无环鸟苷亲脂性前体药物脂质体的制备及体外抗病毒活性(英文)

本文通过将无环鸟苷(acyclovir,简称ACV)2’位羟基分别与月桂酰氯或棕榈酰氯进行酯化反应,制得亲脂性前体药物无环鸟苷月桂酸酯和无环鸟苷棕榈酸酯(分别简称为C₁₂-ACV和C₁₆-ACV),使脂质体包封率从ACV的29.9%提高到C₁₂-ACV的95.6%和C₁₆-ACV的97.1%;漏泄实验表明在4℃透析60h后,一半以上的ACV从脂质体中漏泄,而C₁₂-ACV和C₁₆-ACV的滞留率分别为70%和80%;体外抗疱疹病毒的试验中,在最低试验浓度0.044μmol/L时,ACV不显示抗病毒活性,而C₁₆-ACV脂质体抑制细胞病变率达75%,说明前体药物通过与脂质体脂膜的结合增加了药物的进入细胞能力,从而提高了ACV的抗病毒能力。     

The DSM Diagnostic Criteria for Vaginismus

The DSM-IV-TR attempted to create a unitary category of dyspareunia based on the criterion of genital pain that interfered with sexual intercourse. This classificatory emphasis of interference with intercourse is reviewed and evaluated from both theoretical and empirical points of view. Neither of these points of view was found to support the notion of dyspareunia as a unitary disorder or its inclusion in the DSM-V as a sexual dysfunction. It seems highly likely that there are different syndromes of dyspareunia and that what is currently termed “superficial dyspareunia” cannot be differentiated reliably from vaginismus. It is proposed that the diagnoses of vaginismus and dyspareunia be collapsed into a single diagnostic entity called genito-pelvic pain/penetration disorder. This diagnostic category is defined according to five dimensions: percentage success of vaginal penetration; pain with vaginal penetration; fear of vaginal penetration or of genito-pelvic pain during vaginal penetration; pelvic floor muscle dysfunction; medical co-morbidity.     

Priapism: an avoidable complication of pharmacologically induced erection

Priapism is an alarming complication during treatment of erectile dysfunction with vasoactive drugs, particularly papaverine alone or in combination with phentolamine mesylate. An investigational protocol was designed to identify patients who are more susceptible to priapism after intracavernous injection of papaverine alone or with phentolamine. The protocol was applied in 331 men with impotence of various etiology. The association of a positive response to visual sexual stimulation and penile brachial index of more than 0.8 represented a higher risk for post-injection priapism. We were able to reduce the incidence of this compliance to 1% in the last 101 patients.     

因子分析分光光度法在多组分复方制剂中的应用

因子分析分光光度法在多组分的系统中,可用来推断出系统中组分的个数及系统中各组分在各样品中的浓度。本文采用因子分析法的目标检测法对两组分的复方磺胺甲氧吡嗪片,用微机对其紫外光谱数据进行处理。结果表明,回收率分别为102.0%和102.7%,平均标准差小于2.2%。并对三组分样品(复方扑热息痛片)的模拟数据进行了处理,其结果也较理想。     

N-(4-乙氧羰基-4-取代丁酰基)-N-取代甘氨酸的合成

本文报道9个估计具有血管紧张素转化酶抑制活性的N-(4-乙氧羰基-4-取代丁酰基)-N-取代甘氨酸及其相应叔丁酯的合成和鉴定。药理初试结果,化合物Ⅶ₇和Ⅶ₉显示明显降压活性。     

Denial as a defense against depression in end-stage renal disease: an empirical test

End-stage renal disease (ESRD) is recognized as imposing severe psychosocial stresses upon patients with the result that depression is believed to be highly prevalent. A number of studies have reported low levels of depression, however, and this contradictory finding has been explained via the construct of defensive denial-i.e., patients may minimize the impact of illness-related experiences upon their overall experiences of life. The present study tested this hypothesis in a sample of seventy ESRD patients. Participants rated a series of twelve life dimensions (e.g., work, family and martial relations, recreation) in terms of perceived intrusiveness and control as well as indicating their perceived similarity using a card sort task. Standard measures of depression, positive and negative moods, somatic symptoms of distress, self-esteem, and life happiness were also obtained via structured interviews. A multidimensional scaling analysis applied to the card sort data indicated that ESRD patients do, indeed, perceive illness-related and nonillness aspects of life as independent. However, an analysis of partial variance-controlling for age and nonrenal health-failed to provide evidence of defensive denial. The suggestion is forwarded that previous findings of a high prevalence of depression in ESRD may be in error due to the misidentification of uremic symptoms as symptoms of depression.     

Body image and sexuality in oophorectomized women

Five groups of women ages 35 to 55 years were studied, including a nonsurgical control group (CTL), a hysterectomy-only (HYS), and three oophorectomy groups: an untreated group (UNT), women on estrogen replacement therapy (EST), and women on androgen-estrogen replacement therapy (COM). The interview/questionnaire session assessed mood, body image, and sexual functioning. In a second session completed by 58 of 129 subjects (45%), a photoplethysmograph measured vaginal blood flow in response to an erotic stimulus while subjects concurrently monitored subjective arousal. Overall, the UNT and EST groups had significantly lower self-reported desire and arousal than the remaining three groups. Body image was significantly poorer in the UNT group. All surgical groups reported more sexual problems than the control group. Furthermore, about a third of the CTL group reported positive changes in body image and sexuality in the previous 5 years. This effect was attenuated in the HYS, COM, and EST groups and almost absent in the UNT group. No significant group differences were obtained, however, on mood or vaginal blood flow and subjective arousal to an erotic stimulus. The role of differential levels of testosterone on sexuality is discussed as well as its clinical implications.This research was conducted as part of the first author's Ph.D. thesis requirement under the direction of the second author at McGill University and was supported by grants from the Medical Research Council of Canada (Studentship), Fonds pour la Formation de Chercheurs et l'Aide à la Recherche, and McGill Faculty of Graduate Studies and Research-Social Science Research Grant. Dr. Bellerose is currently at the Douglas Hospital in Verdun, Quebec.     

硝基甘油对狗缺血区冠脉循环的作用

用实验性犬冠脉狭窄模型,冠脉内恒流灌注硝基甘油0.5μg/kg.min^-1,使冠脉血流量(CBF)增加、远端小动脉压(DCP)、冠脉血管总阻力(R_T)、小冠脉血管阻力(R_S)及冠状静脉低切血粘(η_b)减少;而主动脉压和心率无明显变化。恒流灌注硝基甘油1μg/kg.min^-1时,在开始5min内冠脉循环的变化同上,并伴大冠脉血管阻力(R_L)减少,10 min后出现CBF减少和R_T,R_{L及ηb增加。结果提示,硝基甘油有缓解和加重心肌缺血的双重作用,其作用可能与剂量张扩张远端小动脉压的程度有关。}     

Psychosocial predictors of sudden death: A review and critique

Research and selected case studies concerning psychosocial prediction of sudden death are evaluated under three categories: sudden cardiac, sudden infant and sudden traumatic death. The psychosocial predictors reviewed include novelty-pre-exposure, control-helplessness, restraint, Type A behavior, life change, bereavement, denial, social support and contact, voodoo, psychiatric illness, mother infant separation, submission-defeat, housing, handling and environmental enrichment. Four of these predictors, controllability-helplessness, pre-exposure-novelty, depressive affect and physical restraint are repeatedly cited in both human and animal studies and their importance is critically evaluated. Methodological and substantive recommendations for future research are made and a discussion of possible mechanisms is presented.