中文摘要：

目的: Saquinavir (SQV ) 是为 HIV 感染的处理的第一个朊酶禁止者，但是与差的溶解度。这研究的目的是为改进 SQV 的口头的吸收准备胶体的 nanocrystal 暂停。

英文摘要：

Aim： Saquinavir （SQV） is the first protease inhibitor for the treatment of HIV infection, but with poor solubility. The aim of this study was to prepare a colloidal nanocrystal suspension for improving the oral absorption of SQV. Methods： SQV nanocrystals were prepared using anti-solvent precipitation-high pressure homogenization method. The nanocrystals were characterized by a Zetasizer and transmission electron microscopy （TEM）. Their dissolution, cellular uptake and transport across the human colorectal adenocarcinoma cell line （Caco-2） monolayer were investigated. Bioimaging of ex vivo intestinal sections of rats was conducted with confocal laser scanning microscopy. Pharmacokinetic analysis was performed in rats administered nanocrystal SQV suspension （50 mg/kg, ig）, and the plasma SQV concentrations were measured with HPLC. Results： The SQV nanocrystals were approximately 200 nm in diameter, with a uniform size distribution. The nanocrystals had a rod-like shape under TEM. The dissolution, cellular uptake, and transport across a Caco-2 monolayer of the nanocrystal formulation were significantly improved compared to those of the coarse crystals. The ex vivo intestinal section study revealed that the fluores- cently labeled nanocrystals were located in the lamina propria and the epithelium of the duodenum and jejunum. Pharmacokinetic study showed that the maximal plasma concentration （Cmay.） was 2.16-fold of that for coarse crystalline SQV suspension, whereas the area under the curve （AUC） of nanocrystal SQV suspension was 1.95-fold of that for coarse crystalline SQV suspension. Conclusion： The nanocrystal drug delivery system significantly improves the oral absorption of saquinavir.