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%.