| 卡巴拉汀脂质体的制备及其大鼠鼻腔给药的药代动力学 |
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| 作者姓名： | Yang ZZ Wang ZZ Wu K Qi XR |
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| 作者单位： | 北京大学药学院; |
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| 基金项目： | 国家重点基础研究发展计划(973计划)资助项目(2007CB935801); 国家自然科学基金资助项目(30970785) |
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| 摘 要： | 制备卡巴拉汀脂质体,研究其在大鼠鼻腔给药的药代动力学。采用硫酸铵梯度法制备包载卡巴拉汀的脂质体,考察粒径、zeta电位和包封率,测定脂质体在磷酸盐缓冲液中的释放;大鼠鼻腔给予卡巴拉汀脂质体,以安替比林为内标,采用高效液相色谱-串联质谱法(HPLC/MS)测定血浆中卡巴拉汀的浓度,运用DAS 2.0软件拟合药代动力学参数。经筛选制备的脂质体包封率为(33.41±6.58)%,平均粒径在154～236 nm,zeta电位(-10.47±2.41)mV。脂质体的体外释放符合一级动力学方程。大鼠鼻腔给药后,Cmax,Tmax和AUC0-∞分别为(1.50±0.15)mg.L-1,15 min和(89.06±8.30)mg.L-1.min。卡巴拉汀制备成脂质体经大鼠鼻腔给药后,吸收迅速,血药浓度可以达到一定水平。
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| 关 键 词： | 卡巴拉汀 脂质体 鼻腔给药 药代动力学 |
Preparation of rivastigmine liposome and its pharmacokinetics in rats after intranasal administration |
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| Yang ZZ,Wang ZZ,Wu K,Qi XR.Preparation of rivastigmine liposome and its pharmacokinetics in rats after intranasal administration[J].Acta Pharmaceutica Sinica,2011,46(7):859-863. |
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| Authors: | Yang Zhen-Zhen Wang Zhan-Zhang Wu Kai Qi Xian-Rong |
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| Institution: | YANG Zhen-zhen,WANG Zhan-zhang,WU Kai,QI Xian-rong(School of Pharmaceutical Sciences,Peking University,Beijing 100191,China) |
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| Abstract: | To prepare rivastigmine liposome,rivastigmine was loaded into liposome via ammonium sulfate gradient method.Its pharmacokinetic profile in rats was evaluated after intranasal administration.The size,zeta potential,entrapped efficiency and release of rivastigmine from the liposome in vitro were determined.Plasma concentration of rivastigmine was determined by high performance liquid chromatography-tandem mass spectrometry(HPLC/MS) using antipyrine as internal standard.The pharmacokinetic parameters were calc... |
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| Keywords: | rivastigmine liposome intranasal delivery pharmacokinetics |
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