Preparation And Pharmacodynamics Reserch Of Florfenicol-PEG6000 Solid Dispersion

Florfenicol is a special broad-spectrum antibacterial for animals. Its configuration is similar with the thiamphenicol, but its activity, antibacterial spectrum and side effect are more excellent than that of thiamphenicol, and its antibacterial ability is more 10 times as thiamphenicol. Florfenicol was a broad-spectrum zoic antibiotic opened out and developed by American Schering-Plough Company in the evening of 1980's, and it was one of the best zoic antibiotics at the present time in the world. Florfenicol was broadly used in the killing and inhibiting of the multitudinous Galan's positive and negative bacteria and the microorganism with the tolerance of the thiamphenicol.Solid decentralization technology is a new technology that a solid is spreaded around in another solid. Usually, a drug is decentralized in another water-solubility material or in another no water-solubility and intestine-solubility materials by a molecule, pastern, crystallite and amorphism state, becoming a solid dispersion. The solid dispersion is a molecule decentralization system that is formed by a no water-solubility druggery, for the improving of the dissoluble performance of the druggery and the increasing of the pharmic dissoluble speed and absorbing speed in intestine tract, consequently for the improving of the biologic utilization of the druggery.Now, the marketing dosage forms of the florfenicol have the injection, the premix and the planting beyond the sea, but still not have the dosage forms of the solid decentralization. Along with the development of the stockbreeding, the variety and the quality of the animal drugs have strictly been controlled. It must be carried through to develop and exploit the new variety, new preparation and new dosage form of the animal druggery and to improve the effect and the security of the animal druggery and to reduce the drug residua. At the same time, following the rapid development of the preparation science and the gradually increasing of the drug variety, only using of the preparations generated by the old preparation technology often can not meet the clinical demand. Therefore, we shall try hard to apply the new craftworks and the newtechniques in the manufacture of the preparation by the experiment and to develop and exploit the florfenicol solid dispersion, for the meeting of the clinical demand of the veterinary, the reducing of the drug dosage and the decreasing of the drug residua.The florfenicol-PEG6000 solid dispersion was manufactured by the fusing in this experiment. The dispersing state of the florfenicol-PEG6000 solid dispersion was identified by the differential scanning calorimetery, the X-ray diffraction and infrared spectrum. The results indicated that after the solid dispersion was made by the florfenicol and the PEG6000 by using the solid dispersing technique, the crystal model of the florfenicol with the carrier had formed a new substance posture, and the primary crystal state had translated into the molecule or the crystallite, consequently equably dispersing in the carrier.The result of the research of dissolution rate indicated that the PEG6000 had evidently dissoluble effect. The dissoluble curve showed that the dissoluble rate of the florfenicol-PEG6000 solid dispersion (1:9) was rapider in 20 min, its dissoluble rate were 76.8% in 20 min and 93.7% in 45 min. But the dissoluble rate of the physical compound of the florfenicol and the PEG6000 (1:9) were 20.5% in 20 min and 41.8% in 45 min. The water-solubility of the florfenicol is very bad.The curative effect of the florfenicol-PEG6000 solid dispersion (1:9) on the avian colibacillosis was conducted in this experiment compared with the florfenicol powder. The result of this research showed that the curative effect of the high, middle and low dosage groups of the florfenicol-PEG6000 solid dispersion (1:9) and the control of the florfenicol on the avian colibacillosis were all higher. Thereinto, the curative effect of the high and middle dosage groups were best (the protecting rate and available rate were 100%, the curative rate were 95.5% and 90.9%), but there was significantly different between the high and middle dosage groups. The available rate of the low dosage group was significantly higher compared with the control, indicating that the curative effect of the florfenicol-PEG6000 solid dispersion (1:9) on the avian colibacillosis was very good.