目的 探究诺西那生钠治疗罕见病脊髓性肌萎缩症(spinal muscular atrophy,SMA)的实验室指标变化及用药安全性.方法 回顾性纳入 2021 年 12 月-2022 年 12 月于西安交通大学第一附属医院神经内科就诊的 6 例诺西那生钠治疗的 SMA患者.汇总分析患者的基因检测结果、疾病分型、临床表现等临床基线资料.于治疗第 0、14、28、63天鞘内注射诺西那生钠 5 mL/12 mg,之后每 4 个月给予 1 次维持治疗.每次给药后,对患者的脑脊液、血常规及肝肾功能、凝血功能与基线值进行比较评估;定期随访并记录给药后发生的不良反应,评价用药安全性.结果 共 6 例患者确诊为 SMA,其中 SMA3 型 4 例,SMA4 型 2 例.患者神经元存活基因 1(survival motor neuron gene 1,SMN1)外显子 7 的缺失导致了运动神经元改变,多以肢体无力起病,严重者无法站立.患者的实验室检验异常基线结果包括脑脊液乳酸脱氢酶(CSF-LDH)升高、肌酸激酶(CK)升高、肌酐(Cr)降低.经过 4 次诺西那生钠治疗,患者脑脊液中的白细胞(CSF-WBC)、葡萄糖(CSF-Glu)、蛋白(CSF-Pro)、CSF-LDH 及血白细胞(WBC)、血小板(PLT)、红细胞(RBC)等血常规指标和肝肾功指标谷氨酸转氨酶(ALT)、天冬氨酸转氨酶(AST)、谷氨酰转移酶(GGT)、尿素氮(BUN)、尿酸(UA)及凝血功能指标凝血酶原国际标准化比值(INR)、活化部分凝血酶时间(aPTT)、D-二聚体较基线均无显著性变化(P＞0.05),且除穿刺后出现头疼、头晕、背疼外,无其他明显不良反应.结论 诺西那生钠治疗SMA有良好的安全性.

观察苦瓜提取物对Ⅱ型糖尿病胰岛素抵抗大鼠糖脂代谢及胰岛功能的影响.采用4周龄SD大鼠,以高脂饲料喂养大鼠16周后,单次给予腹腔小剂量注射链脲佐菌素(STZ)30 mg/kg,建立Ⅱ型糖尿病胰岛素抵抗动物模型,随机分为7组(正常组、模型组、二甲双胍实验组、吡格列酮实验组、苦瓜提取物实验组、二甲双胍-苦瓜提取物组、吡格列酮-苦瓜提取物组),每组12只.比较各药物干预4周后对Ⅱ型糖尿病胰岛素抵抗大鼠体重、饮水、摄食量、空腹血糖(FBG)、甘油三酯(TG)、胆固醇(TC)、低密度脂蛋白(LDL-C)、高密度脂蛋白(HDL-C)、游离脂肪酸(FFA)、胰岛素抵抗指数及胰岛β细胞功能的影响.结果表明:苦瓜提取物联合西药能缓解大鼠糖尿病症状(P<0.05)、苦瓜提取物、吡格列酮、苦瓜提取物联合西药可显著降低大鼠FBG;二甲双胍、吡格列酮、苦瓜提取物及苦瓜提取物联合西药均可降低TG、TC、LDL、FFA水平,升高HDL水平(P<0.05),并且能够降低胰岛素抵抗指数,改善胰岛β细胞功能(P<0.05).苦瓜提取物对Ⅱ型糖尿病胰岛素抵抗大鼠的空腹血糖、血脂水平及胰岛功能有一定调节作用.

目的:从医疗服务角度,对急性冠状动脉综合征(ACS)患者行经皮冠状动脉介入治疗(PCI)术后两种抗血小板药物治疗方案进行经济学评价.方法:两种治疗方案为在使用阿司匹林基础上,经验性给予国产氯吡格雷,或经验性给予替格瑞洛,由此建立决策树及Markov模型并进行成本-效果分析,评价中国ACS患者PCI术后使用氯吡格雷和替格瑞洛的成本-效果.结果:经验性给予国产氯吡格雷联合阿司匹林治疗方案为成本最低方案,但直接给予替格瑞洛联合阿司匹林治疗方案具有较好的成本-效果.结论:对于PCI术后的ACS患者抗血小板治疗,最推荐直接采用替格瑞洛联合阿司匹林的治疗方案.

