Abstract: In drug development the most important step after drugs active discovery is its formulation. The drug should be designed in such a dosage form that could deliver the most of its active to the biological system imparting its pharmacokinetic properties through its physicochemical characteristics. The pharmacokinetic properties of drug depends upon drugs permeability, solubility, lipophillicity, protein binding etc. which are determined by its physicochemical properties including acid-base Dissociation constant (pKa), Molecular weight (MW), hydrogen bonds available (h-donors & h-acceptors), polar surface area (PSA) and partition coefficient (logP). Physicochemical characteristics are determined during structural modelling of the active i.e. studying & developing a Structural activity relationship of drug’s chemical structure. In this experiment, pKa & logP of the physicochemical properties are under consideration and the impact of physicochemical parameters on solubility permeability & ADME in oral & dermal preparations of Fluconazole. We determined the buffer capacity by titration method using an acid (0.1M HCl) & a base (0.1M NaOH). When the ratio of conjugate base & weak acid are in equilibrium i.e. having the same values, then the pH values are equal to pKa. While, pH is inversely proportional to concentration of weak acid & directly proportional to conjugate base. It was found that microemulsion formulation with diethyleneglycole monoethylene ether for fluconazole provides best drug delivery system than with the one with Polyethylene glycol & is favourable for advance clinical assessment. Also, fluconazole has low lipophilicity consequently when administered orally it extensively dispenses into body, particularly in serum or blood.
Keywords: Physicochemical properties, Flucanozole, buffer capacity, logP, pKa, titration curves.
Title: Implications of Physicochemical Properties on Drug’s Absorption
Author: Richa Kaushal
International Journal of Mathematics and Physical Sciences Research
ISSN 2348-5736 (Online)
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