Transdermal drug delivery system for β-lactam antibiotics
A drug, diethylaminoethyl ester technology, applied in antibacterial drugs, anti-infective drugs, nervous system diseases, etc., can solve the problem of inability to deliver therapeutically effective drug concentrations
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[0072] 6-(2,6-dimethoxybenzamide) penicillin acid-2-diethylaminoethyl ester hydrochloride
[0073] 38 g (0.1 mole) of 6-(2,6-dimethoxybenzamide) penicillinic acid was dissolved in 300 ml of chloroform. 20.6 g of N,N'-dicyclohexylcarbodiimide, 11.7 g of N,N-dimethylaminoethanol and 2 g of 4-dimethylaminopyridine were added to the reaction mixture. The reaction was stirred at room temperature for 10 hours. The solids were removed by filtration. The chloroform layer was washed twice with 5% sodium bicarbonate solution, 100 ml each time, and washed 3 times with water, 100 ml each time. The organic layer was dried over anhydrous sodium sulfate. Sodium sulfate was removed by filtration. To the reaction mixture was added 3.5 g of hydrogen chloride dissolved in 50 ml of diethyl ether with stirring. The solid product was collected by filtration. After drying, 40 g of the hygroscopic product was obtained with a yield of 77.5%. Solubility in water: 50 mg / ml; Elemental analysis: C ...
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