Intranasal and inhaled fluticasone propionate for pollen-induced rhinitis and asthma

BACKGROUND: Studies suggest that nasal treatment might influence lower airway symptoms and function in patients with comorbid rhinitis and asthma. We investigated the effect of intranasal, inhaled corticosteroid or the combination of both in patients with both pollen-induced rhinitis and asthma. METHODS: A total of 262 patients were randomized to 6 weeks' treatment with intranasal fluticasone propionate (INFP) 200 microg o.d., inhaled fluticasone propionate (IHFP) 250 microg b.i.d., their combination, or intranasal or inhaled placebo, in a multicentre, double-blind, parallel-group study. Treatment was started 2 weeks prior to the pollen season and patients recorded their nasal and bronchial symptoms twice daily. Before and after 4 and 6 weeks' treatment, the patients were assessed for lung function, methacholine responsiveness, and induced sputum cell counts. RESULTS: Intranasal fluticasone propionate significantly increased the percentages of patients reporting no nasal blockage, sneezing, or rhinorrhoea during the pollen season, compared with IHFP or intranasal or inhaled placebo. In contrast, only IHFP significantly improved morning peak-flow, forced expiratory volume in 1 second (FEV1) and methacholine PD20, and the seasonal increase in the sputum eosinophils and methacholine responsiveness. CONCLUSIONS: In patients with pollen-induced rhinitis and asthma, the combination of intranasal and IHFP is needed to control the seasonal increase in nasal and asthmatic symptoms.     

Effect of intranasal fluticasone propionate and triamcinolone acetonide on basal and dynamic measures of hypothalamic–pituitary–adrenal-axis activity in healthy volunteers

BACKGROUND : Most published studies show that intranasal corticosteroids have no effect on the hypothalamic-pituitary-adrenal (HPA) axis, but there have been isolated reports to the contrary, contradicting accumulated knowledge on pharmacokinetics. OBJECTIVE : To re-evaluate the effect of fluticasone propionate aqueous nasal spray (FPANS) and triamcinolone acetonide (TAA) aqueous nasal spray on the HPA axis using an improved study design. METHODS : Twenty-three healthy volunteers were randomized in a double-blind, three-way crossover study. The study comprised a 4-day placebo run-in phase followed by three 4-day treatment periods (placebo, FPANS (200 microg once daily) or TAA aqueous nasal spray (220 microg once daily)), separated by 7-14 days washout intervals. Before the first, and on the last day of each treatment period, 12-h overnight urine was collected to assess cortisol excretion and cortisol creatinine ratio. Approximately 26 h after the last administration of study medication, volunteers underwent stimulation with 0.5 microg adrenocorticotropic hormone (ACTH). Serum cortisol concentrations were measured before and 20 and 30 min after injection. Blood and urine samples were analysed for cortisol by liquid chromatography tandem mass spectrometry. RESULTS : Compared with placebo, EP or TAA had no significant effect on mean overnight (12 h) urinary cortisol excretion, and did not significantly suppress the overnight geometric mean urinary cortisol/creatinine excretion ratio. Values for serum cortisol before and after ACTH simulation showed no significant suppression, although there was a slight blunting of the HPA-axis response following TAA treatment. CONCLUSION : This study confirms that there are no detectable effects on the HPA axis following short-term intranasal FP or TAA at their recommended dosages.     

Microphotometric investigation of oxidative enzyme activity in endometrial epithelium of rats after ovariectomy and injection of testosterone propionate

Activity of oxidative enzymes in the epithelium lining the uterine cavity and in the glandular epithelium of ovariectomized rats in the period of climacteric disorders was investigated by a comparative microphotometric method. An increase in lactate dehydrogenase (LD) and glucose-6-phosphate dehydrogenase (G6PD) activity and a decrease in succinate dehydrogenase (SD) and NAD- and NADP-diaphorase activity were found in the epithelial cells lining the uterine cavity. LD activity was increased in the glandular epithelium but SD, and NAD- and NADP-diaphorase activity was sharply reduced. Injection of testosterone propionate caused a marked increase in the activity of the oxidative enzymes studied in the endometrial epithelium of the rats compared with their activity in control rats and in rats not receiving the hormone.Research Institute of Human Morphology, Academy of Medical Sciences of the USSR, Moscow. Department of Obstetrics and Gynecology, Daghestan Medical Institute, Makhachkala. (Presented by Academician of the Academy of Medical Sciences of the USSR A. P. Avtsyn.) Translated from Byulleten' Éksperimental'noi Biologii i Meditsiny, Vol. 85, No. 2, pp. 209–212, February, 1978.     

