高效液相色谱法测定马来酸阿塞那平的有关物质

目的：建立反相高效液相色谱法定量测定马来酸阿塞那平中的8个杂质。方法：色谱柱采用Inertsil ODS-3 C18（250 mm ×4.6 mm,5μm）,流动相A为0.1%三氟乙酸水溶液,流动相B为乙腈,以1.0 ml·min^-1的流速进行梯度洗脱,检测波长为220 nm,柱温为35℃。结果：阿塞那平与各杂质峰良好分离,阿塞那平在0.45~1458μg·ml^-1浓度范围内线性关系良好（r=1.0000）,各杂质在0.4~30.0μg·ml-^1浓度范围内线性关系良好（r〉0.999）;平均回收率93.1%~106.7%（n=9）。结论：本方法操作简便、灵敏度高、重复性好、专属性和耐用性较强,可用于测定马来酸阿塞那平原料药的有关物质。     

HPLC法测定复方愈酚麻黄糖浆中四种成分的含量

目的建立测定复方愈酚麻黄糖浆中盐酸麻黄碱、愈创甘油醚、马来酸氯苯那敏、双氯芬酸含量的HPLC方法。方法采用Insteril ODS-3C18色谱柱,梯度洗脱,流速：1．0mL·min^-1,柱温：30℃,检测波长：257nm。结果盐酸麻黄碱、愈创甘油醚、马来酸氯苯那敏、双氯芬酸分别在0．4018～6．4287μg（r=0．9999）、3．1836～50．9379μg（r=0．9999）、0．1610～2．5762μg（r=1．0000）、0．1485～2．3759μg（r=0．9999）范围内线性关系良好,平均回收率分别为99．589／6（RSD=0．39％）、99．58％（RSD=0．30％）、99．36％（RSD=0．29％）、99．40％（RSD=0．46％）（n=9）。结论本方法经方法学验证可用于复方愈酚麻黄糖浆中盐酸麻黄碱、愈创甘油醚、马来酸氯苯那敏、双氯芬酸的含量检测。     

连翘银花浸膏制备工艺研究

目的 优化连翘银花浸膏的制备工艺,为制备双黄连等制剂提供实验依据.方法 采用正交试验法设计对水提醇沉工艺进行优化,HPLC法测定绿原酸和连翘苷的含量,作为正交实验的评价指标.结果 优选工艺为水量每次分别为药材量的10倍、8倍,煎煮时间分别为2h、1.5h,水提膏浓缩比重为相对密度1.2,侵泡时间可以根据生产需要进行调节.结论 优化的水提醇沉工艺的有效成分提取率高,且具有一定的调节空间,适合于工业大生产.     

黛力新联合马来酸曲美布汀治疗腹泻型肠易激综合征的疗效观察

目的：观察黛力新联合马来酸曲美布汀治疗腹泻型肠易激综合征的疗效。方法将2012年8月~2013年8月来本院治疗腹泻型肠易激综合征的38例患者随机分为观察组和对照组,每组19例。两组患者均给予马来酸曲美布汀治疗,观察组加用黛力新,治疗6周。比较两组患者的治疗有效率,记录患者治疗前后的SDS评分和SAS评分,并进行比较。结果观察组总有效率94.74%高于对照组68.42%,两者差异有统计学意义（P〈0.05）;观察组治疗后SDS评分以及SAS评分均低于对照组,两者差异有统计学意义（P〈0.05）。结论黛力新联合马来酸曲美布汀治疗腹泻型肠易激综合征的疗效可靠,值得临床推广应用。     

