Gelucire 14/44 是一种潜在且安全的吸收促进剂，可通过肺部输送改善包括胰岛素和降钙素在内的难吸收药物的吸收。
Gelucire 44/14 is a potential and safe absorption enhancer for improving the absorption of poorly absorbable drugs including insulin and calcitonin by pulmonary delivery.
Gelucire 44/14 is a potential and safe absorption enhancer for improving the absorption of poorly absorbable drugs including insulin and calcitonin by pulmonary delivery. It is found that pulmonary absorptions of FD4, FD10 and FD70 are enhanced in different degree by Gelucire 44/14 in a concentration-dependent manner, and the maximal absorption-enhancing effect is obtained when the concentration of Gelucire 44/14 reaches to 2.0% (w/v). It is also found that the absorption enhancing ability of Gelucire 44/14 is correlated with the molecular weight of model drugs, and the highest absorption enhancement ratio of Gelucire 44/14 is observed when the molecular weight of model drugs reaches to nearly 10000 Da[1].
[1]. Zhang H, et al. Improvement of pulmonary absorptions of poorly absorbable drugs using Gelucire 44/14 as an absorption enhancer. J Pharm Pharmacol. 2014 Oct;66(10):1410-20.
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Animal experiment: |
Male Sprague Dawley rats are used to evaluate the pulmonary membrane toxicity of Gelucire 44/14. PBS (pH 7.4) with or without Gelucire 44/14 are directly administered to the tracheae of the rats according to the in-situ pulmonary absorption experiments. Four hours later, the rats are bled from the abdominal aorta, and then PBS (pH7.4) is perfused into the rat lung along the trachea. Afterwards, bronchoalveolar lavage fluid (BALF) of rat in each group is collected and kept in ice immediately until determination[1]. |
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参考文献: [1]. Zhang H, et al. Improvement of pulmonary absorptions of poorly absorbable drugs using Gelucire 44/14 as an absorption enhancer. J Pharm Pharmacol. 2014 Oct;66(10):1410-20. |
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