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.1; Pei L.1; Tong H.H.Y.2; Zheng Y.1![]() | |
2011 | |
Source Publication | AAPS PharmSciTech
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ISSN | 1530-9932 |
Volume | 12Issue:1Pages: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. |
Keyword | Baicalein Bioavailability Solid Dispersion Solvent Evaporation (Se) Spray Freeze Drying (Sfd) |
DOI | https://doi.org/10.1208/s12249-010-9560-3 |
URL | View the original |
Indexed By | SCI |
Language | 英语 |
WOS Research Area | Pharmacology & Pharmacy |
WOS Subject | Pharmacology & Pharmacy |
WOS ID | WOS:000288954100012 |
The Source to Article | Scopus |
Fulltext Access | |
Citation statistics | |
Document Type | Journal article |
Collection | Institute of Chinese Medical Sciences |
Co-First Author | He X. |
Corresponding Author | Zheng Y. |
Affiliation | 1.Institute of Chinese Medical Sciences, University of Macau, Macao SAR, China 2.School of Health Sciences, Macao Polytechnic Institute, Macao SAR, China |
First Author Affilication | Institute of Chinese Medical Sciences |
Corresponding Author Affilication | Institute of Chinese Medical Sciences |
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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