PVP and surfactant combined carrier as an effective absorption enhancer of poorly soluble astilbin in vitro and in vivo
PVP and surfactant combined carrier as an effective absorption enhancer of poorly soluble astilbin in vitro and in vivo
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PVP与表面活性剂复合载体作为难溶性落新妇苷体内外有效吸收促进剂
DOI：
10.3109/03639045.2012.756008
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发表时间：
2014-01
期刊：
影响因子：
--
通讯作者：
He Y, Liu H, Xie Z, Liao Q, Lai X, Du Z.
中科院分区：
文献类型：
--
作者：
He Y, Liu H, Xie Z, Liao Q, Lai X, Du Z.
抽象上下文：落新妇苷被认为是治疗免疫相关疾病的新型免疫抑制剂，但由于其水溶性差，口服吸收困难，生物利用度低，限制了其临床应用。目的：研究聚乙烯吡咯烷酮（PVP）与表面活性剂复合载体对药物吸收的影响。材料与方法：将PVP K30-Tween 80组合载体应用于落新妇苷固体分散体中，在Beagle犬体内和在Caco-2细胞单层的体外转运实验中进行测试。结果和讨论：在动物研究中，与活性药物成分（API）相比，观察到药物在PVP K 30-吐温80组合载体中的固体分散体的血浆AUC增加许多倍。Caco-2单层作为预测落新妇苷与溶解度增强载体组合的体内转运行为的工具的适用性被示出。体外转运研究证实了组合载体对落新妇苷吸收行为的影响。MTT研究表明，落新妇苷和固体分散体中的细胞活力随着药物浓度的增加而逐渐下降，并呈剂量依赖性。Caco-2细胞的渗透性和表观渗透系数（Papp）随药物浓度的增加而增加。结论：PVP K30和吐温80在一定量范围内对药物的促渗作用最好。PVP K30与表面活性剂联合载体对落新妇苷的口服生物利用度有较强的提高潜力。
Abstract Context: Astilbin is considered to be a new and promising immunosuppressant for immune related diseases, but limited in clinical application due to its poor water solubility, difficult oral absorption and low bioavailability. Objective: The present work studied the effect of PVP and surfactant combined carrier on its capability to improve drug absorption. Materials and methods: PVP K30-Tween 80 combined carries was applied into the astilbin solid dispersions, tested both in vivo in beagle dogs and in vitro in transport experiments across Caco-2 cell monolayers. Results and discussion: In the animal studies a many fold increase in plasma AUC was observed for the solid dispersions of drug in PVP K30-Tween 80 combined carries compared to active pharmaceutical ingredient (API). The applicability of Caco-2 monolayers as a tool for predicting the in vivo transport behavior of Astilbin in combination with a solubility enhancing carries was shown. In vitro transport studies confirmed the effect of combined carries on the absorption behavior of the astilbin. MTT studies showed the cell viability gradually decreased with the increase of the drug concentration in a dose dependent manner for astilbin and that in solid dispersions. The permeability and apparent permeability coefficients (Papp) increased with drug in the Caco-2 cell. Conclusion: In this study, it was found that PVP K30 and Tween 80 promoted the permeability of drugs best within a certain amount. For astilbin PVP K30 and surfactant combined carrier had a strong potential to improve oral bioavailability.
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影响因子：
--
作者：
Zou Jie-ming
通讯作者：
Zou Jie-ming
DOI：
10.3109/13880209309082916
发表时间：
1993
期刊：
--
影响因子：
--
作者：
Eliane Carneiro;J. Calixto;F. Monache;R. Yunes
通讯作者：
Eliane Carneiro;J. Calixto;F. Monache;R. Yunes
DOI：
10.4268/cjcmm20100612
发表时间：
2010-03
期刊：
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica
影响因子：
--
作者：
Chao Wang;Liping Zhu;Jing-zhi Yang;Chuang-jun Li;Dongming Zhang
通讯作者：
Chao Wang;Liping Zhu;Jing-zhi Yang;Chuang-jun Li;Dongming Zhang
DOI：
--
发表时间：
1998-11
期刊：
Yao xue xue bao = Acta pharmaceutica Sinica
影响因子：
--
作者：
Y. Yi;Z. Cao;D. Yang;Y. Cao;Y. Wu;S. Zhao
通讯作者：
Y. Yi;Z. Cao;D. Yang;Y. Cao;Y. Wu;S. Zhao
影响因子：
3.4
作者：
S. Vithlani;S. Sarraf;C. Chaw
通讯作者：
S. Vithlani;S. Sarraf;C. Chaw