目的:研究红花-甘草配伍对寒凝血瘀模型大鼠血浆及脑组织中三磷酸腺苷(ATP)、二磷酸腺苷(ADP)、一磷酸腺苷(AMP)及能荷(EC)水平的影响,从能量代谢角度探讨该配伍对寒凝血瘀证的影响.方法:采用冷水冰浴方法成功建立寒凝血瘀证SD大鼠模型,将造模成功大鼠随机分为4组,即模型对照组、红花组、甘草组、红花-甘草组,另设正常对照组.造模成功后,给药组灌胃相应的药物,剂量为20 g·kg-1,模型对照组和正常对照组给予等容积的纯净水,各组均连续灌胃15 d,检测大鼠血浆及脑组织中3种腺苷酸的含量并计算能荷值.结果:与正常对照组相比,模型对照组ATP、ADP的含量及EC值均显著降低(P＜0.01),AMP的含量降低不明显.与模型对照组相比,各给药组ATP、ADP的含量及EC值均显著升高,红花-甘草组改善上述指标的作用强于单药组,差异有显著性(P＜0.05).结论:红花和甘草均可改善寒凝血瘀模型大鼠的能量代谢,促进机体对能量物质的利用,红花-甘草配伍对改善寒凝血瘀证能量代谢显示出更佳的疗效.

目的 系统分析西安市某三甲医院H2受体阻滞剂(H2RAs)和质子泵抑制剂(PPIs)的使用情况,为临床合理用药提供参考依据.方法从该院信息管理系统(HIS)中提取2017年H2RAs和PPIs的用药数据,计算用药频度(DDDs)和限定日费用(DDC)等药物经济学指标,进行回顾性分析.结果 该医院使用抑酸剂99％以上是PPIs,几乎很少使用H2RAs.门诊患者使用口服抑酸剂的比例占93％,住院或急诊患者用静脉抑酸剂的比例占99％.PPIs全年的销售金额达到5 000多万元.其中静脉用药的销售金额为89％左右,使用量排名前3位的是兰索拉唑、泮托拉唑和雷贝拉唑,DDDs排名前3位的是兰索拉唑、泮托拉唑和奥美拉唑,DDC排序前3位的是雷贝拉唑(256.5元)、埃索美拉唑(118.23元)和兰索拉唑(84.8元).口服PPIs用量排名前3位的是泮托拉唑、兰索拉唑和奥美拉唑,DDC排序前3位的是雷贝拉唑(26.84元)、埃索美拉唑(11.26元)和奥美拉唑(7.15元).结论 该三甲医院抑酸剂主要使用PPIs,静脉使用过多,销量较大的几种静脉用PPIs的DDC值较高,不符合社会性及经济性的需求.兰索拉唑与其他PPIs相比无优势,但销售金额占50％,存在滥用现象.建议进一步加强PPIs的点评机制,促进其安全、有效使用.

A series of 2-phenoxy-N-phenylacetamides were designed and synthesized with a view to develop novel anticancer agents. All compounds were prepared with varied substitutions in the phenyl ring of aniline and evaluated for their anticancer activity. The majority of them displayed a moderate degree of cytotoxicity against several human cancer cell lines. Six compounds displayed potent cell growth inhibitory activity with IC50 values below 20 μM. Two compounds (TC-5 and TC-14) exhibited the most pronounced antiproliferative activity equivalent to or higher than that of positive control. The structure – activity relationship of these anticancer agents has been reviewed. The results indicate that incorporation of halogen into the benzene ring is beneficial for anticancer activity.

