Permeabilities of rebamipide via rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier

AIM: To investigate the permeability characteristics of rebamipide across intestinal mucosa, and examine the effects of some absorption enhancers on the permeability across the colonic tissue. Another purpose is to demonstrate the colon-specific delivery of rebamipide with or without absorption enhancers using chitosan capsule as a carrier. METHODS: The permeability of rebamipide was evaluated using an in vitro diffusion chamber system, and the effects of some absorption enhancers on the permeability via colon were further investigated. The release of rebamipide from chitosan or gelatin capsule was studied by Japan Pharmacopoeia rotating basket method. The colonic and plasma concentrations were analyzed by high performance liquid chromatography (HPLC) to evaluate colon-targeting action after oral administration of various dosage forms, and rebamipide with absorption enhancers in chitosan dosage forms. RESULTS: The permeability of rebamipide across the jejunal or ileal membranes was higher than the colonic membranes. Both sodium laurate (C12) and labrasol signifi cantly increased permeability across the colon membranes. On the other hand, the release of rebamipide from chitosan capsule was less than 10%totally within 6 h. The area under concentration-time profile of drug in the colon mucosa using chitosan capsules (AUCLI, 1 6011.2 ng·h/g) was 2.5 times and 4.4 times greater than using gelatin capsules and CMC suspension, respectively. Meanwhile, the area under concentration-time profile of drug in the plasma (AUCPL) was 1016.0 ng·h/mL for chitosan capsule, 1887.9 ng·h/mL for CMC suspension p and 2163.5 ng·h/mL for gelatin capsule. Overall, both AUCLI and AUCPL were increased when C12 was co-administrated, but the increase of AUCLI was much greater; the drug delivery index (DDI) was more than 1 compared with simple chitosan capsule group. CONCLUSION: There was a regional difference in the permeability of Rabamipide across the jejunum, ileum and the colon, and passive diffusion seems to be one of the major transport mechanisms of rebamipide. Absorption enhancers can increase the permeability of rebamipide across the colon tissue signifi cantly. In addition, chitosan capsule may be a useful carrier to deliver rebamipide to the colon specifi cally and the co-administration of C12 with rebamipide may also be very useful in local treatment.

Multiyear Observations of Deposition-Mode Ice Nucleating Particles at Two High-Altitude Stations in India

Ice nucleating particle(INP) measurements were made at two high-altitude stations in India. Aerosols collected on filter paper at Girawali Observatory, Inter University Center for Astronomy & Astrophysics(IGO), and at the Radio Astronomy Center, Ooty(RAC), were activated in deposition mode using a thermal gradient diffusion chamber to determine the INP concentrations. The measurement campaigns at IGO were conducted during 2011, 2013 and 2014, and at RAC during 2013 and 2014. When the aerosol samples were exposed to an ice supersaturation of between 5% and 23% in the temperature range-17.6?C to-22?C, the maximum INP number concentration at IGO and RAC was 1.0 L-1and 1.6 L-1, respectively.A maximum correlation coefficient of 0.76 was observed between the INP number concentration and ice supersaturation. The airmass trajectories analyzed for the measurement campaigns showed that the Arabian Desert and arid regions were the main INP contributors. Elemental analysis of particles showed the presence of Na, Cl, Si, Al, Fe, Cu, Co, Cd, S, Mn and K, as well as some rare-Earth elements like Mo, Ru, La, Ce, V and Zr. When aerosols in the size range 0.5–20 μm were considered, the fraction that acted as INPs was 1 : 104to 1 : 106at IGO, and 1 : 103to 1 : 104at RAC. The higher ratio of INPs to aerosols at RAC than IGO may be attributable to the presence of rare-Earth elements observed in the aerosol samples at RAC, which were absent at IGO.

The Characteristics of Atmospheric Ice Nuclei Measured at Different Altitudes in the Huangshan Mountains in Southeast China

The concentration of ice nuclei （IN） and the relationship with aerosol particles were measured and analyzed using three 5-L mixing cloud chambers and a static diffusion cloud chamber at three altitudes in the Huangshan Mountains in Southeast China from May to September 2011.The results showed that the mean total number concentration of IN on the highest peak of the Huangshan Mountains at an activation temperature （Ta） of-20℃C was 16.6 L-1.When the supersaturation with respect to water （Sw） and with respect to ice （Si） were set to 5％,the average number concentrations of IN measured at an activation temperature of-20℃C by the static diffusion cloud chamber were 0.89 and 0.105 L-1,respectively.A comparison of the concentrations of IN at three different altitudes showed that the concentration of IN at the foot of the mountains was higher than at the peak.A further calculation of the correlation between IN and the concentrations of aerosol particles of different size ranges showed that the IN concentration was well correlated with the concentration of aerosol particles in the size range of 1.2-20 μtm.It was also found that the IN concentration varied with meteorological conditions,such as wind speed,with higher IN concentrations often observed on days with strong wind.An analysis of the backward trajectories of air masses showed that low IN concentrations were often related to air masses travelling along southwest pathways,while higher IN concentrations were usually related to those transported along northeast pathways.