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目的建立高效液相色谱法测定人血浆中前体药物帕瑞昔布及其产物伐地昔布的浓度。方法色谱柱为Diamonsil C18柱(150 mm×4.6 mm,5μm),柱温30℃,流动相为乙腈-水-磷酸(57∶43∶0.01,V/V/V),流速1.0 mL.min-1,检测波长240 nm;内标为塞来昔布。结果帕瑞昔布的线性方程为Y=0.017 8X-0.022 9(r2=0.999 9),线性范围为1~100 mg.L-1。伐地昔布回归方程为Y=0.315 2X-0.005 1,(r2=0.999 8),线性范围为0.05~5 mg.L-1。帕瑞昔布和伐地昔布日内及日间RSD均小于15%,回收率均大于85%。结论本方法灵敏度高、专一性好、操作简单,可同时检测血浆中帕瑞昔布和伐地昔布,能满足药动学研究需要。 相似文献
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目的 探索头孢地尼的制备方法.方法 三苯甲基头孢地尼甲磺酸N,N-二甲基乙酰胺复合物为原料在磷酸和硫酸的乙腈溶液中脱除三苯甲基形成新的三元复合物;精制得到头孢地尼.结果 目标化合物经过1H-NMR和13C-NMR确证,且含量在98%以上,纯度高于99%,E-构型异构体含量小于0.1%,产品质量符合2010版药典标准.结论 操作简单,收率高,易于产业化. 相似文献
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戊地昔布抑制Lewis肿瘤生长的作用 总被引:1,自引:4,他引:1
目的检测戊地昔布抑制肿瘤生长的作用并初步探讨其作用机制。方法流式细胞术检测戊地昔布对肿瘤细胞凋亡和细胞周期的影响,Westernblot检测戊地昔布对肿瘤组织Bcl2、Bax、Caspase3,MMP2和VEGF表达的影响,用MTT法检测脾淋巴细胞转化率。结果①戊地昔布抑制Lewis肿瘤的生长,提高荷瘤小鼠的存活率。②10~40mg·kg-1·d-1戊地昔布增加肿瘤细胞的凋亡率,从对照组的19.1%增加到23.1%~29.1%。但对细胞周期分布没有影响。③戊地昔布对Caspase3,Bax,MMP2和VEGF的表达没有明显影响,但降低抗凋亡蛋白Bcl2的表达。④戊地昔布对荷瘤小鼠体重,胸腺指数和脾脏指数,脾脏淋巴细胞增殖没有影响。结论戊地昔布抑制肿瘤细胞生长的作用与其诱导肿瘤细胞凋亡有关。 相似文献
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目的 基于立方液晶载体将奥昔布宁制成一种高渗透性的纳米经皮给药制剂。方法 采用超声法制备奥昔布宁立方液晶纳米粒(OXY-CS)。以粒径、多分散指数、包封率为评价指标,优化搅拌温度、搅拌时间、搅拌速度、超声时间、超声功率、单油酸甘油酯/泊洛沙姆407(GMO/F127)质量比、载体(GMO+F127)/药物质量比及药物浓度;以累计渗透量和皮肤滞留量为评价指标,考察药物浓度、促渗剂、凝胶基∶质种类对皮肤渗透性的影∶响。结果 制得的OXY-CS分别在搅拌温度50℃、搅拌时间30 min、搅拌速度1 000 r/min、超声时间10 min、超声功率100 W、GMO/F127质量比2体/药物质量比3≥3%时具有较高的累积渗透量和皮肤滞留量。OXY-CS中添加促渗剂不能提高药物的累计渗透量。以卡波姆为凝胶基质制得的奥昔布宁立方液晶凝胶剂皮肤渗透性显著优于其他凝胶基质。结论 本研究将奥昔布宁制备成一种立方液晶凝胶剂,有望能改善口服给药带来的诸多不良反应。 相似文献
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抗抑郁药地昔帕明辅助肿瘤治疗的药理和临床应用进展 总被引:2,自引:0,他引:2
主要介绍三环类抗抑郁药地昔帕明的药物动力学以及在辅助肿瘤治疗方面的应用。地昔帕明不仅可缓解肿瘤病人的抑郁症以及肿瘤引起的疼痛 ,还可增强化疗药物对肿瘤细胞的杀伤作用 ,逆转肿瘤的多药耐药性。 相似文献
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戊地昔布对人胃癌细胞生长的抑制作用 总被引:1,自引:3,他引:1
目的 探讨选择性环氧化酶 2 (COX 2 )抑制剂戊地昔布对人胃癌BGC 82 3细胞的作用及其作用机制。方法 用MTT法检测戊地昔布对人胃癌BGC 82 3细胞生长的作用 ,用流氏细胞仪检测细胞凋亡和细胞周期分布 ,用激光共聚焦显微镜、透射电镜和DNA片段进一步检测细胞凋亡 ,用乳酸脱氢酶 (LDH)试剂盒测定BGC 82 3细胞的LDH含量。结果 戊地昔布 (2 5~ 4 0 0 μmol·L-1 )可时间和浓度依赖性抑制人胃癌BGC 82 3细胞的生长 ,作用 72h后 ,对细胞生长抑制率可达 2 4 0 %~ 92 0 % ,凋亡率由 (2 6± 0 7) %增加到 (7 6±1 5 ) %~ (1 6 5± 1 5 ) %。 1 0 0~ 4 0 0 μmol·L-1 也降低增殖指数 ,减少细胞周期S期细胞 ,增加G0 /G1 期细胞。随浓度增加 ,戊地昔布引起的LDH释放率有增加趋势 ,但只有 4 0 0μmol·L-1 戊地昔布可显著增加LDH释放率。结论 戊地昔布可通过诱导凋亡和细胞周期停滞而抑制人胃癌BGC 82 3细胞生长 ,4 0 0 μmol·L-1 戊地昔布抑制BGC 82 3细胞生长作用与细胞坏死有关 相似文献
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摘 要 目的:观察前列地尔联合更昔洛韦常规治疗带状疱疹的疗效和安全性。方法:120例带状疱疹住院患者随机分为两组各60例。对照组给予更昔洛韦注射液常规治疗;观察组在对照组基础上加用前列地尔注射剂。两组疗程均为12 d。比较两组止疱时间、疼痛缓解时间、皮损痊愈时间,治疗后随访1~3个月,比较两组后遗神经痛(PHN)发病率。结果:两组止疱时间和皮损痊愈时间比较,差异无统计学意义(P>0.05)。观察组疼痛缓解时间、PHN发病率显低于对照组(P<0.05)。结论:前列地尔联合更昔洛韦常规治疗能明显缩短带状疱疹患者的疼痛时间、降低PHN的发病率,且安全性好。 相似文献
