卡络磺钠葡萄糖注射液制剂处方及工艺的研究

目的研究卡络磺钠葡萄糖注射液的制备工艺。方法对抗氧剂和金属螯合剂用量、pH值、活性炭用量和灭菌条件进行了筛选。用高效液相色谱法测定卡络磺钠的含量和有关物质。结果加入0.1%甲硫氨酸和0.005%依地酸钙钠,调pH值在4.5~5.5,加入0.05%的活性炭,115℃热压灭菌30 min。制剂质量符合药典有关注射剂的质量标准。结论本品制备工艺可靠,适于工业化生产,质量可控。     

左旋卡尼汀氯化钠注射液制备工艺研究

目的研究左旋卡尼汀氯化钠注射液的制备工艺.方法对活性炭用量、pH值、灭菌条件进行了筛选,并考察制剂稳定性.用HPLC法检测含量及有关物质.结果制备工艺采用浓配法,加入0.1%的活性炭,调pH值在5.5～6.5,115℃热压灭菌30 min.制剂质量符合药典有关注射剂的质量标准.结论本品制备工艺可靠,适于工业生产.质量可控.     

盐酸艾司洛尔注射液的处方工艺研究

目的研究盐酸艾司洛尔注射液的制备工艺。方法对缓冲剂和稳定剂用量、pH值、活性炭用量等条件进行了筛选。结果加入10%盐酸艾司洛尔和0.71%磷酸二氢钠,1.7%磷酸氢二钠,0.9%氯化钠,调pH值在4.5-5.5,加入0.1%的活性炭,100℃流通蒸汽灭菌30min。制剂质量符合药典有关注射剂的质量标准。结论本品制备工艺可靠,适于工业化生产,质量可控。     

卡络磺钠葡萄糖注射液制剂处方及工艺的研究

目的：研究卡络磺钠葡萄糖注射液的制备工艺。方法：对抗氧剂和金属螫合剂用量、pH值、活性炭用量和灭菌条件进行了筛选。用高效液相色谱法测定卡络磺钠的含量和有关物质。结果加入0.1％甲硫氨酸和0.005％依地酸钙钠，调pH值在4．5～6．5，加入0．05％的活性炭，115℃热压灭菌30min。制剂质量符合药典有关注射剂的质量标准。结论：本品制备工艺可靠，适于工业化生产，质量可控。     

木糖醇注射液的处方和工艺研究

目的研究大输液木糖醇注射液的处方和制备工艺。方法研究活性炭、pH值和灭菌条件等对木糖醇注射液质量的影响;用氧化还原滴定法测定木糖醇注射液的含量和用高效液相色谱法测定有关物质。结果木糖醇注射液加入0.1%活性炭,pH值在4.5～7.5,115℃热压灭菌30min F0≥8,质量符合药典的质量标准。结论本品制备工艺可靠,质量可控,适于工业化生产。     

硫普罗宁葡萄糖注射液处方及工艺的研究

目的研究硫普罗宁葡萄糖注射液的制备工艺。方法对抗氧剂和金属螯合剂用量、pH值、活性炭用量和灭菌条件进行了筛选。用高效液相色谱法测定硫普罗宁的含量和有关物质。结果加入0．05％甲硫氨酸和0．01％依地酸钙钠,调pH值在3．5～4．5,加入0．03％的活性炭,115℃热压灭菌30min。制剂质量符合药典有关注射剂的质量标准。结论本品制备工艺可靠,适于工业化生产,质量可控。     

