吉非替尼乳剂单次与多次给药后在大鼠体内的药动学研究
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篇名: 吉非替尼乳剂单次与多次给药后在大鼠体内的药动学研究
TITLE:
摘要:
摘 要 目的研究吉非替尼乳剂单次和多次给药后在大鼠体内的药动学特征方法将大鼠分为单次给药组和多次给药组次给药组大鼠分为吉非替尼原料药组50 mg/kg和吉非替尼乳剂组50 mg/kg),每组6灌胃给药1多次给药组大鼠分为吉 非替尼原料药组50 mg/kg和吉非替尼乳剂组50 mg/kg),每组8连续灌胃给药7 d每天1吉非替尼原料药组大鼠于给药 前和给药后122.533.53.7544.254.5681224 h取血0.3 mL吉非替尼乳剂组大鼠于给药前和给药后多次给药组为给 7 d24689101112131416243648 h取血0.3 mL采用高效液相色谱法测定大鼠血浆中吉非替尼的血药浓度绘制药-时曲线并用 DAS 2.0 软件拟合药动学参数结果单次给药后与吉非替尼原料药组 tmax[ 2.67±0.75h]MRT0-24 h [ 8.68±0.91h]MRT0-[ 14.20±3.45h]比较吉非替尼乳剂组tmax[ 8.33±4.41h]MRT0-48 h[ 15.00±1.60h]MRT0-[ 17.60± 2.66h]均显著增加P<0.05)。多次给药后与吉非替尼原料药组 tmax[ 6.79±3.75h]AUC0-48 h[ 41.10±8.92mg·h/L]Vz/F
[ 16.30±5.45L/kg]CLz/F[0.94±0.19L/h·kg]MRT0-48 h[ 10.10±0.36h]比较吉非替尼乳剂组Vz/F[44.20±30.30L/kg]CLz/F[1.89±1.56L/h·kg]MRT0-48 h[ 16.20±2.52h]均显著增加P<0.05),AUC0-48 h[ 38.70±26.20mg·h/L]显著减少P0.05),tmax[ 10.40±3.25h]增加但差异无统计学意义结论与吉非替尼原料药比较单次和多次给药吉非替尼乳剂均可延长 药物的达峰时间本研究结果可为吉非替尼新型给药系统的研究提供参考
ABSTRACT:
ABSTRACT OBJECTIVETo study pharmacokinetic characteristics of single dose and multiple dose administration of Gefitinib
emulsion in rats. METHODSThe rats were divided into single administration group and multiple administration group. Single
administration group was subdivided into Gefitinib raw medicine group50 mg/kgi.g.and Gefitinib emulsion group50 mg/kgi.g.),with 6 rats in each groupgavage once. Multiple administration group were subdivided into Gefitinib raw medicine group 50 mg/kgand Gefitinib emulsion group50 mg/kg),with 8 rats in each groupthey were given relevant medicine intragastricaly for consecutive 7donce a day. 0.3 mL blood of rats in Gefitinib raw medicine group was taken before medication and 122.533.53.7544.254.56812 and 24 h after medication0.3 mL blood of rats in Gefitinib emulsion group was taken before medication and 246891011121314162436 and 48 h after administrationMultiple administration group is after 7 d of administration. HPLC method was used to determine the plasma concentration of gefitinib in ratand plasma concentration-time curves were drawn. Pharmacokinetic parameters were fitted by using DAS 2.0 software. RESULTSAfter single administrationcompared with the tmax[ 2.67±0.75h]MRT0-24 h [ 8.68±0.91h]MRT0- [ 14.20±3.45h] of Gefitinib raw medicine grouptmax [ 8.33±4.41h]MRT0-48 h
[ 15.00±1.60h]MRT0-[ 17.60±2.66h] of Gefitinib emulsion group were increased significantlyP<0.05. After multiple administrationcompared with the tmax [ 6.79±3.75h]AUC0-48 h [ 41.10±8.92mg·h/L]Vz/F [16.30±5.45L/kg]CLz/F [0.94±0.19L/h·kg]MRT0-48 h [ 10.10 ± 0.36h] of Gefitinib raw medicine groupVz/F [44.20±30.3L/kg]CLz/F[1.89± 1.56L/h·kg]MRT0-48 h [ 16.20 ± 2.52h] of Gefitinib
emulsion group were increased significantly P<0.05AUC0-48 h [ 38.70±26.20mg·h/L] was decreased significantly
P<0.05),and tmax [ 10.40±3.25h] was increasedwithout statistical significance. CONCLUSIONSCompared with
Gefitinib raw medicinesingle and multiple administration of Gefitinib emulsion can effectively prolong the peak timethe results
of this study can provide reference for new delivery system study of Gefitinib.
期刊: 2020年第31卷第1期
作者: 李 莹 ,文 周 ,马风伟 ,刘志刚 ,田 驰 ,刘治芳 ,程泽能
AUTHORS: LI Ying,WEN Zhou,MA Fengwei,LIU Zhigang,TIAN Chi,LIU Zhifang,CHENG Zeneng
关键字: 吉非替尼;乳剂;单次;多次;高效液相色谱法;药动学;大鼠
KEYWORDS: Gefitinib;Emulsion;Single;Multiple;HPLC;Pharmacokinetics;Rats
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