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1、RP-HPLC法灵敏度高,分离度和重现性好,可以满足体内外样品分析要求。测定了PNS中活性单体三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1的百分含量,R1、Rg1和Rb1的百分含量分别为:9.64%、51.10%和36.38%。⑵PNS静脉注射及灌胃后,R1、Rb1和Rg1在大鼠体内的药时曲线均符合二室模型,经过剂量校正后的口服绝对生物利用度分别为1.76%、0.78%和2.44%。⑶从最佳制剂处方进行PNS肠溶微丸的制备,f2因子评价结果表明,3批样品的体外释放度均有良好的重现性,R1、Rb1和Rg1的释放行为没有
2、显著性差异,且在制剂制备过程中三种成分的含量也无明显变化。⑷PNS肠溶微丸(胶囊),外形完整,无软化塌陷现象,内容物色泽变化不大;含量、含量均匀度、装量差异、体外释放度和初步稳定性考察均符合要求。⑸实验表明单剂量给予Beagle犬供试品和参比制剂后,PNS肠溶微丸(胶囊)与普通制剂相比,相对生物利用度提高3.81倍,有显著性差异,绝对生物利用度也有提高。结论:本课题在生物药剂学及药物动力学理论的指导下,以PNS的胃肠道吸收特性为基础进行制剂的研究,减少了制剂开发的盲目性,其研究结果为今后PNS口服剂型的研究包括处方工
3、艺、质量评价、体内动力学等方面提供参考。关键词:三七总皂苷;肠溶微丸;制备;质量标准;药代动力学2ResearchofPanaxNotoginsengSaponinsintestinesdissolvingmicropill(capsule)preparationandpharmacokineticAbstractObjective:Xueshuantonginjectionhasbeenwidelyusedtotreatcoronarydiseaseinclinic.Inthispaper,itsmaingroup
4、thatispanaxnotoginsengsaponions(PNS)wasusedasmodeldrug.TheobjectivewastostudyabsorptionmechanismofPNSandtodeveloporalentericpreparationofPNSwhichcouldavoidbeingdestroyedbystomachacidandenzymes,onthebasisofprinciplesinbiopharmaceuticsandpharmacokinetics.PNSordin
5、arydailydoseoralpreparationsfor600mg,oralabsorptionispoor,thelivingcreatureexploitationdegreeislow,inordertoimproveproductquality,reducetheirdoseandfrequencyofuse,reduceblooddrugconcentrationinthebodyofthepeakandvalleyeffect,inviewofthecharacteristicsofcardiova
6、scularanddrugdemand,combinedwithmicropillslow-releaseformulationintheapplicationofuniqueadvantages,thismedicinewillbeproposedtomadeintestinesdissolvingmicropill(capsule)preparations.Methods:(1)tothephysicalandchemicalpropertiesandstabilityPNSinvestigation,inclu
7、dingpHvalue,solubility,oilandwaterdistributioncoefficientandtheapparenttotemperature,light,thestabilityofthepHandRP-HPLCPNSimprovedquantitativeanalysismethod.(2)theratveinsandirrigationtostomachPNS,withHPLCtotrackwhichR1,Rgl,Rb1activemonomers,theratsinadruginth
8、ebodydynamics,andestablishPNSinmiceanalysismethod.(3)theblankpillcoreirrigationmethod,withefficientcoatingmachineelementpillcoatingpreparationintestinesdissolvingmicropill.T