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苯佐那酯软胶囊在中国健康受试者中的药代动力学研究
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作者 满珈羽 焦菲菲 +3 位作者 王逸雅 顾月清 舒畅 丁黎 《药学与临床研究》 2019年第4期241-245,共5页
目的:研究中国健康受试者口服苯佐那酯软胶囊后苯佐那酯及其代谢产物4-N-丁基氨基苯甲酸(BBA)的药代动力学特征。方法:36名健康受试者分为A、B、C 3组,A、C组分别单次口服苯佐那酯软胶囊100 mg(低)、400 mg(高),B组单次及多次口服苯佐... 目的:研究中国健康受试者口服苯佐那酯软胶囊后苯佐那酯及其代谢产物4-N-丁基氨基苯甲酸(BBA)的药代动力学特征。方法:36名健康受试者分为A、B、C 3组,A、C组分别单次口服苯佐那酯软胶囊100 mg(低)、400 mg(高),B组单次及多次口服苯佐那酯软胶囊200 mg(中)。通过HPLC-MS/MS法检测血浆中BBA的浓度,推算血浆中苯佐那酯的浓度,估算药代动力学参数。结果:A、B、C 3组受试者单次给药苯佐那酯软胶囊后,BBA的Tmax分别为(0.74±0.40)、(0.54±0.24)、(0.61±0.43) h,Cmax分别为(1 603±443)、(2 833±1131)、(6 549±2 009) ng·mL^-1,AUC0-10h分别为(2 395±1 062)、(3 403±1 228)、(9 104±4 134) ng·h·mL^-1,t1/2分别为(1.42±0.52)、(1.84±0.89)、(1.70±0.75) h;苯佐那酯的Tmax分别为(0.62±0.25)、(0.62±0.27)、(0.58±0.37) h,Cmax分别为(1 201± 449)、(1 838±700)、(3 554±1 775) ng·mL^-1,AUC0-10h分别为(1 314±589)、(1 751±656)、(3 452± 2 111) ng·h·mL^-1,t1/2分别为(1.57±1.17)、(1.80±1.05)、(1.68±1.04) h。B组受试者多次给药苯佐那酯软胶囊200 mg后,BBA的Cav为(604±220) ng·mL^-1,DF为(5.34±1.26),RCmax为(1.20±0.45),RAUC为(1.10±0.13);苯佐那酯的Cav为(356±126) ng·mL^-1,DF为(5.91±1.35),RCmax为(1.24±0.57),RAUC为(1.31±0.33)。结论:在100~400 mg的给药剂量范围内,苯佐那酯不具有线性药代动力学特征。多次给药苯佐那酯软胶囊200 mg后,BBA和苯佐那酯在体内会产生蓄积。 展开更多
关键词 苯佐那酯 4-N-丁基氨基苯甲酸 聚合物 HPLC-MS/MS 药代动力学
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Protease-activated quantum dot probes based on fluorescence resonance energy transfer 被引量:4
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作者 LI Xin XUE Bing +1 位作者 LI Yang gu yueqing 《Chinese Science Bulletin》 SCIE EI CAS 2013年第21期2657-2662,共6页
A novel sensing system based on fluorescence resonance energy transfer (FRET) between CdTe quantum dots (QDs) and Rhoda-mine B (RB) was established for the detection of matrix metalloproteinases (MMOL/LPs). In this sy... A novel sensing system based on fluorescence resonance energy transfer (FRET) between CdTe quantum dots (QDs) and Rhoda-mine B (RB) was established for the detection of matrix metalloproteinases (MMOL/LPs). In this system, 535-nm-emitting quantum dots (QDs) were bound to Rhodamine B (RB) via a MMOL/LP-specific peptide. A 76% reduction in luminescence was achieved because of FRET. Release of RBs by peptide cleavage restores radiative QD photoluminescence. Initial studies observed a 73% rise in luminescence over 60 min. The design platform of the nanosensor is flexible and can be fine-tuned for a wide array of applications such as the detection of biomarkers, early diagnosis of disease, and monitoring therapeutic efficacy simply by changing the sequence of the peptide linker. 展开更多
关键词 荧光共振能量转移 基质金属蛋白酶 发光量子点 基础 酶激活 纳米传感器 探针 FRET
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Synthesis and evaluation of methionine and folate co-decorated chitosan self-assembly polymeric micelles as a potential hydrophobic drug-delivery system 被引量:3
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作者 CHEN YuQi CAO Jie +4 位作者 ZHU HongYan CUI SiSi WANG AQin QIAN ZhiYu gu yueqing 《Chinese Science Bulletin》 SCIE EI CAS 2013年第19期2379-2386,共8页
In this study, an amphiphilic copolymer folate-succinyl-methionine-chitosan-octyl (FSMCO) was successfully synthesized step by step for self-assembling polymeric micelles. The copolymers formed micelle-like nanopartic... In this study, an amphiphilic copolymer folate-succinyl-methionine-chitosan-octyl (FSMCO) was successfully synthesized step by step for self-assembling polymeric micelles. The copolymers formed micelle-like nanoparticles by their amphiphilic characteristics and structures were examined by UV-Vis absorption and Fourier transform spectroscopy. The sizes of blank and ICG derivativeloaded micelles measured by dynamic light scattering were about 170 and 140 nm, respectively, which were spherical in shape with an average zeta potential of 10 mV. Further studies on the stability showed that the micellar solutions maintain their sizes at room temperature for 1 month without distinct aggregation or dissociation. ICG derivative was much better photostable after being entrapped by the new carrier. The prepared FSMCO micelles displayed a good drug loading content (11.7%), entrapment efficiency (66.5%) and sustained release rate for the model drug fluorescein. The copolymers demonstrated weeny cytotoxicity toward Bel-7402, L02 and A549 cells when incubated for 2 d. Ligands modified micelles endowed preferable cell targeting capability and beautiful cell inhibition of HCPT-FSMCO on Bel-7402 tumor cells. This kind of polymeric micelles may be a promising nanovehicle in delivering near-infrared dyes for tumors imaging and chemotherapeutic drugs for cancer therapeutics. 展开更多
关键词 聚合物胶束 化疗药物 输送系统 合成 叶酸 两亲性共聚物 疏水性 组装体
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