Preparation And Performance Characterisation Of Micronized Indissolvable Drug

The micronized or nanosized drug has a lot of advantages, such as improved dissolution rate, higher bioavailability, lower side effect, drug targeting or breakthrough through biology obstruction and so on. Therefore, the development of the micronization technology becomes an important research direction in modern pharmacology study. In this dissertation, a novel preparation method of irbesartan, which was prepared by antisolvent recrystallization. On the basis of previous research, the micronized CFA was prepared by antisolvent precipitation, then the stability, in vitro and in vivo antibacterial properties of drug and tablet dissolution were investigated as well.In this work, the optimum solvent-antisolvent system was determined according to the experiments results of various solvent systems. The factors affecting the particle size, including the concentration of the solution, the volume ratio of solvent to the antisolvent and the stirring speed were investigated. The results in beaker demonstrated that methanol/deionised (DI) water was the suitable system to obtain ultra-fine particles. The optimum micronization conditions were experimentally determined as follows: irbesartan concentration of0.01g/mL, system temperature of15℃, solution/anti-solvent ratio of1:20, stirring speed of1000rpm and oven drying. The as-prepared particles had a particle size distribution of1～2μm. IR spectra indicated that the micronized IBS powder had the same chemical compositions as those of the crude drug. XRD analyses revealed that the product was amorphous while the crude drug was crystalline.In addition, micronized amorphous cefuroxime axetil (CFA) was prepared by antisolvent recrystallization under a high gravity environment. The stability experiment results showed that the crystal form of micronized CFA would change in high humid and high temperature environment. More agglomeration was easily formed as well.The results of in vivo and in vitro antibacterial tests showed that the micronized CFA has the advantage over the crude drug. The tablets dissolution experiments indicated that the micronized CFA has a dissolution rate with an increase of about10%compared to crude drug in the same dissolution period,...