PhD Scientific Days 2022

Pharmaceutical Sciences II. (Poster discussion will take place in the Aula during the Coffee Break)

Investigation of Factors Influencing the Solubility and Permeability of Drugs

Előadó neve

Dr. Szolláth, Rita

Előadó munkahelye

Semmelweis University, Department of Pharmaceutical Chemistry

Előadó telefonszáma

+36302535139

Előadó e-mail címe

szollathrita@gmail.com

Az előadás címe

Investigation of Factors Influencing the Solubility and Permeability of Drugs

Szerző(k) neve és munkahelye

Szolláth Rita
Semmelweis Univesity, Department of Pharmaceutical Chemistry, Budapest

Bemutatás módja

Poszter

Szekció

Pharmaceutical Sciences II. (Poster discussion will take place in the Aula during the Coffee Break)

Language of the presentation

Hungarian

Preferred session

Pharmaceutical Sciences

Összefoglaló szövege

Introduction: Pharmacokinetics are greatly determined by the physico-chemical properties of the drug. Solubility, dissolution and permeability are playing an important role in the absorption of drug molecules. The Biopharmaceutical Classification System also classifies compounds based on their solubility and permeability.
Aims: The aim of this study was to investigate the effect of particle size, different excipients, pH and biomimetic medium on the above mentioned physicochemical properties. Solubility, dissolution, and permeability of niflumic acid were investigated under biorelevant conditions. Measurements were performed with macrocrystalline, micronized, and nanonized forms. For nanonization, two excipients, polyvinyl alcohol (PVA) and polyvinylpyrrolidone (PVPK25) were used.
Methods: Measurements were performed in Fasted and Fed State Simulated Intestinal Fluid (FaSSIF and FeSSIF) blank and full buffers. Properties of macrocrystalline and micronized forms were also determined in the presence of excipients (1: 1 ratio, like used in case of nanonization). Equilibrium solubility was measured by the saturated shake flask method, dissolution was monitored in situ with UV probes. Permeability was measured with the µFlux apparatus.
Result: Solubility was the highest in FaSSIF full medium. In blank buffers, nanonization resulted a nearly twofold increase in solubility. PVPK25 increased the solubility more than PVA. A solubilizing effect was observed in the biomimetic medium: the solubility in FeSSIF full was nearly ten times higher than the concentration measured in FeSSIF blank buffer.
The permeability of the macrocrystalline niflumic acid was the highest. Using PVA or PVPK25 as a physical mixture next to the macrocrystalline form resulted a decrease in permeability. The micronized sample showed the same permeability alone and in the presence of excipients.
Conclusion: Reducing particle size can be an effective way to improve solubility. Excipients used for nanonization may have a solubilizing effect in themselves. The solubilizing effect of the biorelevant medium is more pronounced, when some of the molecules are in a non-ionized state at a given pH.

University and Doctoral School

Semmelweis University, Doctoral School of Pharmaceutical Sciences

Supervisor

Dr. Völgyi Gergely

Publication of my abstract

I give consent to the publication of my abstract on the website of the congress.

Kind

Szabad

Status

elfogadva

Accepted presentation method

poszter

Előadás fájl jóváhagyás

nem rendelkezett róla

Előadó

6863

Start

11:05

End

11:10

Authors (legacy)

Szolláth Rita
Semmelweis Univesity, Department of Pharmaceutical Chemistry, Budapest