苯扎氯铵对大鼠结肠神经及平滑肌的影响

目的研究苯扎氯铵对大鼠结肠神经及平滑肌的影响。方法8~9周龄SD大鼠50只,随机分为两组。氯胺酮麻醉下开腹,实验组用0.1%苯扎氯铵处理大鼠降结肠浆膜40min,温盐水冲洗后关腹,对照组用生理盐水代替苯扎氯铵。分别于术后1、2、3、4、8周取处理段结肠行组织学检查,反转录-聚合酶链反应(RT-PCR)检测乙酰胆碱酯酶(AchE)、巢蛋白(nestin)、乙酰胆碱M3受体(Chrm3)的表达,循环水浴药理学检测平滑肌收缩功能变化。结果苯扎氯铵处理后1周,大鼠结肠神经节细胞明显减少、空泡变,3周后完全消失;结肠平滑肌对乙酰胆碱敏感性增强。结论采用0.1%苯扎氯铵可使大鼠结肠产生去神经作用,结肠平滑肌对乙酰胆碱敏感性增强。     

苯扎溴铵酊处方改进及苯扎溴铵的含量测定

目的：改进苯扎溴铵酊处方,并建立容量分析法测定苯扎溴铵醇溶液（苯扎溴铵酊去除曙红成分）中苯扎溴铵的含量。方法在建立容量分析法测定苯扎溴铵的含量时,发现曙红在不同程度上均能影响含量测定结果,故将曙红成分从处方中删去。采用四苯硼钠（0.02 mol/L）为滴定液,滴定苯扎溴铵醇溶液中苯扎溴铵的含量。结果苯扎溴铵酊制剂更改为苯扎溴铵醇溶液,在含量测定中,滴定终点变化明显,易于判断。苯扎溴铵在浓度0.4~1.4 mg/mL的范围内与消耗四苯硼钠滴定液体积呈良好线性关系,r=0.9995,回归方程为V=18.3C-0.32。高、中、低3种剂量苯扎溴铵的平均回收率为99.12%,R SD为0.84%。结论本实验方法简便、快捷、准确,可作为苯扎溴铵醇溶液的质量控制标准。     

建立HPLC法测定盐酸洛美沙星滴眼液中5种抑菌剂

目的 建立同时测定盐酸洛美沙星滴眼液中5种抑菌剂(羟苯甲酯、羟苯乙酯、硫柳汞、苯扎溴铵和苯扎氯铵)的HPLC方法。方法 采用Extend C18(4.6mm×250mm, 5μm)色谱柱,流动相为1%三乙胺溶液(磷酸调pH值至3.0)-甲醇,梯度洗脱,流速为1.0mL/min,柱温35℃,检测波长为262nm。结果 羟苯甲酯、羟苯乙酯、硫柳汞、苯扎溴铵/苯扎氯铵各峰均分离良好;羟苯甲酯在0.0410~0.8204mg/mL范围内线性关系良好(r=1.0000),平均回收率为100.2%(RSD=0.8%, n=9);羟苯乙酯在0.0400~0.7996mg/mL范围内线性关系良好(r=1.0000),平均回收率为100.3%(RSD=0.7%, n=9);硫柳汞在0.0806~1.6112mg/mL范围内线性关系良好(r=0.9995),平均回收率为100.8%(RSD=0.9%, n=9);苯扎溴铵在0.0204~0.4076mg/mL范围内线性关系良好(r=0.9998),平均回收率为100.0%(RSD=0.9%, n=9);苯扎氯铵0.0197~0.3932mg/mL范围内线性关系良好(r=1.0000),平均回收率为100.4%(RSD=1.0%, n=9)。结论 该方法准确、灵敏、简便,可用于盐酸洛美沙星滴眼液中羟苯甲酯、羟苯乙酯、硫柳汞、苯扎溴铵及苯扎氯铵5种抑菌剂的检查。     

Quaternary ammonium compounds and occupational asthma

Objective: Quaternary ammonium compounds, among which benzalkonium chloride is one of the best-known, are commonly used as antiseptics, disinfectants, detergents and preservatives. They can cause occupational asthma, which however, has been rarely reported so far, despite wide use of these products. We report three such cases. Possible mechanisms causing asthma are discussed, taking into account their characteristics. Methods and results: Our patients, all female nurses, manifested asthma symptoms upon handling disinfectant solutions containing benzalkonium chloride. Work-related fall in PEFR was observed in all of them. The diagnosis was confirmed by challenge tests where the patients were exposed, in a closed chamber, to suspected disinfectant contained in a tray. All of the women developed early or delayed symptoms upon exposure. Similar challenge tests to placebo or other disinfectants devoid of quaternary ammonium compound were negative. Conclusion: These three cases, in addition to others reported in the literature, point out an as yet poorly known etiology of occupational asthma to quaternary ammonium compounds in hospital employees. The exact mechanism of the action remains unexplained. Received: 20 October 1999 / Accepted: 25 March 2000     

Application of the HPLC method for benzalkonium chloride determination in aerosol preparations

Benzalkonium chloride (BAC) is a bacteriostatic agent used in the pharmaceutical industry as a preservative. BAC is a mixture of alkylbenzyldimethylammonium chlorides, the three most important of which being those with alkyl substituents C12, C14, C16 at the quaternary ammonium salt.

