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拉西地平固体分散体在Beagle犬体内的药动学和生物等效性研究 被引量:3
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作者 吴春暖 孙进 +1 位作者 何仲贵 宋晓坤 《现代药物与临床》 CAS 2018年第12期3096-3101,共6页
目的研究不同拉西地平固体分散体在Beagle犬体内的药动学和生物等效性。方法采用Thermo C_(18)色谱柱(50 mm32.1 mm,2.6μm);流动相:0.2%甲酸水溶液–乙腈(17∶83);体积流量:0.2 mL/min;柱温:30℃;进样室温度:15℃;进样量:10μL。采用... 目的研究不同拉西地平固体分散体在Beagle犬体内的药动学和生物等效性。方法采用Thermo C_(18)色谱柱(50 mm32.1 mm,2.6μm);流动相:0.2%甲酸水溶液–乙腈(17∶83);体积流量:0.2 mL/min;柱温:30℃;进样室温度:15℃;进样量:10μL。采用电喷雾离子源(ESI),多反应监测(MRM)方式扫描,以正离子方式进行检测;用于定量分析的离子对分别为拉西地平m/z 473.47(母离子)→354.28(子离子),内标尼莫地平m/z 419.25(母离子)→343.18(子离子)。6只健康Beagle犬分别给予4 mg参比制剂拉西地平片(R)、拉西地平-HPMC E5固体分散体(T_1)和拉西地平-Soluplus固体分散体(T_2),绘制血药浓度–时间曲线,采用DAS 2.1.1软件非隔室模型计算主要药动学参数,并进行生物等效性分析。结果拉西地平在0.25~100 ng/mL线性关系良好,定量下限为0.25 ng/mL。在0.5、5.0、80.0 ng/mL的提取回收率和基质效应分别为100.92%~102.89%和100.71%~102.89%,RSD值<11%。T_1、T_2和R的主要动力学参数分别为峰浓度(C_(max))为(24.45±6.53)、(28.80±11.89)、(26.647±4.44)ng/mL;达峰时间(t_(max))为(1.13±0.70)、(1.29±0.64)、(1.79±1.36)h;t_(1/2)分别为(8.39±4.60)、(7.10±6.73)、(5.20±6.16)h。受试制剂相对生物利用度为(112.2±57.8)%、(110.6±51.6)%。生物等效性分析两组受试制剂与参比制剂均不具备生物等效性。结论该方法准确、灵敏度高、专属性强,可用于拉西地平制剂的药动学和生物等效性研究。自制拉西地平固体分散体与市售拉西地平片生物等效性不一致。 展开更多
关键词 拉西地平固体分散体 拉西地平片 拉西地平 Beagle犬 药动学 生物等效性
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Probing the new strategy for the oral formulations of taxanes:changing the method with the situation 被引量:2
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作者 WANG He-Lin SUN Jin +1 位作者 TIAN Chu-Tong he zhong-gui 《Chinese Journal of Natural Medicines》 SCIE CAS CSCD 2021年第9期656-665,共10页
The first-generation taxanes(including paclitaxel and docetaxel)are widely used for the treatment of various cancers in clinical settings.In the past decade,a series of new-generation taxanes have been developed which... The first-generation taxanes(including paclitaxel and docetaxel)are widely used for the treatment of various cancers in clinical settings.In the past decade,a series of new-generation taxanes have been developed which are effective in the inhibition of tumor resistance.However,intravenous(i.v.)infusion is still the only route of administration,and may result in serious adverse reactions with respect to the utilization of Cremophor EL or Tween-80 as solvent.Besides,the dosing schedule is also limited.Therefore,oral administration of taxanes is urgently needed to avoid the adverse reactionss and increase dosing frequency.In this review,we first outlined the discovery and development of taxane-based anticancer agents.Furthermore,we summarized the research progress on the oral formulations of taxanes and proposed some thoughts on the future development of oral taxane formulations. 展开更多
关键词 TAXANES Oral delivery Oral bioavailability ANTI-TUMOR
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