| 產(chǎn)品描述： | Saquinavir is a potent HIV protease inhibitor, is an antiretroviral drug used together with other medications to treat or prevent HIV/AIDS. |
| 靶點(diǎn)： |
HIV Protease;SARS-CoV;SARS-CoV;?HIVProtease |
| 體內(nèi)研究： |
The AUC was not affected by grapefruit juice after intravenous administration, but it increased significantly from 76+/-96 (water, mean (s.d.) to 114+/-70 (microg l[-1] h) (grapefruit juice) after oral saquinavir. Similarly, the oral bioavailability of saquinavir increased by a factor of 2 with grapefruit juice (from 0.7% to 1.4%). In contrast, clearance, volume of distribution and elimination half-life of saquinavir were not affected by grapefruit juice. After oral, but not after intravenous administration, the plasma concentration-time curve showed a second peak after lunch irrespective of pretreatment, suggesting enhancement of absorption by food |
| 動(dòng)物實(shí)驗(yàn)： |
After an overnight fast, eight healthy volunteers were treated with either 400 ml grapefruit juice or water before intravenous (12 mg) or oral saquinavir (600 mg) was administered.?Serial blood samples were obtained over the following 24 h and standardized meals were served 5 and 10 h after the administration of saquinavir.?The plasma concentrations of saquinavir were determined by high-performance liquid chromatography and pharmacokinetic parameters were calculated by routine methods |
| 參考文獻(xiàn)： |
1.Kupferschmidt H H T , Fattinger K E , Ha H R , et al. Grapefruit juice enhances the bioavailability of HIV protease inhibitor saquinavir in man[J]. British Journal of Clinical Pharmacology, 1998, 45(4):355-359. 2.Walmsley S , Avihingsanon A , Slim J , et al. Gemini: A Noninferiority Study of Saquinavir/Ritonavir Versus Lopinavir/Ritonavir as Initial HIV-1 Therapy in Adults[J]. JAIDS Journal of Acquired Immune Deficiency Syndromes, 2009, 50(4):367-374. |
| 溶解性： |
DMSO:100 mg/mL (149.07 mM) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.491 ml |
7.453 ml |
14.907 ml |
| 5 mM |
0.298 ml |
1.491 ml |
2.981 ml |
| 10 mM |
0.149 ml |
0.745 ml |
1.491 ml |
| 50 mM |
0.03 ml |
0.149 ml |
0.298 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京