马来酸桂哌齐特治疗急性脑梗死的疗效及对血液流变学的影响

目的：观察马来酸桂哌齐特注射液治疗急性脑梗死的临床效果及对血液流变学的影响。方法选择2009-12-2012-12我院内科收治的急性脑梗死患者133例,随机分为治疗组68例和对照组65例。2组均给予常规基础治疗,治疗组在对照组基础上应用马来酸桂哌齐特注射液320 mg加入500 mL 0.9％氯化钠注射液中静滴,1次/d ,共应用14 d ,治疗前后采用改良爱丁堡-斯堪的那维亚量表（SSS ）与日常生活能力（ADL ）量表对2组患者的疗效进行评定。对比治疗前后2组患者血液流变学指标变化。结果治疗7 d、14 d后治疗组SSS评分、ADL评分与对照组比较差异有统计学意义（ P＜0.05）。治疗组治疗前后SSS评分、ADL评分比较差异有统计学意义（ P＜0.05）。2组治疗后总有效率比较差异有统计学意义（ P＜0.05）。治疗组治疗后血液流变学指标均较治疗前有显著改善（ P＜0.05）。结论马来酸桂哌齐特注射液治疗急性脑梗死安全有效,且能显著改善患者的血液流变学指标。     

HPLC法测定含体外培育牛黄复方制剂中马来酸氯苯那敏的含量

目的：现有测定小儿氨酚黄那敏颗粒中马来酸氯苯那敏（CM）含量的HPLC方法均是针对含有人工牛黄的制剂,由于人工牛黄和体外培育牛黄成分差异巨大,体外培育牛黄干扰这些HPLC法测定CM,所以本研究建立了含体外培育牛黄的小儿氨酚黄那敏颗粒中马来酸氯苯那敏含量测定的新HPLC方法,该法同时也适用于含人工牛黄的小儿氨酚黄那敏颗粒中CM含量测定。方法：采用Intersil ODS-3 C18色谱柱,以磷酸盐缓冲液（取磷酸二氢铵5.75 g,磷酸0.5 mL,加水1000 mL）- 乙腈（78 : 22）为流动相,检测波长为262 nm,流速为 1.0 mL? min-1,柱温为30℃,进样量为20 μL。结果：马来酸氯苯那敏在5 μg? mL-1 ～ 30 μg? mL-1范围内峰面积与测定浓度呈良好的线性关系,回归曲线为：y = 14.45349x - 1.7506,r = 0.9995,准确度为100.7 %,精密度RSD为0.7 %。室温下,马来酸氯苯那敏溶液在24 h内稳定。结论：该方法快速简便,专属性强、重现性好,适用于含体外培育牛黄和人工牛黄的小儿氨酚黄那敏颗粒中马来酸氯苯那敏的含量测定。     

Functional characterization of histamine H4 receptor on human mast cells

Among the four different types of histamine receptors (H1-H4), H4R is predominantly expressed in immune cells and involved in immunomodulatory response. Here, in this study we determined the expression of H4R in human mast cells (HMC-1, LAD-2 and primary cord blood derived CD34+ human mast cells) and characterized its functional properties. Interestingly, we found that human mast cells responded to both histamine (natural ligand) and 4-methylhistamine (selective H4R agonist) for sustained intracellular calcium mobilization, degranulation and cytokine production. However, only histamine induced the release of cAMP, but 4-methylhistamine down regulates cAMP indicating that H4R mediates its effect through Gαi/o protein and H1R via Gαq protein. Furthermore, both histamine and 4-methylhistamine induced the production of cysteinyl leukotrienes and LTB4. Using human inflammation antibody array membrane, we found that H4R induced the expression of various inflammatory proteins, involving pro-inflammatory cytokines and chemokines and these are TGF-β1, TNF-α, TNF-β, PDGF-BB, TIMP-2, M-CSF, IP-10, IL-16, IL-6, IL-3, IL-10, MIP-1α, IL-1α, ICAM-1, Eotaxin-2, RANTES, IL-8, MCP-1, and IL-6sR. We also quantified the level of various inflammatory cytokines produced by human mast cells through H4R. It was observed that, the production level of Th2 cytokines IL-4(401.34 pg/ml), IL-5 (64.21 pg/ml) and IL-13 (1044 pg/ml) and classical proinflammatory cytokines IL-6 (221.27 pg/ml) and IL-1β (34.24 pg/ml) and chemokines MCP-1(106 pg/ml) and IL-8 (818.32 pg/ml). Furthermore, activation of H4R caused the phosphorylation of ERK and PI3 K in a time dependent manner. Taken together these data demonstrate that, the activation of H4R in human mast cells produced not only inflammatory mediators that are associated with allergic reactions but also other inflammatory conditions.     

