What is Mupirocin?

Sep 28,2021

Mupirocin, also known as pseudomonas acid A, is an ideal skin surface antibacterial preparation. It was marketed by GlaxoSmithKline under the trade name of "Bactroban" in 1985 . The US FDA approved the drug to be used in the United States in 1987, and my country approved the production and sale of the drug in 1993 by Sino-American Schick Pharmaceuticals. Mupirocin is mainly used to prevent and treat skin bacterial infections caused by gram-positive cocci, such as impetigo, boils, folliculitis and other primary skin infections, as well as eczema co-infection, ulcer co-infection, and trauma co-infection Infection and other secondary skin infections. The main mechanism of mupirocin's antibacterial effect is to inhibit protein synthesis in bacteria.

Purification method

A purification method of mupirocin specifically includes the following steps:

(1) After 2275ug/ml mupirocin fermentation broth 60L is adjusted to pH 2.5 with dilute hydrochloric acid, the water-soluble protein, pigment and other macromolecular substances in the mupirocin fermentation broth are removed by plate and frame filtration to obtain mupirocin Luoxing bacteria residue; after weighing the bacteria residue, add 5% ammonium bicarbonate solution, the volume (ml) is 1.5 times of the bacteria residue weight (g), stir for 4 hours and then carry out plate and frame filtration to remove further Pigment and other impurities, 40L of mupirocin filtrate was obtained, with a content of 3345.72ug/ml;

(2) Concentrate the mupirocin filtrate by nanofiltration once, and concentrate until the content of mupirocin in the concentrate is 40g/L;

(3) Adjust the pH of the concentrated solution to 3.0 with dilute hydrochloric acid for one crystallization, and obtain 115.34 g of crude mupirocin after centrifugation;

(4) Dissolve the crude mupirocin with water to 10g/L, add 2% sodium chloride, adjust the pH to 6.0, and load the column at a flow rate of 1 times the bed. The chromatographic column is HZ-806 from Shanghai Huazhen , After washing the column with water (the volume is 3 times the column bed), desorb with 0.025% ammonium bicarbonate after washing, collect the desorbed liquid with chromatographic purity greater than 90%, containing 103.00g of mupirocin;

(5) Concentrate the qualified mupirocin desorption liquid by second nanofiltration, and concentrate it until the content of mupirocin in the concentrated liquid is 40g/L;

(6) Adjust the pH of the concentrated solution to 4.0 with dilute hydrochloric acid for secondary crystallization, and obtain the tide crystals of mupirocin after centrifugation;

(7) Dry the wet crystals in a vacuum at a temperature of 55° C. and a vacuum of -0.092 MPa to obtain 88.61 g of a finished product of mupirocin with a chromatographic purity of 99.4%.

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Mupirocin

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