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马钱子碱聚乳酸-羟基乙酸共聚物纳米粒表征及体内药动学评价
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作者 管庆霞 林泽榆 +4 位作者 夏昭睿 张雪 张国帅 李秀妍 杨志欣 《吉林中医药》 2023年第10期1193-1198,共6页
目的研究马钱子碱(brucine,B)聚乳酸-羟基乙酸共聚物polylactic acid glycolic acid copolymer(PLGA)纳米粒的表征及体内药动学表现。方法采用沉淀法制备B-PLGA纳米粒并测定其Zeta电位、粒径、包封率及载药量。建立马钱子碱含量测定方... 目的研究马钱子碱(brucine,B)聚乳酸-羟基乙酸共聚物polylactic acid glycolic acid copolymer(PLGA)纳米粒的表征及体内药动学表现。方法采用沉淀法制备B-PLGA纳米粒并测定其Zeta电位、粒径、包封率及载药量。建立马钱子碱含量测定方法。将雌性和雄性大鼠各6只随机分成2组,分别尾静脉注射B溶液和B-PLGA纳米粒(10 mg/kg),HPLC法测定马钱子碱血药浓度,并计算主要药动学参数。结果成功制备了B-PLGA马钱子碱纳米粒,测得其平均粒径为(99.80±1.11)nm,PDI为0.112±0.045,Zeta电位为(-27.6±0.32)m V,平均包封率和载药量分别为(67.35±1.24)%、(2.83±0.06)%。马钱子碱血药浓度的线性范围为0.66~52.80μg/mL(R^(2)=0.998),最低定量限为0.660μg/mL,日内、日间RSD<10%。大鼠尾静脉注射B溶液与B-PLGA纳米粒溶液后的药-时曲线均符合二室模型,消除半衰期分别为(63.23±4.35)h、(182.96±7.60)h。结论B-PLGA纳米粒使马钱子碱可以发挥长效的治疗作用并具有缓释效果,同时提高了药物生物利用度。 展开更多
关键词 马钱子碱 聚乳酸-羟基乙酸共聚物 药动学 HPLC
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聚乳酸-羟基乙酸共聚物负载坎地沙坦酯纳米粒的制备及体内外评价 被引量:3
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作者 徐天蛟 刘艳霞 《中国药师》 CAS 2021年第10期1817-1822,共6页
目的:制备坎地沙坦酯纳米粒并考察其生物利用度。方法:以聚乳酸-羟基乙酸共聚物(PLGA)作为载体材料,以聚乙烯醇(PVA)和D-α-维生素E聚乙二醇1000琥珀酸酯(TPGS)共同作为乳化剂,采用乳化溶剂蒸发法制备坎地沙坦酯PLGA-PVA/TPGS纳米粒,通... 目的:制备坎地沙坦酯纳米粒并考察其生物利用度。方法:以聚乳酸-羟基乙酸共聚物(PLGA)作为载体材料,以聚乙烯醇(PVA)和D-α-维生素E聚乙二醇1000琥珀酸酯(TPGS)共同作为乳化剂,采用乳化溶剂蒸发法制备坎地沙坦酯PLGA-PVA/TPGS纳米粒,通过中心复合设计-效应面法实验设计优化得到PLGA-PVA/TPGS纳米粒的最优处方,在透射电镜下观察坎地沙坦酯PLGA-PVA和PLGA-PVA/TPGS两种纳米粒的微观形态,并比较两种纳米粒的体外药物释放特性;考察坎地沙坦酯PLGA-PVA和PLGA-PVA/TPGS纳米粒经大鼠灌胃给药后的体内药动学特征。结果:坎地沙坦酯PLGA-PVA/TPGS纳米粒的最优处方组成为:PLGA浓度为100 mg·ml^(-1),PVA浓度为15 mg·ml^(-1),TPGS浓度为0.8 mg·ml^(-1),透射电镜下可观察到两种纳米粒分布均匀、无聚集;其体外释药特性均表现为前期释药较快,后期平缓;大鼠体内药动学结果显示,坎地沙坦酯PLGA-PVA和PLGA-PVA/TPGS纳米粒均能提高药物的达峰浓度,增加药物生物利用度,但是坎地沙坦酯PLGA-PVA/TPGS纳米粒提高的更显著(P<0.05)。结论:将坎地沙坦酯制备成PLGA-PVA/TPGS纳米粒能够提高药物在大鼠体内的生物利用度,对坎地沙坦酯的二次开发利用具有重要意义。 展开更多
关键词 聚乳酸-羟基乙酸共聚物 聚乙烯醇 D-α-维生素E聚乙二醇1000琥珀酸酯 乳化溶剂蒸发法 坎地沙坦酯纳米粒 生物利用度
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In vitro Degradation Study of a Braided Thin-Walled Biodegradable Ureteral Stent 被引量:1
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作者 尚亚峰 邹婷 +6 位作者 张明庆 王富军 周君梅 王文祖 谢华 王璐 陈方 《Journal of Donghua University(English Edition)》 EI CAS 2012年第5期385-388,共4页
The main disadvantage of conventional ureteral stents commonly used to provide urinary drainage after urological practice is that the patients have to undergo a secondary surgical procedure to remove stents. A new bra... The main disadvantage of conventional ureteral stents commonly used to provide urinary drainage after urological practice is that the patients have to undergo a secondary surgical procedure to remove stents. A new braided thin-walled biodegradable ureteral stent composed of PGA ( polyglycolic acid) and PLGA ( eopolymer of polylactic and polygiycolic acid) mnltifilaments was evaluated in v/tro in this study. In vitro degradation was performed in artificial urine with pH of 5.8 and the temperature of 37~C. The mass loss, mechanical properties, and morphology were observed at different degradaing time intervals of 0, 1, 2, 3, 4, and 5 weeks. The stent had a thinner wail than those of other degradable stents and provided better mechanical properties. The braided thin-walled biodegradable ureteral stents began to degrade after 2 weeks. At the week of 5, the stents were fully degraded. The degradative process of stents is smooth and well controlled. 展开更多
关键词 braided THIN-WALLED degradable ureteral stent PGA(polyglycolic acid plga copolymer of polylactic and polyglycolicacid in vitro degradation mechanical property