The purpose of this study was to develop a method for determining benzalkonium chloride identity and content in aerosol preparations in which protein or steroid hormones are the active components. The high performance liquid chromatography (HPLC) method was used for this purpose. In the performed comparison of the influence of selected factors on the process of the separation of BAC homologues, a column with packing modified with cyan groups and mobile phase containing 0.075 M acetate buffer with acetonitrile (45:55), in an isocratic elution, was used for qualitative and quantitative determinations and for method validation. The developed method may be used for the assessment of the identity and content of BAC homologues in various pharmaceutical preparations. It is simple and it does not require particular sample preparation for the tests. It is characterized by good selectivity and high precision of the determinations.     

苯扎溴铵选择性电极的研制

The PVC membrane selective electrode for benzalkonium bromide was studied. It is based on the use of benzalkonium tetraphenylborate ion pair complex as the active material. The PVC membrane electrode showed Nernstian response over the concentration range from 10^-3 mol/L to 5×10^-6mol/L with a slope of 53～57 mV/pC, and the detection limit was found to be 3×10^-6 mol/L. The electrode showed rapid response and good reproducibility. The selectivity coefficients of 16 substances were determined. Using direct potentiometric determination, the recovery of pure benzalkonium bromide was 101.8%. The present method is more rapid and simpler than the volumetric method given in the Chinese Pharmacopoeia.     

HPLC法同时测定阿奇霉素滴眼液中阿奇霉素及苯扎氯铵的含量

目的建立一种高效液相色谱法同时测定阿奇霉素滴眼液中阿奇霉素及苯扎氯铵的含量。方法采用十八烷基硅烷键合硅胶色谱柱(4.6 mm×150 mm,5μm),柱温30℃,以乙腈-磷酸盐缓冲液(取0.05 mol.L-1磷酸氢二钾溶液,用20%磷酸调节pH至8.2)(58∶42)为流动相;检测波长210 nm;流速:1.0 mL.min-1。结果阿奇霉素在1.002 8～5.014 0 mg.mL-1的浓度范围内,苯扎氯铵在6.15μg.mL-1～14.35μg.mL-1的浓度范围内均呈线性。阿奇霉素的平均回收率100.68%,RSD为0.50%(n=9);苯扎氯铵的平均回收率100.59%,RSD为0.92%(n=9)。阿奇霉素与苯扎氯铵的定量限分别为750 ng.mL-1、46 ng.mL-1,平均含量分别为106.94%及100.04%,RSD分别为0.94%及0.67%。仪器重复性RSD值均在2.0%以下。结论本方法简单、准确,可同时测定样品中阿奇霉素及苯扎氯铵的含量。     

Meta analysis about the efficacy and safety of anti-ocular hypertension eye drops without benzalkonium chloride

ObjectiveTo explore the safety and efficacy of eye drops without benzalkonium chloride (BAK) in treating glaucoma and ocular hypertension.MethodsThe clinical case-control literatures about eye drops without BAK treating glaucoma and ocular hypertension were retrieved in PubMed, EMBASE, Cochrane and Chinese Biological and Medical database. Meta 5.0 software was used to analyze the literatures.ResultsFive clinical control studies were included. The results indicated both eye drops could lower the intraocular pressure, and the intraocular pressure-lowering difference between two eye drops was 0.07 mmHg (95% CI: 0.04, 0.19) (P>0.05). Two adverse reactions occurred more were conjunctival injection (10.78%) and allergic conjunctivitis (4.78%). The odd ratio of two eye drops occurring conjunctival injection and allergic conjunctivitis was 0.67 (95% CI, 0.25, 1.10) and 0.82 (95% CI, 0.09, 1.54), respectively (P<0.05) in fixed effect model.ConclusionsThere is no difference between the eye drops with or without BAK in lowering intraocular pressure, but the latter is of higher safety. In consideration of the relatively small sample size of this research, more high-quality clinical research contrasts are needed as evidence.     

ClO4-场效应敏感器件的研制及其在药物分析中的应用

应用碱性染料和乙基紫与ClO_4~-离子形成缔合物作为活性材料研制的PVC膜ClO_4~-电极,国内已有报道,本器件离子敏感膜是以十六烷基吡啶与ClO_4~-离子形成离子缔合物为活性材料,研制成涂丝ClO_4~-场效应敏感器件(ClO~4~-—ion sensitive field effect transistor简称为ClO_4~--ISFET);测定了器件的各项性能参数,并用于测定了药物溴化丙胺太林、苯扎溴铵,获得了较为满意的结果。