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Jinke Xu, Mifong Tam, Sepideh Samadei, Sophie Lerouge, Jake Barralet, Mary M Stevenson, Marta Cerruti
Mucoadhesive drug delivery systems stick to mucosal tissues and prolong the local retention time of drugs. Since the colon is covered by a mucosal layer, mucoadhesive rectal formulations may improve treatment of such diseases as hypertension or colon cancer. Ulcerative colitis (UC) is an inflammatory bowel disease characterized by chronic inflammation of the colonic mucosa. It is commonly treated with sulfasalazine (SSZ), which is metabolized by the intestinal flora into the therapeutic 5-aminosalicylic acid (5-ASA) and a toxic by-product sulfapyridine (SP)...
October 18, 2016: Acta Biomaterialia
Mahesh Kandula, K B Sunil Kumar, Sivanesan Palanichamy, Ashok Rampal
Mesalamine (5-ASA) is one of the drugs indicated as first line therapy in ulcerative colitis for induction and maintenance of remission. Sulfasalazine and formulations of 5-ASA (pH-dependent and controlled release formulations) were developed to minimize the systemic absorption and maximize the delivery of the mesalamine to colon. Although, its efficacy and safety is well documented there are approximately 30% nonresponders to 5-ASA therapy. This necessitates the need for novel therapeutic options to improve the efficacy and safety of the currently available 5-ASA therapy...
October 4, 2016: International Immunopharmacology
Helena Shifrin, Dorit Moradov, Corina Bejar, Donna Schorer-Apelbaum, Marta Weinstock
BACKGROUND: In search of safer treatments for inflammatory bowel disease in subjects not responding to, or showing adverse effects to TNF-α antagonists, we tested three novel indoline carbamates in the 2,4-dinitrobenzene sulfonic acid (DNBS) model of colitis in rats. The compounds have anti-inflammatory activity in other disease models in mice. METHODS: AN827 (3-(2-(methoxy carbonyl) ethyl) indolin-4-ylethyl methyl) carbamate (0.1 or 1mg/kg), AN680 (3-(2-(methoxy carbonyl) ethyl) indolin-6-ylethyl methyl) carbamate (1...
August 31, 2016: Pharmacological Reports: PR
Payaswini Vasanth, Michelle Parmley, Jose Torrealba, Tamim Hamdi
Tubulointerstitial nephritis in patients with inflammatory bowel disease has been linked to the use of 5-ASA derivatives. Various aspects of this theory have been challenged with a potential role for the underlying autoimmune disorder. Steroids are the mainstay of treatment and mycophenolate mofetil might be an effective alternative. We report a patient who responded well to mycophenolate despite continuing mesalamine, the suspected offending agent.
2016: Case Reports in Nephrology
Makoto Naganuma, Shinta Mizuno, Kosaku Nanki, Shinya Sugimoto, Takanori Kanai
Recently, several medical treatments for ulcerative colitis (UC) have been developed, including 5-aminosalicylic acids (5-ASAs), corticosteroids, thiopurine, calcineurin inhibitors, and anti-tumor necrosis factor (TNF) α treatments. Treatment options including calcineurin inhibitors and anti-TNF treatment for refractory UC are discussed in this article. Furthermore, upcoming treatments are introduced, such as golimumab, vedolizumab, AJM300, tofacitinib. Budesonide foamwill be used as one treatment option in patients with distal colitis...
October 3, 2016: Clinical Journal of Gastroenterology
Dan Turner, Baruch Yerushalmi, Michal Kori, Efrat Broide, Yael Mozer-Glassberg, Ron Shaoul, Kaija-Leena Kolho, Eyal Shteyer, Hussein Shamaly, Oren Ledder, Shlomi Cohen, Sarit Peleg, Avi On, Arie Levine
BACKGROUND: Trials in adults suggested once-daily (QD) dosing of 5-ASA may be as or more effective as twice-daily (BID) dosing in ulcerative colitis (UC). In this induction of remission, investigator-blinded, randomized-controlled-trial we aimed to compare effectiveness and safety of once vs. twice daily mesalazine (Pentasa®), in paediatric UC. METHODS: Children, 4-18 years with a PUCAI ( Paediatric Ulcerative Colitis Activity Index) of 10-55 points at inclusion, were randomized in blocks of 6 with blinded allocation to QD or BID mesalamine using a weight-based dosing table...
