Design and Evaluation of Novel Solid Self-Nanodispersion Delivery System for Andrographolide
Design and Evaluation of Novel Solid Self-Nanodispersion Delivery System for Andrographolide
复制标题
穿心莲内酯新型固体自纳米分散递送系统的设计与评价
DOI：
10.1208/s12249-016-0627-7
复制
发表时间：
2016-09
影响因子：
3.3
通讯作者：
Ming Yang
中科院分区：
文献类型：
--
作者：
Junnan Xu;Yueqin Ma;Yuanbiao Xie;Yingchong Chen;Yang Liu;Pengfei Yue;Ming Yang
难于溶于水的药物给开发具有足够生物利用度的制剂产品带来了挑战。为了提高穿心莲内酯的溶出度，提高其生物利用度，本研究利用穿心莲内酯的纳米特性和直接压片技术，开发了一种新型的穿心莲内酯固体自纳米分散系统。采用均质技术制备了粒径约为500 nm的Andro纳米悬浮液(Andro-NS)，并通过喷雾干燥将其转化为干燥的纳米晶颗粒(Andro-NP)。采用直接压制法制备了固体自纳米分散系统(ANDRO-SNDS)-ANDRO-NP。差示扫描量热法(DSC)和X射线衍射法(PXRD)结果表明，ANDRO纳米晶保持了原有的结晶度。Andro-SNDS在纯水中30min的溶出度为85.87%，优于粗品Andro和Andro与稳定剂的物理混合物。ANDRO-SNDS制剂的Cmax(299.32 ± 78.54 ng/mL)和AUC0-∞(4440.55 ± 764.13 mg/L · h)显著高于ANDRO粗品(77.52 ± 31.73 ng/mL和1437.79 ± 354.25 mg/L · · h)。Andro-snds的AUC是原始Andro的3.09倍。这项研究展示了一种新的方法，将纳米晶和复合颗粒的特性结合起来，用于提高难溶药物的口服生物利用度。
Poorly water-soluble drugs offer challenges in developing a formulation product with adequate bioavailability. This study took advantage of the features of nanocrystals and direct compression technologies to develop a novel solid self-nanodispersion delivery system for andrographolide (Andro) in order to increase its dissolution rate for enhancing bioavailability. Andro nanosuspensions (Andro-NS) with a particle size of about 500 nm were prepared by homogenization technology and further converted into dried nanocrystal particles (Andro-NP) via spray-drying. The solid self-nanodispersion delivery system (Andro-SNDS)-loaded Andro-NP was prepared via direct compression technology. The DSC and PXRD results demonstrated that the Andro nanocrystals retained its original crystallinity. The dissolution of the Andro-SNDS formulation was 85.87% in pure water over 30 min, better than those of the coarse Andro and physical mixture of Andro and stabilizer. And the Cmax (299.32 ± 78.54 ng/mL) and AUC0-∞ (4440.55 ± 764.13 mg/L · h) of the Andro-SNDS formulation were significantly higher (p < 0.05) than those of the crude Andro (77.52 ± 31.73 ng/mL and 1437.79 ± 354.25 mg/L · h). The AUC of the Andro-SNDS was 3.09 times as high as that of the crude Andro. This study illustrated a novel approach to combine the features of nanocrystals and composite particles used to improve oral bioavailability of poorly soluble drug.
登录
查看更多内容
影响因子：
5.8
作者：
Puneet Sharma;W. Denny;S. Garg
通讯作者：
Puneet Sharma;W. Denny;S. Garg
DOI：
10.1046/j.1359-4117.2003.01090.x
发表时间：
2003-05-01
影响因子：
--
作者：
Rajagopal, Sriram;Kumar, R Ajaya;Rajagopalan, R
通讯作者：
Rajagopalan, R
影响因子：
5.8
作者：
Yu Zhang;Xi Hu;Xiaolin Liu;Yun Dandan;Donghua Di;Tian Yin;Shu Zhang;Xing Tang
通讯作者：
Yu Zhang;Xi Hu;Xiaolin Liu;Yun Dandan;Donghua Di;Tian Yin;Shu Zhang;Xing Tang
DOI：
--
发表时间：
2009-08
期刊：
Die Pharmazie
影响因子：
--
作者：
Ke Ren;Zhirong Zhang;Yanzhen Li;Jie Liu;Dong Zhao;Yi Zhao;T. Gong
通讯作者：
Ke Ren;Zhirong Zhang;Yanzhen Li;Jie Liu;Dong Zhao;Yi Zhao;T. Gong
DOI：
10.1124/jpet.103.059683
发表时间：
2004-03-01
影响因子：
3.5
作者：
Wang, TG;Liu, B;Hong, JS
通讯作者：
Hong, JS