Formula Optimization of Ibuprofen Sustained-release Dropping Pills by Box-Behnken Response-surface Method / 中国药师

Objective: To prepare ibuprofen sustained-release dropping pills, to evaluate the accumulative release percentage in vitro and to study the drug state in the base.Methods: With the drug content, mass ratio of water-soluble base to insoluble base and mass ratio of stearic acid to glyceryl monostearate as the investigation factors, and the comprehensive score of 2-hour and 10-hour cumulative dissolution rate as the evaluation index, a Box-Behnken response-surface method was used to screen the optimal formula of ibuprofen sustained-release dropping pills.The drug state in the matrix was examined by differential scanning calorimetry (DSC).Results: The optimal formula of ibuprofen sustained-release dropping pills was as follows: the drug content of 10%, water-soluble and insoluble matrix ratio of 4∶1, and stearic acid and glyceryl monostearate ratio of 3∶1.The maximum cumulative dissolution rate of ibuprofen sustained-release dropping pills was 78.85%.The DSC analysis showed that the drug crystallization peak disappeared in the sustained-release dropping pills, and formed a solid dispersion.Conclusion: The preparation has good sustained-release effect, and the preparation process is simple.

Protective Effects of Bifidobacterium on Intestinal Barrier Function in LPS-Induced Enterocyte Barrier Injury of Caco-2 Monolayers and in a Rat NEC Model.

Zonulin protein is a newly discovered modulator which modulates the permeability of the intestinal epithelial barrier by disassembling intercellular tight junctions (TJ). Disruption of TJ is associated with neonatal necrotizing enterocolitis (NEC). It has been shown bifidobacterium could protect the intestinal barrier function and prophylactical administration of bifidobacterium has beneficial effects in NEC patients and animals. However, it is still unknown whether the zonulin is involved in the gut barrier dysfunction of NEC, and the protective mechanisms of bifidobacterium on intestinal barrier function are also not well understood. The present study aims to investigate the effects of bifidobacterium on intestinal barrier function, zonulin regulation, and TJ integrity both in LPS-induced enterocyte barrier injury of Caco-2 monolayers and in a rat NEC model. Our results showed bifidobacterium markedly attenuated the decrease in transepithelial electrical resistance and the increase in paracellular permeability in the Caco-2 monolayers treated with LPS (P < 0.01). Compared with the LPS group, bifidobacterium significantly decreased the production of IL-6 and TNF-α (P < 0.01) and suppressed zonulin release (P < 0.05). In addition, bifidobacterium pretreatment up-regulated occludin, claudin-3 and ZO-1 expression (P < 0.01) and also preserved these proteins localization at TJ compared with the LPS group. In the in vivo study, bifidobacterium decreased the incidence of NEC from 88 to 47% (P < 0.05) and reduced the severity in the NEC model. Increased levels of IL-6 and TNF-α in the ileum of NEC rats were normalized in bifidobacterium treated rats (P < 0.05). Moreover, administration of bifidobacterium attenuated the increase in intestinal permeability (P < 0.01), decreased the levels of serum zonulin (P < 0.05), normalized the expression and localization of TJ proteins in the ileum compared with animals with NEC. We concluded that bifidobacterium may protect against intestinal barrier dysfunction both in vitro and in NEC. This protective effect is associated with inhibition of proinflammatory cytokine secretion, suppression of zonulin protein release and improvement of intestinal TJ integrity.

Survey on basic data of risk estimation of lung cancer among non-uranium miners in China / 中华放射医学与防护杂志

Objective To investigate the basic data of risk estimation of lung cancer among non-uranium miners in China.Methods 2836 workers from 24 mines in 9 provinces/regions were face-to-face interviewed to collect information including age at exposure,exposure duration,cigarette smoking among others.Results Age of the investigated non-uranium miners ranged from 17 to 72(36.9±8.0)years.The miners received low and poor education,3% of them were illiterate,58% with primary and middle school education,only 7% with junior college and higher education.Seventy-five percent of the uranium miners are migrant rural workers.Ethnic minority miners accoungted for 16% of all the investigated miners.Among the migrant rural workers age at initial exposure was estimated to be 29.6±8.0 years.By the time of the investigation,46.7% of the miners had worked in the mine for five years and longer,working years in the mine was 6.7±6.8 years with a median of 4.1years.3.4% of the non-uranium miners began the initial radon exposure in mines before their 18 years of old.17.5% of the investigated miners reported working more than 8 h every working day.Among the males,58.0% were current smokers with a median of 16 cigarettes per day.Age to begin the cigarette smoking was 20 years on average.Current smoking rate was age-dependent,the rate as high as 69.2% for the males aged 15-19 years.Current smoking rate was significantly statistically lower in coal mines than that in other mines,49.0% vs 62.5%.Compared with other miners,more frequent mechanical ventilations were reported by coal miners,Conclusions In China non-uranium mines,75% were migrant rural workers,by the time of the investigation about half of them had worked in the mines for at least five years.Non-uranium miners began their mining at 30 years on average,with a very small percentage of 3%,exposed to the mining radon before their 18 years.Current cigarette smoking rate in non-uranium male miners was the same as the general male population in China.