摘要
目的:制备漆黄素纳米混悬剂及其冻干粉末,提高药物溶解度及溶出度。方法:高压均质法制备漆黄素纳米混悬剂。以粒径为评价指标,单因素考察聚乙烯吡咯烷酮K30(PVP K30)用量、有机相与水相体积比、均质压力和次数的影响。采用Box-Behnken响应面法优化漆黄素纳米混悬剂的处方工艺,并制备成冻干粉。扫描电镜观察纳米混悬剂的外观,测定溶解度和体外溶出情况。X射线粉末衍射法(XRPD)分析存在状态。结果:漆黄素纳米混悬剂最佳处方:PVP K30用量为34.6 mg,均质压力为86 MPa,均质次数为9次,其粒径为(143.06±5.37) nm,与模型预测值接近。纳米混悬剂外貌为球形或类球形,溶解度由(13.92±0.28)μg·mL^(-1)提高至(94.76±0.71)μg·mL^(-1)。体外溶出度结果表明,漆黄素纳米混悬剂的溶出速率及累积溶出度得到明显提高。漆黄素以无定形状态存在于纳米混悬剂中。结论:Box-Behnken响应面法可用于优化漆黄素纳米混悬剂的处方工艺,明显改善漆黄素纳米混悬剂的溶解度和溶出度。
OBJECTIVE To prepare fisetin nanosuspensions and lyophilized powder to enhance the solubility and drug release.METHODS Nanosuspensions were prepared by high pressure homogenization.Particle size was employed as evaluation index, single factor analysis was used to study the effects of polyvinylpyrrolidone(PVP K30)amounts, volume ratio of organic phase to water, homogenization pressure and times.Box-Behnken response surface design method to investigate the optimal prescriptions of fisetin nanosuspensions, and then its lyophilized powder was prepared.The morphology of fisetin nanosuspensions was observed by scanning electron microscope(SEM).The solubility and drug release of fisetin nanosuspensions was detected.The presence state was analyzed by X-ray powder diffraction(XRPD).RESULTS The optimal formulation: dosage of PVP K30 was 34.6 mg, homogeneous pressure was 86 MPa, homogeneous times were 9.The particle size of optimal formulation was(143.06±5.37)nm, which were close to that of predicted values.The appearances of nanosuspensions were spherical or nearly spherical.Solubility of fisetin was enhanced from(13.92±0.28)μg·mL^(-1) to(94.76±0.71)μg·mL^(-1).The in vitro release results showed that the dissolution rate and cumulative dissolution were obviously enhanced.Fisetin was an amorphous form in nanosuspensions.CONCLUSION Box-Behnken response surface design method could be used to optimize prescriptions of fisetin nanosuspensions, and the solubility and in vitro release were improved significantly.
作者
毛艳婷
陶兴茹
张胜男
周甜
崔传锋
范明松
MAO Yan-ting;TAO Xing-ru;ZHANG Sheng-nan;ZHOU Tian;CUI Chuan-feng;FAN Ming-song(Department of Pharmacy,Children′s Hospital Affiliated to Zhengzhou University,Henan Zhengzhou 450000,China;School of Pharmaceutical Sciences,Zhengzhou University,Henan Zhengzhou 450001,China;Shanghai Leiyunshang Phar-maceutical Co,.Ltd.,Shanghai 201401,China)
出处
《中国医院药学杂志》
CAS
北大核心
2022年第4期393-398,共6页
Chinese Journal of Hospital Pharmacy
基金
2019年度河南省医学科技攻关计划联合共建项目(编号:LHGJ20190974)。
作者简介
毛艳婷,女,硕士,主管药师,研究方向:药剂学;通信作者:范明松,男,博士,高级工程师,研究方向:新药工艺及质量控制。
