复方氯已定洗剂的制备与临床应用

目的探讨复方氯己定洗剂的制备方法、质量控制及临床疗效。方法复方氯己定洗剂由醋酸氯己定、甲硝唑经溶解后,滤过,再加纯化水至全量,即得;阴道炎患者70例,随机分为治疗组35例,使用复方氯己定洗剂,对照组35例,使用洁尔阴洗液,观察治疗后两组临床疗效及症状的改善情况。结果治疗组总有效率97.1%,对照组总有效率82.9%。经χ2检验,两组差异显著(P<0.05)。结论复方氯己定洗剂易于制备,方法简单,质量稳定,临床疗效安全、可靠。     

复方甲硝唑氯己定栓剂的制备与质量评价

目的制备复方甲硝唑氯己定栓,并评价其质量。方法用混合脂肪酸甘油酯、樟脑等辅料配制复方甲硝唑氯己定栓,采用高效液相色谱(HPLC)法测定醋酸氯己定、甲硝唑的含量。色谱柱为C18柱(4.6 mm×250 mm,5μm),流动相为甲醇-水-三乙胺(70∶30∶0.3)(含庚烷磺酸钠10 mmol.L-1,用磷酸调pH至4.0),流速1 mL.min-1,检测波长260 nm。结果栓剂的性状、鉴别、融变时限、含量测定等质量可控。甲硝唑、醋酸氯己定分别在8.94～107.28,0.764 8～8.952 0μg.mL-1浓度范围内线性关系良好。甲硝唑、氯己定回收率平均值分别为100.2%(RSD=0.5%),100.2%(RSD=1.0%)。结论该栓剂的制备方法简单易行,质量控制方法可靠。     

高效液相色谱法测定复方替硝唑洗剂中主药的含量

目的建立复方替硝唑洗剂中替硝唑和醋酸氯己定的含量测定方法。方法采用高效液相色谱法,色谱柱为岛津VP—ODS柱（150mm×4．6mm,5um）,流动相为磷酸盐缓冲溶液（取磷酸二氢钾4g,三乙胺2．5mL,庚烷基磺酸钠1g,加水至1000mL,用磷酸调pH至2．5）-甲醇（40：60）,流速为1．0mL／min,检测波长为260nm,柱温为35℃。结果替硝唑和醋酸氯己定质量浓度分别在37．6—376ug／mL和6．55～65．5ug／mL范围内与峰面积呈良好线性关系,r分别为0．9998和0．9999,平均回收率分别为99．51％和98．92％,RSD分别为1．25％和0．71％（n=6）。结论该法可同时测定制剂中替硝唑和醋酸氯己定的含量,操作便捷,结果准确。     

对甲硝唑氯己定洗剂处方的商榷

甲硝唑氯己定洗剂收载于《卫生部药品标准》(新药转正标准 )第十五册 1998。该药主要用于细菌性阴道炎、霉菌性阴道炎及原虫性阴道炎。在某单位欲仿制该药时 ,笔者对该药“处方”进行了认真思考 ,提出了自己的看法 ,认为有必要对原处方进行改进。1　对处方的改进1.1　改进处方的组成醋酸氯己定 (C2 2 H3 0 Cl2 N10 ·2C2 H4O2 )　　 1.0g甲硝唑 (C6H9N3 O3 ) 2 .0g薄荷脑 (C10 H2 0 O ) 0 .2 g丙二醇 (C3 H8O2 ) 80mL纯化水 (H2 O)适量全量 10 0 0mL1.2　原料来源醋酸氯己定 :锦州九泰药业有限责任公司 (原锦州制药一厂 ) ,批号 2 …     

高效液相色谱法测定复方替硝唑漱口液中主药的含量

目的 :测定复方替硝唑漱口液中替硝唑和醋酸氯己定的含量。方法 :采用高效液相色谱法 ,以ODS为固定相 ,乙腈 -水(35∶65)为流动相 ,甲硝唑为内标,检测波长为254nm。结果 :替硝唑在0 01～0 10mg/ml浓度范围内线性关系良好(r=0 9999) ;醋酸氯己定在0 01～0 10mg/ml浓度范围内线性关系良好 (r=0 9997)。替硝唑和醋酸氯己定的平均回收率分别为97 06%～102 02 %、97 21%～103 40% ;日内差分别为0 20%～1 26 %、0 71 %～1 11% ,日间差分别为0 50 %～2 06 %、0 80%～2 17%。结论 :本法可用于测定替硝唑、醋酸氯己定在各种制剂中的含量。     

