Details

Autor(en) / Beteiligte

• Yi, Yueneng
• Tu, Liangxing
• Hu, Kaili
• Wu, Wei
• Feng, Jianfang

Titel

The construction of puerarin nanocrystals and its pharmacokinetic and in vivo–in vitro correlation (IVIVC) studies on beagle dog

Ist Teil von

• Colloids and surfaces, B, Biointerfaces, 2015-09, Vol.133, p.164-170

Ort / Verlag

Netherlands: Elsevier B.V

Erscheinungsjahr

2015

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• •The nanocrystals prepared was smaller than 229nm.•Redispersion of nanocrystals powder was performed above 30°C.•A fine in vivo–in vitro correlation was established.•Cmax and AUC improved and CL/F reduced with particle size decreased. Puerarin is widely used in clinics in China as a therapeutic agent for cardiovascular diseases by intravenous administration. Adverse drug reactions caused by cosolvents often increase the patients’ treatment burden (high drug costs and low compliance). The development of oral formulation is urgently needed and nanocrystal technique has become a preferred way to develop oral dosage form, nowadays. In this study, high pressure homogenization (HPH) was employed to prepare puerarin nanocrystals by employing SDS as the stabilizer, and redispersibility of the nanocrystals powder was also studied. The nanocrystals prepared was characterized using DLS, DSC, XRD and SEM. A preferred in vivo–in vitro correlation was also established in this study. Pharmacokinetic studies on beagle dog showed that comparing to raw puerarin powder, both of the Cmax and AUC of puerarin nanocrystals were enhanced. From the above results, we can conclude that nanocrystal technique is an efficient technology to improve the oral bioavailability of puerarin.