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地昔帕明对脑胶质瘤C6细胞的增殖抑制和凋亡诱导作用 总被引:2,自引:0,他引:2
目的研究地昔帕明(DMI)对大鼠脑胶质瘤C6的增殖抑制和凋亡诱导作用,为三环类抗抑郁药作为肿瘤辅助治疗提供新的理论和实验依据。方法用MTT比色法测定C6细胞活力,用透射电镜、流式细胞术(FCM)检测细胞凋亡,用免疫组化法分析bcl-2蛋白的表达。结果DMI对C6细胞的增殖具有明显的浓度依赖性抑制作用, IC50( 95 %置信区间)为20.7(17.3~24.2)μmol·L-1,细胞阻滞于G0~G1期。DMI(40μmol·L-1)使细胞发生典型的凋亡形态改变,DNA含量分析显示 G0峰左侧出现亚二倍体细胞凋亡峰,呈浓度依赖性,蛋白合成抑制剂CHX可显著抑制DMI诱导的细胞凋亡。同时,DMI(10 μmol·L-1)可下调细胞 bcl-2蛋白的表达。结论DMI体外对C6细胞的增殖具浓度依赖性抑制作用,并诱导细胞凋亡。 相似文献
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目的观察和评价地佐辛联合帕瑞昔布钠对急性疼痛小鼠镇痛作用的影响。方法将40只C57小鼠随机分为四组:空白对照组(A组)、地佐辛组(B组)、帕瑞昔布钠组(C组)、地佐辛联合帕瑞昔布钠组(D组),每组10只。各组分别给予腹腔注射无菌双蒸水0.2mL;地佐辛5mg/kg;帕瑞昔布钠10mg/kg;地佐辛3mg/kg联合帕瑞昔布钠10mg/kg。每天1次,连续给药3d,第3天给药15min后.制作扭体法和甲醛疼痛模型,观察小鼠痛阈变化。结果与A组比较,其余各组小鼠扭体次数和舔足时间均明显减少,差异有统计学意义(P〈0.05);与C组比较,B组小鼠明显减少了扭体次数和舔足时间,差异有统计学意义(P〈O.05);D组小鼠扭体次数和舔后足时间显著少于B组,差异有统计学意义(P〈0.05)。结论地佐辛和帕瑞昔布钠均可以有效缓解小鼠急性疼痛,地佐辛的镇痛作用较帕瑞昔布钠明显,而地佐辛联合帕瑞昔布钠能进一步增强镇痛效果,且可以减少地佐辛的用药量。 相似文献
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《中国药物化学杂志》2017,(4)
目的研究博舒替尼合成新方法。方法用取代的邻氨基苯甲酸酯和3-二甲氨基丙烯腈合成了关键中间体4-(3-氯丙氧基)-2-(2-氰基乙烯基氨基)-5-甲氧基苯甲酸甲酯。结果与结论以香草醛为起始原料,经10步反应合成博舒替尼,总收率为35.5%(以香草醛计),终产品HPLC含量为99.9%。该路线操作简便,适合大量制备。 相似文献
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A simple method for preparation of immuno-magnetic liposomes 总被引:7,自引:0,他引:7
A simple and readily manoeuverable method for preparing immuno-magnetic liposomes that indigenously contain binding sites for attaching other molecules like antibodies on their exterior surface is described. In this method magnetic unilamellar vesicles are prepared from a mixture of phosphatidylcholine, cholesterol, small amounts of a linear chain aldehyde and colloidal particles of magnetic iron oxide, using a reverse phase evaporation technique. The aldehyde (dedecanal) molecules align themselves among the lipid molecules in the bilayer with their aldehyde groups exposed to the aqueous phase, allowing straight attachment of antibody molecules (human-antimouse IgG-FITC in this case) in one single step. The success of this approach is confirmed by fluorescence microscopy as well as binding of the resulting immuno-magnetic liposomes to their corresponding target cells. 相似文献
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A new one-step method for the preparation of 3',5'-bisphosphates of acid-labile deoxynucleosides 总被引:1,自引:0,他引:1
