Study On The Micronization Of Ibuprofen

Ibuprofen is a kind of non-steroidal antipyretic,analgesic and anti inflammatory drugs, which was developed in 1960s.It is a kind of water-insoluble drug, as it is hard to dissolve in water, so there is the problem of low absorption,low bioavailability and low effect speed. The application in clinical medicine is limited. To solve this problem, in this research, raw ibuprofen is micronized so as to reduce particle size and increase the specify surface area, which is beneficial to enhance its dissolution and solubility, further to improve the bioavailability.By screening of the micronized preparation technique, the best preparation: put the 250ml conical beaker, adding 150ml poloxamer solution with 2% concentration as the stabilizer, into the ice-water bath at 0-5℃.In conditions of continuous ultrasound, dropping 50ml ibuprofen ethanol solution with 0.04g/ml concentration at 1ml/min uniform dropping rate. when the aqueous solution become turbid, standing for 6 hours at low temperature. With 10min high-speed centrifugation until solid product is completely separated from the aqueous solution, then re-washed and high-speed centrifugation 5min, remove the supernatant solution. Solid product is placed in vacuum drying oven at 50℃,then grounded and sieved by mesh.Through the investigation of the dissolution of different ibuprofen tablets, the results show that the accumulation dissolution rate in various dissolution media of two kinds ibuprofen micronization tablets is much larger than the ibuprofen raw material tablets. The accumulation dissolution rate of tablets that are produced with ibuprofen micronization can reach nearly 80% in a certain period of time. The research of the drug release pattern of ibuprofen micronization sustained-release tablets shows that the drug release pattern is consistent with Higuchi equation.