葛根素在环氧乙烷-环氧丙烷共聚物/磷酸氢二钾体系中的分配行为研究

目的:研究葛根素在环氧乙烷-环氧丙烷共聚物(EOPO)/磷酸氢二钾(K2HPO4)体系中的分配行为。方法:利用温度诱导相分离,结合双水相萃取技术,确定EOPO型号、诱导温度及时间。结果:当EOPO型号为EOPOSDP30,诱导温度为70℃,诱导时间为60min,EOPO质量分数为28%,K2HPO4质量分数为24%时,葛根素最大总收率可达42.26%。结论:该方法解决了传统双水相萃取技术中聚合物回收的难题,可以使EOPO循环使用,且方法设备投资少、操作简单,为工业化提取葛根黄酮提供了一条新途径。     

HPLC法测定酮戊二酸的含量

反相高效液相色谱法测定酮戊二酸的含量.采用Agilent ODS C18柱,以0.5%(NH4)2HPO4-H3PO4缓冲液为流动相,流速为1.0mL·min-1,紫外检测波长为233nm.酮戊二酸在0.04～0.09g·L-1浓度范围内线性关系良好(r=0.9999).平均回收率为99.56%(n=9).该方法简便、快捷、灵敏,可作为酮戊二酸含量测定方法.     

HPLC法同时测定葡萄糖酸钙锌口服溶液中盐酸赖氨酸与苯甲酸钠的含量

目的建立高效液相色谱法(HPLC)同时测定葡萄糖酸钙锌口服溶液中盐酸赖氨酸与苯甲酸钠含量的方法。方法采用C18色谱柱,流动相K2HPO4缓冲液(取K2HPO42.2822 g,加水溶解并稀释至1000 ml,用H3PO4调pH值至4.8后,加1.08 g辛烷磺酸钠)—乙腈(90∶10),流速1.0 ml/min,检测波长203 nm,柱温40℃。结果盐酸赖氨酸在0.03~1.21 mg/ml范围内,浓度与峰面积呈良好线性关系,平均回收率为101.06%(RSD%=0.8%)。苯甲酸钠在0.39~196.98μg/ml范围内,浓度与峰面积呈良好线性关系,平均回收率为100.27%(RSD%=0.7%)。结论本法简单、灵敏、准确、重现性好,可同时测定葡萄糖酸钙锌口服溶液中盐酸赖氨酸与苯甲酸钠的含量。     

大承气汤颗粒剂对正常豚鼠离体回肠运动的影响

目的观察大承气汤颗粒剂对正常豚鼠离体回肠运动的影响.方法检测豚鼠回肠在离体状态下加入不同剂量大承气汤颗粒剂的收缩幅度及速度.结果大承气汤颗粒剂在浓度1×10-4～2.5×103范围时,其作用是随剂量加大而逐渐加强,当浓度大于2.5×10-3时其作用是随剂量加大而逐渐减弱;浓度在1×10 5～1×10-3之间时,可使乙酰胆碱(Ach)作用增强,浓度在1×10-3～1×10-2时可使Ach作用逐渐减弱.结论大承气汤颗粒剂对豚鼠离体回肠有兴奋作用,小剂量时是随剂量加大而加强,大剂量时是随剂量加大而减弱.     

温敏型原位凝胶的热力学及流变学性质研究

目的:以磷酸川芎嗪为模型药物,探讨运用泊洛沙姆P407(P407)制备鼻用温敏型原位凝胶的可行性。方法:采用搅拌转子法测定不同处方磷酸川芎嗪原位凝胶的胶凝温度(胶凝温度:T);在不同温度下,以旋转式黏度计测定加入不同浓度辅料后P407溶液的黏度,以考察黏度随温度的变化规律。结果:P407溶液浓度越高,T越低;辅料的加入可以使P407溶液T升高,而处方药物和等渗调节剂(0.9%NaCl)使P407溶液T降低。当温度升高时,P407黏度增大,而辅料的加入会使P407黏度突变点的温度升高,黏度变小。结论:通过调节P407溶液的浓度或加入一定量辅料的方法,可以使TMPP原位凝胶在鼻腔温度(33℃左右)下胶凝,从而达到增大生物利用度和减少给药流失的要求。     

