ABSTRACT
Mogroside V is the most abundant [approximately 0.50%] cucurbitane-type triterpene glycoside in Siraitia grosvenorii and exhibits significant antitussive, expectorant, anti-carcinogenic, and anti-inflammatory effects. A sensitive, robust and selective liquid chromatography tandem with mass spectrometry [LC-MS/MS] was developed and validated for the determination and pharmacokinetic investigation of mogroside V in rat plasma. Samples were prepared through an one-step deproteinization procedure with 250 microL of methanol to a 75-microL plasma sample. Plasma samples were effectively separated on a Shiseido Capcell Pak UG120 C18 column [2.0 × 50mm, 3.0microm] using a mobile phase consisting of methanol: water [60:40, v/v] with an isocratic elution program. The running time for each sample was 7.0 min and the elution times of mogroside V and IS were 2.0 and 4.8 min, respectively. The detection relied on a triplequadrupole tandem with mass spectrometer equipped with negative-ion electrospray ionization interface by selectedreaction monitoring [SRM] of the transitions at m/z 1285.6 - 1123.7 for mogroside V and m/z 1089.6 - 649.6 for IS. The calibration curve was linear over the range of 96.0-96000 ng/mL with a limit of quantitation [LOQ] of 96.0ng/mL. Intra-day and inter-day precisions were both <10.1%. Mean recovery and matrix effect of mogroside V in plasma were in the range of 91.3-95.7% and 98.2-105.0%, respectively. This method was successfully applied in the pharmacokinetic study of mogroside V after intravenous or intraperitoneal administration of 1.12mg/kg mogroside V in rats
ABSTRACT
Objective To review pharmacological mechanism, pharmacokinetics, clinical research progress and prospects of pradefovir, a liver targeted medicine for hepatitis B.Methods The studies of pradefovir were summarized by searching literature databases of Web of Science,Elsevier ScienceDirect,Springer Link,Wiley Online Library, Pubmed, CNKI, Wanfang and VIP datebase.Results Pradefovir is a prodrug that targets to the liver, which absorbs rapidly by oral administration.Pradefovir could be quickly converted to adefovir with hepatic drug metabolizing enzyme CYP3A4. Compared with adefovir dipivoxil, it has shown smaller nephrotoxicity and larger liver targeting.Conclusion Pradefovir has shown favorable safety and effectiveness in the clinical study and has no durg resistance to be found.The approval Ⅲ clinical trial has been acquired of pradefovir in USA and has enteredⅠ clinical trial currently in our country, which has good prospects for clinical application in future.
ABSTRACT
Pinoresinol diglucoside [PD], a typical marker compound in Ecommia ulmoides Oliv., is an important and natural antihypertensive drug. A selective, sensitive, and rapid liquid chromatography tandem mass spectrometric [LCMS/ MS] analytical method was developed for the determination of PD in rats. After simple protein precipitation with acetonitrile, chromatographic separation of PD was conducted using a reversed-phase ZORBAX SB C[18] analytical column [4.6mm × 150mm, 5[micro]m particles] with a mobile phase of 10mM ammonium acetate-methanol-acetic acid [50:50:0.15, v/v/v] and quantified by selected reaction monitoring mode under positive electrospray ionization condition. The chromatographic run time was 3.4 min for each sample, in which the retention times of PD and the internal standard were 2.87 and 2.65min, respectively. The calibration curves were linear over the range of 1.003000ng/mL and the lower limit of quantification was 1.00ng/mL in rat plasma. The precision expressed by relative standard deviations were <8.9% for intra-batch precision and <2.0% for inter-batch precision, and the intra- and inter-batch accuracy by relative error was within the range of -3.9%-7.3%, which met acceptable criteria. The LC-MS/MS method was successfully applied to investigate the pharmacokinetics and oral bioavailability of PD in rats, with the bioavailability being only 2.5%
ABSTRACT
A large number of literatures at home and abroad in recent years about Schisandrin B were viewed and its pharmacological effects were summarized. Schisandrin B has a variety of pharmacological activities, which can reduce transaminase activity in liver cells, inhibit lipid peroxidation, anti-oxidant, hepatoprotection, anti-tumor and so on. Its pharmacological effects are accurate and worthy of research and development as a potential drug.