A method is described for preparing 3',5'-bisphosphates of labile deoxynucleosides. Under strictly anhydrous conditions, pyrophosphoryl tetrakistriazole apparently forms a ring structure bridging the 3'- and 5'-hydroxyl groups of deoxynucleosides, since upon the addition of water the ring opens and the 3',5'-bisphosphate is formed. Due to the presence of triethylamine no acid is generated at any time so that the entire procedure is in neutral solution. The bisphosphates of N2,3-ethenodeoxyguanosine, O2-ethyldeoxythymidine, and O4-methyldeoxythymidine, all of which are acid-labile, were prepared in good yield without degradation. Other modified bisphosphates prepared include O6-benzyldeoxyguanosine and 1,N6-ethenodeoxyadenosine, as well as those of unmodified deoxyguanosine and thymidine. Characterization was by 31P NMR and UV spectroscopy. Both 5'p(dT)p3' and 5'p(dG)p3' were substrates for RNA ligase, further proving the structure of the phosphorylated compounds. 相似文献
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V. V. Zakusov 《Pharmaceutical Chemistry Journal》1979,13(10):1094-1097
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A novel technique for the preparation of Eudragit RL microcapsules is described. The technique is based on the principle of solvent evaporation. Diclofenac sodium is used as a model drug for encapsulation. A solution of drug and Eudragit RL dissolved in acetone-isopropyl alcohol (1:1) is sprayed in liquid paraffin. The microcapsules obtained were uniform and free flowing particles. The release rate was more sustained by increasing the polymer concentration. The experimental procedure promises a rapid and convenient method for the preparation of Eudragit RL-microcapsules. 相似文献
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A series of p-nitroanilides of t-butyloxycarbonylamino acids, including Boc-Trp, Boc-Asn, Boc-Gln, Boc-Ser(Bu′), Boc-Thr(Bu′), Boc-Asp(OBu′), Boc-Lys(TFA), and Boc-His(Boc), were prepared conveniently by the mixed anhydride method using 2,2-dimethylpropanoic chloride (pivaloyl chloride). The products were obtained in 40-60% yields after purification by column chromatography on Sephadex LH-20. p-Nitroanilide of histidine was purified after deprotection of Boc-His(Boc)-pNA and obtained as H-His-pNA-2HCl. 相似文献
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A novel technique for the preparation of Eudragit RL microcapsules is described. The technique is based on the principle of solvent evaporation. Diclofenac sodium is used as a model drug for encapsulation. A solution of drug and Eudragit RL dissolved in acetone-isopropyl alcohol (1:1) is sprayed in liquid paraffin. The microcapsules obtained were uniform and free flowing particles. The release rate was more sustained by increasing the polymer concentration. The experimental procedure promises a rapid and convenient method for the preparation of Eudragit RL-microcapsules. 相似文献