磷酸与磷酸二氢钾混合溶液的电导率初探

本文以磷酸和磷酸二氢钾混合溶液为研究对象,测量了混合溶液在不同温度下的电导率;研究了电解质溶液的电导率随摩尔比的变化规律。结果表明:溶液的电导率随磷酸与磷酸二氢钾的摩尔比增加而增加,电导率与摩尔比之间的关系可用函数式δ=ln(x+P3)P1×ln(x+P3)+P2表示。     

RP-HPLC梯度洗脱法测定痰咳净散剂中咖啡因和甘草酸的含量

目的　测定痰咳净散剂中咖啡因和甘草酸的含量。方法　在C18柱上 ,以 (A) 0 .0 1mol/LNa2 HPO4溶液 (用H3 PO4调pH为 3.0 ) ,(B)乙腈组成流动相 ,进行线性梯度洗脱 ,检测波长为 2 5 0nm ,外标法定量。 结果　线性关系良好 ,咖啡因的平均回收率为 99.7% ,RSD =0 .36 % (n =5 ) ,甘草酸的回收率为 99.6 % ,RSD =0 .4 2 % (n =5 )。结论　本法简便 ,重现性好 ,共存组分无干扰     

校正参数在血气分析中的意义

目的探讨体温、吸氧浓度（FIO2）、血红蛋白浓度（Hb）对血气分析结果的影响。方法检测血气后,输入不同校正参数,观察测量值、校正值及计算值的变化。结果随温度增加,pH、POz（A-a）渐降低,PCO2、PO2、PO2（a／,A）渐升高;随FIO2增加,PO2（A-a）渐增加,PO2（a／A）渐下降;随Hb增加,BE（B）、O2CT渐增加。结论校正参数对血气分析结果影响重大。     

PI3K-Akt信号转导通路在舒芬太尼后处理减轻大鼠心肌缺血再灌注损伤中的作用

目的探讨磷脂酰肌醇-3-激酶/丝氨酸-苏氨酸激酶(PI3K-Akt)信号转导通路在舒芬太尼后处理减轻大鼠心肌缺血再灌注损伤中的作用。方法健康雄性SD大鼠50只,体质量230²80 g,2280 g,2³月龄,采用随机数字表法,将其随机分为5组(n=10):假手术组(S组)、心肌缺血再灌注损伤组(I/R组)、舒芬太尼后处理组(PO组)、舒芬太尼后处理组+PI3K特异性抑制剂LY294002组(PO+L组)、PI3K特异性抑制剂LY294002组(L组)。I/R组,PO组,PO+L组,L组采用结扎左冠状动脉前降支30 min,再灌注120 min的方法来建造心肌缺血再灌注的模型。I/R组在再灌注前5 min时尾静脉注射0.9%氯化钠注射液1 ml,PO组在再灌注前5 min时尾静脉注射1ml舒芬太尼稀释液1μg/kg,PO+L组尾静脉注射1 ml舒芬太尼稀释液1μg/kg+LY2940020抑制剂0.3mg/kg,L组尾静脉注射1 ml LY2940020抑制剂0.3 mg/kg。于再灌注120 min时处死大鼠,取缺血部位心肌组织,用10%甲醛固定,常规石蜡包埋,切片。光镜下观察病理学结果,采用免疫组织化学方法测定心肌细胞Akt及磷酸化Akt(p-Akt)的表达,计算p-Akt平均吸光度值与Akt平均吸光度值的比值(p-Akt/Akt),采用TUNEL染色法检测心肌细胞凋亡,计算心肌细胞凋亡指数(AI)。结果与S组比较,其余4组AI、p-Akt/Akt的表达均升高(P<0.05);PO组比I/R组、PO+L组、L组AI降低,p-Akt/Akt的表达升高(P<0.05);PO+L组比L组AI降低,p-Akt/Akt的表达升高(P<0.05);I/R组与PO+L组及L组上述指标比较差异无统计学意义(P>0.05)。结论 PI3K-Akt信号转导通路参与了舒芬太尼后处理减轻大鼠心肌缺血再灌注损伤的作用。     

