Gürsoy A, Akbuğa J, Eroğlu L, Ulutín S
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Marmara, Nişantaşi, Istanbul, Turkey.
J Pharm Pharmacol. 1988 Jan;40(1):53-4. doi: 10.1111/j.2042-7158.1988.tb05150.x.
A comparison has been made between liposome-encapsulated and free indomethacin for their anti-inflammatory activities in the carrageenan paw oedema test in rats, and their inhibitory effect on platelet aggregation induced by adenosine 5-diphosphate (ADP) in-vitro. Free indomethacin, 3 mg kg-1, strongly inhibited carrageenan-induced oedema and a similar inhibitory activity was shown by 0.3 mg kg-1 of encapsulated drug. For the inhibition of platelet aggregation, the threshold concentration of free drug was 0.559 mM. At this concentration, at least 5 min incubation was needed to achieve 12.5% and 45 min for 50% inhibition. The inhibition was much stronger with encapsulated drug, and pre-incubation of 28 microM encapsulated drug for 10 min with platelet-rich plasma before addition of ADP completely inhibited platelet aggregation.
在大鼠角叉菜胶足爪水肿试验中，对脂质体包裹的吲哚美辛和游离吲哚美辛的抗炎活性，以及它们在体外对二磷酸腺苷（ADP）诱导的血小板聚集的抑制作用进行了比较。3mg/kg的游离吲哚美辛能强烈抑制角叉菜胶诱导的水肿，0.3mg/kg的包裹药物也表现出类似的抑制活性。对于血小板聚集的抑制，游离药物的阈值浓度为0.559mM。在此浓度下，至少需要孵育5分钟才能达到12.5%的抑制率，孵育45分钟才能达到50%的抑制率。包裹药物的抑制作用要强得多，在添加ADP之前，将28μM的包裹药物与富血小板血浆预孵育10分钟可完全抑制血小板聚集。
