高效液相色谱法测定联苯苄唑凝胶的含量

目的建立联苯苄唑凝胶质量标准的分析方法。方法采用高效液相色谱法(RP-HPLC)测定联苯苄唑凝胶中联苯苄唑的含量,色谱柱:Hypersil C18柱(4.6 mm×250 mm,5μm);流动相:甲醇-水-乙腈(80∶15∶5);流速1 mL.m in-1;柱温:40℃;检测波长:254 nm。结果联苯苄唑在12.56~125.60μg.mL-1的浓度范围内线性关系良好(r=0.999 9)。联苯苄唑平均回收率(n=3)分别为99.0%(RSD=0.74%),100.5%(RSD=0.96%),98.7%(RSD=0.55%)。结论该方法可以用于测定联苯苄唑凝胶中联苯苄唑的含量。     

高效液相色谱法测定联苯苄唑凝胶的含量

目的:建立测定联苯苄唑凝胶 (必伏 )中联苯苄唑含量的方法.方法:采用高效液相色谱法 (HPLC法 ),以甲酸-水-四氢呋喃( 79 : 20 : 1)为流动相,检测波长为 254 nm.结果:联苯苄唑在 0.1～ 5 μ g范围内,峰面积与进样量呈良好线性关系,平均加样回收率为 100.3%( RSD=0.58%, n=9).结论: HPLC法简便、快速、准确,能有效控制联苯苄唑凝胶的质量.     

紫外分光光度法测定联苯苄唑凝胶剂的含量

目的：用紫外分光光度法测定凝胶剂中联苯苄唑的含量。方法：用甲醇作提取溶剂,以２５３ｎｍ为测定波长。结果：联苯苄唑浓度在２．３２～６．９６ｕｇ．ｍｌ＾－１范围内线性关系良好（ｒ＝０．９９９９）,平均回收率为１００．３％,ＲＳＤ为０．７％。结论：该法可用于凝胶剂中联苯苄唑的含量测定。     

联苯苄唑栓剂制备工艺与质量评价研究

摘 要 目的：优选联苯苄唑栓剂的制剂工艺,并评价其质量。方法: 以栓剂外观、硬度、融变时限等为评价指标,优化栓剂的基质、药物粒度、注模温度、搅拌条件等工艺条件,并采用HPLC法测定联苯苄唑含量。结果: 优选出的最佳处方组成为：混合脂肪酸甘油酯 36为基质,联苯苄唑过100目筛,最佳成型温度为 45℃。用以上方法制备的栓剂,其性状、融变时限、硬度、含量测定等质量可控。结论: 该栓剂处方设计合理,制备工艺合理可行,质量控制方法可靠。     

联苯苄唑中空泡腾栓的制备及质量标准研究

目的:制备联苯苄唑中空泡腾栓并建立其质量标准。方法:用半合成脂肪酸甘油酯作为栓剂基质,碳酸氢钠、柠檬酸为发泡剂,联苯苄唑为主药,热熔法制备中空泡腾栓,用紫外分光光度法对主药进行含量测定。结果:所制中空泡腾栓栓重约为2.3g,最大发泡量体积平均值大于8mL;联苯苄唑检测浓度线性范围为1.015～10.15μg·mL-(1r=0.9999),平均回收率99.74%(RSD=1.28%)。结论:联苯苄唑中空泡腾栓制备方法简便可行,达到了设计要求;含量测定方法精密度高,结果准确。     

联苯苄唑凝胶治疗体股癣手足癣疗效观察

目的:观察联苯苄唑凝胶治疗体股癣、手足癣的临床疗效。方法:选择体股癣117例和手足癣104例,给予1%联苯苄唑凝胶外涂,每日1次,共2周。结果:有效率:体股癣94.87%,手足癣92.31%,两组比较差异无显著性(P>0.05);真菌清除率:体股癣98.29%,手足癣95.19%,两组比较差异无显著性(P>0.05)。结论:联苯苄唑凝胶对体股癣、手足癣有较好的疗效。     

