Yang Zhen-Zhen, Wang Zhan-Zhang, Wu Kai, Qi Xian-Rong
School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Yao Xue Xue Bao. 2011 Jul;46(7):859-63.
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 calculated by DAS 2.0. The entrapped efficiency of rivastigmine liposome was (33.41 +/- 6.58) %, with the mean diameter of 154-236 nm and zeta potential of (-10.47 +/- 2.41) mV. The release behavior of rivastigmine was fitting the first order equation in vitro. The pharmacokinetic studies indicated that the C(max), T(max) and AUC(0-infinity), of rivastigmine liposome were (1.50 +/- 0.15) mg x L(-1), 15 min and (89.06 +/- 8.30) mg x L(-') x min, respectively. Rivastimine liposome was absorbed rapidly, and could reach a certain concentration in rat plasma after intranasal delivery.
为制备卡巴拉汀脂质体，采用硫酸铵梯度法将卡巴拉汀载入脂质体。经鼻给药后评估其在大鼠体内的药代动力学特征。测定了卡巴拉汀脂质体的粒径、ζ电位、包封率及体外释放情况。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。用DAS 2.0计算药代动力学参数。卡巴拉汀脂质体的包封率为（33.41±6.58）%，平均粒径为154 - 236 nm，ζ电位为（-10.47±2.41）mV。卡巴拉汀的体外释放行为符合一级方程。药代动力学研究表明，卡巴拉汀脂质体的C(max)、T(max)和AUC(0 - ∞)分别为（1.50±0.15）mg·L⁻¹、15分钟和（89.06±8.30）mg·L⁻¹·min。卡巴拉汀脂质体吸收迅速，经鼻给药后能在大鼠血浆中达到一定浓度。
