Category: Formulation and Quality
Purpose: The purpose of this research was to develop a novel revaprazan-loaded surface-modified solid dispersion (SMSD) with improved drug solubility and oral bioavailability.
Methods: The impact of carriers on aqueous solubility of revaprazan was investigated. HPMC and Cremophor A25 were selected as an appropriate polymer and surfactant, respectively, due to their high drug solubility. Numerous SMSDs were prepared with various concentrations of carriers, using distilled water, and the drug solubility of each was assessed. Moreover, the physicochemical properties, dissolution and pharmacokinetics of selected SMSD in rats were assessed in comparison to revaprazan powder.
Results: Of the SMSDs assessed, the SMSD composed of revaprazan/HPMC/Cremophor A25 at the weight ratio of 1:0.28:1.12 had the most enhanced drug solubility (approximately 6,000-fold). It was characterized by particles with a relatively rough surface, suggesting that the carriers were attached onto the surface of the unchanged crystalline revaprazan powder. It had a significantly higher dissolution rate, AUC and Cmax, and a faster Tmax value in comparison to revaprazan powder, with a 5.3-fold improvement in oral bioavailability of revaprazan.
Conclusion: From an environmental perspective, this SMSD system prepared with water, and without organic solvents, should be recommended as a revaprazan-loaded oral pharmaceutical alternative.
Dong Shik Kim– Hanyang University, Ansan, Kyonggi-do, Republic of Korea
Yoo Jin Choi– Ansan, Kyonggi-do, Republic of Korea
Mi Ran Woo– Ansan-si, Kyonggi-do, Republic of Korea
Ji eun Choi– Cheonan-si, Ch'ungch'ong-namdo, Republic of Korea
Bo Kyun Kim– Student, Yeungnam University, Gyeongsan-si, Kyongsang-bukto, Republic of Korea
Chul Soon Yong– College of Pharmacy, Yeungnam University, South Korea, Gyeongsan, Kyongsang-bukto, Republic of Korea
Jong Oh Kim– College of Pharmacy, Yeungnam University, South Korea, Gyeongsan, Kyongsang-bukto, Republic of Korea
Sung Giu Jin– Department of Pharmaceutical Engineering, Dankook University, South Korea, Cheonan-si, Ch'ungch'ong-namdo, Republic of Korea
Han-Gon Choi– College of Pharmacy, Hanyang University, South Korea, Ansan-si, Kyonggi-do, Republic of Korea