Lin Wei, Yao Jing, Zhou Jian-Ping
China Pharmaceutical University, Nanjing, China.
Yao Xue Xue Bao. 2009 Feb;44(2):192-6.
To prepare self-assemble nobiletin proliposomes and study its pharmacokinetic behavior in rats after ig administration, and nobiletin suspension was used as control, self-assemble nobiletin proliposomes were prepared by a new proliposome preparation method, their physicochemical properties including encapsulation efficiency, particle size and stability of formed liposome were determined. Plasma concentration of nobiletin was determined by HPLC taking nimodipine as internal standard. The pharmacokinetic parameters were calculated by Kinetica 4.4 software. The encapsulation efficiency of nobiletin liposomes was more than 80%, with an average particle size of 212.1 nm and very good stability. Compared to nobiletin suspension, nobiletin liposomes possessed higher absorptive rate and longer MRT, and the relative bioavailability was 264.3% in rats. It could be concluded that self-assemble nobiletin proliposome was a simple and feasible preparation, and showed greater absorption compared with nobiletin suspension.
为制备自组装诺米林前体脂质体并研究其在大鼠灌胃给药后的药代动力学行为，以诺米林混悬液为对照，采用一种新的前体脂质体制备方法制备自组装诺米林前体脂质体，测定其包封率、粒径和形成脂质体的稳定性等理化性质。以尼莫地平为内标，采用高效液相色谱法测定血浆中诺米林的浓度。通过Kinetica 4.4软件计算药代动力学参数。诺米林脂质体的包封率大于80%，平均粒径为212.1 nm，稳定性良好。与诺米林混悬液相比，诺米林脂质体具有更高的吸收率和更长的平均滞留时间，大鼠体内相对生物利用度为264.3%。可以得出结论，自组装诺米林前体脂质体是一种简单可行的制剂，与诺米林混悬液相比具有更高的吸收性。
