Related Experiment Video
Updated: Aug 13, 2026

Visualizing and Quantifying Pharmaceutical Compounds within Skin using Coherent Raman Scattering Imaging
Published on: November 24, 2021
Skin permeation of acyl derivatives of stobadine
Magdaléna Májeková1, Vasil Koprda, L'ubor Bohácik
1Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, Slovak Republic. magdalena.majekova@savba.sk
Abstract:
Stobadine is a model drug with pyridoindole structure with cardioprotective and antioxidant properties. Permeation properties of its acyl derivatives were studied to find a proper prodrug form. The experimental study of transdermal delivery of derivatives was combined with the theoretical approach in which the partition coefficients of substances were estimated by means of fragmentation or quantum chemical calculations. All modes applied showed differences in the transport properties of derivative S1 (N-acetyl stobadine). The experimental results obtained for the flux of S1 were higher by one order of magnitude than for the other derivatives and the parent drug. The results are discussed from the point of view of physicochemical properties of derivatives. We concluded that the exceptional permeation value of S1 derivative results from the concurrence of partitioning coefficient, dissociation constant, and arrangement of permeation set.
Related Concept Videos
Bioavailability Enhancement: Drug Permeability Enhancement
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
Non-Oral Extravascular Drug Absorption Routes
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more effectively...
Indirect-Acting Cholinergic Agonists: Pharmacokinetics
Reversible agents containing quaternary amines, such as neostigmine and edrophonium, are not easily absorbed orally because they are...
Drug Absorption Mechanism: Passive Membrane Transport
Methods for Studying Drug Absorption: In situ
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
