Comparison of spray freeze drying and the solvent evaporation method for preparing solid dispersions of baicalein with pluronic F68 to improve dissolution and oral bioavailability

doi:10.1208/s12249-010-9560-3

	Comparison of spray freeze drying and the solvent evaporation method for preparing solid dispersions of baicalein with pluronic F68 to improve dissolution and oral bioavailability
	He X.; Pei L.; Tong H.H.Y.; Zheng Y.
	2011
Source Publication	AAPS PharmSciTech
ISSN	15309932
Volume	12 Issue:1 Pages:104
Abstract	The objective of this study was to prepare solid dispersions consisting of baicalein and a carrier with a low glass transition/melting point (Pluronic F68) by spray freeze drying (SFD). We compared these powders to those produced from the conventional solvent evaporation method. In the SFD process, a feeding solution was atomized above the surface of liquid nitrogen following lyophilization, which resulted in instantaneously frozen microparticles. However, solid dispersions prepared by the solvent evaporation method formed a sticky layer on the glass flask with crystalline baicalein separated out from the carrier. The powder samples were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), surface area measurement, differential scanning calorimetry, and Fourier transform infrared spectrometry. SEM and PXRD results suggested that the majority of baicalein in the SFD-processed solid dispersion was in the amorphous state, which has a higher specific surface area than pure baicalein. However, the majority of baicalein was recrystallized in the solid dispersion at the same composition prepared by the solvent evaporation method, which showed a similar dissolution rate to the physical mixture. SFD product was physically and chemically stable after being stored at 40°C with low humidity for 6 months. After enzyme hydrolysis, baicalein in the SFD product displayed a significantly shorter T max and higher C max than pure baicalein after oral dosing. The relative bioavailability of the SFD product versus pure baicalein determined by comparing the AUC0-12 was 233%, which demonstrated the significantly improved oral bioavailability of baicalein produced by the SFD technique. © 2010 American Association of Pharmaceutical Scientists.
Keyword	baicalein bioavailability solid dispersion solvent evaporation (SE) spray freeze drying (SFD)
DOI	10.1208/s12249-010-9560-3
URL	View the original
Language	英语
The Source to Article	Scopus
Fulltext Access	View Full-Text via DOI View Full-Text via Web of Science View Full-Text via Scopus
Citation statistics	Cited Times [WOS]:42 [WOS Record] [Related Records in WOS]
Document Type	Journal article
Collection	University of Macau
Recommended Citation GB/T 7714	He X.,Pei L.,Tong H.H.Y.,et al. Comparison of spray freeze drying and the solvent evaporation method for preparing solid dispersions of baicalein with pluronic F68 to improve dissolution and oral bioavailability[J]. AAPS PharmSciTech,2011,12(1):104.
APA	He X.,Pei L.,Tong H.H.Y.,&Zheng Y..(2011).Comparison of spray freeze drying and the solvent evaporation method for preparing solid dispersions of baicalein with pluronic F68 to improve dissolution and oral bioavailability.AAPS PharmSciTech,12(1),104.
MLA	He X.,et al."Comparison of spray freeze drying and the solvent evaporation method for preparing solid dispersions of baicalein with pluronic F68 to improve dissolution and oral bioavailability".AAPS PharmSciTech 12.1(2011):104.

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