葛根素双水相体系中的分配特性及分配系数的关联

目的研究葛根素分别在PEG(NH4)2SO4双水相体系与丙酮K2HPO4双水相体系中的分配特性。方法研究系统总质量为20 g的PEG(NH4)2SO4中和体系总体积为10 mL丙酮K2HPO4中的体积比φ和分配系数K。结果确定了PEG(NH4)2SO4双水相最佳体系:PEG1500质量分数20%,(NH4)2SO4质量分数16%;丙酮K2HPO4双水相最佳体系:V(丙酮)∶V(水)=8∶2,K2HPO4质量为1.5 g。结论分别对这两个双水相最佳体系的分配系数进行了关联,lnK/φ2K2=A*+b*(w″-w′)这个模型适用于这两个双水相体系,关联结果与实验值符合良好。     

Ruxolitinib phosphate

Ruxolitinib phosphate是由美国Incyte公司研制开发的首个作用于Janus激酶1型和2型(JAK1,JAK2)的抑制剂,于2011年11月16日获美国FDA批准上市,其商品名为Jakafi。这是FDA至今唯一批准的治疗骨髓纤维化（myelofibrosis,MF）的药物。 Ruxolitinib phosphate的中文化学名称：(R)-3-环戊基-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)丙腈磷酸盐;英文化学名称：(3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile phosphate (1:1);分子式：C17H18N6&#8226;H3PO4;分子量：404.4;CAS号：1092939-17-7。     

Fludarabine phosphate

Fludarabine phosphate is a purine antimetabolite approved for use in the management of patients with chronic lymphocytic leukemia. Fludarabine works primarily by inhibiting DNA synthesis. The compound also possesses lymphocytotoxic activity with preferential activity toward T-lymphocytes.Initial preclinical studies demonstrated antitumor activity with fludarabine against L1210 murine leukemia. In phase I studies, myelosuppression was identified as the dose-limiting toxicity in patients with solid tumors and fatal neurotoxicity as the dose-limiting toxicity in adult patients with acute hematologie malignancies. The recommended dose and schedule was determined to be 18–25 mg/m²/d for five days, repeated every 28 days.Unlike preclinical studies, phase II trials showed a lack of significant effect when fludarabine was given to patients with solid tumors. However, phase II investigations have confirmed the efficacy of fludarabine in lymphoid malignancies, including non-Hodgkin's lymphoma, mycosis fungoides, prolymphocytic leukemia, and chronic lymphocytic leukemia. The place of fludarabine in the management of leukemias in children is under investigation. Early results indicate an unusual degree of antitumor activity when the agent is used in combination chemotherapy for patients with refractory disease.Fludarabine is an effective antitumor agent in the management of lymphoid malignancies. Studies are ongoing to more completely define the role of fludarabine in these malignancies as well as in the pediatrie leukemias. Additional studies evaluating the activity of fludarabine as an immunomodulator are warranted, due to the lymphocytotoxic properties associated with this agent.     

磷酸泰地唑胺

<正>磷酸泰地唑胺(tedizolid phosphate)是美国Cubist制药公司开发的一种口恶唑烷酮类抗生素,商品名为Sivextro,用于治疗金黄色葡萄球菌(包括耐甲氧西林菌株和甲氧西林敏感菌株)、各种链球菌及肠球菌等革兰阳性细菌引起的成人急性细菌性皮肤和皮肤组织感染。Sivextro的药用成分为磷酸泰地唑胺的钠盐,现有针剂和片剂两种剂型,于2014年6月20日获美国FDA批准上市。     

高效液相色谱法测定磷酸苯丙哌林胶囊中磷酸苯丙哌林的含量

目的建立高效液相色谱法测定磷酸苯丙哌林胶囊中磷酸苯丙哌林含量的方法。方法用C18色谱柱（4.6mm×250 mm,5μm）,流动相：甲醇-0.1 mol.L-1醋酸铵缓冲液（用冰醋酸调节pH至3.3）（65∶35）,流速：1.0 mL.min-1 检测波长：270 nm 柱温：室温。结果苯丙哌林的线性范围40.5~1012.0μg.mL-1,r=0.9995,平均回收率为99.2%,RSD=0.8%。结论方法简便、可靠、快速。     

Estramustine phosphate sodium

Estramustine phosphate is approved by the Food and Drug Administration for oral use in the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate. Estramustine is a conjugate of 17 beta-estradiol and the carbamate of nitrogen mustard. Although its therapeutic efficacy has been demonstrated, it is not clear to what extent each constituent contributes to estramustine's effectiveness. Estramustine phosphate therapy achieves objective response rates of 60-90 percent in advanced stage D prostatic cancer patients with no prior hormonal therapy. These results are consistent with those obtained with conventional hormonal therapy in similar patient populations. Therapeutic efficacy does not appear to increase when estramustine is used concurrently with other cytotoxic chemotherapeutic agents. An objective response rate of 20-30 percent can be anticipated in patients refractory to conventional hormonal therapy. It is in this group, the estrogen-resistant patients, that estramustine shows the most promise. Adverse effects of estramustine are similar to those of diethylstilbestrol. Gastrointestinal and cardiovascular side effects appear to be the most important and may be severe enough to require discontinuation of therapy.     

