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Prulifloxacin composition and preparation method thereof, and synthesis method of raw material drugs

A technology of prulifloxacin and its composition, which is applied in the field of medicine, can solve the problems of affecting the safety of medication, the lack of strictness of pharmaceutical excipients, intestinal stimulation, etc.

Active Publication Date: 2012-07-04
SHANDONG LUOXIN PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The provided prulifloxacin uses talcum powder as a lubricant. However, talc powder has certain pharmacological effects, and it is not very strict to use it as a pharmaceutical excipient.
And talcum powder has been proved to have stimulating effect on the intestinal tract, which further affects the safety of the drug

Method used

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  • Prulifloxacin composition and preparation method thereof, and synthesis method of raw material drugs
  • Prulifloxacin composition and preparation method thereof, and synthesis method of raw material drugs
  • Prulifloxacin composition and preparation method thereof, and synthesis method of raw material drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] prescription

[0099] Prulifloxacin 132.1g

[0100] Lactose 40g

[0101] Hydroxypropyl Cellulose 9.5g

[0102] Magnesium Stearate 2g

[0103] Povidone K30 18g

[0104] Sodium Carboxymethyl Starch 6g (tablet)

[0105] Make 1000 capsules

[0106] Described prulifloxacin can be a commercially available product or can be prepared according to the following method:

[0107] (1) 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazetidin[3,2-a]quinoline-3-carboxylic acid (I )Synthesis:

[0108] With 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazetidin[3,2-a]quinoline-3-carboxylic acid ethyl ester 100g and 645ml of glacial acetic acid, 970ml of concentrated hydrochloric acid, and 640ml of water were reacted at 72°C for 12 hours, concentrated under reduced pressure, diluted with 16.13 times of water, filtered and washed until the pH was neutral, and dried to obtain 88.5g of compound (I). 97.3%, elemental analysis C 12 h 7 f 2 NO 3 S, calculated value C 50.88%, H 2.4...

Embodiment 2

[0118] prescription

[0119] Prulifloxacin 132.1g

[0120] Lactose 40g

[0121] Hydroxypropyl Cellulose 9.5g

[0122] Magnesium Stearate 2g

[0123] Povidone K30 18g

[0124] Sodium Carboxymethyl Starch 6g (tablet)

[0125] Make 1000 capsules

[0126] Described prulifloxacin can be a commercially available product or can be prepared according to the following method:

[0127] (1) 6,7-difluoro 1-methyl-4-oxo-4H-[1,3]thiazetidin[3,2-a]quinoline-3-carboxylic acid (I) Synthesis:

[0128] With 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazetidin[3,2-a]quinoline-3-carboxylic acid ethyl ester 100g and 645ml of glacial acetic acid, 970ml of concentrated hydrochloric acid, and 640ml of water were reacted at 68°C for 12 hours, concentrated under reduced pressure, diluted with 16.13 times of water, filtered and washed until the pH was neutral, and dried to obtain 89.0g of compound (I). 97.8%;

[0129] (2) Synthesis of 5-methyl-4-piperazinemethyl-1,3-dioxolenedione (I...

Embodiment 3

[0138] prescription

[0139] Prulifloxacin 132.1g

[0140] Lactose 40g

[0141] Hydroxypropyl Cellulose 9.5g

[0142] Magnesium Stearate 2g

[0143] Povidone K30 18g

[0144] Sodium Carboxymethyl Starch 6g (tablet)

[0145] Make 1000 capsules

[0146] Described prulifloxacin can be a commercially available product or can be prepared according to the following method:

[0147] (1) 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazetidin[3,2-a]quinoline-3-carboxylic acid (I )Synthesis:

[0148] With 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazetidin[3,2-a]quinoline-3-carboxylic acid ethyl ester 10kg and 64.5L of glacial acetic acid, 9.7L of concentrated hydrochloric acid, and 6.4L of water were reacted at 76°C for 12 hours, concentrated under reduced pressure, diluted with 16.13 times of water, filtered and washed until the pH was neutral, and dried to obtain 8.87kg of compound (I) , yield 97.5%;

[0149] (2) Synthesis of 5-methyl-4-piperazinemethyl-1,3-dioxolenedi...

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Abstract

The invention discloses a Prulifloxacin composition. The composition comprises the following components: 130 to 135 parts of Prulifloxacin, 35 to 45 parts of lactose, 9 to 10 parts of hydroxypropyl cellulose, 1.5 to 2.5 parts of magnesium stearate and 15 to 20 parts of povidone K30. Quality and yield of the Prulifloxacin are greatly improved by adjusting parameters during synthesis, such as addition speed of reactants. The method for preparing the composition comprises the following steps of preparing solution of povidone K30 ethanol; uniformly mixing the Prulifloxacin with the hydroxypropyl cellulose, and crushing the mixture with mechanical crusher; screening, and screening crushed lactose; adding lactose into mixed powder of the Prulifloxacin and the hydroxypropyl cellulose, and uniformly mixing with a three-dimensional mixer; then adding the prepared solution of povidone K30; uniformly mixing, granulating, and straightening granules after drying; and adding the magnesium stearate into the prepared granules and uniformly mixing with the three-dimensional mixer. The composition prepared by the method has advantages of good quality, less disintegration time and high dissolution efficiency.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a prulifloxacin composition, a preparation method thereof, and a synthesis method of a crude drug. Background technique [0002] Infectious diseases are the most common clinical diseases, involving almost all clinical specialties, and are also one of the most common causes of patient death. According to the report of the World Health Organization in 1997, the number of deaths from infectious diseases was as high as 33.3% of the total number of deaths from various causes. Anti-infective drugs are a powerful weapon for human beings to fight against infectious diseases. They are the largest in number, most in variety, and fastest growing, and the market demand for drugs in this area has always been very strong. According to statistics, the sales of anti-infective drugs account for about 15% of the world's drug sales, second only to cardiovascular drugs. In my country, anti-infective drugs ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496C07D513/04A61K9/48A61K9/20A61P31/04
Inventor 李明华刘延珍马红娟
Owner SHANDONG LUOXIN PHARMA GRP CO LTD
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