Jiang Zhi-qiang, Lu Jian
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 200032, China.
Yao Xue Xue Bao. 2002 May;37(5):378-82.
To investigate the relative bioavailability of pulmonary-delivered insulin lipid suspension (INS-LIP-SP) in normal Wistar rats.
INS-LIP-SP were prepared by two different methods and then delivered to the rat lung using an intratracheal instillation method. Blood glucose levels and INS concentrations in serum were determined by glucose oxidase method and radioimmunoassay method, respectively. The relative pharmacological bioavailability (f%) and relative bioavailability (F%) of INS-LIP-SP were calculated from the area above the curve (AAC) and the area under the curve (AUC) compared with subcutaneous injection of INS solution.
The mean particle diameter, span of dispersity and entrapment efficiency of INS-LIP-SP prepared by a membrane-formed with sonication method and a reversed phase evaporation method were 1.91 microns, 0.94 and 16.45% and 2.08 microns, 1.28 and 39.51%, respectively. The values of f% and F% of both INS-LIP-SP were up to 37% and 32%, separately, and there was a statistically significant difference between INS-LIP-SP and INS solution. However, there was no significant difference between the two INS-LIP-SP and the physical mixture of INS solution and blank liposomes.
The results showed that INS-LIP-SP could achieve higher bioavailability following pulmonary delivery to rats.
研究肺部给药胰岛素脂质混悬液（INS-LIP-SP）在正常Wistar大鼠体内的相对生物利用度。
采用两种不同方法制备INS-LIP-SP，然后通过气管内滴注法将其递送至大鼠肺部。分别采用葡萄糖氧化酶法和放射免疫分析法测定血清中的血糖水平和胰岛素浓度。与皮下注射胰岛素溶液相比，根据曲线下面积（AUC）和曲线外面积（AAC）计算INS-LIP-SP的相对药理生物利用度（f%）和相对生物利用度（F%）。
采用超声成膜法和反相蒸发法制备的INS-LIP-SP的平均粒径、分散度跨度和包封率分别为1.91微米、0.94和16.45%，以及2.08微米、1.28和39.51%。两种INS-LIP-SP的f%和F%值分别高达37%和32%，INS-LIP-SP与胰岛素溶液之间存在统计学显著差异。然而，两种INS-LIP-SP与胰岛素溶液和空白脂质体的物理混合物之间没有显著差异。
结果表明，INS-LIP-SP经肺部给药后可在大鼠体内实现更高的生物利用度。