欣母沛、缩宫素联合马来酸麦角新碱预防二次剖宫产术后出血的效果

目的探讨欣母沛、缩宫素联合马来酸麦角新碱预防二次剖宫产术后出血的效果。方法将72例二次剖宫产产妇按照随机数表法分为观察组(欣母沛、缩宫素联合马来酸麦角新碱治疗)与对照组(缩宫素治疗),各36例。比较两组的预防效果。结果观察组的术后2、24 h出血量、产后出血发生率及子宫复旧情况均优于对照组(P<0.05)。治疗后24 h,两组的Hb、HCT、Ca2+、FIB、D-D水平均有所改善,且观察组优于对照组(P<0.05)。结论欣母沛、缩宫素联合马来酸麦角新碱可有效预防二次剖宫产术后出血,且不增加不良反应。     

The protective impact of adapted trimebutine maleate-loaded nanostructured lipid carriers for alleviating the severity of acute colitis

Nanoparticles for colon-drug delivery were designed and evaluated to solve many discrepancy issues such as high adverse effects of released drugs, insufficient drug amount at diseased areas, and unintentionally premature drug release to noninflamed GIT regions. Herein, the goal of this work was to convert trimebutine maleate (TMB) into nanostructured lipid carriers (NLC) in order to improve its protective effects in ulcerative colitis. NLC of TMB was prepared by the hot homogenization followed by ultra-sonication method. A full 4²-factorial design was used to estimate the produced TMB-NLC. The study design included the exploration of the impact of two independent variables namely lipid mix amount and ratio (glyceryl mono stearate and capryol 90), surfactant concentration (0.5, 1, 1.5, and 2%), on the particle size, polydispersity index, and the entrapment efficiency (EE%). The protective activity of F9 was examined through macroscopical scores, histopathological changes, immunohistochemical localization of tumor necrosis factor-α (TNF-α) and examination of oxidative stress such as reduced glutathione (GSH), superoxide dismutase (SOD), and malondialdehyde (MDA) against acetic acid-induced colitis in rats. Consistent with our expectations, the orally administered optimized formula (F9) alleviated the severity of colitis in acetic acid-induced rat model of colitis likely owing to the controlled release compared to free TMB. We aimed to develop TMB-loaded NLC for the treatment of acute colitis with the goal of providing a superior drug safety profile over long-term remission and maintenance therapy.     

奥替溴铵、匹维溴铵、马来酸曲美布汀和酪酸茵治疗肠易激综合征药物经济学研究

目的 初步探讨奥替溴铵（斯巴敏）、匹维溴铵（得舒特）、马来酸曲美布汀（舒丽启能）和酪酸菌（米雅BM）治疗肠易激综合征的药物经济学。方法 从中国生物医学文献数据库和学术期刊检索相关文献，选择符合标准（随机、双盲、安慰剂对照）的临床试验论文，提取临床试验数据，进行药物经济学评价。结果 服用斯巴敏40mg,tid,2wk药费71.16元；服用得舒特50mg,tid,2wk药费120.12元；服用舒丽启能200mg,tid,2wk药费110.46元；服用米雅BM80mg,tid,2wk药费282.24元。产生单位效果所需的成本分别为斯巴敏80.86；得舒特143.17；舒丽启能135.37；米雅BM351.04。以斯巴敏治疗成本最低。结论 斯巴敏是治疗肠易激综合征最优的选择。