正交实验法探讨氧氟沙星氯化钠注射液的生产工艺

目的探讨氧氟沙星氯化钠注射液生产中,金属离子、半成品pH值、活性炭及灭菌温度等因素对氧氟沙星氯化钠注射液质量的影响。方法采用多因素、多水平正交实验法[L16(45)]以及多指标评价方法,用方差分析进行数据统计分析,用F检验验证其显著性。因素及水平分别为:半成品pH值(4.0,5.0,6.0,7.0),活性炭用量(0,0.01%,0.05%,0.1%),EDTA-Na2用量(0,0.01%,0.05%),金属离子Fe3 微量,灭菌条件(室温放置,105℃45m in,115℃30m in,121℃20m in),质量评价指标[成品颜色(T450),含量(△A293),pH值(△pH)]。结果①影响产品颜色的主要因素为pH值、金属离子及活性炭用量,尤以pH值和金属离子最为显著,颜色随pH值升高、活性炭用量增高及金属离子浓度降低而变浅(T450增大);②影响产品含量的主要因素为活性炭用量和灭菌条件,含量随活性炭用量增加和灭菌温度升高而下降(︱△A293︱增大);③影响产品pH值的主要因素为活性炭用量,pH值随活性炭用量增加而降低(︱△pH︱增大)。结论根据实验数据的方差分析及F检验,得出生产氧氟沙星氯化钠注射液的最优生产工艺条件组合为:pH值控制为7.0左右,加入0.01%的EDTA-Na2作为金属离子络合剂,加入0.01%的活性炭,在105℃45m in条件下灭菌,经生产验证,产品质量好。     

甲萘氢醌二磷酸酯钠注射液处方和工艺研究

目的研究甲萘氢醌二磷酸酯钠注射液的制备工艺。方法对抗氧剂用量、pH值,灭菌条件进行筛选。用紫外分光光度法测定甲萘氢醌二磷酸酯钠的含量及有关物质。结果加入0．4％抗氧剂,药液pH值调为7．0～8．0,105℃热压灭菌30分钟,制剂质量符合药典有关注射剂的质量标准。结论本品处方工艺合理,质量稳定。     

血浆代用品注射液生产工艺的优化

目的对羟乙基淀粉类代血浆注射液的制备工艺进行研究,确定切实可行的生产工艺。方法分析影响羟乙基淀粉类代血浆注射液成品质量的因素,采用单因素方法,以成品的含量、可见异物的合格率及成品率为评价指标,考察了不同因素对注射液质量的影响。结果溶液温度、过滤温度、煮沸时间、药液pH值、活性炭用量及灭菌条件等因素对注射液的质量均有影响。最佳生产工艺条件为:在80℃以上溶解原料,加入0.1%的活性炭,煮沸30min,将药液pH值调至3.5~5.5,采用121℃,12min灭菌,即能得到质量可靠稳定的产品。结论该生产工艺设计合理,切实可行,代血浆类注射液质量稳定。     

替硝唑注射液制备工艺探讨

探讨替硝唑注射液制备工艺中活性炭用量对注射液的pH值和替硝唑含量的影响。结果：活性炭用量对替硝唑含量有极显影响,对pH值无显影响;灭菌对含量及pH值无显影响。     

高效液相色谱法测定膦甲酸钠氯化钠注射液中膦甲酸钠的含量

目的建立HPLC法测定膦甲酸钠氯化钠注射液中膦甲酸钠含量的方法.方法采用阴离子交换柱(Waters IC Pak A柱,50 mm× 4.6 mm,5 μm);以0.05 mol·L-1邻苯二甲酸氢钾溶液(取邻苯二甲酸氢钾0.204 g,加水适量,振摇使溶解,加1mol·L-1硝酸溶液5 mL,加水稀释至2 000 mL,摇匀即得)为流动相;流速1.4 mL·min-1,检测波长290nm.结果本方法在0.98～4.90g·L-1浓度范围呈良好线性关系(r=0.999 4),进样重现性RSD为0.71%(n=5),平均回收率为98.93%.结论本法简便、快速、结果准确可靠,可用于膦甲酸钠氯化钠注射液中膦甲酸钠的含量测定.     

Talaporfin sodium

Importance of the field: Despite therapeutic advances, cancer remains the cause of an estimated 23% of deaths in the USA. New treatments for malignancy are greatly needed.

