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本文研制川陈皮素自组装前体脂质体,并以混悬剂为对照考察其经大鼠灌胃给药后的药代动力学行为。采用一种新型前体脂质体法制备川陈皮素自组装前体脂质体,考察其水合后粒径、包封率和稳定性等理化性质;大鼠分别灌胃给予川陈皮素混悬剂和水合后的脂质体,以尼莫地平为内标,采用HPLC法测定血浆中药物浓度,用Kinatica4.4程序计算药代动力学参数。制得的川陈皮素前体脂质体经水合后包封率可达80%以上,平均粒径为212.1nm,稳定性好;药代动力学研究显示,与混悬剂相比川陈皮素脂质体在体内吸收较快,相对生物利用度为264.3%,MRT增加。结果表明,川陈皮素自组装前体脂质体制备工艺简单可行;川陈皮素制成自组装前体脂质体后,大鼠口服吸收显著增加。
In this paper, the preparation of nobiletin self-assembly precursor liposomes, and the suspension as a control study of its rat gavage pharmacokinetics after administration. A new type of liposome method was used to prepare the liposomes of chuan-Cortexin self-assembled precursor. The physico-chemical properties such as particle size, encapsulation efficiency and stability of the liposomes were investigated. Pharmacokinetics and hydration of liposomes, nimodipine as internal standard, the concentration of drug in plasma was determined by HPLC, and pharmacokinetic parameters were calculated by Kinatica 4.4 program. The prepared liposomal nobiletin precursor encapsulated by hydration up to 80%, the average particle size of 212.1nm, good stability; pharmacokinetic studies showed that compared with the suspension of nobiletin Liposomes absorbed faster in the body, the relative bioavailability was 264.3%, MRT increased. The results showed that the preparation of nobiletin by self-assembly of precursor liposomes was simple and feasible. Oral absorption of rat was significantly increased by nobiletin after self-assembly of precursor liposomes.