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Preparation of osthole-polymer solid dispersions by hot-melt extrusion for dissolution and bioavailability enhancement.
Int J Pharm. 2014 Apr 25; 465(1-2):436-43.IJ

Abstract

The aim of this study was to investigate the potential of solid dispersion to improve the dissolution rate and bioavailability of osthole (Ost), a coumarin derivative with various pharmacological activities but with poor aqueous solubility. In present studies, the Ost solid dispersions were prepared with various polymers including Plasdone S-630, HPMC-E5, Eudragit EPO, and Soluplus by hot-melt extrusion method. In vitro characterizations were performed with differential scanning calorimetry (DSC), X-ray powder diffraction (XPRD), Fourier transform infrared (FT-IR) spectroscopy, and in vitro dissolution studies. In addition, in vivo pharmacokinetic studies of Ost solid dispersions were also conducted in rats after a single oral dose. In comparison to the untreated Ost coarse powder and the physical mixture with polymers, the solid dispersions prepared with Plasdone S-630 or HPMC-E5 (drug/polymer: 1:6) showed a significant enhancement of dissolution rate (∼3-fold higher D30). In addition, such preparations exhibited a significantly decreased Tmax, ∼5-fold higher Cmax and ∼1.4-fold higher AUC when comparing with Ost coarse powder. In conclusion, solid dispersion prepared with appropriate polymer could serve as a promising formulation approach to enhance the dissolution rate and hence oral bioavailability of Ost.

Authors+Show Affiliations

School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Street, Nanjing 210046, China.School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Street, Nanjing 210046, China.First College of Clinical Medicine, Nanjing University of Chinese Medicine, 138 Xianlin Street, Nanjing 210046, China.School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Street, Nanjing 210046, China.School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Street, Nanjing 210046, China.School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Street, Nanjing 210046, China.School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Street, Nanjing 210046, China. Electronic address: diliuqing@hotmail.com.

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24576810

Citation

Yun, Fei, et al. "Preparation of Osthole-polymer Solid Dispersions By Hot-melt Extrusion for Dissolution and Bioavailability Enhancement." International Journal of Pharmaceutics, vol. 465, no. 1-2, 2014, pp. 436-43.
Yun F, Kang A, Shan J, et al. Preparation of osthole-polymer solid dispersions by hot-melt extrusion for dissolution and bioavailability enhancement. Int J Pharm. 2014;465(1-2):436-43.
Yun, F., Kang, A., Shan, J., Zhao, X., Bi, X., Li, J., & Di, L. (2014). Preparation of osthole-polymer solid dispersions by hot-melt extrusion for dissolution and bioavailability enhancement. International Journal of Pharmaceutics, 465(1-2), 436-43. https://doi.org/10.1016/j.ijpharm.2014.02.040
Yun F, et al. Preparation of Osthole-polymer Solid Dispersions By Hot-melt Extrusion for Dissolution and Bioavailability Enhancement. Int J Pharm. 2014 Apr 25;465(1-2):436-43. PubMed PMID: 24576810.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation of osthole-polymer solid dispersions by hot-melt extrusion for dissolution and bioavailability enhancement. AU - Yun,Fei, AU - Kang,An, AU - Shan,Jinjun, AU - Zhao,Xiaoli, AU - Bi,Xiaolin, AU - Li,Junsong, AU - Di,Liuqing, Y1 - 2014/02/25/ PY - 2013/10/08/received PY - 2014/01/17/revised PY - 2014/02/23/accepted PY - 2014/3/1/entrez PY - 2014/3/1/pubmed PY - 2014/12/17/medline KW - Bioavailability KW - Dissolution rate KW - Hot-melt extrusion KW - Osthole KW - Solid dispersion KW - Solubility parameter SP - 436 EP - 43 JF - International journal of pharmaceutics JO - Int J Pharm VL - 465 IS - 1-2 N2 - The aim of this study was to investigate the potential of solid dispersion to improve the dissolution rate and bioavailability of osthole (Ost), a coumarin derivative with various pharmacological activities but with poor aqueous solubility. In present studies, the Ost solid dispersions were prepared with various polymers including Plasdone S-630, HPMC-E5, Eudragit EPO, and Soluplus by hot-melt extrusion method. In vitro characterizations were performed with differential scanning calorimetry (DSC), X-ray powder diffraction (XPRD), Fourier transform infrared (FT-IR) spectroscopy, and in vitro dissolution studies. In addition, in vivo pharmacokinetic studies of Ost solid dispersions were also conducted in rats after a single oral dose. In comparison to the untreated Ost coarse powder and the physical mixture with polymers, the solid dispersions prepared with Plasdone S-630 or HPMC-E5 (drug/polymer: 1:6) showed a significant enhancement of dissolution rate (∼3-fold higher D30). In addition, such preparations exhibited a significantly decreased Tmax, ∼5-fold higher Cmax and ∼1.4-fold higher AUC when comparing with Ost coarse powder. In conclusion, solid dispersion prepared with appropriate polymer could serve as a promising formulation approach to enhance the dissolution rate and hence oral bioavailability of Ost. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/24576810/Preparation_of_osthole_polymer_solid_dispersions_by_hot_melt_extrusion_for_dissolution_and_bioavailability_enhancement_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(14)00133-1 DB - PRIME DP - Unbound Medicine ER -