Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti · 2026
Justification of a medicinal form development based on the api dimethylammonium 3-methyl-2-(2-((e)-styryl)quinazolin-4-ylthio)butanoate with hepatoprotective and antioxidant effects for the needs of military medicine.
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Avramenko Antonina, Kaplaushenko Andrii, Salionov Volodymyr
Аннотация
OBJECTIVE: The study aims to substantiate the development of an oral dosage form for military medicine based on the API dimethylammonium 3-methyl-2-(2-((E)-styryl)quinazolin-4-ylthio)butanoate, which demonstrates antioxidant and hepatoprotective activity. The molecule's physicochemical properties and dissociation constant were evaluated.
MATERIALS AND METHODS: Computer modelling was used to assess lipophilicity, physicochemical parameters, and ADME characteristics via the SwissADME service. Drug-likeness was evaluated according to Lipinski's Rule of Five. Conductometric studies of API solutions (0.0625-0.5 M) were performed with a Konduktometr N 5721 M to determine χ, λv, λ∞, α, and the dissociation constant (7.45 × 10-8-9.2 × 10-8). The ionization constant was used to calculate pK = 7.13, indicating the pH range of optimal absorption.
RESULTS: ADME analysis showed high gastrointestinal absorption and suitable solubility, supporting the feasibility of an oral dosage form. Conductometric data confirmed the API to be a weak electrolyte with increasing dissociation at lower concentrations. The pK value suggests preferential absorption in the neutral to slightly alkaline environment of the small intestine. Considering its pharmacological activity, the API is promising for further development of tablets or capsules for military and clinical use.
CONCLUSIONS: The findings justify designing a gastro-resistant oral dosage form ensuring API stability in gastric acid and efficient intestinal absorption. Such a form is particularly valuable for military medicine due to its stability, portability, and suitability for emergency and rehabilitation settings.
MATERIALS AND METHODS: Computer modelling was used to assess lipophilicity, physicochemical parameters, and ADME characteristics via the SwissADME service. Drug-likeness was evaluated according to Lipinski's Rule of Five. Conductometric studies of API solutions (0.0625-0.5 M) were performed with a Konduktometr N 5721 M to determine χ, λv, λ∞, α, and the dissociation constant (7.45 × 10-8-9.2 × 10-8). The ionization constant was used to calculate pK = 7.13, indicating the pH range of optimal absorption.
RESULTS: ADME analysis showed high gastrointestinal absorption and suitable solubility, supporting the feasibility of an oral dosage form. Conductometric data confirmed the API to be a weak electrolyte with increasing dissociation at lower concentrations. The pK value suggests preferential absorption in the neutral to slightly alkaline environment of the small intestine. Considering its pharmacological activity, the API is promising for further development of tablets or capsules for military and clinical use.
CONCLUSIONS: The findings justify designing a gastro-resistant oral dosage form ensuring API stability in gastric acid and efficient intestinal absorption. Such a form is particularly valuable for military medicine due to its stability, portability, and suitability for emergency and rehabilitation settings.