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Method for preparing norfloxacin capsule

The technology of norfloxacin and capsules is applied in the field of preparation of norfloxacin capsules, which can solve the problems of low oral bioavailability, insoluble norfloxacin in water, unstable properties, etc. Enhanced stability and fast release effect

Inactive Publication Date: 2009-08-12
WUHAN POLYTECHNIC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] But norfloxacin is insoluble in water, and oral bioavailability is low (about 50%), and taste is bitter, and property is also unstable, and can oxidize and decompose when meeting light

Method used

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  • Method for preparing norfloxacin capsule
  • Method for preparing norfloxacin capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] ①Take norfloxacin and β-cyclodextrin (norfloxacin: β-cyclodextrin = 1:1mol / mol) in a mortar and mix well, then add water to grind into a paste, and keep grinding For 6 hours, the temperature was controlled at 30°C until the inclusion complex of norfloxacin β-cyclodextrin was formed. ② Spread the clathrate flat, and bake it in an oven at 60°C for 7-8 hours until it is completely dry. ③ pulverize the dried medicine, pass through an 80-mesh sieve to granulate, and dry at 60°C until the water content is below 9%. ④ Determine the content of norfloxacin, fill it into No. 0 empty capsules after conversion, so that each capsule contains 0.1 g of norfloxacin, and finally pack it.

[0018] The inclusion rate is 70%. The cumulative dissolution rate within 5 minutes was 99.3%.

Embodiment 2

[0020] ①Take norfloxacin and β-cyclodextrin (norfloxacin: β-cyclodextrin = 1:1mol / mol) in a mortar and mix well, then add water to grind into a paste, and keep grinding For 10 hours, the temperature was controlled at 20-25°C until the inclusion complex of norfloxacin β-cyclodextrin was formed. ② Spread the clathrate flat, place it in a decompression drying oven at 50°C for vacuum drying, and bake for 3 to 4 hours until it is completely dry. ③ pulverize the dried medicine, pass through an 80-mesh sieve to granulate, and place in a decompression drying oven at a temperature of 50° C. under vacuum (2 × 10 4 ~3×10 4 Pa), dried to below 9% moisture. ④ Determine the content of norfloxacin, fill it into No. 0 empty capsules after conversion, so that each capsule contains 0.1 g of norfloxacin, and finally pack it.

[0021] The inclusion rate is 84%. The cumulative dissolution rate within 5 minutes was 99.5%.

Embodiment 3

[0023] ①Take norfloxacin and β-cyclodextrin (norfloxacin: β-cyclodextrin = 1:1mol / mol) in a mortar and mix well, then add water to grind into a paste, and keep grinding For 10 hours, the temperature was controlled at 30° C. until the inclusion complex of norfloxacin β-cyclodextrin was formed. ② Spread the clathrate flat, and place it in an oven at 60°C to dry completely. ③ pulverize the dried medicine, pass through an 80-mesh sieve to granulate, and dry at 60°C until the water content is below 9%. ④ Determine the content of norfloxacin, fill it into No. 0 empty capsules after conversion, so that each capsule contains 0.1 g of norfloxacin, and finally pack it.

[0024] The inclusion rate is 74%. The cumulative dissolution rate within 5 minutes was 99.2%.

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Abstract

The invention relates to a method for preparing norfloxacin capsules, which comprises the following steps: (1) evenly stirring norfloxacin and beta-cyclodextrin by the substance ratio of norfloxacin to Beta-cyclodextrin being 1:1, then, adding water and evenly grinding the mixture into paste for 6 to 10 hours at the temperature of 20 to 35 DEG C until the norfloxacin / Beta-cyclodextrin inclusion compound is formed; (2) tiling and drying the inclusion compound at the temperature of 45 to 60 DEG C; (3) pulverizing the dried inclusion compound, granulating the ground medicine through a 80-mesh sieve and drying at the temperature of 45 to 60 DEG C until the water content is lower than 9%; and (4) measuring the norfloxacin content of the granules, converting and filling a No.0 empty capsule with the granules to ensure that each granule contains 0.1g of norfloxacin, and finally packaging to obtain the norfloxacin capsules. The product of the invention has good water-solubility and improves the bioavailability and the stability.

Description

technical field [0001] The invention relates to a preparation method of norfloxacin capsules. Background technique [0002] Norfloxacin is a fluoroquinolone antibacterial drug with broad-spectrum antibacterial effect, especially high antibacterial activity against aerobic Gram-negative bacilli, and has good antibacterial effect on the following bacteria in vitro: most bacteria of Enterobacteriaceae, including citrate Acidobacterium, Enterobacter cloacae, Enterobacter aerogenes, Escherichia coli, Klebsiella, Proteus, Salmonella, Shigella, Vibrio, Yersinia Wait. Norfloxacin also has antibacterial activity against multidrug-resistant bacteria in vitro. It also has good antibacterial effect on penicillin-resistant Neisseria gonorrhoeae, Haemophilus influenzae and Moraxella catarrhalis. Norfloxacin is a fungicide that inhibits DNA synthesis and replication by acting on the A subunit of bacterial DNA helicase, leading to bacterial death. It is suitable for urinary tract infect...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/496A61K47/40A61P31/04
Inventor 樊少静郝清华于平平王少华
Owner WUHAN POLYTECHNIC
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