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Faropenem sodium and tablet thereof

A technology of faropenem sodium and sodium hydroxide, applied in the pharmaceutical field, can solve the problems of unstable temperature, increased impurities and the like

Inactive Publication Date: 2013-03-13
SUZHOU ERYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the faropenem sodium stability test, the samples were placed at 40°C and 60°C for 5 days and 10 days, and the impurities increased a lot, suggesting that the samples were unstable to temperature and should be stored at low temperature

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1: Preparation of Faropenem Sodium

[0016] Put (R)-tetrahydrofuran-2-thiocarboxylic acid in a 3L reaction flask, add 1mol / L sodium hydroxide solution (1.5L), adjust the pH to 9-10, add 4AA (287 g) acetone solution dropwise at 0°C (1L), after dropping, adjust the pH value to about 8 with 1 mol / L sodium hydroxide, react at room temperature for 2 hours, add 500 ml of water to dilute, extract with ethyl acetate (600 ml×3), combine the organic layers, and wash with 5% Wash with sodium bicarbonate solution (300ml×2) and water (300ml×2), dry over anhydrous sodium sulfate, filter, and concentrate the filtrate to obtain product 1;

[0017] Mix product 1, triethylamine (170 g, 1.7 mol) and dichloromethane (1.5 L), add allyl monooxalyl chloride (250 g, 1.7 mol) dropwise at 0°C, react at the same temperature for 2 hours after dropping, add water ( 1L), dilute with dichloromethane (500 ml×4), combine the organic layers, wash with water (300 ml×2) and 5% sodium bicarbonate...

Embodiment 2

[0020] Example 2: Preparation of Faropenem Sodium Tablets

[0021] The faropenem sodium was pulverized through a 100-mesh sieve, and the mannitol, sodium starch glycolate, stearyl alcohol, hypromellose and magnesium stearate were respectively passed through a 80-mesh sieve for later use. Accurately weigh the prescribed amount of raw material (183.5 g), mannitol (10 g), sodium starch glycolate (5.5 g), stearyl alcohol (20 g), potassium hydroxypropyl cellulose (30 g) and mix evenly, 5 Appropriate amount of %PVP65% ethanol solution is made into soft material, granulated with 18 mesh, dried at 40°C, granulated with 18 mesh sieve, added with prescribed amount of magnesium stearate (1g) and mixed evenly. The main drug content of the granules is determined, the weight of the tablet is determined, and the tablet is compressed by a tablet machine. Measure the difference in tablet weight, inspect the quality, and pack it.

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PUM

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Abstract

The invention provides faropenem sodium and a preparation method thereof. The preparation method comprises the steps of: (1) putting (R)-tetrahydrofuran-2-thionocarboxylic acid in a reaction bulb, adding 1 mol / L sodium hydroxide solution to regulate the pH to 9-10, dripping 4AA acetone solution at 0 DEG C, regulating the pH to about 8 through 1 mol / L sodium hydroxide after dripping the acetone solution, reacting at room temperature, and extracting to obtain a product 1; (2) mixing the product 1 with triethylamine and dichloromethane, dripping oxalyl chloride allyl ester at 0 DEG C, reacting at the same temperature after dripping the oxalyl chloride allyl ester, and extracting to obtain a light yellow oily product 2; (3) dissolving the product 2 in dimethylbenzene, adding hydroquinone and triethyl phosphate, heating and refluxing, and extracting to obtain a product 3; and (4) dissolving the product 3 in acetonitrile, adding 0.1 mol / L hydrochloric acid at room temperature, stirring to react, adding saturated sodium bicarbonate solution, distilling to remove the organic solvent, extracting and recrystallizing to obtain a pure faropenem sodium product. The invention further provides a tablet of faropenem sodium.

Description

technical field [0001] The invention belongs to the field of pharmacy. Specifically, the invention relates to faropenem sodium and a preparation method thereof, and also relates to faropenem sodium tablets. Background technique [0002] Faropenem is an atypical β-lactam antibiotic, which is a derivative of penems. Two types of compounds, carbapenems and penems, have attracted great interest. Penems have more unique advantages. Currently, five penem derivatives are under development, and faropenem is convenient. is one of them. In addition to being weak against Pseudomonas aeruginosa, it has a broad antibacterial spectrum and is particularly effective against anaerobic bacteria, which is better than carbapenem antibiotics. It shows broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive bacteria and Gram-negative bacteria, especially against drug-resistant Staphylococcus, Enterococcus and other Gram-positive bacteria and Bacteroides and other anaer...

Claims

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Application Information

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IPC IPC(8): C07D499/893C07D499/16A61K9/20A61K31/431A61P31/04
Inventor 陆夕明陈洋洋洪志娟王宁
Owner SUZHOU ERYE PHARMA CO LTD
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