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Preparation and in vitro Release of Donepezil Hydrochloride Microspheres
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作者 Yingzhou WANG Hao QI +2 位作者 Dongze ZHANG Zixuan ZHAO Chunyan ZHANG 《Medicinal Plant》 CAS 2018年第6期65-67,共3页
[Objectives]To prepare donepezil hydrochloride microspheres and evaluate their quality.[Methods]The donepezil hydrochloride microspheres were prepared by emulsification-solvent evaporation method.The morphology was ob... [Objectives]To prepare donepezil hydrochloride microspheres and evaluate their quality.[Methods]The donepezil hydrochloride microspheres were prepared by emulsification-solvent evaporation method.The morphology was observed by scanning electron microscopy and the particle size distribution was determined by Laser Diffraction Method.The encapsulation efficiency,drug loading capacity,and in vitro release were determined by HPLC.[Results]The prepared donepezil hydrochloride microspheres were spherical with the average particle diameter of 15.927 μm.The drug loading capacity was 35.62%.The encapsulation efficiency was 90.32%.The drug release in vitro lasted for14 d.The release curve accorded with the first-order kinetic equation.[Conclusions]The prepared donepezil hydrochloride microspheres performed good sustained release effect in vitro,and it was expected to be used for research on Parkinson's disease. 展开更多
关键词 DONEPEZIL HYDROCHLORIDE polylactic acid-glycolic acid copolymer MICROSPHERE
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Preparation and in vitro Evaluation of Salidroside Nanoparticle
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作者 Yue FENG Wei ZOU +2 位作者 Mengran GUO Xing LAN Lili HE 《Medicinal Plant》 CAS 2022年第2期12-15,共4页
[Objectives]To use poly(lactic-co-glycolic acid)(PLGA)nanoparticles to improve the bioavailability and brain entrance capability of Salidroside(Sal).[Methods]An emulsion solvent evaporation approach was used to create... [Objectives]To use poly(lactic-co-glycolic acid)(PLGA)nanoparticles to improve the bioavailability and brain entrance capability of Salidroside(Sal).[Methods]An emulsion solvent evaporation approach was used to create PLGA nanoparticles(Sal-NP).The preparation parameters were optimized using a single factor experiment.The particle size and zeta potential were determined using the laser particle analyzer,and the morphology of the nanoparticles was observed using transmission electron microscopy.The encapsulation efficiency and drug loading were determined using HPLC.Subsequently,the in vitro drug release was determined using a dynamic dialysis method,and the cellular uptake and cytotoxicity were determined using the bEnd3 cell model.[Results]The ultrasonic time and power for preparing Sal-NP were 6 min and 100 W,respectively.The size of the nanoparticles was 162.0±74.86 nm,and the morphology of Sal-NP was spherical like.After 48 h,the cumulative release of Sal-NP was 62%,indicating that Sal showed a controlled release property in Sal-NP.Cellular uptake study showed that the PLGA nanoparticles remarkably increased the internalization than control group(P<0.001).In addition,Sal-NPs were non-toxic to cells at concentrations ranging from 12.5 to 100μM.[Conclusions]PLGA nanoparticles is promising to be exploited in Alzheimer's disease research due to the increasing absorption and controlled release advantages for Sal. 展开更多
关键词 SALIDROSIDE polylactic acid-glycolic acid copolymer NANOPARTICLES Controlled release Alzheimer's disease
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