granulation equipment together with 49.01g of microcrystalline cellulose and 26.00g of cross-linked polyvinylpyrrolidone after crushing and sieving, stir and mix, and add 14.70g of polyvinylpyrrolidone 5% w / w Aqueous solution of 80-120 r / min stirring and 150-200 r / min shearing force to make granules, after drying, granulate and add 3.90g magnesium stearate to mix and tablet , weighing.

[0048] Scheme B: Fluidized bed granulation steps:

[0049] Put 426.39g of gemifloxacin mesylate into the fluidized bed after crushing and sieving treatment, together with 49.01g of microcrystalline cellulose and 26.00g of cross-linked polyvinylpyrrolidone, and mix with the bottom air blower, and use 0.80mm-1.2 mm spray gun into 14.70g poly...

Embodiment 2

[0061] Prepare gemifloxacin mesylate tablets according to the method of scheme C wet pre-granulation in Example 1 combined with fluidized bed granulation, the type of binder used is specifically shown in Table 3, wherein the wet pre-granulation step and fluidized bed The type of binder used in the granulation step was consistent.

[0062] The influence of different binders (polyvinylpyrrolidone, hydroxypropylmethylcellulose, sodium carboxymethylcellulose, sodium carboxymethylstarch) on wet pregranulation combined with fluidized bed granulation is shown in Table 3 below. Show:

[0063] Table 3: Effect of different binders on wet pre-granulation combined with fluidized bed granulation process

[0064]

[0065] It can be seen from Table 3 that in the process of wet pre-granulation combined with fluidized bed granulation, the gemifloxacin mesylate granules prepared by selecting polyvinylpyrrolidone and hydroxypropyl methylcellulose as binders have good uniformity and can be c...

Embodiment 3

[0067] Wet pre-granulation: Put 426.39g of gemifloxacin mesylate through a 60-mesh sieve and 49.01g of microcrystalline cellulose for pre-mixing in a high-shear one-step granulator, and then add 150ml of aqueous solution of polyvinylpyrrolidone in groups A-E Perform primary granulation. Granules are made under two forces of 80-120 rpm stirring and 150-200 rpm shearing. The time of wet pre-granulation is 20-240 seconds, the temperature is 60°C, and the pressure is 1.5p.

[0068] Fluidized bed re-granulation: Add the material obtained by wet pre-granulation into the fluidized bed, and spray 150ml of aqueous solution of polyvinylpyrrolidone in groups A-E respectively under the state of atomization, and control the injection speed to 1-100g / min, atomize The pressure is 0.4-1.0mbar, the temperature of the material is 30-60°C, then granulate and dry, add 26.00g cross-linked polyvinylpyrrolidone and 3.90g magnesium stearate to the dried granules, mix well, press into tablets, and wei...

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Abstract

The invention provides a preparation method of gemifloxacin mesylate medicinal composition with large medicine loading capacity. The preparation method comprises a wet-method grain pre-manufacturing step and a fluidized bed grain manufacturing step. According to the preparation method of the gemifloxacin mesylate medicinal composition, disclosed by the invention, the wet-method grain pre-manufacturing step and the fluidized bed grain manufacturing step are combined, a suitable amount of disintegrating agents, and lubricant and the like are externally added after grains are dried and finished so that the gemifloxacin mesylate medicinal composition is pressed into tablets. The gemifloxacin mesylate tablets obtained by the preparation method disclosed by the invention avoids adverse factors of weight variation of pressed tablets influenced by grain unevenness generated because materials are adhered on the wall of a granulator during a wet-method grain manufacturing step or the fluidized bed grain manufacturing step, low grain yield after the materials are adhered on the wall of a granulator, and the like.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, in particular, the invention relates to a preparation method of a pharmaceutical composition containing gemifloxacin mesylate. Background technique [0002] Gemifioxacin mesylate is 7-[3-(aminomethyl)-4-(methoxyimino)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4- Oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate, its structural formula is as follows: [0003] [0004] Gemifloxacin mesylate (domestic product name: Jisuxing) is a fourth-generation fluoroquinolone antibacterial new drug jointly developed by South Korean LG Company and British GSK Company. It was approved by FDA in April 2003 and launched in the United States in July 2006. Approved by SFDA for listing in China. As a new type of oral broad-spectrum fluoroquinolone antibiotics, gemifloxacin mesylate has a good effect on the common pathogens of respiratory tract infection, Streptococcus pneumoniae, Haemophilus influ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/4375A61P31/04
Inventor 马小玲李菁
Owner LIVZON PHARM GRP INC
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