STUDY OF THE PHYSICOCHEMICAL PROPERTIES AND ORAL BIOAVAILABILITY OF THE SOLID DISPERSION OF CANTHARIDIN WITH POLYETHYLENE GLYCOL 4000
STUDY OF THE PHYSICOCHEMICAL PROPERTIES AND ORAL BIOAVAILABILITY OF THE SOLID DISPERSION OF CANTHARIDIN WITH POLYETHYLENE GLYCOL 4000
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DOI：
10.1358/mf.2010.32.3.1423886
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发表时间：
2010-04-01
影响因子：
--
通讯作者：
Zhu, C. Y.
中科院分区：
文献类型：
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作者：
Dang, Y. J.;Hu, C. H.;Zhu, C. Y.
斑蝥素 (CA) 部分溶于水。采用溶剂熔融法将CA（CA-SD）在聚乙二醇4000（PEG 4000）中进行固体分散，以提高其溶出度和口服生物利用度。制备后立即通过差示扫描量热法（DSC）、粉末X射线衍射（PXRD）和扫描电子显微镜（SEM）评估该固体分散体（SD）的理化性质，并研究口服体内生物利用度。在体外实验中，CA通过高压液相色谱法(HPLC)进行分析，在体内实验中通过气相色谱质谱法(GC-MS)进行分析。 SD技术提高了CA的溶解度和溶出率。在大鼠中比较了 CA-SD 和游离 CA 的药代动力学。结果表明，口服给药后CA-SD比游离CA具有更高的生物利用度。通过比较CA和CA-SD的AUC(0-t)，CA-SD与游离CA的相对生物利用度为295.4%。从这些观察结果可以得出结论，CA-SD 比纯 CA 具有更高的吸收率，这与体外溶出结果相符。
Cantharidin (CA) is partially water-soluble. Solid dispersion of CA (CA-SD) in polyethylene glycol 4000 (PEG 4000) was carried out by a solvent-fusion method to increase its dissolution rate and oral bioavailability. The physicochemical properties of this solid dispersion (SD) were evaluated immediately after preparation by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM), and the oral in vivo bioavailability was studied. In in vitro experiments CA was analyzed by high-pressure liquid chromatography (HPLC) and by gas chromatography mass spectrometry (GC-MS) in in vivo experiments. The solubility and dissolution rate of CA were improved by the SD technique. A comparison of the pharmacokinetics between CA-SD and free CA was performed in rats. The results showed that CA-SD had a higher bioavailability than free CA after oral dosing. By comparing the AUC(0-t) of CA and CA-SD, the relative bioavailability of CA-SD to free CA was 295.4%. From these observations it could be concluded that the CA-SD has a higher absorption than pure CA and this corresponds with the dissolution result in vitro.