| Description | Saquinavir (Ro 31-8959) is a potent HIV protease inhibitor, is an antiretroviral drug used together with other medications to treat or prevent HIV/AIDS. |
| In vivo | 静脉给药后，葡萄柚汁对AUC没有影响，但是口服saquinavir后，AUC从76+/-96 (water, mean (s.d.)) 显著增加至114+/-70 (microg l[-1] h) (葡萄柚汁)。同样，葡萄柚汁使saquinavir的口服生物利用度增加了2倍（从0.7%增加到1.4%）。相比之下，葡萄柚汁未对saquinavir的清除率、分布体积及消除半衰期产生影响。口服给药后（而非静脉给药后），血浆浓度-时间曲线在午餐后显示出第二峰值，不论预处理如何，这暗示了食物增强了吸收[1]。 |
| Animal experiments | 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[1]. |
| Synonyms | Ro 31-8959, 沙奎那韦 |
| molecular weight | 670.84 |
| Molecular formula | C38H50N6O5 |
| CAS | 127779-20-8 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (149.07 mM) |
| References | 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. |