灯盏花素缓释片在兔体内的绝对生物利用度

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1、万方数据中国临床药学杂志CHINESEJOURNALOFCLINICALPHARMACY2008年第17卷第1期·25·灯盏花素缓释片在兔体内的绝对生物利用度沈腾1，郁韵秋2，翁伟宇1，李妮2，黄照昌3，蔡佳1，黄建明2(复旦大学药学院1药剂学教研室，2药物分析教研室，上海200032；3昆明制药集团股份有限公司。昆明650loo)【摘要】目的测定兔静注灯盏花素注射剂25zIlg及兔1：3服灯盏花素缓释片120mg后血浆中野黄芩苷的浓度，研究2种制剂的药动学参数和缓释片的绝对生物利用度。方法采用q固相萃取法预处理血浆样

2、品，兔静注和1：3服灯盏花素后的血药浓度分别采用高效液相色谱一紫外检测法和高效液相色谱一质谱检测法测定。结果兔静注灯盏花素注射剂后的药一时曲线符合三室模型。兔口服灯盏花素缓释片后的药一时曲线难以用现有的房室模型拟合，6只兔的药一时曲线及药动学参数差异较大。经剂量校正，口服给药的绝对生物利用度，为(O．18±0．15)％。结论兔口服灯盏花素缓释片后的绝对生物利用度很低。【关键词】灯盏花素；野黄芩苷；生物利用度；高效液相色谱【文献标识码】A【文章编号】10074406f2008)01，{)025-04Absolutebio

3、availabilityofbreviscapinesustainedreleasetabletinrabbitSHENTe耐，YUYunqiu2，WENGWeiyul，LINi2，HUANGzhaochan矿，CAIJial，HUANGJianmin92(1Department矿确彻瑚砒s，2DepartmentofPharmaceuticAnalysis，SchoolofPharmacy，FudanUniversity，Shanghai200032，China；3KunmingPharmaceuticalCorpo

4、rationLtd．，陷腑盹喈650100，China)【A咖ACT】删ToinvestigatethephannaeokineticsofscuteUarinafterintravenousinjection(iv)andoralad．ministrationofbreviscapinetorabbitsandtostudytheabsolutebioavailabilityofbreviscapinesustainedreleasetabletinrabbits．船THODSScuteUarinandintermd

5、standard(IS)baicalinwereextractedfromplasmabysolid．phase甑trac．tionusingC8cartridges．neconcentrationofscutellarininrabbitplasmaafterintravenousinjectionofbreviscapinem—jec．fionwasdeterminedbyaⅢ)I￡一ultraviolet(}玎?LC．uv)method，andthatafteroraladministrafionofbrevis

6、capineSU8一tainodreleasetabletWasdeterminedbyallHPLC．massspectrometry(MS)method．RESULTSAfterintravenousinieC—tionofbmviscapineinjection25mg．theconcentration-timeprofileswerefittedtOathree—compartmentmodel，andthemainpharmacokineticparameterswereasfollows：‘{pi(O．04

7、±O．01)h，‰(0．32±O．23)h．t_}13(3．3±1．1)h，锄dAUG嗍h(12．6±2．3)mg·h·L～．Afteroraladministrationofsustainedreleasetablet120mg。theconcentration—timeprofilescouldnotbedescribedbyclassicalcompartmentmodel，andthemainpharmacokineticparameterswereasf01．h：IDM(12．7±12．4)腭·L～，tⅢ(9

8、．3±7．3)handAUCp24h(110．9±79．0)to·h·L一．1heabsolutebioavail．ability(F)oforaladministrationWasonly(O．18±0．15)％．∞臌7S，。?v11leabsolutebioavailabilityofbreviscap．inesustaine