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Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability.
Pharmaceutics. 2019 Feb 03; 11(2)P

Abstract

In this study, supercritical fluid (SCF) technology was applied to prepare reliable solid dispersions of pharmaceutical compounds with limited bioavailability using ibuprofen (IBU) as a model compound. Solid-state characterization of the dispersions was conducted by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The PXRD and DSC results suggested that the amorphous form of IBU was maintained in the solid dispersions. Furthermore, in vitro dissolution and in vivo pharmacokinetic (PK) studies in rats were also performed. The dissolution performance of the SCF-prepared IBU dispersions was significantly improved compared to that of the physical mixtures of crystalline IBU and a polymer. In addition, the PK results revealed that the SCF-prepared IBU dispersions produced remarkably high blood drug concentrations (both the AUC and Cmax) and a rapid absorption rate (Tmax). Finally, molecular modeling was used to evaluate the binding energy of interactions between IBU and the polymers. The negative binding energy suggests a relatively stable system. Hence, SCF technology can be used as a very effective approach to prepare IBU solid dispersions with good physical stability and enhanced in vitro and in vivo performance.

Authors+Show Affiliations

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. hanfei_spu@163.com.School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. zhangwei9501@126.com.Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. wangying7061blus@163.com. School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China. wangying7061blus@163.com.School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. lnxiziyue@163.com.School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. chenlu182125@163.com.School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. lisanming2018@163.com.School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. xulu@syphu.edu.cn.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30717471

Citation

Han, Fei, et al. "Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions With Improved Oral Bioavailability." Pharmaceutics, vol. 11, no. 2, 2019.
Han F, Zhang W, Wang Y, et al. Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability. Pharmaceutics. 2019;11(2).
Han, F., Zhang, W., Wang, Y., Xi, Z., Chen, L., Li, S., & Xu, L. (2019). Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability. Pharmaceutics, 11(2). https://doi.org/10.3390/pharmaceutics11020067
Han F, et al. Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions With Improved Oral Bioavailability. Pharmaceutics. 2019 Feb 3;11(2) PubMed PMID: 30717471.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability. AU - Han,Fei, AU - Zhang,Wei, AU - Wang,Ying, AU - Xi,Ziyue, AU - Chen,Lu, AU - Li,Sanming, AU - Xu,Lu, Y1 - 2019/02/03/ PY - 2019/01/04/received PY - 2019/01/24/revised PY - 2019/01/31/accepted PY - 2019/2/6/entrez PY - 2019/2/6/pubmed PY - 2019/2/6/medline KW - bioavailability KW - ibuprofen KW - solid dispersion KW - supercritical fluid JF - Pharmaceutics JO - Pharmaceutics VL - 11 IS - 2 N2 - In this study, supercritical fluid (SCF) technology was applied to prepare reliable solid dispersions of pharmaceutical compounds with limited bioavailability using ibuprofen (IBU) as a model compound. Solid-state characterization of the dispersions was conducted by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The PXRD and DSC results suggested that the amorphous form of IBU was maintained in the solid dispersions. Furthermore, in vitro dissolution and in vivo pharmacokinetic (PK) studies in rats were also performed. The dissolution performance of the SCF-prepared IBU dispersions was significantly improved compared to that of the physical mixtures of crystalline IBU and a polymer. In addition, the PK results revealed that the SCF-prepared IBU dispersions produced remarkably high blood drug concentrations (both the AUC and Cmax) and a rapid absorption rate (Tmax). Finally, molecular modeling was used to evaluate the binding energy of interactions between IBU and the polymers. The negative binding energy suggests a relatively stable system. Hence, SCF technology can be used as a very effective approach to prepare IBU solid dispersions with good physical stability and enhanced in vitro and in vivo performance. SN - 1999-4923 UR - https://www.unboundmedicine.com/medline/citation/30717471/Applying_Supercritical_Fluid_Technology_to_Prepare_Ibuprofen_Solid_Dispersions_with_Improved_Oral_Bioavailability_ L2 - https://www.mdpi.com/resolver?pii=pharmaceutics11020067 DB - PRIME DP - Unbound Medicine ER -
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