Effects of PPARγ agonist on calpain expression in model of acute experimental autoimmune encephalomyelitis

AIM: To explore the effects of peroxisome proliferator-activated receptor γ （PPARγ） agonist on calcium-activated neutral proteinase, calpain, expression in the brain of rats with acute experimental autoimmune encephalomyelitis (EAE). METHODS: EAE model was established in rats by inoculating the homogenate contained spinal cord of guinea pig and complete Freunds adjuvant. Respectively, the PPARγ agonist rosiglitazone and non-steroid anti-inflammatory drug (NSAID) ibuprofen were used to treat the EAE rats. Outcome measures (Kohs scale) were applied at baseline and after treatment to assess the improvement of clinical symptoms. Calpain expression levels were detected by RT-PCR and Western blotting. RESULTS: All the groups showed significant improvements of scales scores after treatment with rosiglitazone and ibuprofen. No significant difference of the expression of calpain mRNA was found among EAE group, rosiglitazone and ibuprofen groups (P>0.05), but the expression of calpain reduced markedly in rosiglitazone and ibuprofen groups compared with that in EAE group (P<0.05). CONCLUSION: Rosiglitazone and ibuprofen inhibit the expression of calpain and improve the clinical symptoms of EAE rats. PPARγ agonist plays a neuroprotective role in EAE rats.     

布洛芬缓释片中布洛芬含量测定方法的优化

[目的]建立布洛芬缓释片的含量测定的最佳方法。[方法]采用紫外分光光度法(检测波长为263 nm)和高效液相色谱法(色谱柱为Agilent C18,流速为1.0 m L/min,检测波长263 nm)测定布洛芬缓释片中布洛芬的含量,最终确定布洛芬缓释片中布洛芬含量的最佳质量控制方法。[结果]以流动相为乙酸铵缓冲液∶乙腈(40∶60)的HPLC方法最佳,布洛芬质量在1.05~6.30μg范围内线性关系很好(r=1.000 0),平均回收率为99.71%,RSD=1.14%,重现性好。[结论]采用高效液相色谱法测定布洛芬缓释片含量最佳,该方法操作简单、分离效果好、重现性好、灵敏度高。     

释放改性剂对聚己内酯-布洛芬贴片可打印性及释药性能的影响

以聚己内酯为药物载体材料、布洛芬为模型药物,以微晶纤维素、羟丙基甲基纤维素、乙基纤维素为释放改性剂,采用熔融沉积成型打印技术制备具有类石墨烯层间交错网络结构的经皮给药贴片。经力学性能、动态流变性能、红外分析、结晶性能、体外药物释放性能测试并结合释放动力学模型拟合,分析释放改性剂对聚己内酯基药物复合材料熔融沉积成型打印性能、聚己内酯-布洛芬经皮给药贴片药物释放性能的影响。结果表明:微晶纤维素的添加提高了聚己内酯-布洛芬线材的拉伸强度,而乙基纤维素、羟丙基甲基纤维素的添加均在不同程度上降低了线材的拉伸强度;3种释放改性剂均提高了聚己内酯-布洛芬熔体的复数黏度、储能模量,其中微晶纤维素的提高最为显著;红外分析表明释放改性剂与聚己内酯和布洛芬之间仅为物理混合,未发生化学反应;3种释放改性剂均降低了聚己内酯-布洛芬贴片的结晶度;与乙基纤维素、羟丙基甲基纤维素相比,微晶纤维素对熔融沉积成型打印的经皮给药贴片的累积释药率提高最为明显,120 h内累积释药率从62.3%提高到99.4%。     

微乳液凝胶固定化脂肪酶催化消旋布洛芬辛酯水解反应的研究

初步研究了AOT-正庚烷-明胶微乳液凝胶固定化脂肪酶催化消旋布洛芬辛酯水解反应的影响因素。结果表明:在正庚烷中,布洛芬辛酯水解反应能够顺利进行,产物为光学纯度很高的S-构型布洛芬,转化率为0.3217时,其对映体过量值为0.9826;凝胶R值(水与AOT的摩尔数之比)对酶催化反应有较大影响,最佳R值为73;当酶含量固定,底物浓度为0.10 mol/L时,转化率最大并能得到较高对映体过量值的产物;当反应时间超过16 h时,水解反应达到平衡;固定化酶的重复使用次数与溶剂中的含水量有关,正庚烷中少量的水有助于增加酶的重复使用次数。