| DOI: 10.29090/psa.2021.05.20.090 | Pharm Sci Asia 2021; 48(5), 432-449 |
Low density alfuzosin hydrochloride floating tablets: in vitro characterization and in vivo gastroretentive MRI tracking in healthy volunteersMarwa Abd El-Aziz1, Soha Ismail1, Mina Ibrahim Tadros2*, Mohamed El-Nabarawi2
1 Department of Pharmaceutics, National Organization for Drug Control and Research, Giza, Egypt
2
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt
The current work aimed to develop promising floating sustained release systems for alfuzosin hydrochloride (ALF) utilizing sublimation technique. Gastroretentive tablets were prepared by direct compression and subsequent sublimation of the loaded sublimable agents. Polyethylene oxide WSR N-60K (PEO) or Carbopol 934 (CP) were used as release retarding polymers. Camphor or menthol were used as sublimable agents at concentrations of 3%, 6%, 9% or 12% w/w. FTIR and DSC were performed to check possible drug-excipients incompatibility. The tablets were evaluated for appearance, hardness, friability, density, floating characters, and in-vitro drug release. The drug release percentages after 0.5h (Q0.5h) and 8h (Q8h) were estimated. Based on estimation of the desirability values, the best-achieved formula (F1) was morphologically evaluated via SEM. The gastroretentive tracking of the magnetite-loaded F1 tablets was performed via MRI in healthy human volunteers. FT-IR spectra and DSC thermograms confirmed drug-excipients compatibility. PEO- and CP-based systems exhibited acceptable physicochemical characteristics regarding their appearance, hardness and friability. They exhibited low bulk density values (< 1 g/cm3) allowing them to float spontaneously (zero lag times), for at least 8h. Significantly higher (p<0.0001) Q0.5h were revealed with CP-based tablets. No significant difference (p=0.3529) was elucidated between Q8h values of the corresponding CP-based and PEO-based tablets. Following sublimation, SEM micrographs of F1 confirmed the presence of a low bulk density porous matrix. The gastroretentive potential of F1 was suggested for at least 5 h in healthy human volunteers. F1 is a promising gastroretentive system for ALF.
Keyword:
Alfuzosin hydrochloride, Floating porous tablets, Sustained release, Sublimation, Gastroretentive tracking, Magnetic resonance imaging
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