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首页> 外文期刊>Journal of pharmaceutical sciences. >Azone? decreases the buccal mucosal permeation of diazepam in a concentration-dependent manner via a reservoir effect
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Azone? decreases the buccal mucosal permeation of diazepam in a concentration-dependent manner via a reservoir effect

机译：Azone？通过储库效应以浓度依赖的方式降低地西epa的颊粘膜渗透

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摘要

The purpose of this study was to examine concentration-dependent effects of Azone? (AZ) on the buccal absorption of diazepam (DIAZ). Porcine buccal mucosa was placed in modified Ussing chambers and pretreated with 10 μL of 0%, 5%, 20%, and 50% (w/v) AZ in ethanol. DIAZ was administered to the donor chamber either in solution or a chitosan-based gel. The donor chamber disappearance, receptor chamber appearance, and tissue retention of DIAZ were monitored over 2 h by HPLC, with AZ tissue disposition also measured by liquid chromatography-mass spectrometry profiling of tissue cryosections. DIAZ steady-state flux values significantly (p < 0.05) decreased 1.4- and 2.4-fold in 20% and 50% AZ-pretreated tissues, respectively. Only 20% and 50% AZ-pretreated tissues were also accompanied by an increased loss of DIAZ from the donor chamber, suggesting DIAZ was forming a reservoir in the buccal mucosa with higher AZ concentrations. Indeed, the percentage of the initial DIAZ dose remaining in the mucosa following a 2 h experiment was increased 3.0-fold with a 50% AZ pretreatment compared with control. AZ provided a concentration- dependent reservoir for DIAZ in buccal mucosa, resulting in retarded release into the receptor chamber, an approach that may be exploited for controlled release of DIAZ.
机译：这项研究的目的是检查Azone？的浓度依赖性作用。 （AZ）对地西epa（DIAZ）的口腔吸收。将猪颊粘膜置于改良的Ussing室中，并用10μL乙醇中的0％，5％，20％和50％（w / v）AZ预处理。将DIAZ以溶液或基于壳聚糖的凝胶施用于供体室。通过HPLC监测DIAZ的供体室消失，受体室外观和组织保留时间超过2小时，还通过组织冷冻切片的液相色谱-质谱分析法测量了AZ组织的位置。在20％和50％AZ预处理的组织中，DIAZ稳态通量值分别显着降低（p <0.05）1.4和2.4倍。只有20％和50％的AZ预处理组织还伴随着DIAZ从供体腔的损失增加，这表明DIAZ在颊粘膜中形成了更高AZ浓度的储库。实际上，与对照组相比，使用50％AZ预处理后2小时实验后，粘膜中剩余的DIAZ初始剂量的百分比增加了3.0倍。 AZ为颊粘膜中DIAZ提供了浓度依赖性的储库，导致延迟释放入受体腔，该方法可用于DIAZ的控制释放。

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