Areas covered in this review: Talaporfin sodium is a light-activated drug that causes tissue death through induction of apoptosis. Systemic antitumor effects mediated by CD8⁺ T cells have been demonstrated in preclinical studies, providing a mechanism for distant response of tumors noted in clinical trials. Talaporfin sodium is approved in Japan for early-stage endobronchial cancer. Phase I and II studies in solid tumors have shown tumor regression in patients refractory to other therapies. Phase III pivotal studies against hepatocellular carcinoma as monotherapy and liver-metastatic colorectal cancer in combination with chemotherapy are ongoing. Talaporfin sodium is also in studies in men with symptomatic benign prostatic hyperplasia. Substantial safety data from clinical trials so far indicate that the drug is well tolerated.

What the reader will gain: Talaporfin sodium has a broad safety profile and a mode of action that could affect growth in treated and untreated tumors.

Take home message: Clinical and preclinical studies indicate that talaporfin sodium treatment may offer a powerful option to synergize current therapies, as well as an alternative monotherapy in treating cancer.     

头孢哌酮钠-舒巴坦钠致血小板减少

1名83岁男性患者因胆道系统感染,静脉给予注射用头孢哌酮钠-舒巴坦钠2.0g,1次/白天;1.0g,1次/晚上。用药6d内血小板进行性下降,由164×109/L下降到68×109/L。停用头孢哌酮钠-舒巴坦钠,改用左氧氟沙星治疗。1周后患者PLT恢复正常。     

哌拉西林钠他唑巴坦钠致抽搐

1例26岁男性患者,4年前行肾移植术,近5个月接受血液透析,因肺部感染给予哌拉西林钠他唑巴坦钠4.5 g加入0.9%氯化钠注射液100 ml、1次/d静脉滴注。第2次用药后5 h,患者突发抽搐、意识丧失、双眼上翻、双腿抽动。先后给予地西泮10 mg肌内注射及7 mg静脉注射,上述症状消失。     

Inhaled sodium metabisulphite induced bronchoconstriction: inhibition by nedocromil sodium and sodium cromoglycate.

1. The effects of nedocromil sodium and sodium cromoglycate on bronchoconstriction induced by inhaled sodium metabisulphite have been studied in eight atopic subjects, three of whom had mild asthma. 2. Nedocromil sodium (4 mg, 7.8 X 10(-6) M), sodium cromoglycate (10 mg, 24.1 X 10(-6) M) and matched placebo were administered by identical metered dose inhalers 30 min before a dose-response to sodium metabisulphite (5-100 mg ml-1) was performed. 3. Maximum fall in sGaw after placebo pre-treatment was -43.9 +/- 3.3% baseline (mean +/- s.e. mean). At the same metabisulphite concentration maximum fall in sGaw after sodium cromoglycate was -13.0 +/- 3.6% and after nedocromil sodium was +4.3 +/- 6.8%. Nedocromil sodium prevented any significant fall in sGaw even after higher concentrations of metabisulphite. 4. Both nedocromil sodium, 4 mg, and sodium cromoglycate, 10 mg, inhibited sodium metabisulphite induced bronchoconstriction but nedocromil sodium was significantly more effective. Relative in vivo potency of the two drugs is broadly in line with other in vivo and in vitro studies.     

Dalteparin sodium

Dalteparin sodium (Fragmin?, Pharmacia Corporation) is a low molecular weight heparin (LMWH) with a mean molecular weight of approximately 5000 Da. As with the other LMWHs, dalteparin sodium has certain advantages over unfractionated heparin (UFH), most important of which are improved bio-availability by sc. injection, a prolonged antithrombotic activity which is highly correlated with body weight permitting the o.d. administration of the drug. Dalteparin sodium has been subjected to a large number of well-designed randomised clinical trials for the prevention and treatment of thrombotic disorders. Based on data from the randomised clinical trials, dalteparin sodium has been approved internationally for a wide spectrum of clinical indications (e.g., prevention of thromboembolic events after surgery). Dalteparin sodium has also been studied in randomised controlled trials in the maintenance of graft patentcy following peripheral vascular surgery, in place of warfarin for the long-term treatment of patients presenting with deep vein thrombosis (DVT), in the prevention of upper extremity thrombosis in patients with indwelling portacath devices and in pregnant patients with a history of previous venous thromboembolism with or without thrombophilia. Dalteparin sodium has been compared with heparin for the prevention of thrombotic complications during haemodyalisis and haemofiltration. These studies have shown promising results but further work is required before dalteparin sodium can be recommended for these indications.     

