title: In-Vitro Characterization and Oral Bioavailability of Organic Solvent-free Solid Dispersions Containing Telmisartan.
abstract: Poorly water-soluble drugs often suffer from limited or irreproducible clinical response due to their low solubility and dissolution rate. In this study, organic solvent-free solid dispersions (OSF-SDs) containing telmisartan (TEL) were prepared using polyvinylpyrrolidone K30 (PVP K30) and polyethylene glycol 6000 (PEG 6000) as hydrophilic polymers, sodium hydroxide (NaOH) as an alkalizer, and poloxamer 188 as a surfactant by a lyophilization method. In-vitro dissolution rate and physicochemical properties of the OSF-SDs were characterized using the USP I basket method, differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and fourier transform-infrared (FT-IR) spectroscopy. In addition, the oral bioavailability of OSF-SDs in rats was evaluated by using TEL bulk powder as a reference. The dissolution rates of the OSF-SDs were significantly enhanced as compared to TEL bulk powder. The results from DSC, XRD showed that TEL was molecularly dispersed in the OSF-SDs as an amorphous form. The FT-IR results suggested that intermolecular hydrogen bonding had formed between TEL and its carriers. The OSF-SDs exhibited significantly higher AUC0-24 h and Cmax, but similar Tmax as compared to the reference. This study demonstrated that OSF-SDs can be a promising method to enhance the dissolution rate and oral bioavailability of TEL.
authors.affiliation: College of Pharmaceutical Sciences, Soochow University, Suzhou, 199 Ren-Ai Road, Suzhou Industrial Park, Jiangsu, 215123, China.
authors.forename: Yue
authors.initials: Y
authors.lastname: Cao
authors.affiliation: College of Pharmaceutical Sciences, Soochow University, Suzhou, 199 Ren-Ai Road, Suzhou Industrial Park, Jiangsu, 215123, China.
authors.forename: Li-Li
authors.initials: LL
authors.lastname: Shi
authors.affiliation: College of Pharmaceutical Sciences, Soochow University, Suzhou, 199 Ren-Ai Road, Suzhou Industrial Park, Jiangsu, 215123, China.
authors.forename: Qing-Ri
authors.initials: QR
authors.lastname: Cao
authors.affiliation: Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
authors.forename: Mingshi
authors.initials: M
authors.lastname: Yang
authors.affiliation: College of Pharmaceutical Sciences, Soochow University, Suzhou, 199 Ren-Ai Road, Suzhou Industrial Park, Jiangsu, 215123, China.
authors.forename: Jing-Hao
authors.initials: JH
authors.lastname: Cui
keywords: In-vitro characterization; Oral bioavailability; Organic Solvent-free; Solid dispersions; Telmisartan