小鼠体内脂质体干扰素的药代动力学研究

The pharmacokinetics of liposome-encapsulated interferon in mice

目的 研究脂质体干扰素（L-IFN）对乙型病毒性肝炎的治疗价值。方法 通过临床药理实验测定L-IFN在小鼠体内的药代动力学参数。结果在小鼠血中，L-IFN的消除相半衰期、表观分布容积、清除率分别为（9.64(0.08）h、(77.83(1.62) ml、(5.59(0.02) ml/h，纯干扰素（IFN）则分别为（7.02(0.04）h、(1 619.00(40.48) ml、(159.80(1.67) ml/h；在小鼠肝中，L-IFN的消除相半衰期、表观分布容积、清除率分别为(10.55(0.30) h、(271.40 (3.89) ml、(17.83(0.23) ml/h，IFN则分别为 (9.45(0.45) h、(4 709.00(50.42) ml、(345.00(4.26) ml/h。L-IFN在血中的相对生物利用度是IFN的286%，在肝中则为IFN的194%。结论 L-IFN作为一种新剂型，有望日后应用于临床肝炎病人的治疗。

Objective To study the therapeutic value of liposome-encapsulated interferon (L-IFN) in the management of hepatitis B. Method By way of clinical pharmacological test, the pharmacokinetic parameters of L-IFN in mice were determined. Results The half-life time (t1/2() of L-IFN in the blood of mice was (9.46 (0.08) h [that of IFN was (7.02 (0.04) h], the apparent volume of distribution (Vd) was (77.83(1.62) ml [IFN was (1 619.00(40.48) ml], and the clearance rate (CL) was (5.59(0.02) ml/h for L-IFN and (159.80(1.67) ml/h for IFN. In the liver, the t1/2( of L-IFN was (10.55(0.30) h [(9.45(0.45 h) for IFN], Vd was (271.440 (3.89) ml [ (4 079.00(50.42) ml for IFN), CL was (17.83(0.23) ml/h [(345.00(4.26) ml/h for IFN]. The relative bioavailability of L-IFN in the blood was 286% that of IFN, and in the liver was 194% as much as that of IFN. Conclusion L-IFN, as a new dosage form of IFN, is possible to be used clinically in the treatment of hepatitis patients.