PhD Scientific Days 2025

Poster Session III. - H: Pharmaceutical Sciences and Health Technologies

Evaluation Methods for Measuring Amorphous and Kinetic Solubility

Előadó neve

Dr. Szolláth Rita

Neptun code

OWGGMO

Előadó munkahelye

Semmelweis University, Department of Pharmaceutical Chemistry

Előadó telefonszáma

+36302535139

Előadó e-mail címe

szollath.rita.mariann@semmelweis.hu

Az előadás címe

Evaluation Methods for Measuring Amorphous and Kinetic Solubility

Szerző(k) neve és munkahelye

Dr. Rita Szolláth¹

1: Semmelweis University Department of Pharmaceutical Chemistry

Bemutatás módja

Poszter

Szekció

Poster Session III. - H: Pharmaceutical Sciences and Health Technologies

Language of the presentation

Hungarian

Preferred session

Pharmaceutical Sciences and Health Technologies

Összefoglaló szövege

The bioavailability of a drug is greatly influenced by its solubility, therefore it is important to know the solubility of a drug in an early state of drug development.
Nowadays, as the proportion of pharmaceutical formulations that rely on nanonization, amorphous active ingredient formulations, or using other methods to achieve supersaturation is increasing, more and more emphasis is being placed on determining kinetic and amorphous solubility.
Kinetic solubility is the concentration that can be measured when a precipitate first appears in the solution. Amorphous solubility is the maximum concentration that a solution of the substance can reach, it is the maximum degree of supersaturation. There are different methods for its theoretical estimation and experimental determination. By exceeding amorphous solubility, a new phase rich in active substance can be created, called liquid-liquid phase separation (LLPS).
Kinetic solubility can be determined by using an auxiliary solvent, changing pH, and dissolving ASDs. There are also different methods for interpreting the data, which can lead to different results to varying degrees, thereby questioning the validity.
Our aim was to investigate the effect of using different evaluation methods on the same data, to check, which could be the best suited for interpreting the results. Molecules belonging to BCS II with different acid-base characteristics were chosen as model compunds. The pH was always set to values where the molecule is in its neutral form. Measurements were carried out at 37 °C, aliquots of stock solution were added to a continuously stirred glass vial containing the buffer, and the absorbance was measured with in-line UV probes. Three paralel measurements were carried out for each substance. Three different evaluation methods were chosen: detection based on the 2nd derivate of the spectra, baseline elevation, and Zero Intercept Method (ZIM).
In all cases, ZIM produced the lowest results. The results evaluated based on the second derivative and the baseline elevation are significantly higher than those calculated with ZIM. The degree of discrepancies were different for each molecule.
Choosing the right type of method to evaluate our data can be crucial in determining solubility values. These results show, how important it is to know how different evaluation methods can influence our results.

University

Semmelweis University

Supervisor

Mazák Károly

Publication of my abstract

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

phd.section.field

in doctoral studies after complex exam (PhD)

Kind

Szabad

Status

elfogadva

Accepted presentation method

poszter

Előadás fájl jóváhagyás

nem rendelkezett róla

Előadó

6863

Start

14:36

End

14:42