Pol O, Planas E, Puig M M
IMIM, Department of Anesthesiology, Hospital Universitario del Mar, Barcelona, Spain.
Pharmacology. 1996 Sep;53(3):180-9. doi: 10.1159/000139429.
We have investigated the antitransit effects of free and liposomal morphine in a model of intestinal inflammation. Mice received saline or croton oil orally, 3 h prior to evaluation, and gastrointestinal transit was measured 20 min afterwards. Peak/duration of effects, potency (ED50) and antagonism by naloxone and naloxone methiodide were evaluated. Peak effects occurred 30 and 40 min after administration of morphine and liposomal morphine, respectively. Encapsulated morphine had a more pronounced and prolonged effect than morphine. Comparison of the ED50S demonstrated that the potency of liposomal morphine was 3.5 times higher than that of morphine during inflammation; in addition, inflammation increased the potency of morphine and liposomal morphine, 3 and 9.2 times, respectively. The effects of morphine and liposomal morphine in croton oil-treated mice were reversed by naloxone and naloxone methiodide. The results show that during inflammation, the potency and duration of the antitransit effects of morphine are significantly enhanced by encapsulation.
我们已经在肠道炎症模型中研究了游离吗啡和脂质体吗啡的抗蠕动作用。在评估前3小时,小鼠口服生理盐水或巴豆油,然后在20分钟后测量胃肠道蠕动。评估了效应的峰值/持续时间、效价(ED50)以及纳洛酮和甲碘化纳洛酮的拮抗作用。吗啡和脂质体吗啡给药后分别在30分钟和40分钟出现峰值效应。包封的吗啡比吗啡具有更明显和更持久的作用。ED50的比较表明,在炎症期间,脂质体吗啡的效价比吗啡高3.5倍;此外,炎症分别使吗啡和脂质体吗啡的效价提高了3倍和9.2倍。纳洛酮和甲碘化纳洛酮可逆转巴豆油处理小鼠中吗啡和脂质体吗啡的作用。结果表明,在炎症期间,通过包封可显著增强吗啡抗蠕动作用的效价和持续时间。