阿昔洛韦片剂和胶囊在人体的生物利用度

10名男性受试者按交叉实验设计口服阿昔洛韦片剂和胶囊各400 mg 后,用改良的 HPLC 测定血药浓度,计算表明阿昔洛韦胶囊口服后吸收快于片剂,峰浓度也较高,但吸收程度(AUC_(0-12h))相似。     

阿昔洛韦软膏的稳定性研究

目的 :建立阿昔洛韦软膏高效液相色谱测定方法 ,考察该制剂的稳定性。方法 :采用高效液相色谱法测定软膏中阿昔洛韦的含量 ,考察湿度、光照及温度对阿昔洛韦软膏稳定性的影响。结果 :标准曲线方程为C=9 310×10-3A +0 159 ,r=0 9999(n=6) ;线性浓度范围为0 6～19 2μg/ml ;回收率为98 51 % ,RSD=0 42 %。阿昔洛韦软膏对湿度和强光照射不敏感 ;于40℃、60℃和80℃温度下放置10d ,其标示量分别为98 36 %、98 47 %和98 26 %。结论 :建立的方法具有简便、快速和准确度高等优点 ;该制剂对强光照射不敏感 ,室温保存稳定。     

高效液相色谱法测定阿昔洛韦眼用凝胶的含量

目的 :建立测定阿昔洛韦眼用凝胶中阿昔洛韦含量的高效液相色谱法。方法 :采用反相HypersilC18色谱柱 (5 μm ,2 5 0mm× 4.6mm)为分离柱 ;流动相 :水 甲醇 冰醋酸 (92∶8∶0 .1) ,检测波长 :2 5 2nm ,以峰面积计算。结果 :线性范围 :12～ 32mg·L-1,r =0 .9999。平均回收率为 99.72 % ,RSD为 0 .40 %。日内平均RSD为 0 .70 % ,日间平均RSD为 0 .85 %。结论 :本法简便 ,快捷 ,灵敏 ,可作为该制剂质量控制的有效方法。     

6-O-取代苯基阿昔洛韦衍生物的合成及其抗病毒活性

目的设计合成6-O-取代苯基阿昔洛韦衍生物,并进行抗病毒活性测定.方法以阿昔洛韦(ACV)为先导化合物,对阿昔洛韦分子中的碱基进行结构修饰,合成一系列6-O-取代苯基阿昔洛韦衍生物,并以阿昔洛韦为阳性对照进行体外抗HSV-Ⅰ和HSV-Ⅱ病毒活性测定.结果合成了11个未见文献报道的6-O-取代苯基阿昔洛韦衍生物,其结构均经元素分析、1H-NMR和MS确证.结论部分目标化合物具有一定的体外抗HSV-Ⅰ和HSV-Ⅱ病毒活性,但较阿昔洛韦作用弱.     

更昔洛韦眼用凝胶和阿昔洛韦滴眼液治疗病毒性角膜炎疗效对比

目的：探讨病毒性角膜炎应用更昔洛韦眼用凝胶的疗效。

方法：随机选择2013-05/2014-10我院收治的84例101眼病毒性角膜炎患者作为研究对象,随机分为更昔洛韦组和对照组,分别给予更昔洛韦眼用凝胶和阿昔洛韦滴眼液治疗,2wk后观察疗效。

结果：两组患者治疗后较治疗前病毒性角膜炎各症状(畏光、流泪、疼痛、异物感)及各体征(睫状充血、角膜上皮缺损、角膜基质水肿、角膜荧光素染色)评分均有显著改善,更昔洛韦组改善更为明显(P<0.05); 更昔洛韦组有效率(92.9%)明显高于对照组(59.5%),差异有统计学意义(P<0.05); 两组患者不良反应无统计学差异(P>0.05),更昔洛韦组复发率明显低于对照组(P<0.05)。

结论：更昔洛韦眼用凝胶是一种安全有效的抗病毒滴眼液,治疗病毒性角膜炎疗效确切,值得临床中推广应用。     

荔枝核提取物体外抗病毒活性及其机制研究

目的:研究荔枝核提取物(LSE)的体外抗病毒活性,并初步研究其抗病毒的作用机制.方法:采用细胞病变效应(CPE)减少法和MTY法检测LSE对柯萨奇B3病毒(Cox B3)、呼吸道合胞病毒(RSV)以及单纯疱疹病毒1型和2型(HSV-1和HSV-2)的体外抗病毒活性,并通过观察直接杀病毒作用、对宿主细胞的保护作用、抑制病毒吸附作用以及在病毒感染后不同时间加入实验,对LSE抑制HSV-1的作用机制进行探讨.结果:LSE有一定的细胞毒性,它不能抑制Cox B3在宿主细胞内的增殖,但对RSV、HSV-1和HSV-2表现出明显的浓度依赖性抗病毒活性,其IC<,50>值分别为32.3,27.9和20.4μg/mL.该提取物预培养Vero细胞后不能保护细胞免受HSV-1感染,但它对HSV-1有直接的灭活作用.LSE可影响HSV-1对Vero细胞的吸附,当浓度为31.3μg/mL时对病毒吸附的抑制率为51%.ISE对HSV-1在细胞内的增殖表现出很强的抑制活性.结论:LSE具有较强的体外抗RSV和HSV活性,它对HSV的抑制作用可能通过多种方式和途径实现.     

Intermittent oral cyclosporin for recurrent herpes simplex-associated erythema multiforme

Recurrent erythema multiforme is one of three distinct clinical subtypes of erythema multiforme. We present a 42-year-old man with a 10-year history of recurrent herpes simplex virus-induced erythema multiforme. Our patient was debilitated by the frequency of his attacks and the associated pain, for which he often required leave from work. The frequency, duration and morbidity of the attacks were poorly controlled using oral prednisone and oral aciclovir. Three episodes of his recurrent herpes simplex virus-induced erythema multiforme were treated with intermittent oral cyclosporin. Oral cyclosporin rapidly reduced his symptoms and led to rapid resolution of his erythema multiforme, provided the cyclosporin was commenced on day 1 or 2 of the erythema multiforme episode. Consequently, his quality of life has dramatically improved. We recommend the use of intermittent oral cyclosporin for recurrent, debilitating episodes of erythema multiforme.     

Recurrent herpes labialis: efficacy of topical therapy with penciclovir compared with acyclovir (aciclovir)

This study compares the effects of topical acyclovir and penciclovir in the treatment of recurrent herpes labialis. The study patients were a population of 40 patients with in excess of five recurrences annually, and were separated into four homogeneous groups each of 10 subjects. The antiviral creams were used to achieve total lesional cover, every 2 h during waking hours. The effects on the time to lesion crusting and to resolution of pain, were assessed. The results not only confirmed that aciclovir is ineffective, but confirmed that penciclovir is effective, and that penciclovir is superior to aciclovir.     

阿昔洛韦过量致急性肾衰竭

例19岁男性传染性单核细胞增多症患者拟给予阿昔洛韦600 mg加入10%葡萄糖注射液250 ml中静脉滴注.但因用药错误将阿昔洛韦3.0 g加入10%葡萄糖注射液250 ml中静脉滴注.输注完毕后9 h,患者出现明显腰痛,尿量减少,尿蛋白(+ +),尿潜血(+ +).随后出现24 h无尿.第3天肾功能检查:血清肌酐557 μmol/L,尿素9.2 mmol/L.肾脏超声示双肾弥漫性病变.行血液净化,并给予甲泼尼龙40 mg/d静脉滴注,治疗2 d.肾功能逐渐好转,尿量增多.第15天患者肾功能及尿常规检查均无异常,痊愈出院.