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Nifedipine penetration through human epidermis

机译:硝苯地平通过人表皮的渗透

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摘要

Decisions regarding selection of components are crucial in the early phases of dosage form design yet it remains unclear how to determine a priori the optimal features required in a transdermal delivery system to best overcome the barrier properties of skin. Nifedipine (N) does not penetrate the skin at rates sufficint to permit clinically useful transdermal application, presumably due to its poor solubility in both lipophilic and hydrophilic media. Earlier studies showed that N penetration into the deeper layers of the skin was not favorable dur to the markedly poor affinity for systems structured by extensive hydrogen bonding. Thus, a certain enhancer considered appropriate for plar compounds, might be considered less apprpriate for nonpolar permeants.
机译:在剂型设计的早期阶段,有关成分选择的决定至关重要,但目前尚不清楚如何先验确定透皮给药系统所需的最佳特征,以最好地克服皮肤的屏障特性。硝苯地平(N)不能以足以使临床上有用的经皮应用的速率渗透皮肤,大概是由于其在亲脂性和亲水性介质中的溶解性差。较早的研究表明,由于对广泛氢键构成的系统的亲和力明显较差,因此N渗入皮肤深层并不有利。因此,某些被认为适合于普拉化合物的增强剂,可能被认为不适用于非极性渗透剂。

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