高效液相色谱法测定联苯苄唑凝胶中联苯苄唑的含量

目的　 测定联苯苄唑凝胶中联苯苄唑的含量。 方法 　采用反相高效液相色谱法 ,用C1 8色谱柱 ,以甲醇 - 0 0 5mol/L三乙胺水溶液 (用磷酸调pH 7 0 ) (85∶15 ,V/V )为流动相 ,流速为 1 0ml/min ,检测波长为2 5 4nm。结果 　联苯苄唑在 35 0～ 6 0 0 μg/ml范围内线性关系良好 (r =0 9998) ,平均加样回收率为 99 3%(RSD =1 6 3% ,n =5 ) ,3批样品的含量分别为 10 0 9%、10 2 4 %、98 5 %。 结论 　该法快速、准确 ,可以用来测定联苯苄唑凝胶中联苯苄唑的含量     

高效液相色谱法测定联苯苄唑凝胶中联苯苄唑的含量

目的 测定联苯苄唑凝胶中联苯苄唑的含量。方法 采用反相高效液相色谱法，用C18色谱柱，以甲醇-0．05mol／L三乙胺水溶液(用磷酸调pH7．0)(85：15，V／V)为流动相，流速为1．0ml／min，检测波长为254nm。结果 联苯苄唑在35．0～60．0μg／ml范围内线性关系良好(r=0．9998)，平均加样回收率为99．3％(RSD=1．63％，n=5)，3批样品的含量分别为100．9％、102．4％、98．5％。结论 该法快速、准确，可以用来测定联苯苄唑凝胶中联苯苄唑的含量。     

来曲唑凝胶剂的制备及质量评价

目的 制备来曲唑凝胶剂并对其质量进行评价.方法 制备来曲唑凝胶剂,并考察其黏度、pH值、含量等指标,然后分别进行离心实验、耐热实验及耐寒实验对其制剂稳定性进行考察.结果 来曲唑凝胶剂处方合理,制备工艺简单,制剂含量均一,易于涂抹,手感舒适,稳定性好.结论 为来曲唑凝胶剂的质量控制提供依据.     

高效液相色谱法测定联苯苄唑乳膏中联苯苄醇含量

目的建立测定联苯苄唑乳膏中的联苯苄醇含量的高效液相色谱（HPLC）法。方法以十八烷基硅烷键合硅胶为填充剂,以甲醇-水-四氢呋喃（84：15：1）为流动相,检测波长254nm。结果联苯苄醇质量浓度在1．04—10．44μg／mL范围内与峰面积线性关系良好,平均回收率为99．89％,RSD为0．82％（n=6）。结论HPLC法可用于测定联苯苄唑乳膏的联苯苄醇含量。     

Bifonazole. A review of its antimicrobial activity and therapeutic use in superficial mycoses

Bifonazole is a substituted imidazole antifungal agent structurally related to other drugs in this group. It possesses a broad spectrum of activity in vitro against dermatophytes, moulds, yeasts, dimorphic fungi and some Gram-positive bacteria. Both non-comparative and comparative clinical trials have clearly demonstrated the efficacy and safety of various formulations of bifonazole 1% (cream, gel, solution and powder) applied once daily in the treatment of superficial fungal infections of the skin such as dermatophytoses, cutaneous candidiasis and pityriasis versicolor. In comparative studies bifonazole was significantly superior to placebo and at least as effective as alternative imidazole antifungal drugs including clotrimazole, econazole, miconazole, oxiconazole and sulconazole. Preliminary studies in other superficial skin and nail infections/dermatoses suggest that bifonazole may be useful for treating onychomycoses (in a combination cream; bifonazole 1% plus urea 40%), otomycoses, erythrasma, sebopsoriasis, seborrhoeic dermatitis and rosacea. However, controlled trials are needed in each of these clinical settings to assess accurately its relative place in therapy. Thus, bifonazole is an effective and well-tolerated treatment for superficial fungal infections of the skin. Compared with the majority of topical antifungal drugs, which need to be applied at least twice daily, bifonazole offers the convenience of once daily administration, which may improve patient compliance.     

