Asymmetric Synthesis of Rupestonic Acid and Pechueloic Acid.

In this report, the originally proposed rupestonic acid (5) and pechueloic acid (3) were efficiently synthesized. The chiral lactone 13, recycled from the degradation of saponin glycosides, was utilized to prepare the key chiral fragment 11. During the exploration of this convergent assembly strategy, the ring-closing metathesis (RCM), SmI-prompted intermolecular addition, and [2,3]-Wittig rearrangement proved to be effective transformations for the synthesis of subunits.

Transport of aripiprazole across Caco-2 monolayer model.

This study aimed to investigate the transport characteristics of aripiprazole. A human intestinal epithelial cell model Caco-2 cell in vitro cultured had been applied to study the transport of aripiprazole. The effects of time, concentration of donor solutions, pH, temperature and P-glycoprotein inhibitor on the transport of aripiprazole were investigated.

[Physicochemical stability and purification technology of caffeic acid tetramer from Arnebia euchroma].

Objective: To purify caffeic acid tetramer (CAT) with macroporous resin on the basis of its fundamental physicochemical stability research.

Method: The changes of CAT content were compared by HPLC method before and after the purification process, or while other conditions were altered.

Result: LK001 was the best one among 7 kinds of macroporous resin in regard of purifying ability.

[Preparation, characterization of paclitaxel-loaded Pluronic P105 polymeric micelles and in vitro reversal of multidrug resistant tumor].

Drug delivery system (DDS) is a novel approach to overcome multidrug resistance (MDR) in tumors nowadays. This work was designed to investigate a new micellar delivery system for in vitro reversal of resistant ovarian tumor cells, based on a nonionic triblock copolymer Pluronic P105 and paclitaxel (PTX). The PTX-loaded polymeric micelles (P105/PTX) were prepared by thin film-hydration methods.

Pharmacokinetics and bioequivalence studies of galantamine hydrobromide dispersible tablet in healthy male Chinese volunteers.

A randomized, two-way, crossover study was conducted in 18 healthy male Chinese volunteers to compare pharmacokinetics profiles of galantamine hydrobromide dispersible tablet with that of conventional tablet. A single oral dose of 10 mg galantamine was administrated to each volunteer. Plasma concentrations of galantamine were determined by a validated high-performance liquid chromatography (HPLC) method with fluorescence detection, which allowed 1 ng/mL to be assayed as the lowest quantifiable concentration.

Determination of glucosamine sulfate in human plasma by precolumn derivatization using high performance liquid chromatography with fluorescence detection: its application to a bioequivalence study.

A simple, rapid, selective and specific high-performance liquid chromatography (HPLC) method with fluorescence detection was developed for determination of glucosamine sulfate in human plasma and application to a bioequivalence in healthy volunteers. Precipitation of plasma was accomplished with acetonitrile to separate interfering endogenous products from the compound of interest. After vortex mixing and centrifugation, the supernatant was transferred and derivatized with 9-fluorenylmethoxycarbonyl chloride-acetonitrile solution in borate buffer (pH=8.

[Effect of self-microemulsifying system on cell tight junctions].

Aim: To study the effect of negatively charged and positively charged self-microemulsifying systems (SMES) on the cellular tight junction complex was to be investigated at molecular cell level.

Methods: Human intestinal epithelial Caco-2 cell model was established. Effect of formulations on the transepithelial electrical resistance (TEER) and permeability of the paracellular transport marker mannitol were measured to evaluate the cell integrity.

[9-nitrocamptothecin nanostructured lipid carrier system: in vitro releasing characteristics, uptake by cells, and tissue distribution in vivo].

Aim: To study the release and cell uptake characteristics of 9-nitrocamptothecin (9-NC) nanostructured lipid carrier system (NLC) in vitro and its tissue distribution characteristics in vivo.

Methods: Mouse peritoneal macrophages were used to investigate the uptake of nanoparticles by cells in vitro. The tissue distribution of 9-nitrocamptothecin solution and stealth nanostructured lipid carrier system (S-NLC) was determined after intravenous administration to mice at a single dose of 1.

[The pharmacokinetics and pharmacodynamics of intranasal preparation of Panax notoginseng Saponins].

Aim: To investigate the pharmacokinetic course of intranasal powders of Panax notoginseng Saponins (PNS) in a rat model and its protective effects against cardio-cerebrovascular diseases administrated in the form of its suspension.

Methods: After administration, Rgl concentration in the serum was analyzed by HPLC and the absolute bioavailability was calculated. The protective effects against cardia-cerebrovascular diseases were studied on actue myocardial infarction model in rats built by occlusion of left coronary artery and cerebral ischemia-reperfusion model in gerbils built by occlusion of bilateral common carotid artery (CCA).

[The in vitro kinetics of uptake, transport and efflux of 9-nitrocamptothecin in Caco-2 cell model].

Aim: To study the kinetics of uptake, transepithelial transport and efflux of 9-nitrocamptothecin (9-NC).

Methods: A human intestinal epithelial cell model Caco-2 cell in vitro cultured had been applied to study the kinetics of uptake, transport and efflux kinetics of 9-NC at small intestine. The effects of time, pH, temperature and P-glycoprotein inhibitors on the uptake of 9-NC were investigated.