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Copyright @ Pol J Cosmetol
 
ISSN 1731-0083
Saturday, 08.02.2025
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Pol J Cosmetol 2023, 26(1): 40-48pladd to cart

Pharmaceutical availability of bezafibrate from a model tablet containing non-ionic surfactants in the formulation


Marian M. Zgoda 1/, Michał J. Nachajski 2/, Michał K. Kołodziejczyk 2/, Sławomira Nowak 3/, Zbigniew Marczyński 4/, Magdalena Piechota-Urbańska 4/, Andrzej Stańczak 4/

1/ Wyższa Szkoła Kosmetyki i Nauk o Zdrowiu w Łodzi
2/ Zakład Technologii Postaci Leku, Katedra Farmacji Stosowanej, Uniwersytet Medyczny w Łodzi
3/ Katedra i Zakład Farmakognozji, Uniwersytet Medyczny w Łodzi
4/ Zakład Farmacji Aptecznej, Katedra Farmacji Stosowanej, Uniwersytet Medyczny w Łodzi

Summary
Introduction. Bezafibrate is a derivative of fibric acid, it is characterized by a strong hypolipemic effect by inhibiting the synthesis of cholesterol and reducing its share in the LDL fraction. The bioavailability of the lipophilic bezafibrate structure (a gemini molecule, a compound that is sparingly soluble in water) depends in vivo on the physiological solubilizing capacity of bile A (duodenal content, Lindblat index).
Aim. In the presence of Vivapur 200 (a fast disintegrating tablet), in artificial intestinal juice with pH(aH+)=6.80, there was analyzed the quantitative course of bezafibrate solubilization process by micellar solutions of non-ionic surfactants compatible with bile A of cholesterol ethoxylation products, ursodeoxycholic acid and rapeseed oil acid methyl esters (Rofams of nTE=50 and 60).
Material and methods. With the participation of Vivapur 200, a model fast disintegrating tablet was manufactured, in which the formulation composition included ethoxylated ursodeoxycholic acid cholesterol derivatives and Rofams with nTE=50 and 60 as excipients. Appropriate mathematical models, including the Higuichi, Krosmeyer-Peppas and Hix-Crowell equations, were used to quantify the process of micellar solubilization of bezafibrate.
Results. Calculated area regardless of the analyzed mathematical model, enables the identification of those non-ionic surfactants that effectively solubilize bezafibrate in in vitro conditions. They can be the basis for designing an original form of the preparation for the treatment of cholesterolemia and cholelithiasis.
Conclusions. Ethoxylated cholesterol derivative with nTE=50 and Rofams with nTE=50 and 60, due to their physicochemical and gravimetric properties may be an inspiration for the manufacturing of a model solid drug form (fast disintegrating tablet) by direct tableting. The presence of the discussed classes of non-ionic surfactants in the form of the preparation may, under physiological conditions (in vivo), supplement the lithogenolytic index of bile A (Lindblat index).

Key words: bezafibrate, Vivapur 200, fast disintegrating tablet, micellar solubilization, mathematical models