目的 评价连续性肾脏替代疗法(continuous renal replacement therapy,CRRT)在重症医学科(intensive care unit,ICU)患者中的应用现状.方法 回顾性分析2014年1～12月西安交通大学第一附属医院ICU的CRRT适应证患者171例的临床资料,分为行CRRT组(n=148)和未行CRRT组(n=23),其中CRRT组分为两个亚组:连续静脉-静脉血液滤过(continuous veno-venous hemofihration,CVVH)组(n=66)和非CVVH组(n=82).行CRRT治疗的148例患者按治疗效果分为好转组(n=83)、无好转组(n=46)及死亡组(n=19);行CVVH治疗的66例患者按治疗效果分好转组(n=39)和无好转组(n=27).对171例患者的适应证及行CRRT的148例患者的首选抗凝方案、置管方案、置换液、CRRT管路冲洗的5个指标进行统计评估,并对患者临床数据与CRRT治疗模式和患者治疗效果(好转、无好转及死亡)之间的相关性进行统计学分析.结果 171例患者的适应证及行CRRT的148例患者的首选抗凝方案、置管方案、置换液、CRRT管路冲洗这5个方面指标的合理率分别为86.55％、84.76％、66.89％、100％、100％.单因素分析显示,在3种治疗模式下(CVVH组、非CVVH组、未行CRRT组),171例患者的尿素氮基线(P=0.035)、肌酐基线(P=0.007)、治疗前3天每日尿量中d2(P =0.004)、d3(P=0.034),差异有统计学意义;CRRT组中首选置管方案与患者存活率(P=0.01)间差异有统计学意义、首选置管方案与存活患者预后之间(P=0.007)差异有统计学意义.多因素分析显示,CVVH组中ICU入住时长[P=0.005,OR:0.734,95％ CI(0.592,0.910)]、首选置管方案[P=O.016,OR:5.302,95％CI(1.369,20.527)],与患者预后呈显著相关性.结论 本研究中,171例患者的适应证及行CRRT的148例患者的首选抗凝方案、置管方案这3个指标存在不合理性,其不合理率分别为13.45％、15.24％、33.11％.临床药师应该结合患者的病理生理基础特征,考虑到ICU患者用药的复杂性,对患者行CRRT过程中的整体化用药,进行重点追踪、个体化监测,提高临床药物治疗水平,发挥药学人员在临床药物治疗管理方面的优势.

Twenty chalcone derivatives were designed and synthesized with a view to developing novel anticandidal agents. All the compounds were evaluated for their antifungal activity against Candida albicans (ATCC 10231 and ten clinical isolates). Most of them exhibited moderate anticandidal potency with MIC values ranging from 2.0 to 32.0 μg/mL. Four compounds ( T4 , T6 , T19 , T20 ) displayed potent anticandidal activity with MIC values of 2.0 μg/mL. Compound T6 showed the most potent activity against Candida albicans (ATCC 10231 and four clinical isolates). In addition, attempts have also been made to correlate anticandidal activity to physicochemical properties. The results indicated that incorporation of halogen on the benzene ring is beneficial for anticandidal activity.

Houttuynia cordata Thunb. (HC) is a medicinal herb that generally used in traditional Chinese medicine for treating allergic inflammation. The present study investigated the inhibitory effect of the volatile oil from HC Thunb. on animal models of inflammation and the production of inflammatory mediators in vivo and in vitro. In vivo, xylene‐induced mouse ear edema, formaldehyde‐induced paw edema and carrageenan‐induced mice paw edema were significantly decreased by HC volatile oil. HC volatile oil showed pronounced inhibition of prostaglandin (PG) E2 and malondialdehyde production in the edematous exudates. In vitro exposure of mouse resident peritoneal macrophages to 1, 10, 100 and 1000 µg/mL of HC volatile oil significantly suppressed lipopolysaccharide (LPS)‐stimulated production of NO and tumor necrosis factor‐α (TNF‐α) in a dose‐dependent manner. Exposure to HC volatile oil had no effect on cell viability and systemic toxicity. Furthermore, HC volatile oil inhibited the production of NO and TNF‐α by down‐regulating LPS‐stimulated iNOS and TNF‐α mRNA expression. Western blot analysis showed that HC volatile oil attenuated LPS‐stimulated synthesis of iNOS and TNF‐α protein in the macrophages, in parallel. These findings add a novel aspect to the biological profile of HC and clarify its anti‐inflammatory mechanism. Copyright © 2012 John Wiley & Sons, Ltd.