HPLC法测定复方洗必泰漱口液中主药的含量

目的建立复方洗必泰漱口液中替硝唑和醋酸氯己定含量的测定方法。方法采用日本分光JASCO-1500系列高效液相色谱仪,Krom asil C1 8柱(250 mm×4.6 mm,5μm),以泼尼松(predn isone,PDS)为内标,流动相组成为甲醇-乙睛-水-四甲基乙二胺-冰醋酸(V/V)50∶50∶100∶0.1∶0.08,流速为1.0 m l.m in-1,紫外检测波长254 nm,灵敏度AuFs=0.02,柱温为30℃。结果替硝唑在0.02~0.10 g.L-1浓度范围内线性关系良好(r=0.9998),醋酸氯己定在0.02~0.10 g.L-1浓度范围内线性关系良好(r=0.9999),平均回收率分别为99.9%、99.7%,日内差分别为0.51%、1.18%。结论该法操作简便、结果可靠,可用于测定复方洗必泰漱口液中主药的含量。     

复方醋酸氯己定涂剂含量测定方法研究

目的：建立复方醋酸氯己定涂剂的含量测定方法。方法：采用紫外分光光度法,经三氯甲烷和1．5mol／L醋酸溶液提取后用乙醇溶解,在260nm波长处与对照品同法测定吸光度,计算醋酸氯己定含量。结果：醋酸氯己定在2．0—20．0μg／ml浓度范围内,与吸光度呈良好线性关系（r=0．999 7）,醋酸氯己定的平均回收率为101．0％,RSD为1．6％（n=9）。结论：该方法快速、简便、准确,可控制药品质量。     

高效液相色谱法测定复方甲硝唑漱口液中两组分的含量

目的 :测定复方甲硝唑漱口液中甲硝唑和醋酸氯己定的含量。方法 :采用高效液相色谱法 ,色谱柱为Shim PackCLC ODS ;流动相为 0 .3 %庚烷磺酸钠甲醇液%D水 (5 :2 ) ,用冰醋酸调节 pH至 3.2 ;流速为 1.0ml/min ;检测波长为 2 6 0nm。 结果 :甲硝唑和醋酸氯己定的回收率分别为 99.7% ,RSD =0 .5 1% ;99.5 % ,RSD =0 .5 9%。结论 :方法简便 ,准确 ,可作为该制剂的质控标准。     

薄层色谱法同时鉴别双唑泰泡腾片中的3种成分

双唑泰泡腾片用于治疗单纯或混合性感染所引起的妇科、肛肠科、皮肤科常见病 ,每片含甲硝唑2 0 0ｍｇ ,克霉唑 16 0ｍｇ ,醋酸氯己定 8ｍｇ。卫生部标准[1] 中此 3种成分的鉴别均采用颜色反应 ,专属性不强。每个成分分别鉴别 ,方法也较繁琐。本文以薄层色谱法同时鉴别 3种成分 ,专一性强 ,斑点明显 ,操作简便 ,结果较为满意。可作为双唑泰泡腾片的鉴别方法之一。1　仪器与试药三用紫外线分析仪 (上海顾村电光仪器厂 ) ,硅胶ＧＦ2 54 薄层板 (10ｃｍ× 2 0ｃｍ ,自制 ) ;甲硝唑、克霉唑、醋酸氯己定对照品 (中国药品生物制品检定所 ) ;双唑泰…     

HPLC法测定口宁含片中替硝唑与氯己定的含量

应用高效液相色谱法测定口宁含片中替硝唑、醋酸氯己定的含量 ,以甲醇 -水相 (取磷酸二氢钾 4g、三乙胺 2 .5ml、辛烷基磺酸钠 1 g,加水至 1 0 0 0 ml,磷酸调 p H至 2 .5) 65∶ 35为流动相 ,两种药物保留时间分别为2 .9min,6.3min;检测波长 :替硝唑 32 0 nm,氯己定 2 60 nm;平均回收率分别为 99.5% ,99.7%。     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.