Quality evaluation and bioequivalence study of posaconazole enteric-coated tablets

WANG Hua-wei; SUI Xin; WU Xiu-jun; CAO Ying; CHEN Lu; LI Xiao-bin; LI Mei-ye; GE Yu-xin; WANG Wen-ping

doi:10.20251/j.cnki.1003-3734.2025.08.009

Abstract：Objective:To compare the quality of domestic and original posaconazole enteric-coated tablets and investigate whether there are quality and bioavailability differences between the two preparations.Methods:The quality standards of posaconazole enteric-coated tablets produced by the two manufacturers were compared,and the appearance,UV spectrum,HPLC chromatogram,related substances,water content,dissolution rate,content uniformity,content and microbial limit were compared.The test preparation was domestic posaconazole enteric-coated tablets(100 mg),and the reference preparation was the original posaconazole enteric-coated tablets(100 mg).Human bioequivalence tests were carried out under fasting and fed conditions,respectively.Results:The impurity control of related substances in domestic posaconazole enteric-coated tablets was stricter than that of the reference preparation.Other indicators such as appearance,moisture content,content uniformity,content and microbial limit met the quality standards,and there was no significant difference between domestic and original products.In the bioequivalence study,the 90％confidence intervals of the geometric mean ratios of Cmax and AUC of domestic posaconazole enteric-coated tablets to the original preparation were within the acceptable range of 80％～125％under fasting and fed conditions,which could be judged as bioequivalent by statistical analysis.Conclusion:The qualities of domestic and original posaconazole enteric-coated tablets are both within the limit,but domestic posaconazole enteric-coated tablets are superior to the original tablets in terms of related substances.Bioequivalence studies in human have shown that domestic and originator posaconazole enteric-coated tablets are bioequivalent.