高效液相色谱法测定复方替硝唑栓剂中两组分的含量

目的 建立高效液相色谱法分离并测定复方替硝唑栓剂中两组分的含量，为该制剂制订质量标准提供科学依据。方法 采用Symmetry C18柱（2．5cm×4．6mm，5μm），流动相为甲醇：水：磷酸（65：35：0．1），pH值=3．65，检测波长为282nm，流速为1．0ml／min。结果 替硝唑、克霉唑的浓度线性范围分别为41．50～207．50μg·ml^-1；21．22—106．10μg·ml^-1。平均回收率分别为97．63％、98．02％，RSD分别为0．85％、1．09％；结论 方法简便，结果准确，重现性好，可用于该制剂的质量控制。     

Clotrimazole, an Imidazole Antimycotic, Is a Potent Inhibitor of Angiogenesis

Clotrimazole, an imidazole antimycotic, interferes with the rise in cytosolic Ca²⁺ and inhibits cell proliferation in a reversible manner. Here we describe the effect of clotrimazole on vascular endothelial cells (ECs). Clotrimazole inhibited the proliferation of ECs stimulated with typical angiogenic growth factors; vascular endothelial growth factor and basic fibroblast growth factor (bFGF). This inhibitory effect of clotrimazole was dose-dependent and the maximal inhibition was observed at a concentration of 10 m M . We did not observe any increase in ⁵¹Cr release from ECs during treatment with 10 μ M . clotrimazole. Moreover, clotrimazole inhibited the basal and bFGF-stimulated migration of ECs. As clotrimazole inhibited two principle components of angiogenesis; the proliferation and migration of ECs, we examined whether clotrimazole inhibited angiogenesis. Tube formation by ECs in type 1 collagen gel was investigated, and clotrimazole was found to be significantly inhibitory. The inhibitory effect of clotrimazole on angiogenesis was further confirmed in an in vivo angiogenesis model of murine Matrigel plug assay. These results demonstrate that clotrimazole is a potent inhibitor of angiogenesis.     

HPLC法测定复方醋酸氯己定洗剂中醋酸氯己定和克霉唑含量

目的:建立复方醋酸氯己定洗剂的含量测定方法.方法:采用高效液相色谱法,μBndapak-C18柱(5μm,250 mm×3.9 mm);流动相为乙腈-甲醇-水(21:37:42),每1000ml内含磷酸5ml,三氟乙酸1 ml,三乙胺调pH3.9～4.0;流速为1 ml·min-1;检测波长为230 nm.结果:醋酸氯己定和克霉唑分别在10～125μg·m1和2～25 μg·ml-1范围内线性关系良好;平均回收率分别为95.6%及96.5%(RSD 1.2%,1.5%).结论:本法色谱分离效率高,专属性好,同时测定两种成份,方法简便.     

克霉唑栓微生物限度检查方法的验证

目的探讨克霉唑栓微生物限度方法学验证。方法采用45℃1%吐温80的p H 7.0无菌氯化钠-蛋白胨缓冲液制备供试液,采用薄膜过滤法。结果各菌的回收率达到70%以上。结论该方法适合不同基质的克霉唑栓微生物限度方法检查。     

复方莪术油栓联合克霉唑阴道片治疗老年性阴道炎的临床研究

目的研究复方莪术油栓联合克霉唑阴道片治疗老年性阴道炎的临床疗效。方法选取2018年6月—2019年6月在平顶山市第二人民医院治疗的120例老年性阴道炎患者为研究对象,将所有患者随机分为对照组和治疗组,每组各60例。对照组给予克霉唑阴道片,1片/次,1次/d;治疗组在对照组治疗的基础上给予复方莪术油栓,1枚/次,1次/d。两组患者持续治疗10 d。观察两组患者临床疗效,比较两组临床症状缓解时间、阴道p H值、病原菌检出率、生活质量综合评定问卷(GQOLI-74)量表评分、阴道灌洗液炎性因子水平。结果治疗后,治疗组总有效率为95.00%,显著高于对照组的83.33%(P0.05)。治疗后,治疗组白带减少时间、外阴瘙痒、外阴阴道疼痛、黏膜充血消失时间明显短于对照组(P0.05)。治疗后,两组患者阴道酸碱度(p H)值、病原菌检出率均显著降低,GQOLI-74量表评分显著升高(P0.05);且治疗组指标改善较多(P0.05)。治疗后,两组患者阴道灌洗液白细胞介素-8(IL-8)、白细胞介素-6(IL-6)和肿瘤坏死因子-α(TNF-α)水平显著降低(P0.05);并且治疗组阴道灌洗液中细胞因子水平降低较多(P0.05)。结论复方莪术油栓联合克霉唑阴道片治疗老年性阴道炎具有较好的临床疗效,可缓解临床症状,提高患者生活质量,降低患者阴道灌洗液中细胞因子水平。     