目的:探讨临床药师开展工作的思路,提高工作技能和服务水平。方法:对参与查房、做好合理用药咨询、协助医师选择药物,参与会诊等临床药学工作的实践进行认识和思考。结果:工作初期积极主动,学习临床相关知识并逐渐融入医疗团队;通过查房、会诊实现药师与医师共同参与制定药物治疗方案,进行用药监护,不良反应监测,共同承担治疗结果。结论:经过两个阶段的临床实践,通过查房、会诊途径坚持实践、及时总结归纳,临床药师能够顺利地胜任本职工作,并能提供优质的药学服务。

<正>凡特鲁斯特种产品公司2011年3月4日对外宣布,从2011年3月开始,该公司对吡啶产品价格进行调整,比2010年第四季度价格提高8%～10%,本次提价针对非协议客户或现有协议所允许的

OBJECTIVE:To develop a method for determining plasma and renal tissue concentrations of cisplatin (DDP) after subcutaneous DDP implantation in mice.METHODS:DDP was extracted from the plasma and tissue of mice receiving subcutaneous DDP implantation and reacted with sodium diethyldithiocarbamate (DDTC). The product Pt (DDTC)(2) extracted by diethyl ether was determined using high-performance liquid chromatography (HPLC) with the mobile phase of water and methanol at the ratio of 25:75 and the flow rate of 1.0 ml/min. The derivatives of DDP and nickel chloride were detected at the wavelength of 254 nm.RESULTS:The linear range of DDP was 0.1-10 microg/ml (r=0.9998 for plasma and 0.9993 for kidney). The intra-day and inter-day RSD was below 10%, and the minimum concentration detectable was 50 ng.CONCLUSION:The method is accurate and effective for determining plasma and tissue DDP levels after subcutaneous DDP administration and can be used in pharmacokinetic study of DDP.

Objective: To prepare Paracetamol (APP) multiloculated implant loaded with poly-lactide-co-glycolide acid (PLGA) and to study the drug release profile in vitro. Methods: APP multiloculated implant was fabricated by micro-electro-mechanical system (MEMS), and high-performance liquid chromato graphy (HPLC) measurement was used to investigate in vitro drug release profile. HPLC analysis was carried out by employing C18 column and a mixture of methanol-water (15:85) as mobile phase. The detection wavelength was 215 nm and flow rate was 0.8 mL/min. Results: With different multiloculated shape, the rate of the drug release in vitro was varied significantly. Moreover, the releasing of APP multiloculated implant with ecto-tetragonum ento-hexagon in vitro conformed to Higuchi equation. Conclusion: The technology of the preparations is feasible, and the structural and morphological characteristics of the multiloculated implant have a significant impact on the release speed of the drug delivery system.

OBJECTIVE:To investigate the effect of protecting liver of brevifolin and 8,9-single-epoxy brevifolin of Phyllanthus simplex.METHOD:Rats were administered with CCl4 (ip) or alcohol (ig) to establish acute or chronic liver injured model, respectively. ALT, AST and TBIL in serum were measured using colorimetric analysis to evaluate liver function. MDA content or SOD activity in serum and liver tissue was measured by thiobarbituric acid chromatometry and xanthine oxidase methods, respectively. The hemorheological parameters were observed.RESULT:Brevifolin and 8,9-single-epoxy brevifolin reduced the increase of ALT induced by CCl4, but they did not influence the increase of AST. And it could inhibit the pathologic increase of serum TBIL induced by alcohol. They could ameliorate the MDA increase or SOD decrease in serum and liver tissue in rats with liver injury, and decrease abnormal changed hemorheological parameters.CONCLUSION:Brevifolin and 8,9-single-epoxy brevifolin show protective effective against acute and chronic liver injuries, and the mechanism is relevant to antagonizing the lipid peroxidation of free radical and improving the blood circulation.