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首页> 外文期刊>Journal of Applied Polymer Science >Inclusion complex of cantharidin with β-cyclodextrin: Preparation, characterization, in vitro and in vivo evaluation
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Inclusion complex of cantharidin with β-cyclodextrin: Preparation, characterization, in vitro and in vivo evaluation

机译：can鱼ari素与β-环糊精的包合物：制备，表征，体内外评价

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摘要

Because of low aqueous solubility and slow dissolution rate, cantharidin has a low oral bioavailability. Our research aims to prepare the inclusion complex of cantharidin and β-cyclodextrin (β-CD) and accomplish characterization, in vitro and in vivo evaluation. CA-β-CD inclusion complex was prepared by saturated solution method. The CA was demonstrated by HPLC in vitro experiment and by GC-MS in vivo experiment. CA-β-CD inclusion complex was characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and nuclear magnetic resonance (NMR). Through complexation with β-CD, the solubility of CA in neutral aqueous solution was improved significantly. CA-β-CD inclusion complex also shows a significantly improved dissolution rate in comparison with free CA. Comparison of the pharmacokinetics between CA-β-CD inclusion complex and free CA was performed in rats. The in vivo results show that CA-β-CD inclusion complex has earlier t_(max), higher C_(max), and higher bioavailability than free CA after oral dosing. By comparing the AUC_(0-t) of CA and CA-β-CD inclusion complex, the relative bioavailability of CA-β-CD inclusion complex to free CA was 506.3%, which highlighted the evidence of significantly improved bioavailability of formulation of CA with β-CD. Thus, this β-CD-based drug delivery system should be an effective oral dosage form to improve oral bioavailability of CA.
机译：由于水溶性低和溶解速度慢，can鱼din素的口服生物利用度低。我们的研究旨在制备邻苯二酚和β-环糊精（β-CD）的包合物，并完成表征，体外和体内评估。采用饱和溶液法制备CA-β-CD包合物。通过HPLC的体外实验和GC-MS的体内实验证明了CA。 CA-β-CD包合物的特征在于差示扫描量热法（DSC），X射线衍射法（XRD）和核磁共振（NMR）。通过与β-CD的络合，CA在中性水溶液中的溶解度显着提高。与游离CA相比，CA-β-CD包涵体复合物还显示出显着改善的溶出速率。在大鼠中比较了CA-β-CD包涵体复合物和游离CA的药代动力学。体内结果表明，口服CA-β-CD包合物比游离CA具有更早的t_（max），更高的C_（max）和更高的生物利用度。通过比较CA和CA-β-CD包合物的AUC_（0-t），CA-β-CD包合物对游离CA的相对生物利用度为506.3％，这突显了CA制剂生物利用度显着提高的证据。与β-CD。因此，这种基于β-CD的药物递送系统应该是有效的口服剂型，以提高CA的口服生物利用度。

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