双歧三联活菌对戒烟后腹泻的改善效应及安全性观察

目的：观察双歧三联活菌对戒烟后腹泻的改善效应及安全性。方法：130例戒烟后腹泻患者按用药情况分为黄连素对照组（n=30,黄连素片0．9g、tid）、双歧三联活菌组（n=50,双歧三联活菌胶囊420mg、tid）、黄连素双歧三联活菌联合组（n=50,同时服用黄连素片0．9g、tid及双歧三联活菌胶囊420mg、tid）。动态观察脱水、腹泻症状改善情况,并评估双歧三联活菌的安全性。结果：所有脱水病例治疗后脱水症状均消失。在第1天,双歧三联活菌组及黄连素双歧三联活菌联合组有效率即显著高于黄连素对照组（P〈0．05）;第2、3天,双歧三联活菌组及黄连素双歧三联活菌联合组显效率及有效率均显著高于黄连素对照组（P〈0．05或P〈0．01）,无效率显著低于黄连素对照组（P〈0．05或P〈0．01）。而双歧三联活菌组及黄连素双歧三联活菌联合组比较,各项指标差异均无统计学意义。治疗过程中,未出现与服用双歧三联活菌有关的毒副作用和其他不良反应。结论：双歧三联活菌对戒烟后腹泻有明显疗效,值得推广应用;双歧三联活菌、黄连素无明显协同治疗效果。     

Transdermal delivery of calcium channel blockers for hypertension

Introduction: Calcium channel blockers are a very important class of antihypertensive drugs. Most calcium channel blockers (CCBs) exhibiting low oral bioavailability are required to be taken more than once a day due to their short half-lives which result in poor patient compliance. There is an ineluctable requirement for improved drug-delivery devices for CCBs because of the quantum of their utilization and shortcoming associated with their conventional dosage forms.

Areas covered: There have been worthwhile research endeavors worldwide to investigate the skin permeation and to develop transdermal formulations of various categories of CCBs. This review explores the investigations on the feasibility and applicability of systemic delivery of various CCBs via skin.

Expert opinion: Transdermal delivery of CCBs has been particularly acknowledged as a potential drug-delivery route in the therapy of hypertension. Several overtures have been made to enhance delivery of these drugs via skin barrier. There have been remarkable research endeavors worldwide to investigate the skin permeation and to develop transdermal systems of various CCBs. Persistent advancement in this area holds promise for the long-term success in technologically advanced transdermal dosage forms being commercialized sooner rather than later.     

The art of attraction: applications of multifunctional magnetic nanomaterials for malignant glioma

Introduction: Malignant gliomas remain one of medicine's most daunting unsolved clinical problems. The development of new technologies is urgently needed to improve the poor prognosis of patients suffering from these brain tumors. Magnetic nanomaterials are appealing due to unique properties that allow for noninvasive brain tumor diagnostics and therapeutics in one multifunctional platform.

Areas covered: We report on the recent advances of magnetic nanomaterials for brain tumor imaging and therapy, with an emphasis on novel approaches and clinical progress. We detail their biomedical applications including brain tumor targeting, MRI contrast enhancement, optical imaging, magnetic hyperthermia, magnetomechanical destruction, drug delivery, gene therapy, as well as tracking of cell-based and viral-based therapies. The clinical cases and obstacles encountered in the use of magnetic nanomaterials for malignant glioma are also examined.

Expert opinion: To accelerate the effective translation of these materials to the clinic as theranostics for brain tumors, limitations such as poor intratumoral distribution, targeting efficiency and nonspecific systemic side effects must be addressed. Future innovations should focus on optimizing and combining the unique therapeutic applications of these magnetic nanomaterials as well as improving the selectivity of the system based on the molecular profiling of tumors.     

An update on the clinical development of drugs to disable tumor vasculature

Traditional methods of improving cancer therapy have focused primarily on achieving increased tumor cell kill. However, more recent strategies involve impairing the nutritional support system of the tumor by targeting the tumor vasculature. Rapid developments in this field in recent years have resulted in the identification of a variety of potential targets and a large number of investigational drugs, many of which are now in clinical development. In the following paper the authors review vascular disrupting therapies.     

Liposomes for Topical Use: A Physico-Chemical Comparison of Vesicles Prepared from Egg or Soy Lecithin

Developments in nanotechnology and in the formulation of liposomal systems provide the opportunity for cosmetic dermatology to design novel delivery systems. Determination of their physico-chemical parameters has importance when developing a nano-delivery system. The present study highlights some technological aspects/characteristics of liposomes formulated from egg or soy lecithins for topical use. Alterations in the pH, viscosity, surface tension, and microscopic/macroscopic appearance of these vesicular systems were investigated. The chemical composition of the two types of lecithin was checked by mass spectrometry. Caffeine, as a model molecule, was encapsulated into multilamellar vesicles prepared from the two types of lecithin: then zeta potential, membrane fluidity, and encapsulation efficiency were compared. According to our observations, samples prepared from the two lecithins altered the pH in opposite directions: egg lecithin increased it while soy lecithin decreased it with increased lipid concentration. Our EPR spectroscopic results showed that the binding of caffeine did not change the membrane fluidity in the temperature range of possible topical use (measured between 2 and 50 °C). Combining our results on encapsulation efficiency for caffeine (about 30% for both lecithins) with those on membrane fluidity data, we concluded that the interaction of caffeine with the liposomal membrane does not change the rotational motion of the lipid molecules close to the head group region. In conclusion, topical use of egg lecithin for liposomal formulations can be preferred if there are no differences in the physico-chemical properties due to the encapsulated drugs, because the physiological effects of egg lecithin vesicles on skin are significantly better than that of soy lecithin liposomes.     

