Preparation of amorphous cefuroxime axetil nanoparticles by controlled nanoprecipitation method without surfactants.
Amorphous nanoparticles of cefuroxime axetil (CFA), a poorly water-soluble drug, were produced by the controlled nanoprecipitation method without any surfactants at room temperature. The influence of the operation parameters, such as the types of solvent and anti-solvent, the stirring speed, the solvent/anti-solvent (S/AS) volume ratio, the drug concentration and the precipitation temperature, were experimentally investigated. The results indicated that increasing the stirring speed and the S/AS volume, decreasing the drug concentration and the temperature favored to decrease the particle size from 700 to 900 nm to approximately 300 nm. The XRD analyses confirmed that the as-prepared CFA was amorphous nanoparticles. Furthermore, the amorphous CFA nanoparticles exhibited significantly enhanced dissolution property when compared to the commercial spray-dried product. The results demonstrated that the controlled nanoprecipitation method is a direct and feasible technology which could be utilized for preparation of the poorly water-soluble pharmaceutical nanoparticles.
Zhang
Ji-Yao
JY
Sin-China Nano Technology Center, Key Lab for Nanomaterials, Ministry of Education, Beijing University of Chemical Technology, Beijing 100029, PR China.
Shen
Zhi-Gang
ZG
Zhong
Jie
J
Hu
Ting-Ting
TT
Chen
Jian-Feng
JF
Ma
Zhong-Qing
ZQ
Yun
Jimmy
J
D002152:Calorimetry, Differential Scanning; D002444:Cefuroxime / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D013501:Surface-Active Agents / Q000737:chemistry; D013696:Temperature; D014961:X-Ray Diffraction
D012997:Solvents; D013501:Surface-Active Agents; D002444:Cefuroxime; C040738:cefuroxime axetil