Príborský J, Takayama K, Nagai T, Waitzová D, Elis J, Makino Y, Suzuki Y
Faculty of Pharmaceutical Sciences, Hoshi University, Tokyo, Japan.
Pharm Weekbl Sci. 1988 Oct 14;10(5):189-92. doi: 10.1007/BF01956869.
The study reports on penetration enhancers used to improve drug absorption through the skin. All experiments were carried out in permeation cells in vitro. Insulin (2.5 mg/ml) and Brilliant Blue (50.0 mg/ml) served as model drugs. They were formulated into a 40% solution of propylene glycol with increasing concentrations of N-methyl-2-pyrrolidone (NMP) (0.0 to 20.0%), dodecylazacycloheptan-2-one (laurocapram) and a new compound dodecyl-L-pyroglutamate (DLP; 0.0 to 0.5%). The maximum amount of insulin permeated within 24 h was almost 200 microU/ml in the case of 0.1% laurocapram, while in the case of 0.1% DLP it was approximately half of that. The optimum concentration of NMP was 12.0%. Experiments performed with Brilliant Blue showed no significant difference among formulations containing either 6.0, 12.0 or 20.0% of NMP. When NMP was omitted, flux, permeability as well as the maximum concentration estimated after 26 h reached 50% of the values obtained with NMP. The lag time was twice as long in this case in comparison with the formulations containing NMP.
该研究报告了用于改善药物经皮吸收的渗透促进剂。所有实验均在体外渗透细胞中进行。胰岛素（2.5毫克/毫升）和亮蓝（50.0毫克/毫升）用作模型药物。它们被配制成40%的丙二醇溶液，其中N-甲基-2-吡咯烷酮（NMP）（0.0%至20.0%）、十二烷基氮杂环庚烷-2-酮（月桂氮卓酮）和一种新化合物十二烷基-L-焦谷氨酸（DLP；0.0%至0.5%）的浓度不断增加。在含0.1%月桂氮卓酮的情况下，24小时内渗透的胰岛素最大量几乎为200微单位/毫升，而在含0.1% DLP的情况下，约为其一半。NMP的最佳浓度为12.0%。用亮蓝进行的实验表明，含6.0%、12.0%或20.0% NMP的制剂之间无显著差异。当省略NMP时，通量、渗透率以及26小时后估计的最大浓度达到含NMP制剂所获值的50%。与含NMP的制剂相比，这种情况下的滞后时间延长了一倍。