基于Heracles NEO超快速气相电子鼻麸炒白术炮制全过程气味变化识别研究

目的 建立麸炒白术Atractylodis Macrocephalae Rhizoma炮制全过程的定性判别模型,筛选出可以表征麸炒白术不同炮制程度的气味成分。方法 制备麸炒白术饮片,不同时间点取样进行分析。采用Heracles NEO超快速气相电子鼻采集气味图谱,与Arochembase数据库对比得到气味成分信息,结合峰面积分析气味成分的变化规律并进行化学计量学分析。结果 通过判别因子分析（discriminant factor analysis,DFA）、正交偏最小二乘-判别分析（orthogonal partial least squaresdiscriminant analysis,OPLS-DA）、层次聚类分析（hierarchical cluster analysis,HCA）等将麸炒白术炮制全过程样品成功分为4类：生品、炮制不及、炮制成品和炮制太过。在炮制过程中,3-甲基十五烷、十二烷基丙酸酯、正辛基环己烷、1,3-二硝基苯、8-甲基十五烷5个气味成分的峰面积占比较高,其中1,3-二硝基苯在炮制全过程中峰面积呈降低趋势;3-甲基十五烷从炮制不及到炮制成品的过程中峰面积呈增加...     

药用昆虫凹纹胡蜂化学成分及抗炎活性研究

目的 研究药用昆虫凹纹胡蜂Vespa velutina auraria的化学成分及其抗炎活性。方法 采用硅胶柱色谱、Sephadex LH-20凝胶和半制备高效液相等色谱技术进行分离纯化,通过核磁共振技术对化合物的结构进行表征和解析。以脂多糖（lipopolysaccharide,LPS）联合γ干扰素（interferon-γ,IFN-γ）诱导小鼠巨噬细胞RAW264.7作为炎症模型,探讨提取物及单体对炎症因子mRNA表达的影响。结果 从凹纹胡蜂醋酸乙酯部位分离鉴定了16个化合物,分别为邻苯二酚（1 ）、对羟基苯甲醛（2 ）、对羟基苯丙酸甲酯（3 ）、4-羟基苯醋酸乙酯（4 ）、3,4-二羟基苯乙醇（5 ）、3,4-二羟基苯酰乙醇（6 ）、3,4-二羟基苯甲酸（7 ）、N-乙酰基-2-乙氧基-2-（3,4-二羟基苯基）乙胺（8 ）、2-（2-羟基丙酰氧基）丙酸甲酯（9 ）、对甲氧基苯甲醇（10 ）、3,4-二羟基苯甲酸甲酯（11 ）、α-乙基葡萄糖苷（12 ）、2-羟基-3-苯基丙酸甲酯（13 ）、N-乙酰基-2-（3,4-二羟基苯基）乙胺（14 ）、对甲基苯乙醇（15 ）和胸腺嘧啶（16 ）。凹纹胡蜂醇提物及提取物醋酸乙酯部位、正丁醇部位和水部位在300 μg/mL时均能有效减少由LPS联合IFN-γ诱导RAW264.7细胞炎症因子一氧化氮合酶（inducible nitric oxide synthase,iNOS）基因相对表达量;化合物2 、3 、5 、6 、9～11 对LPS联合IFN-γ诱导RAW264.7细胞肿瘤坏死因子-α（tumor necrosis factor-α,TNF-α）mRNA表达有抑制作用（P<0.01）。结论 凹纹胡蜂醇提物及不同极性部位能降低炎症细胞中iNOS的表达,具有一定的抗炎作用。化合物1～16 均为首次从凹纹胡蜂分离鉴定,其中2 、3 、5 、6 、9～11 可能为潜在的活性单体。     

Evaluation of various doses of testosterone on accessory reproductive organs and plasma testosterone in intact and gonadectomized rhesus monkeys (Macaca mulatta).

