Cutaneous distribution of orally administered itraconazole in guinea pigs, studied by autoradiography

Background Itraconazole is an orally active antifungal lipophilic drug with high affinity for sebum and keratinocytes. Aim The aim of the study was to investigate the routes of percutaneous egression and the sites of cutaneous action/storage of ³H-labelled itraconazole in an experimental animal model. Material and methods Hartley guinea pigs were dosed orally by gavage for 2 consecutive days at 10 mg/kg/day ³H-itraconazole dissolved in polyethylene glycol 200. At various time points after the second gavage, small full-thickness samples of dorsal skin were excised and processed using dry-apposing autoradiography. Results Our research revealed an accumulation of silver grains over the epidermis and its appendages (hair follicle and sebaceous gland), the dermal fat tissue and the hypodermal muscle tissue on tissue sections at 6, 24 and 48 h time intervals, whereas at the remaining time points (96, 168 and 336 h) the silver grain density was markedly decreased to background level. Discussion The present histological distribution data support the current method of oral treatment with itraconazole as the treatment schedule of choice to eradicate infective organisms residing in the deeper skin layers.     

伊曲康唑不良反应的国内文献综述

目的：了解伊曲康唑的不良反应及安全性。资料与方法：手工检索《中华皮肤科杂志》等3种中文专业期刊，从对照试验的文献中提取治疗例数和各种不良反应例数，计算发生率。结果：共有14725例涉及有关安全性的报道。伊曲康唑不良反应总的发生率约为1．57％。结论：伊曲康唑较为安全。     

Influence of an acidic beverage (Coca-Cola) on the absorption of itraconazole

Objective: To evaluate the effectiveness of Coca-Cola in enhancing the absorption of itraconazole. Methods: Eight healthy volunteers were randomized to receive two treatment sequences in a two-way crossover design with a 1-week wash-out period separating each study treatment. Treatment I, the control, consisted of 100 mg itraconazole with 325 ml water. Treatment II was identical to treatment I, except that itraconazole was administered with 325 ml of Coca-Cola (pH 2.5). Results: Serum itraconazole concentrations, after administration with Coca-Cola (treatment II), were higher than after administration with water (treatment I). The mean AUC was 1.12 vs 2.02 μg · h · ml⁻¹, the mean C_max was 0.14 vs 0.31 μg · ml⁻¹and the mean t_max was 2.56 vs 3.38 h in treatments I and II, respectively. Conclusion: The absorption of itraconazole can be enhanced by Coca-Cola. Received: 4 November 1996 / Accepted in revised form: 21 January 1997     

Disseminated histoplasmosis in a non-immunocompromised host

Histoplasma infections in Europe are rare, and acute disseminated histoplasmosis has only been observed in immunocompromised persons. We describe a case of acute disseminated histoplasmosis in a young, nonimmunocompromised European woman. The probable source of infection was Sri Lanka or the Maldives. At presentation she was severely ill with fever, lymphadenopathy, anemia, thrombocytopenia, hepatosplenomegaly, and polyserositis. Histologically, myelofibrosis and osteosclerosis were observed with extramedullary hematopoiesis. Histoplasma capsulatum yeasts were detected in bone marrow trephine biopsy by methenamine silver staining. Treatment with conventional and liposomal amphotericin B and subsequent itraconazole led to rapid and complete recovery.Abbreviations He Histoplasma capsulatum - AIDS acquired immunodeficiency syndrome - HIV human immunodeficiency virus     

紫外分光光度法测定伊曲康唑注射液的含量

目的建立紫外分光光度法测定伊曲康唑注射液含量的测定方法。方法采用紫外分光光度法测定伊曲康唑注射液的含量,测定波长为262nm。结果线性范围0~38.08μg·ml-1,伊曲康唑的平均回收率为99.1%,RSD为0.24%,r=0.9999(n=6)。结论该法方便快速准确,可作为伊曲康唑注射液含量测定的方法。     

伊曲康唑、特比萘芬和他克莫司单用及联合对皮炎外瓶霉的体外抗真菌作用

目的 探讨他克莫司与伊曲康唑、特比萘芬联合对皮炎外瓶霉的体外抗真菌效果.方法 参考美国临床实验室标准化研究所M38-A2方案,测定特比萘芬和伊曲康唑对12株皮炎外瓶霉的最低抑菌浓度;利用棋盘法,测定他克莫司和伊曲康唑或特比萘芬的联合抗皮炎外瓶霉效果.结果 特比萘芬和伊曲康唑对皮炎外瓶霉最低抑菌浓度范围分别为(0.06 ～0.125) mg/L和(0.5 ～1) mg/L.他克莫司和特比萘芬联合对5株皮炎外瓶霉、他克莫司和伊曲康唑联合对10株皮炎外瓶霉有协同作用.两组均无拮抗作用.结论 他克莫司在体外与伊曲康唑或特比萘芬联合应用时,能够增加皮炎外瓶霉对伊曲康唑和特比萘芬的敏感性.     

伊曲康唑注射液制备研究

介绍了伊曲康唑注射液的制备和质量控制,对制得的伊曲康唑注射液的含量和稳定性等作了研究,结果证明制备方法良好,样品质量可控。