Inhibition of human CYP19 by azoles used as antifungal agents and aromatase inhibitors, using a new LC-MS/MS method for the analysis of estradiol product formation

Azoles are used as fungicides in agriculture or antifungal drugs in medicine. Their therapeutic activity is based on the inhibition of fungal lanosterol-14alpha-demethylase (CYP51). Azoles are also used for the treatment of estrogen-dependent diseases, e.g. in breast cancer therapy. Inhibition of CYP19 (aromatase) is the working principle for tumor therapy, but is an unwanted side effect of azoles used as fungicides or antifungal drugs. The inhibition of recombinant human CYP19 by 21 azoles in use for the three different purposes was investigated using the natural substrate testosterone. Estradiol product formation was measured by a newly developed and fully validated analytical method based on liquid chromatography-tandem mass spectrometry utilizing photospray ionization (APPI). Potency of enzyme inhibition was expressed in terms of IC50 concentrations. The two cytostatic drugs fadrozole and letrozole were the most potent inhibitors. However, azoles used as fungicides, e.g. prochloraz, or as antifungal drugs, e.g. bifonazole, were almost as potent inhibitors of aromatase as the drugs used in tumor therapy. Comparison of plasma concentrations that may be reached in antifungal therapy do not allow for large safety factors for bifonazole and miconazole. The IC50 values were compared to data obtained with other substrates, such as the pseudo-substrate dibenzylfluorescein (DBF). A high correlation was found, indicating that the fluorescence assay with DBF can well be used for potency ranking and screening of chemicals for aromatase inhibition. The data for antifungal drugs show that side effects on steroid hormone synthesis in humans due to inhibition of aromatase should be considered.     

新氢化可的松凝胶的制备及质量控制

目的研制新氢化可的松凝胶。方法以硫酸新霉素、氢化可的松为主药制备凝胶,采用抗生素微生物检定法和紫外分光光度法测定凝胶中硫酸新霉素、氢化可的松的含量。结果硫酸新霉素效价为标示量的90%～110%,氢化可的松的平均回收率为100.16%,RSD为0.18%,临床有效率为86.45%。结论该凝胶制备工艺简单,成本低廉,性质稳定,质量可控,疗效确切。     

等吸收双波长消除法测定复方联苯苄唑洗剂中两组分含量

目的：探索复方联苯苄唑洗剂中两组分含量测定的简便方法。方法：采用等吸收双波长消除法。联苯苄唑、氢化可的松的检测波长分别为254nm ,242nm。参比波长分别为226．6nm,267．8nm。结果：联苯苄唑、氢化可的松回收率分别为100．15％,100．13％,RSD分别为0．49％,0．42％。结论：本法操作简便、结果满意。     

Protective role of L‐ascorbic acid,N‐acetylcysteine and apocynin on neomycin‐induced hair cell loss in Zebrafish

Hair cells are highly sensitive to environmental insults and other therapeutic drugs. The adverse effects of drugs such as aminoglycosides can cause hair cell death and lead to hearing loss and imbalance. The objective of the present study was to evaluate the protective activity of L‐ascorbic acid, N‐acetylcysteine (NAC) and apocynin on neomycin‐induced hair cell damage in zebrafish (Danio rerio) larvae at 5 days post fertilization (dpf). Results showed that the loss of hair cells within the neuromasts of the lateral lines after neomycin exposure was evidenced by a significantly lower number of neuromasts labeled with fluorescent dye FM1‐43FX observed under a microscope. Co‐administration with L‐ascorbic acid, NAC and apocynin protected neomycin‐induced hair cell loss within the neuromasts. Moreover, these three compounds reduced the production of reactive oxygen species (ROS) in neuromasts exposed to neomycin, indicating that their antioxidant action is involved. In contrast, the neuromasts were labeled with specific fluorescent dye Texas‐red conjugated with neomycin to detect neomycin uptake. Interestingly, the uptake of neomycin into hair cells was not influenced by these three antioxidant compounds. These data imply that prevention of hair cell damage against neomycin by L‐ascorbic acid, NAC and apocynin might be associated with inhibition of excessive ROS production, but not related to modulating neomycin uptake. Our findings conclude that L‐ascorbic acid, NAC and apocynin could be used as therapeutic drugs to protect aminoglycoside‐induced listening impairment after further confirmatory studies. Copyright © 2014 John Wiley & Sons, Ltd.     

