Studies On The Preparation And Characterization Of Florfenicol Solid Dispersion

Florfenicol,which is the chloromycetin drug,is a kind of veterinary antibacterial drug.This drug acts as antimicrobials has a broad spectrum of antibacterial activity against gram-negative bacteria(G-)and gram-positive bacteria(G+).Due to its poor solubility,resulted in oral dosage of florfenicol are poorly in body and low bioavailability.The methods to increase the solubility of florfenicol at present included many problems,such as harmful by product residues,poor effect of solubilization and so on.In this research,to solve above these problems of florfenicol,it is made into solid dispersion with binary solid dispersion and united preparation method.And it can provide idea for the study of insoluble drugs.Florfenicol solid dispersion was prepared by the different material and different methods.The characterization,quality research and in vivo bioavailability evaluation were carried out to evaluate the advantage of florfenicol.1 Preparation and characterization of florfenicol solid dispersionsolubility and dissolution rate were used as experimental object,by experiment in the hensen solubility parameter,we did the research on the selection of carriers and the preparation.The result showed that the florfenicol solid dispersion was best when we use PVPK30 as the single carrier and spray drying as the prepared method.The combination of PVPK30 and PEG6000 was best with binary solid dispersion,the method also was spray drying.The result of orthogonal experiment indicated that the ratio of PVPK30 to PEG6000 was 1:1,the ratio of carrier to drug was 1:4,the speed of spray drying was 900 m L/h,inlet temperature was 120 ?,the solubility of florfenicol solid dispersion is 4.032 mg/m L.Its solubility was 3.324 times higher than florfenicol.Meanwhile,we used the methods of UV detection,infrared spectrum and differential scanning calorimetry to identify the florfenicol,solid dispersion,mixture and carriers.2 The quality research of florfenicol solid dispersionIn vitro dissolution test results showed that the dissolution rate of solid dispersion was accelerated in the water,and the dissolution rate reached 98.823% in 30 min,which was higher than the dissolution rate of 19.645% of florfenicol at this time.,we can predicted that the bioavailability of florfenicol had increased based on the theory of Noyes-Whitney.The results of stability test and long-term retention test showed that the solid dispersion should be kept in a dry environment.For three months,the solubility and appearance of the solid dispersion of flofenicol were almost unchanged and the properties were stable.3 The prescription dismantlement study of florfenicol solid dispersionE.coli as the representative of G-and staphylococcus aureus as the representative of G+ to investigate the bacteriostasis of florfenicol solid dispersion.The result showed that the antibacterial effect of solid dispersion is obviously higher than that of the florfenicol,which indicates that the bioavailability can improve when the solubility and dissolution of the solid dispersion were increased.Investigated the plasma concentration of binary solid dispersion used mice,the experimental results showed that,compared with florfenicolthe,the plasma concentration of solid dispersion was significantly increased,Cmax was shortened greatly.It can indicated that not only the solubility of florfenicol was increased,but also the bioavailability of florfenicol was enhanced when the florfenicol was made into solid dispersion.