Xu H, Zhang T, Yang H, Xiao X, Bian Y, Si D, Liu C
The National Laboratory of Pharmacodynamics and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China.
Indian J Pharm Sci. 2011 May;73(3):276-81. doi: 10.4103/0250-474X.93511.
In order to increase the dissolution rate and bioavailability, solid dispersions of evodiamine in PVP K(30) with different enriched samples of evodiamine to PVP K(30) ratios were prepared by solvent method. Our studies showed that the dissolution rate of evodiamine was significantly higher in the solid dispersion system in comparison with that in enriched samples of evodiamine or physical mixtures. The increase of the dissolution rate was evidently related to the ratio of evodiamine to PVP K(30). The solid dispersion system (enriched samples of evodiamine/PVP K(30)= 1/6, w/w) gave the highest dissolution rate: about 27.7-fold higher than that of enriched samples of evodiamine in hard capsules. Powder X-ray diffraction studies showed that enriched samples of evodiamine presented a total chemical stability after its preparation as solid dispersions. In vivo administration studies indicated that solid dispersions of evodiamine in hard capsules had a higher C(max) and a shorter T(max) than those of physical mixture in hard capsules, and the differences of C(max) and T(max) between them were significant. These results suggest that solid dispersions of evodiamine in hard capsules has a notably faster and greater absorption rate than enriched samples of evodiamine in physical mixture hard capsule and corresponds with the in vitro dissolution.
为提高吴茱萸碱的溶出速率和生物利用度，采用溶剂法制备了吴茱萸碱与不同吴茱萸碱富集样品与聚乙烯吡咯烷酮K（30）比例的固体分散体。我们的研究表明，与吴茱萸碱富集样品或物理混合物相比，吴茱萸碱在固体分散体系统中的溶出速率显著更高。溶出速率的提高明显与吴茱萸碱与聚乙烯吡咯烷酮K（30）的比例有关。固体分散体系统（吴茱萸碱富集样品/聚乙烯吡咯烷酮K（30）=1/6，w/w）的溶出速率最高：比硬胶囊中吴茱萸碱富集样品的溶出速率高约27.7倍。粉末X射线衍射研究表明，吴茱萸碱富集样品制成固体分散体后具有完全的化学稳定性。体内给药研究表明，硬胶囊中吴茱萸碱固体分散体的C（max）高于硬胶囊中物理混合物的C（max），T（max）短于硬胶囊中物理混合物的T（max），且两者之间的C（max）和T（max）差异显著。这些结果表明，硬胶囊中吴茱萸碱固体分散体的吸收速率比物理混合物硬胶囊中吴茱萸碱富集样品的吸收速率明显更快、更高，且与体外溶出情况相符。
