Synthesis of 2-hydroxyl-5-butyramidobenzoic acid and its effect on acetic acid-induced colitis in rats / 南方医科大学学报

<p><b>OBJECTIVE</b>To study the method for synthesis of 2-hydroxyl-5- butyramidobenzoic acid and test its effect on acetic acid-induced colitis in rats.</p><p><b>METHODS</b>2-hydroxyl-5-butyramidobenzoic acid was synthesized from 5-aminosalicylic acid and butyric acid by amidation, esterification and hydrolization. The effect of 2-hydroxyl-5-butyramidobenzoic acid on acetic acid enema-induced colitis in rats was investigated.</p><p><b>RESULTS</b>The structure of 2-hydroxyl-5-butyramidobenzoic acid was identified by IR and 1H-NMR. After treatment with acetic acid, the colon mucosal damage index (CMDI), fecal occult blood (OB) test, and activity of myelperoxidase (MPO) increased significantly in the rats as compared to the control levels. 2-hydroxyl-5- butyramidobenzoic acid obviously reduced the CMDI and OB, and reduced the level of MPO in the rats with colitis.</p><p><b>CONCLUSION</b>The synthesis of 2-hydroxyl-5-butyramidobenzoic acid requires only mild conditions with simple procedures, and the synthesized 2-hydroxyl-5-butyramidobenzoic acid shows obvious therapeutic effects on mucosal damage of in rats with acetic acid-induced colitis.</p>

Preparation and liver targeting of floxuridinyl dibutyrate solid lipid nanoparticles / 药学学报

This paper described the preparation and liver targeting traits of new solid lipid nanoparticles (SLN) containing floxuridinyl dibutyrate (FUDRB) modified with beta-D-galactosides (G2). FUDRB-SLN and FUDRB-G2SLN were prepared by thin layer ultrasonic technique. Transmission electron microscopy micrograph analysis demonstrated that the particle sizes of FUDRB-SLN and FUDRB-G2SLN were (137.5 +/- 11.1) nm and (95.0 +/- 10.7) nm. Drug loading were 9.64% and 8.56%, and entrapment efficiency were 99.81% and 96.23%, respectively. The concentrations of floxuridine (FUDR) in serum and some organs (liver, kidney and lung) were determined by RP-HPLC after iv administration of SLN. FUDR release was confirmed, and a significant enrichment of SLN modified with G2 was observed in liver with G2 complex (targeting rates of SLN-G2 was 8.28 for liver) in comparison with FUDR-sol (targeting rate was 2.56). FUDR could be detected in liver in mice at 480 min after iv administration of FUDRB-G2SLN. These results suggested that incorporation of G2 (4%-5%, g/g) into SLN enhanced the liver targeting-ability of FUDRB. SLN containing G2 could be a useful drug carrier system for liver targeting.

Application of macroporous resin in purification for effective part from Polygonum cuspidatum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the technological parameters of the purification process for effective part from Polygonum cuspidatum.</p><p><b>METHOD</b>Using adsorption capacities and desorption rates of polydatin, resveratrol,emodin,physcion and total anthraquinone as the primary screening indexes, six resins were surveyed,and the optimized conditions of adsorption and desorption of the effective ingredients were studied.</p><p><b>RESULT</b>Resin D101 gave good separation performance and was selected to purify the effective part in Polygonum cuspidatum. The optimum parameters were established as the following: 1 BV (bed volume) sample extract was passed through the column with a flow rate of 2.4 BV x h(-1), 30 min later,the column was washed with 2 BV water, 2 BV 20% ethanol, 5 BV 50% ethanol, 2 BV 70% ethanol and 5 BV 95% ethanol, respectively. The combined 50% and 95% ethanolic elutes were concentrated to yield the purified effctive part.</p><p><b>CONCLUSION</b>The purity of the total effective ingredients in the product was up to 36. 87%. Macroporous resin D101 could be well used in separating and purifying the effective part from Polygonum cuspidatum.</p>