Novel Hybrid-Type Antimicrobial Agents Targeting the Switch Region of Bacterial RNA Polymerase

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Pegloticase and the patient with treatment-failure gout

Gout is an inflammatory arthritis characterized by sudden, painful inflammation. Gout can affect any joint in an asymmetric distribution. Gouty attacks may be isolated or can be followed by years of recurrent flares. Over time, elevated serum urate levels and tophaceous deposits can lead to deformity and disability from underlying bony erosion. The concept of ‘treatment-failure gout’ describes a unique population that has been either unable to tolerate allopurinol or who have not experienced normalization of serum urate levels on allopurinol. It is estimated that approximately 1–1.5% of the estimated 3–8 million people with gout in the USA have treatment-failure gout. Pegloticase is an US FDA-approved intravenous medication that is a mammalian recombinant uricase conjugated to monomethoxy polyethylene glycol. Two recent Phase III trials have found pegloticase to be effective in the management of treatment-failure gout. These studies also highlight safety concerns regarding the drug’s immunogenicity.     

The discovery and development of boceprevir

Introduction: Boceprevir was the first direct acting agent developed for the treatment of hepatitis C virus infection. Boceprevir functions by targeting NS3 protease, a viral enzyme essential for replication. This peptidomimetic molecule was optimized from a peptide lead to provide a potent, selective and orally bioavailable drug that can be combined with ribavirin and peg interferon to achieve sustained viral response (undetectable HCV RNA levels for 24 weeks after completion of therapy) in patients infected with Genotype 1 of the virus.

Areas covered: This article provides a review of the pre-clinical and clinical discovery of boceprevir. This review includes the role and function of its molecular target, NS3 protease, as well as the assays used to measure in vitro efficacy, compound optimization and clinical studies to demonstrate safety and efficacy.

Expert opinion: As the first direct acting anti-HCV agent, boceprevir represents an important advance in therapy of this widespread chronic disease. Yet, while this therapy is a valuable approach, it does have limitations. Studies have suggested that 30% of patients do not achieve sustained viral response and 11% of patients have developed anemia and/or neutropenia. Current drug discovery and development efforts are underway to develop novel therapeutic options that address these issues.     

Pharmacotherapy of scleritis: current paradigms and future directions

Introduction: Scleritis is an inflammatory condition affecting the eye wall that may be associated with a number of systemic inflammatory diseases. Because scleritis can be refractory to standard treatment, knowledge of the body of available and emerging therapies is paramount and is reviewed here.

Areas covered: This review focuses on both traditional and emerging therapies for noninfectious scleritis. The authors cover the mechanisms of action and potential adverse effects of each of the treatment modalities. In addition, a summary of the significant MEDLINE indexed literature under the subject heading ‘scleritis', ‘treatment', ‘immunomodulator' will be provided on each therapy, including commentary on appropriate use and relative contraindications. Novel treatments and potential drug candidates that are currently being evaluated in clinical trials with therapeutic potential will also be reviewed.

Expert opinion: While oral nonsteroidal anti-inflammatory drugs and oral corticosteroids are widely used, effective, first-line agents for inflammatory scleritis, refractory cases require antimetabolites, T-cell inhibitors, or biologic response modifiers. In particular, there is emerging evidence for the use of targeted biologic response modifiers, and potentially, for local drug delivery.     

产褥期细节优化护理对自然分娩初产妇产后康复的价值评价

目的 探讨产褥期细节优化护理对自然分娩初产妇产后康复的价值评价.方法 选取2013年1至4月在本院分娩的90例产褥期初产妇为研究对象,随机分为对照组和研究组,各45例.对照组患者实施常规的产后护理,观察组在对照组的基础上实施细节优化护理干预,包括个体化心理疏导、营养饮食、早期中医足浴与子宫物理康复按摩等.比较两组患者产后生理康复指标及心理康复评价.结果 通过实施不同的护理干预措施,观察组切口总愈合率100.0％(26/26),明显高于对照组的60.7％(17/28).产后宫缩痛评分、晚期产后出血率均低于对照组,泌乳始动时间、宫缩痛持续时间、恶露时间均短于对照组;同时观察组在出院时、产后42 d的SDS及SAS评分均低于对照组,组间差异均有统计学意义(P＜0.05).结论 对自然分娩初产妇产褥期实施细节优化护理,可有效促进其产后康复,减少产褥感染、尿潴留等产后并发症发生,使产妇掌握科学的自我护理和生活方式,提高产褥期的健康和生活质量,同时增强初产妇适应新角色的信心和能力,使产科护理质量得到保证,临床价值较高,值得进一步推广.