高效毛细管电泳法分离氟西汀和联苯苄唑的对映体

目的:建立拆分氟西汀和联苯苄唑两种药物手性对映体的方法。方法:采用高效毛细管电泳法,以羧甲基-β-环糊精(CM-β-CD)为手性选择剂,以未涂层熔融石英毛细管柱为分析柱,重力进样5 s,高度差10 cm,柱温20℃。分别对缓冲盐浓度、手性选择剂的浓度、缓冲盐的pH、分离电压进行考察,确定两种药物最佳分离条件;并以分离度为指标对两种药物的原料药进行分离验证试验。结果:氟西汀对映体在pH 4.5的30 mmol/LNaH2PO4缓冲溶液(含1.0%CM-β-CD)为运行电解质时达到最佳分离,分离度为3.70;联苯苄唑对映体在pH 3.0的30 mmol/LNaH2PO4缓冲溶液(含1.0%CM-β-CD)为运行电解质时达到最佳分离,分离度为5.44。方法精密度的RSD均≤0.9%(n=6)。结论:CM-β-CD的加入对氟西汀和联苯苄唑有很高的对映体选择性,可有效分离两种药物;建立的方法精密度好、经济、简便、快捷。     

HPLC-CAD法测定硫酸新霉素中新霉素B、新霉素C、新霉胺及其他有关物质

目的 建立测定硫酸新霉素中新霉素B、新霉素C、新霉胺及其他有关物质的高效液相色谱-电喷雾检测器(HPLC-CAD)方法。方法 采用Waters HSS T3色谱柱(4.6mm×250mm, 5μm)，以0.15mol/L三氟乙酸水溶液为流动相，流速1.0mL/min，柱温30℃，电喷雾检测器的雾化温度为45℃。结果 新建方法对新霉素B、新霉素C、其他有关物质分离度良好，精密度、重复性和回收率均满足分析要求。新霉素B、新霉胺浓度与峰面积线性关系良好(r＞0.995)，检出限可达到0.02μg和0.003μg。结论 新建方法分离度好、灵敏度高，可以检出更多的杂质，可以满足硫酸新霉素原料有关物质分析的要求。     

复方替硝唑凝胶剂的制备及临床应用

目的 建立制备复方替硝唑凝胶剂及含量测定方法，并对制剂进行临床疗效观察。方法 以替硝唑和司帕沙星为主药、羧甲基纤维素钠为基质制备复方替硝唑凝胶剂，采用双波长紫外分光光度法不经分离直接测定两主药含量，将制剂用于阴道感染的治疗。结果 制剂疗效确切，无刺激性，处方配伍合理，质量可控。结论 该凝胶制备工艺简单、质量稳定、临床疗效好，含量测定方法准确。     

氮酮和薄荷醇对联苯苄唑体外经皮渗透性的影响

目的：研究透皮促进剂氮酮和薄荷醇对外用抗真菌药联苯苄唑体外经皮渗透性影响。方法：在离体透皮实验装置上进行透皮吸收试验和贮库效应的研究，采用正交函数分光光度法消除皮肤浸出物的吸收干扰。结果：1％氮酮明显促进联苯苄唑经皮渗透作用，并可明显缩短时滞而增加贮库效应。结论：氮酮对亲脂性极强的药物联苯苄唑的促透皮吸收作用较强，而薄荷醇无明显的促透作用，但可增加贮库效应。