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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。
Rivastigmine liposomes were prepared and their pharmacokinetics in rat nasal administration were studied. The rivastigmine-loaded liposomes were prepared by ammonium sulfate gradient method. The particle size, zeta potential and entrapment efficiency were investigated. The release of liposomes in phosphate buffer was determined. . Antipyrine was used as the internal standard. The plasma concentrations of rivastigmine were determined by high performance liquid chromatography-tandem mass spectrometry (HPLC / MS). The pharmacokinetic parameters were fitted by DAS 2.0 software. The encapsulation efficiency of the prepared liposomes was (33.41 ± 6.58)%, the average particle size was 154 ~ 236 nm and the zeta potential was (-10.47 ± 2.41) mV. In vitro release of liposomes is in accordance with the first-order kinetic equation. After intranasal administration, Cmax, Tmax and AUC0-∞ were (1.50 ± 0.15) mg.L-1,15 min and (89.06 ± 8.30) mg.L-1.min, respectively. Rivastigmine liposome prepared by nasal administration, the rapid absorption, plasma concentration can reach a certain level.