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The lipid solubility of this product is 5 times larger than tetracycline, 50 times larger than oxytetracycline, the antibacterial spectrum is the same as tetracycline, but the effect is 2 ~ 10 times stronger than the latter. It is still effective against Staphylococcus aureus resistant to tetracycline. The clinical use is the same as tetracycline, mainly used for respiratory tract infections, such as pneumonia, bronchitis and biliary tract infection, etc., oral absorption is fast and complete, distributed throughout the body, and the concentration in cerebrospinal fluid is also high. The drug has strong antibacterial effect and long half-life, so the dose is small and the interval is long. The injection and oral preparation made with its hydrochloride are commonly used in clinic.
Uses of Doxycycline Monohydrate.
Preparation of Doxycycline Monohydrate.
1) Add 100g of hydrogenated salt (α-6-deoxyoxyomycin 5-sulfosalicylate crude product) to 200mL of 70% (v/v) ethanol aqueous solution at 15℃, stir for 10min, then start to add ammonia water, when the pH value reaches 5.8, stop adding ammonia water, then the temperature is 18℃, stir for 10min, until the alkali is dissolved. After filtration, the filtrate is heated to 45℃, held for 30min, cooled to 25℃ for discharging, centrifuge separation, and the first alkaline moisture product 65g is obtained.
2) Take 60g of the moisture product of step 1, add it into 180mL, 60% (v/v) ethanol aqueous solution, add 10% hydrochloric acid to adjust the pH to 3.5, and heat up to 55℃, so that the material is completely dissolved, then add 60g sulfonyl salicylic acid, stir for 10min, and then cool down to 25℃, precipitate the secondary salt, centrifuge and separate. The secondary salt product 85g was obtained.
3) Take 80g of the moisture product obtained in step 2, add it to 240mL of 70% (v/v) ethanol at 15℃, stir thoroughly for 30min, then start to add ammonia water, control the process of adding ammonia water, the temperature does not exceed 18℃, when the pH value reaches 6.0, stop adding ammonia water, after the completion of adding ammonia water, the temperature is 6℃, stir for 10min. After the alkalinity is dissolved and filtered, the filtrate is heated to 45℃, held for 30min, cooled to product precipitation, cooled to 15℃ discharge, centrifugal separation, and 50g of the second alkalinity moisture product is obtained.
4) The moisture of step 3 is dried in a vacuum drying oven at 0.08MPa and 70 degrees to obtain 42g doxycycline monohydrate product with a purity of 98.8%.
Product Methods of Bulk Doxycycline Monohydrate powder.
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