Recent patents on inflammation & allergy drug discovery最新文献

Background: Pediatric myocarditis is rare but challenging. This overview summarized the current knowledge and recent patents on childhood myocarditis.

Methods: Clinical queries and keywords of "myocarditis" and "childhood" were used as search engine.

Results: Viral infections are the most common causes of acute myocarditis. Affected children often have a prodrome of fever, malaise, and myalgia. Clinical manifestations of acute myocarditis in children can be nonspecific. Some children may present with easy fatigability, poor appetite, vomiting, abdominal pain, exercise intolerance, respiratory distress/tachypnea, dyspnea at rest, orthopnea, chronic cough with wheezing, chest pain, unexplained tachycardia, hypotension, syncope, and hepatomegaly. Supraventricular arrhythmias, ventricular arrhythmias, and heart block may be present. A subset of patients have fulminant myocarditis and present with cardiovascular collapse, which may progress to severe cardiogenic shock, and even death. A high index of suspicion is crucial to its diagnosis and timely management. Cardiac magnetic resonance imaging is important in aiding clinical diagnosis while, endomyocardial biopsy remains the gold standard. The treatment consists of supportive therapy, ranging from supplemental oxygen and fluid restriction to mechanical circulatory support. Angiotensinconverting enzyme inhibitors, angio-tensin II receptor blockers, β-blockers, and aldosterone antagonists might be used for the treatment of heart failure while, immunosuppression treatments remain controversial. There are a few recent patents targeting prevention or treatment of viral myocarditis, including an immunogenic composition comprising a PCV-2 antigen, glutathione-S-transferase P1, neuregulins, NF-[kappa] B inhibitor, a pharmaceutical composition which contains 2-amino-2- (2- (4-octyl phenyl) - ethyl) propane 1,3-diol, a composition containing pycnojenol, Chinese herbal concoctions, and a Korean oral rapamycin. Evidence of their efficacy is still lacking.

Conclusion: This article reviews the current literature regarding etiology, clinical manifestations, diagnosis, and management of acute myocarditis in children.

Background: Leukotrienes are powerful mediators of inflammation and interact with specific receptors in target cell membrane to initiate an inflammatory response. Thus, Leukotrienes (LTs) are considered to be potent mediators of inflammatory diseases including allergic rhinitis, inflammatory bowel disease and asthma. Leukotriene B4 and the series of cysteinyl leukotrienes (C4, D4, and E4) are metabolites of arachidonic acid metabolism that cause inflammation. The cysteinyl LTs are known to increase vascular permeability, bronco-constriction and mucus secretion.

Objectives: To review the published data for leukotriene inhibitors of plant origin and the recent patents for leukotriene inhibitors, as well as their role in the management of inflammatory diseases.

Methods: Published data for leukotrienes antagonists of plant origin were searched from 1938 to 2019, without language restrictions using relevant keywords in both free text and Medical Subject Headings (MeSH terms) format. Literature and patent searches in the field of leukotriene inhibitors were carried out by using numerous scientific databases including Science Direct, PubMed, MEDLINE, Google Patents, US Patents, US Patent Applications, Abstract of Japan, German Patents, European Patents, WIPO and NAPRALERT. Finally, data from these information resources were analyzed and reported in the present study.

Results: Currently, numerous anti-histaminic medicines are available including chloropheneremine, brompheniramine, cetirizine, and clementine. Furthermore, specific leukotriene antagonists from allopathic medicines are also available including zileuton, montelukast, pranlukast and zafirlukast and are considered effective and safe medicines as compared to the first generation medicines. The present study reports leukotrienes antagonistic agents of natural products and certain recent patents that could be an alternative medicine in the management of inflammation in respiratory diseases.

Conclusion: The present study highlights recent updates on the pharmacology and patents on leukotriene antagonists in the management of inflammation respiratory diseases.

Background: Nummular eczema may mimic diseases that present with annular configuration and the differential diagnosis is broad.

Objective: This article aimed to provide an update on the evaluation, diagnosis, and treatment of nummular eczema.

Methods: A PubMed search was performed in using the key terms "nummular eczema", "discoid eczema", OR "nummular dermatitis". The search strategy included meta-analyses, randomized controlled trials, clinical trials, observational studies, and reviews. The search was restricted to English literature. The information retrieved from the above search was used in the compilation of the present article. Patents were searched using the key terms "nummular eczema", "discoid eczema", OR "nummular dermatitis" in www.google.com/patents and www.freepatentsonline.com.

