Developments in the Pharmaceuticals Industry

China’s pharmaceuticals industry is one of the industries making use of foreign funds and running three kinds of foreign-funded enterprises from an early date. In 1980, it signed a contract with the Japanese Pharmaceu-tical Enterprise to establish the China Otsuka Pharmaceuticals Co. Ltd.---the first joint venture in China’s pharma-ceuticals industry. According to incom-

Effect of paracellular permeation enhancers on intestinal permeability of two peptide drugs,enalaprilat and hexarelin, in rats

Transcellular permeation enhancers are known to increase the intestinal permeability of enalaprilat,a 349 Da peptide,but not hexarelin(887 Da).The primary aim of this paper was to investigate if paracellular permeability enhancers affected the intestinal permeation of the two peptides.This was investigated using the rat single-pass intestinal perfusion model with concomitant blood sampling.These luminal compositions included two paracellular permeation enhancers,chitosan(5 mg/mL) and ethylenediaminetetraacetate(EDTA,1 and 5 mg/mL),as well as low luminal tonicity(100 mOsm) with or without lidocaine.Effects were evaluated by the change in lumen-to-blood permeability of hexarelin and enalaprilat,and the blood-to-lumen clearance of ^(51)chromium-labeled EDTA(CL_(Cr-EDTA)),a clinical marker for mucosal barrier integrity.The two paracellular permeation enhancers increased the mucosal permeability of both peptide drugs to a similar extent.The data in this study suggests that the potential for paracellular permeability enhancers to increase intestinal absorption of hydrophilic peptides with low molecular mass is greater than for those with transcellular mechanism-of-action.Further,the mucosal blood-to-lumen flux of ^(51)Cr-EDTA was increased by the two paracellular permeation enhancers and by luminal hypotonicity.In contrast,luminal hypotonicity did not affect the lumen-to-blood transport of enalaprilat and hexarelin.This suggests that hypotonicity affects paracellular solute transport primarily in the mucosal crypt region,as this area is protected from luminal contents by a constant water flow from the crypts.

Comprehensive analysis of antibacterial and anti-hepatoma activity of metabolites from jujube fruit

Jujube is one of the most produced dried fruits in China,and it is also a traditional Chinese medicine that enhances immunity and has anti-cancer activity.Jujube fruit is rich in phenolic compounds,but few reports are available on its biological activities.To evaluate the biological activities of the phenolic compounds in dried jujube fruit,the composition and content of metabolites in dried jujube fruit were determined by metabolomics,and the antibacterial and anticancer activities of the phenolic compounds were analyzed in dried jujube fruit.The results showed that 463 compounds were identified in dried‘Junzao’fruit,including 102 phenolic compounds.The in vitro activity test showed that the jujube phenolic metabolites had extensive antibacterial effects and caused disruption and nuclear sclerosis of hepatocellular carcinoma(HepG2)cells.Canonical correlation analysis showed that total phenolic content,quercetin-3-rutinose,and procyanidin B1 were the main active antibacterial and anticancer components.The study provides data supporting the application of dried jujube fruit in the development of functional foods,pharmaceuticals and cosmetics.