Fondaparinux sodium

black triangle Fondaparinux sodium, a selective factor Xa inhibitor, is the first in a new class of antithrombotics. It binds selectively with high affinity to antithrombin III and specifically catalyses the inactivation of factor Xa. The elimination half-life of fondaparinux sodium permits once daily treatment. black triangle A randomised, double-blind, parallel-group, dose-ranging, multicentre phase IIb study in 933 eligible patients established that a subcutaneous dose of between 1.5 and 3mg of fondaparinux sodium has the optimum efficacy and safety profile for prophylaxis of venous thromboembolism in patients undergoing major orthopaedic surgery. black triangle Fondaparinux sodium, given to more than 3600 patients undergoing major orthopaedic surgery who participated in prospective, randomised, double-blind, multicentre phase III clinical trials, significantly reduced the incidence of venous thromboembolism, with an overall risk reduction of 55.2% compared with enoxaparin. black triangle Fondaparinux sodium was well tolerated by patients undergoing major orthopaedic surgery, and at the recommended clinical dose of 2.5mg has a similar tolerability profile, including bleeding events, to standard enoxaparin regimens. Fondaparinux sodium has not been reported to cause antibody-induced thrombocytopenia.     

哌拉西林钠他唑巴坦钠致白细胞减少

1例46岁女性患者,因术后颅内感染静脉滴注哌拉西林钠他唑巴坦钠4.5 g,1次/8 h。用药第13、15天外周血白细胞计数从用药前的10.61×109/L分别降至1.79×109/L和1.00×109/L。立即换用其他抗菌药物,同时给予重组人粒细胞巨噬细胞集落刺激因子(rhGM-CSF)150μg皮下注射,1次/d。改变治疗后4 d,血白细胞计数升至6.95×109/L。改变治疗后6 d脑脊液白细胞数由首次用药后15 d的8×106/L升至56×106/L,再次给予哌拉西林钠他唑巴坦钠4.5 g静脉滴注,1次/8 h,rhGM-CSF剂量未变。用药6 d颅内感染治愈,遂停用抗菌药物。治疗第2、5天白细胞计数分别为2.67×109/L和1.65×109/L。第8天停用rhGM-CSF后为5.75×109/L,第15天为4.56×109/L。     

Danaparoid sodium

Danaparoid sodium (Orgaran, Organon) is a heparinoid glycosamino-glycuronan antithrombotic agent approved for the prophylaxis of post-operative deep vein thrombosis (DVT), which may lead to pulmonary embolism (PE) in patients undergoing elective hip replacement surgery. Danaparoid is a low molecular weight heparinoid consisting of a mixture of heparan sulphate (84%), dermatan sulphate (12%) and small amounts of chondroitin sulphate (4%), whose antithrombotic activity has been well established. Its pharmacological effect is exerted primarily by inhibiting Factors Xa (FXa) and IIa (FIIa) at a ratio greater than heparin, with a minimal effect on platelet function. Danaparoid exhibits low cross-reactivity with heparin-induced antibodies when compared with heparin or low molecular weight heparins (LMWH), thereby making it an excellent choice for the management of heparin-induced thrombocytopenia (HIT). It has excellent bioavailability following s.c. injection. Danaparoid has little effect on routine coagulation tests (activated partial thromboplastin time [aPTT], prothrombin time [PT], and thrombin time [TT]). Patients with elevated serum creatinine should be monitored carefully. For its FDA approved indication (DVT prophylaxis during hip replacement surgery), its cost per day is approximately eight times more than LMWH. Even though monitoring is not routinely necessary according to the manufacturer for its approved indication, monitoring is frequently necessary when it is used in other clinical scenarios. Its higher cost than comparable therapies for DVT prophylaxis and the low availability of the FXa assay in most non-tertiary care hospitals has limited the widespread use of danaparoid. Danaparoid has been found to be effective in the treatment of HIT although this is an off label use, despite being the most frequent reason why danaparoid is used.