Results: Nummular eczema is characterized by sharply defined, oval or coin-shaped, erythematous, eczematous plaques. Typically, the size of the lesion varies from 1 to 10cm in diameter. The lesions are usually multiple and symmetrically distributed. Sites of predilection include the lower limbs followed by the upper limbs. The lesions are usually intensely pruritic. The diagnosis is mainly clinical based on the characteristic round to oval erythematous plaques in a patient with diffusely dry skin. Nummular eczema should be distinguished from other annular lesions. Dermoscopy can reveal additional features that can be valuable for correct diagnosis. Biopsy or laboratory tests are generally not necessary. However, a potassium hydroxide wet-mount examination of skin scrapings should be performed if tinea corporis is suspected. Because contact allergy is common with nummular eczema, patch testing should be considered in patients with chronic, recalcitrant nummular eczema. Avoidance of precipitating factors, optimal skin care, and high or ultra-high potency topical corticosteroids are the mainstay of therapy. Recent patents related to the management of nummular eczema are also discussed.

Conclusion: With proper treatment, nummular eczema can be cleared over a few weeks, although the course can be chronic and characterized by relapses and remissions. Moisturizing of the skin and avoidance of identifiable exacerbating factors, such as hot water baths and harsh soaps may reduce the frequency of recurrence. Diseases that present with annular lesions may mimic nummular eczema and the differential diagnosis is broad. As such, physicians must be familiar with this condition so that an accurate diagnosis can be made, and appropriate treatment initiated.

Background: Aspirin is a nonsteroidal anti-inflammatory drug that is very effective in the treatment of inflammation and other health conditions, however, it causes gastric irritation. Recently, researchers have developed patents (US9757529, 2019) of inhalable aspirin for rapid absorption and circumvention of gastric irritation.

Objective: The aim of this work was to formulate aspirin-loaded lipid based formulation in order to enhance oral bioavailability and inhibit gastric irritation.

Methods: This solid lipid microparticles loaded with aspirin (SLM) was formulated by a modified cold homogenization-solvent evaporation method. In vitro studies such as in vitro drug release, particle size, Encapsulation Efficiency (EE), micromeritic properties and loading capacity were carried out. Pharmacodynamics studies such as anti-inflammatory and ulcerative properties of the SLM were also carried out in Wistar rats.

Results: The results showed that aspirin entrapped SLM exhibited the highest EE of 72% and particle size range of 7.60 + 0.141µm to 20.25 + 0.070µm. Formulations had about 55% drug release at 6h in simulated intestinal fluid pH 6.8. The formulations had good flowability that could facilitate filling into hard gelatin capsule shells. The SLM exhibited 100% gastroprotection against aspirin-induced ulcers (p < 0.05). The percentage of anti-inflammatory activities also showed that aspirin-entrapped SLM had 78% oedema inhibition at 7h, while the reference had 68% inhibition at 7h.

Conclusion: Aspirin-entrapped SLM showed good sustained-release properties, enhanced antiinflammatory properties and total gastric protection from aspirin-induced ulcers and could be used as once-daily oral aspirin.

Background: Ascaris lumbricoides is the most common helminthic infection. More than 1.2 billion people have ascariasis worldwide.

Objective: This article aimed to provide an update on the evaluation, diagnosis, and treatment of ascariasis.

Methods: A PubMed search was conducted in February 2020 in Clinical Queries using the key terms "ascariasis" OR "Ascaris lumbricoides". The search strategy included meta-analyses, randomized controlled trials, clinical trials, observational studies, and reviews published within the past 10 years. The search was restricted to English literature. The information retrieved from the above search was used in the compilation of the present article. Patents were searched using the key term "ascariasis" OR "Ascaris lumbricoides" in www.freepatentsonline.com.

Results: Ascaris lumbricoides is transmitted through the ingestion of embryonated eggs from fecal- contaminated material. Ascariasis has high endemicity in tropical and subtropical areas. Predisposing factors include poverty, poor sanitation, inadequate sewage disposal, and poor personal hygiene. The prevalence is greatest in children younger than 5 years of age. The majority of patients with intestinal ascariasis are asymptomatic. For those with symptoms, anorexia, nausea, bloating, abdominal discomfort, recurrent abdominal pain, abdominal distension, and intermittent diarrhea are not uncommon. Other clinical manifestations vary widely, depending on the underlying complications. Complications include Löeffler syndrome, intestinal obstruction, biliary colic, recurrent pyogenic cholangitis, cholecystitis, acalculous cholecystitis, obstructive jaundice, cholelithiasis, pancreatitis, and malnutrition. The diagnosis is best established by microscopic examination of fecal smears or following concentration techniques for the characteristic ova. Patients with A. lumbricoides infection warrant anthelminthic treatment, even if they are asymptomatic, to prevent complications from migration of the parasite. Albendazole and mebendazole are the drugs of choice for children and nonpregnant individuals with ascariasis. Pregnant women with ascariasis should be treated with pyrantel pamoate. Recent patents related to the management of ascariasis are also discussed.

Conclusion: The average cure rate with anthelminthic treatment is over 95%. Unfortunately, most treated patients in endemic areas become re-infected within months. Health education, personal hygiene, improved sanitary conditions, proper disposal of human excreta, and discontinuing the use of human fecal matter as a fertilizer are effective long-term preventive measures. Targeting deworming treatment and mass anthelminthic treatment should be considered in regions where A. lumbricoides is prevalent.