Pharmacodynamic and pharmacokinetic evaluation of lipid microspheres of indomethacin

Pharmaceutica acta Helvetiae Pub Date : 1998-12-01 DOI:10.1016/S0031-6865(98)00023-5

P. Srinath, P.V. Diwan

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引用次数: 12

Abstract

Lipid microspheres (LM) of indomethacin were prepared using phosphatidyl choline and soya bean oil. LM of required size (<1 μm) were obtained by intermittent microscopic observation while homogenization. Anti-inflammatory activity of lipo-indomethacin was compared with free indomethacin by carrageenan induced rat paw edema model. It was found that at 30% edema inhibitory dose, lipo-indomethacin was about 1.5 times more potent than free indomethacin, indicating possible localization of LM at the inflammatory site. Biodistribution studies were performed in rats at the dose of 12 mg/kg. After 2 h of the treatment, concentration of the drug was 0.31 μg/g of inflammatory tissue with lipo-indomethacin, whereas, only 0.05 μg/g of the tissue was found with free indomethacin. Maximum difference in drug concentrations between the above two formulations was observed in lungs. LM were found not to cross the BBB as drug concentration in the brain after lipo-indomethacin treatment was below the detectable level. Thus, the pharmacokinetic data gave a quantitative evidence for high anti-inflammatory potential of lipo-indomethacin.

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吲哚美辛脂质微球的药效学及药动学评价

以磷脂酰胆碱和大豆油为原料制备吲哚美辛脂质微球。在均质过程中，通过间歇显微镜观察获得所需尺寸的LM (<1 μm)。采用卡拉胶诱导大鼠足跖水肿模型，比较脂质吲哚美辛与游离吲哚美辛的抗炎活性。在30%的水肿抑制剂量下，脂质吲哚美辛的效力是游离吲哚美辛的1.5倍左右，表明LM可能定位于炎症部位。以12 mg/kg剂量在大鼠体内进行生物分布研究。治疗2 h后，脂质吲哚美辛炎症组织中药物浓度为0.31 μg/g，而游离吲哚美辛炎症组织中药物浓度仅为0.05 μg/g。在肺中观察到上述两种制剂之间药物浓度的最大差异。由于脂质吲哚美辛治疗后脑内药物浓度低于可检测水平，LM未穿过血脑屏障。因此，药代动力学数据为脂质吲哚美辛具有较高的抗炎潜力提供了定量证据。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Pharmaceutica acta Helvetiae

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