中成药2026，Vol.48Issue(5)：1466-1472,7.DOI:10.3969/j.issn.1001-1528.2026.05.006
高良姜素纳米混悬剂制备及其体内药动学研究
Preparation and in vivo pharmacokinetics of galangin nanosuspensions
摘要
Abstract
AIM To prepare galangin nanosuspensions,and to investigate their in vivo pharmacokinetics.METHODS The nanosuspensions were prepared with glycyrrhizic acid as a stabilizer.With galangin-glycyrrhizic acid ratio,aqueous volume,homogenization pressure and homogenization frequency as influencing factors,particle size and PDI as evaluation indices,the formulation process was optimized by single factor test.The morphology was observed under scanning electron microscope,after which the solubility and dissolution rate were determined,the crystal form was analyzed by X-ray powder diffraction,and the stability was evaluated.Eighteen rats were randomly assigned into three groups and given intragastric administration of the 0.5％CMC-Na suspensions of galangin,physical mixture and galangin nanosuspensions(100 mg/kg),respectively,after which blood collection was made at 0.25,0.5,0.75,1.5,2,3,6,8,10,12 h,HPLC-MS/MS was adopted in the plasma concentration determination of galangin,and main pharmacokinetic parameters were calculated.RESULTS The optimal conditions were determined to be 50 mg for galangin consumption,2.0∶1 for galangin-glycyrrhizic acid ratio,30 mL for aqueous volume,90 MPa for homogenization pressure and 8 times for homogenization frequency,the average particle size,PDI and Zeta potential were(316.77±24.19)nm,0.162±0.018 and-(23.27±1.14)mV,respectively.The oval or near-spherical nanosuspensions obviously enhance the solubility of raw medicine,whose accumulative dissolution rate reached 82.79％within 16 h.The crystal peaks of raw medicine existed in the nanosuspensions,whose intensity was lower than that of physical mixture,along with good stability within six months.Compared with raw medicine and physical mixture,the nanosuspensions displayed shortened tmax(P＜0.05)and increased Cmax,AUC0-t,AUC0-∞(P＜0.01),the relative bioavailability was enhanced to 6.23 times as compared with that of raw medicine.CONCLUSION Nanosuspension can enhance the solubility and dissolution rate of galangin,and promote its in vivo absorption.关键词
高良姜素/纳米混悬剂/制备/体内药动学/HPLC-MS/MSKey words
galangin/nanosuspensions/preparation/in vivo pharmacokinetics/HPLC-MS/MS分类
医药卫生引用本文复制引用
房伟,韩德恩,王奎鹏..高良姜素纳米混悬剂制备及其体内药动学研究[J].中成药,2026,48(5):1466-1472,7.基金项目
河南省高等学校重点科研项目(22A350007) （22A350007）