高效液相色谱法测定地塞米松磷酸钠乳膏中地塞米松磷酸钠含量

目的建立高效液相色谱法测定地塞米松磷酸钠乳膏中地塞米松磷酸钠的含量。方法采用高效液相色谱法,色谱柱为Diamonsil C18(2)柱(250 mm×4.6 mm,5 mm),流动相为乙腈-甲醇-三乙胺溶液(8∶57∶35),检测波长为242 nm。结果地塞米松磷酸钠在4.024~44.26μg·m L-1与峰面积呈良好的线性关系,平均加样回收率均大于98%,方法的精密度与重复性RSD均小于2.0%。结论本方法操作简便,专属性强,检测结果准确稳定,适用于地塞米松磷酸钠乳膏中地塞米松磷酸钠的含量测定。     

磷酸奥司米韦的合成研究

目的 研究磷酸奥司米韦的合成方法。方法 以莽草酸为起始原料,通过酯化、缩酮保护、甲磺酰化、缩酮交换、还原,闭环反应得关键中间体(3R,4S,5S)-4,5-环氧基-3-(1-乙基丙氧基)-1-环己烯甲酸乙酯(2);化合物2在氯化镁催化下和叔丁胺反应,经甲磺酰化、闭环得氮丙啶中间体,再经开环、乙酰化、脱叔丁基、脱烯丙基后成磷酸盐共13步反应得抗病毒药磷酸奥司米韦。结果与结论 合成的磷酸奥司米韦经1H-NMR和MS谱确证结构,总收率为29.5 %。     

Combretastatin A4 phosphate

Combretastatin A4 phosphate (CA4P) is a water-soluble prodrug of combretastatin A4 (CA4). The vascular targeting agent CA4 is a microtubule depolymerizing agent. The mechanism of action of the drug is thought to involve the binding of CA4 to tubulin leading to cytoskeletal and then morphological changes in endothelial cells. These changes increase vascular permeability and disrupt tumor blood flow. In experimental tumors, anti-vascular effects are seen within minutes of drug administration and rapidly lead to extensive ischemic necrosis in areas that are often resistant to conventional anti-cancer treatments. Following single-dose administration a viable tumor rim typically remains from which tumor regrowth occurs. When given in combination with therapies targeted at the proliferating viable rim, enhanced tumor responses are seen and in some cases cures. Results from the first clinical trials have shown that CA4P monotherapy is safe and reduces tumor blood flow. There has been some promising demonstration of efficacy. CA4P in combination with cisplatin is also safe. Functional imaging studies have been used to aid the selection of doses for phase II trials. Both dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) and positron emission tomography can measure the anti-vascular effects of CA4P in humans. This review describes the background to the development of CA4P, its proposed mechanism of action, the results from the first clinical trials with CA4P and the role of imaging techniques in its clinical development.     

儿童过量服用磷酸氯喹/磷酸伯氨喹的毒性特征分析

目的分析儿童过量服用磷酸氯喹/磷酸伯氨喹后的毒性反应特征,为合理用药及毒性反应的防治提供参考。方法收集我院收治的39例过量服用磷酸氯喹/磷酸伯氨喹儿童的病历资料,对服用药物后出现毒性反应的时间、临床症状以及血常规、肝功能、肾功能、心电图等检测指标的变化情况进行分析。结果儿童服用过量磷酸氯喹/磷酸伯氨喹后约3.9 h出现毒性反应。毒性反应主要累及神经系统、消化系统、循环系统,发生率分别为76.92%、74.36%、53.85%,主要临床症状为头晕、头痛、腹痛、腹泻、心律失常、心悸等。结论儿童过量服用磷酸氯喹/磷酸伯氨喹后毒性反应发生率高,毒性反应严重,应予积极救治,并做好肝肾功能等指标的监测。