The effect of 10 days i.m. treatment of testosterone propionate (TP) on plasma testosterone and accessory reproductive organs were studied in adult (6 to 6 1/2 kg) male rhesus monkeys, housed under natural light conditions using six different dose levels. The study was scheduled in the month of September and October. To maintain the weight of accessory reproductive organs and testosterone levels in castrates, different dose levels of exogenous testosterone propionate were required: 3.2 mg/d for seminal vesicles, 4.8 mg/d for ventral prostate and 3.2 mg/d for plasma testosterone titer. The levels of so-called "physiological" doses of exogenous testosterone varied for various target organs under consideration. TP at a dose of 0.4 mg/d had a depressing effect on plasma testosterone in intact monkeys. For higher doses, plasma testosterone increased roughly similarly in both intact and castrated monkeys. It suggests that with otherwise "physiological" doses of testosterone propionate, there is an almost complete blockage of endogenous testosterone secretion.     

丙酸睾酮埋植剂在家兔体内的药动学研究

 目的观察丙酸睾酮埋植剂在家兔体内的释放过程，同时进行药动学研究。方法将自制的丙酸睾酮埋植剂植入家兔皮下，用RIA方法检测血清中睾酮含量，并用3P87软件估算了药动学参数。结果丙酸睾酮埋植剂在家兔体内释放过程符合一房室模型，c_max为4.65 ng·mL^-1，t_max为4.12 h。取出埋植剂后，血药浓度下降迅速，t_1/2为0.24 h，清除率123.88 mL·h^-1。结论认为用硅胶囊控制丙酸睾酮在动物体内的释放是可行的。     

鼻腔应用丙酸氟替卡松对鼻息肉组织中水通道蛋白-2表达的影响

目的 :探讨鼻腔局部应用丙酸氟替卡松 (FP)喷雾剂对鼻息肉组织中水通道蛋白 2 (AQP 2 )表达的影响及类固醇激素治疗鼻息肉的作用机制。方法 :将 2 6例慢性鼻窦炎鼻息肉患者分为Ⅱ型组 (3期Ⅱ型 14例 )和Ⅲ型组 (Ⅲ型 12例 ) ;Ⅱ型组又分为FP组 (7例 )和对照组 (7例 ) ,Ⅲ型组亦分为FP组 (6例 )和对照组 (6例 )。Ⅱ型组和Ⅲ型组中的FP组术前应用FP喷雾剂喷鼻 7d ,对照组术前鼻腔不予任何处理。术中取 2 6例患者的鼻息肉组织 ,采用SP免疫组化技术检测鼻息肉组织中AQP 2的表达。结果 :Ⅱ型组和Ⅲ型组中的FP组鼻息肉体积明显缩小 ,鼻息肉组织中AQP 2表达的阳性细胞数和面密度值均明显低于对照组 (均P <0 .0 1)。结论 :在FP作用下鼻息肉水肿减轻、体积缩小 ,可能与AQP 2表达减少有关 ,这为类固醇激素治疗鼻息肉作用机制的阐明提供了新的方向     

丁丙氢化可的松霜膏治疗皮炎湿疹类皮肤病的疗效

目的:评价丁丙氢化可的松霜膏治疗皮炎湿疹类皮肤病的疗效和安全性。方法:采用随机对照开放试验,试验组188例,用丁丙氢化可的松霜膏涂于患处,tid,对照组120例用丁酸氢化可的松(尤卓尔)霜涂于患处,tid,疗程3～25d。结果:试验组的临床有效率、痊愈率及不良反应率分别为93.6％,77.7％和7.4％,对照组分别为92.5％,75.0％和8.4％,2组疗效和安全性结果经统计学处理均无显著性差异(P>0.05)。结论:丁丙氢化可的松霜膏治疗皮炎湿疹类皮肤病具有较好临床疗效。     

丙酸氟替卡松治疗湿疹皮炎43例

目的：观察丙酸氟替卡松乳膏治疗湿疹、皮炎类皮肤病的临床疗效。方法：对43例湿疹、皮炎患者分别用0．05％丙酸氟替卡松乳膏（治疗侧）和0．1％糠酸莫米松乳膏（对照侧）治疗，qd，共2周。结果：两侧的临床症状、体征评分，治疗后第1周、第2周与治疗前比较明显降低（P〈0．01）。治疗侧与对照侧疗效比较差异无显著性（P〉0．05），均无不良反应发生。结论：0．05％丙酸氟替卡松乳膏治疗湿疹、皮炎类皮肤病有效、安全。