4 - Aminosalicylic Acid Sodium Colon Targeted Pellets

Objective Optimization of 4-ASANa colon-specific pellets prescription and preparation process. To establish one determination method of 4-ASANa colon-specific pellets of the content and release. Examine the 4-ASANa colon-specific pellets adhesion,efficacy and mechanism of action, for the preparation study provides preclinical data.Method Study 4-ASANa stability, balance of solubility and oil/water partition coefficient in different medium. Single factor test examine the impact factor of 4-ASANa colon-specific pellets release rate. Roundness and yield as index,using L9 (34) orthogonal to optimization the best prescription and preparation process of 4-ASANa colon-specific pellets. Testing 4-ASANa colon-specific pellets for colon targeting properties of powders, quantitative analysis and in vitro dissolution;using X-ray and y-ray to detetion pellets adhesion of the human body. Prepared trinitrobenzene sulfonic acid rat ulcerative colitis model, observing the general morphology of rat colon injury and histological changes and IL-1B, TNF-a, SOD, MDA, MPO and other indicators of changes in study 4-ASANa pellets for colon-specific role in ulcerative colitis.Results 4-ASANa are stable at 24h in water, pH1.2 hydrochloric acid, as well as pH6.8, pH7.4 PBS,equilibrium solubility to in water, pH1.2 as well as pH6.8, pH7.4 PBS, respectively14.59mg·mL-1,24.87mg·mL-1,13.05mg·mL-1,14.58mg·mL-1 oil/water distribution in pH1.2 as well as pH6.8, pH7.4 PBS. Respectivelycoefficient is 14.41,16.36,15.86.4-ASANa colon-specific pellets dominated the best prescription drugs and accessories 100g, HPMC:CP=4:1, MCC content of 30g,4-ASANa content of 60g,80mL·L-1PVP adhesive dosage of 33mL, ethyl celluloseaqueous dispersion coating weight gain of 3%;preparation process for the host speed 800r·min-1, spheronization time and spheronization is 7min. Airborne Charging Capacity 30g; 4-ASANa colon-specific pellets roundness is 13.4((?)), bulk density of 0.877g·mL-1, crisp choppeddegree of 72%, the yield was 86.5%, pellets in 4-ASANa the content of 61.23%, in line with Higuchi kinetics of the process of in vitro release; X-ray and y-ray tracking technology have proved to pellets in the colon has a good adhesion; 4-ASANa colon-targeted pellets showed that their treatment in vivo pharmacodynamic mechanism of colitis may suppress the generation of inflammatory factors, significantly lower serum ulcerative colitis IL-1B and TNF-a concentration, the difference with a statisticalsignificant (P<0.05), lower colon tissue MDA and MPO levels and increasing SOD activity, the difference was statistically significant (P<0.05), colitis caused by chemical factors, there is a better therapeutic effect.Conclusion 4-ASANa colon-specific pellets process is simple, economical and practical, show the good characterization adhesion and target in colon is a new agent for treatment of ulcerative colitis...