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目的:提高药物抗病毒疗效,降低其用量及毒副作用。方法:用薄膜法制备脂质体干扰素(L-IFN),用冻融法制备脂质体Ara-AMP(L-Ara-AMP)和ACV(L-ACV)。结果:经药物含量测定其包封率分别为43.2％、55％和35％。用病变抑制法测定,L-IFN抗病毒效价是未包封游离IPN的13倍,在加入胞壁酰二肽(MDP 10～100ng/ml)后,还可增效100倍。临床应用表明,100MU、300MU L-IPN及L-ACV总有效率分别为46.4％(14/30)、4/6、50％(6/12),而等剂量对照组(未包封)分别为14.3％(2/14)、33％(3/9)、25％。两组相比有显著性差异(P<0.05)。L-Ara-AMP 100mg剂量组疗效(37.5％),尚略高于未包封组200mg剂量组(28.5％)(P>0.05)。结论:脂质体可在一定程度上提高药物疗效,降低药物用量,是可取的增效方法。
Objective: To improve the anti-virus drug efficacy, reduce its dosage and side effects. Methods: Liposome interferon (L-IFN) was prepared by membrane method. Liposomes Ara-AMP (L-Ara-AMP) and ACV (L-ACV) were prepared by freeze-thaw method. Results: The encapsulation efficiency of the drug was 43.2%, 55% and 35%, respectively. The lesion inhibition assay showed that the antiviral titer of L-IFN was 13 times higher than that of unbound encapsulated IPN, and 100 times more after addition of muramyl dipeptide (MDP 10-100 ng / ml). The clinical application showed that the total effective rates of 100MU, 300MU L-IPN and L-ACV were 46.4% (14/30), 4/6 and 50% (6/12), respectively, while those of the equal dose control group 14.3% (2/14), 33% (3/9), 25%. There was significant difference between the two groups (P <0.05). The effect of L-Ara-AMP 100 mg (37.5%) was still slightly higher than that of the non-encapsulated group (28.5%) (P> 0.05). Conclusion: Liposomes can improve the curative effect and reduce the dosage of drugs to a certain extent, which is a desirable synergistic method.