激光粒度仪测口服芹菜素固体脂质纳米粒含量

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1、激光粒度仪测口服芹菜素固体脂质纳米粒含量*胡海洋，刘任，刘丹，赵秀丽，陈大为（沈阳药科大学药学院，沈阳110016）摘要：目的本研究对所制得的芹菜素固体脂质纳米粒的制剂学性质和药动学进行研究。方法使用激光粒度仪，Zeta电位值测定仪，透射电镜，X-射线衍射，体外溶出实验考察芹菜素固体脂质纳米粒的制剂学性质；以自制芹菜素混悬液为对照组，考察了大鼠口服芹菜素固体脂质纳米粒的药动学过程。结果透射电镜观察纳米粒的形态发现该纳米粒为类球形粒子；平均粒径为135nm；Zeta电位为-18.90mV；测定药物在释放介质中的释放符合

2、一级释放方程。X-射线衍射证明，芹菜素在-1固体脂质纳米粒中以无定形形式存在。口服药动学结果表明，芹菜素固体脂质纳米粒组的平均AUC0-t为17.337mg·h·L，-1-1-1而对照组为5.3mg·h·L。纳米粒组的ρmax为3.07mg·L，明显高于对照组的1.544mg·L。纳米粒组的消除速率常数Ke较-1低，为0.232h，低于对照组。结论芹菜素固体脂质纳米粒的相对生物利用度为327%。芹菜素固体脂质纳米粒可有效提高芹菜素的生物利用度。关键词：芹菜素；固体脂质纳米粒；体外释放；差示扫描量热；X-射线衍射；药动

3、学中图分类号：R969；R944文献标识码：A文章编号：1001-2494(2009)06-0448-04StudiesonPharmacyCharactersandPharmacokineticsofOralApigeninLoadedSolidLipidNanoparticle*HUHai-yang，LIURen，LIUDan，ZHAOXiu-li，CHENDa-wei（SchoolofPharmacy，ShenyangPharmaceuticalUniversity，Shenyang110016，China）A

4、BSTRACT：OBJECTIVEToinvestigatethepharmacycharactersandpharmacokineticprocessesofthepreparedapigeninloadedsolidlipidnanoparticles(AP-SLN).METHODSThepharmacycharactersofAP-SLNwereinvestigatedwiththemeansize，ζpotential，transmissionelectronmicroscopy，andinvitrodrug

5、release.ThepharmacokineticprocessesoforalAP-SLNoftheratswerealsostudied，whileapigeninsuspensionwasusedascontrolgroup.RESULTSTheappearanceofAP-SLNwasexaminedbytransmissionelectronmicroscopyassphere-likewiththemeansizeof135nm，thepotentialof-18.90mV，respectively.T

6、heinvitroreleaseprofileswereexpressedbyfirst-orderreleaseequation.UsingX-ray，itwascomfirmedthatapigeninwasencapsulatedin-1solidlipidnanoparticlesasamorphous.TheaverageAUC0-tofSLNgroupwas17.337mg·h·L，whiletheAUC0-tofcontrolgroup-1-1-1was5.3mg·h·L.TheρmaxofSLNgro

7、upwas3.07mg·L，obviouslyhigherthan1.544mg·Lofcontrolgroup.Theeliminationrate-1constant，Ke，ofSLNgroupwas0.232h，lowerthanthatofthecontrolgroup.TherelativebioavailabilityoftheAP-SLNwas327%.CONCLUSIONTheresultsoforaladministrationpharmacokineticsindicatedthatSLNsign

8、ificantlyenhancedtheoralbioavailabilityofAP.KEYWORDS：apigenin；solidlipidnanoparticles；invitrorelease；Differentialscanningcalorimetry；X-ray；pharmacokinetics[1-3]芹菜素（apigenin，