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Artificial pulmonary surfactant as a carrier for intratracheally instilled insulin

Acta Pharmacologica Sinica 2007年第5期28卷 744-750页

作者： Ying JI,Chen LIU,Yuan-ying PEI~2Department of Pharmaceuties,School of Pharmacy,Fudan University,Shanghai 200032,China Department of Pharmaceutics School of Pharmacy Fudan University Shanghai China

Aim:The relative bioavailabilities and effects on lung injury alleviation of 4 insu-lin-artificial pulmonary surfactant (INS-APS) preparations were studied in *** relationship between the minimal surface tension (γmin) of INS-APS andthe absorption of insulin was also ***:Four formulations ofAPS[1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC)/lecithin/palmitic acid(PA),DPPC/1-hexadecanol (Hex)/tyloxapol (Tyl),DPPC/L-α-phosphatidyl-DL-glyc-erol sodium salt (PG),DPPC/Tyl]were prepared by thin-film sonication methodand direct *** γminof 4 APS dispersions was examined with andwithout INS by pulsating with a bubble surface *** vivo experimentswere performed in which serum glucose change and the insulin level were mea-sured by an enzymatic glucose reagent kit and a radioimmunology assay kit afterIT to *** reduction in lung injury by INS-APS following 7 d of consecutiveadministration was evaluated by the pulmonary edema index (the weight ratio ofwet lung to dry lung) and histopathology ***:The γminof allAPS dispersions were below 10 mN/*** was no significant difference (P>0.05) between the γ(min)of APS and the corresponding *** vivo experi-ments showed a significant glucose level decrease and insulin absorptionincrease (P0.05) between INS/DPPC/Tyl,INS/DPPC/PG,and the control *** pulmonary edema indices and histopatho-logical observation indicated that INS-APS could alleviate lung ***:The most potent hypoglycemic effect and insulin absorption increase in this studywere obtained with INS/DPPC/*** to the results,there was a linearcorrelation between the γminand relative bioavailability of INS-

关键词： pulmonary drug delivery system pharmacokinetics pharmacodynamics hypoglycemic effect minimal surface tension absorption pulmonary edema index histopathology examination

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