酮康唑联合克霉唑栓治疗老年念珠菌性阴道炎的临床疗效及其安全性

目的探讨酮康唑联合克霉唑栓治疗老年念珠菌性阴道炎的临床疗效及其安全性。方法选取南昌县中医院2017年1月-2019年1月收治的老年念珠菌性阴道炎患者50例,根据单盲分组法分成参照组与研究组,各25例。参照组予以酮康唑治疗,研究组在参照组基础上联合克霉唑栓治疗。两组均治疗9 d。比较两组临床疗效,并观察两组不良反应发生情况。结果研究组治疗总有效率高于参照组,不良反应发生率低于参照组(P<0.05)。结论酮康唑联合克霉唑栓治疗老年念珠菌性阴道炎的临床疗效确切,可有效改善患者临床症状与体征,且安全性较高。     

克霉唑抗肝缺血-再灌注损伤凋亡机制的研究*

目的观察孕烷X受体(PXR)诱导药克霉唑对肝脏缺血-再灌注损伤后肝细胞凋亡影响,并探讨其机制。方法建立大鼠肝脏缺血-再灌注模型,32只雄性SD大鼠随机分为假手术组,模型对照组和克霉唑小剂量组、大剂量组进行肝缺血-再灌注损伤。TUNEL法检测肝组织中凋亡细胞,Western blot检测肝脏CYP3A1、Bcl-2、Bax、PARP表达水平。结果克霉唑小剂量组、大剂量组与模型对照组比较,细胞凋亡数减少,组织损伤减轻,凋亡细胞百分率明显降低,Bcl-2/Bax比值明显升高,抑制PARP剪切,提示有较好的抗凋亡作用,均差异有统计学意义;作为PXR特异性强诱导药克霉唑,与假手术组比,能明显诱导CYP3A1基因表达。结论PXR特异性强诱导药克霉唑可能通过促进Bcl-2表达及抑制Bax表达而拮抗肝细胞凋亡,从而减轻肝脏缺血-再灌注损伤,也与抑制PARP剪切有关。     

肤外洗药联合克霉唑预防念珠菌性外阴阴道病复发的疗效观察

目的：评价肤外洗药联合克霉唑预防念珠菌性外阴阴道炎（vulvovagi-candidiasis, VVC）复发的疗效和安全性。方法：选取本院就诊的患念珠菌性外阴阴道炎的患者73例,随机分组,每组在急性期都用克霉唑治疗,然后以近期临床痊愈者用肤外洗药作为巩固治疗方案的作为治疗组,以不用肤外洗药巩固治疗的作为对照组,比较两组的复发率及不良反应。结果：两组治疗后随访6个月,治疗组复发率明显低于对照组（P＜0.05）。结论：肤外洗药预防VVC患者的复发效果好,值得临床推广应用。     

HPLC测定克霉唑阴道片的主药及有关物质

目的 建立测定克霉唑阴道片含量及其有关物质的方法.方法 采用HPLC法,Luna C18色谱柱,甲醇-0.0125 mol·L-1磷酸氢二钠(78:22,磷酸调pH5.5)为流动相,检测波长220 nm.结果 克霉唑2.5～40.0 μg·ml-1与峰面积的线性关系良好(r＝0.9999),平均回收率为99.5%～100.2%,RSD＝0.1% (n＝6).有关物质咪唑为0.032%～0.037%,单一最大杂质为0.16%,有关物质总量为0.36%～0.37%.结论 所建方法准确、简便、快速,适用于克霉唑阴道片的质量控制.     

Clotrimazole decreases glycolysis and the viability of lung carcinoma and colon adenocarcinoma cells

Glycolysis is known to be the primary energy source in most cancer cells. We investigated here the effect of clotrimazole (1-(alpha-2-chlorotrityl)imidazole), the antifungal azole derivative, which was recently recognized as calmodulin antagonist, on the levels of glucose 1,6-bisphosphate and fructose 1,6-bisphosphate, the two stimulatory signal molecules of glycolysis, and on ATP content and cell viability in LL/2 Lewis lung carcinoma cells and CT-26 colon adenocarcinoma cells. We found that clotrimazole induced a significant, dose- and time-dependent reduction in the levels of glucose 1,6-bisphosphate, fructose 1,6-bisphosphate, ATP, and cell viability. These findings suggest that clotrimazole causes a reduction in glycolysis and ATP levels, which eventually leads to cell destruction after 3 h of treatment. Since cell proliferation was also reported to be inhibited by calmodulin antagonists, this substance is most promising agent in treatment of cancer by inhibiting both cell proliferation and the glycolytic supply of ATP required for cancer cell growth.