October 3, 2016: Journal of Crohn's & Colitis
Anthony K Akobeng, Dongni Zhang, Morris Gordon, John K MacDonald
BACKGROUND: The prevention of relapse is a major issue in the management of Crohn's disease. Corticosteroids, the mainstay of treatment of acute exacerbations, are not effective for maintenance of remission and its chronic use is limited by numerous adverse events. Randomised controlled trials assessing the efficacy of oral 5-aminosalicylic acid (5-ASA) agents for maintenance of medically-induced remission in Crohn's disease have produced conflicting results. OBJECTIVES: To conduct a systematic review to evaluate the efficacy and safety of oral 5-ASA agents for the maintenance of medically-induced remission in Crohn's disease...
September 28, 2016: Cochrane Database of Systematic Reviews
Muzna Sadia, Agata Sośnicka, Basel Arafat, Abdullah Isreb, Waqar Ahmed, Antonios Kelarakis, Mohamed A Alhnan
This work aims to employ fused deposition modelling 3D printing to fabricate immediate release pharmaceutical tablets with several model drugs. It investigates the addition of non-melting filler to methacrylic matrix to facilitate FDM 3D printing and explore the impact of (i) the nature of filler, (ii) compatibility with the gears of the 3D printer and iii) polymer: filler ratio on the 3D printing process. Amongst the investigated fillers in this work, directly compressible lactose, spray-dried lactose and microcrystalline cellulose showed a level of degradation at 135°C whilst talc and TCP allowed consistent flow of the filament and a successful 3D printing of the tablet...
September 15, 2016: International Journal of Pharmaceutics
Anders Rönnblom, Tommy Holmström, Urban Karlbom, Hans Tanghöj, Mari Thörn, Daniel Sjöberg
OBJECTIVE: The aim of the study was to describe the medical treatment, change in phenotype, need for surgery and IBD-associated mortality during the first 5 years after diagnosis. MATERIAL AND METHODS: Patients diagnosed with Crohn's disease including all age groups in the Uppsala healthcare region in the middle of Sweden 2005-2009 were included in the study. Medical notes were scrutinised and patients contacted. Out of 269 patients, 260 (96.3%) could be followed for 5 full years or until death...
September 15, 2016: Scandinavian Journal of Gastroenterology
Suhrid Banskota, Han-Eol Kang, Dong-Guk Kim, Sang Won Park, Hyeonjin Jang, Ujjwala Karmacharya, Byeong-Seon Jeong, Jung-Ae Kim, Tae-Gyu Nam
Although the pathogenesis of inflammatory bowel disease (IBD) is complex, attachment and infiltration of leukocytes to gut epithelium induced by pro-inflammatory cytokines such as tumor necrosis factor-α (TNF-α) represents the initial step of inflammation in IBD. Previously, we have reported that some 6-amino-2,4,5-trimethylpyridin-3-ols have significant levels of antiangiogenic activity via PI3K inhibition. Based on the reports that angiogenesis is involved in the aggravation of IBD and that PI3K is a potential target for IBD therapy, we investigated whether the scaffold has inhibitory activity against in vitro and in vivo models of colitis...
October 1, 2016: Bioorganic & Medicinal Chemistry Letters
Yan-Hong Li, Man Zhang, Hai-Bo Fu, Hai-Tao Xiao, Zhao-Xiang Bian
Our previous study demonstrated that a combination of alternative medicine berberine and conventional 5-aminosalicylic acid (5-ASA) showed promise to be a novel therapeutic strategy for ulcerative colitis (UC). This present study aims to sketch the pre-clinical toxicity profile of this combination (1:10 dose ratio) on mice. In acute toxicity test, the determined median lethal dose (LD50) was 278.7 mg/kg berberine plus 2787 mg/kg 5-ASA. The results from subacute toxicity test demonstrated that no toxic signs of clinical symptoms, no significant changes in hematological or biochemical parameters were detected in mice treated with 14 + 140, 28 + 280 or 56 + 560 mg/kg of berberine plus 5-ASA treatment...
August 30, 2016: Food and Chemical Toxicology
Xin Zhao, Nan Li, YiMing Ren, Tao Ma, ChunLi Wang, Jun Wang, ShengYi You
BACKGROUND: Ulcerative colitis (UC) is a chronic and remitting inflammatory disease that is characterized by chronic idiopathic inflammation of the colon and bloody diarrhea. Currently drug treatment is the main intervention for patients with mild to moderate UC. Mesalazine (5-ASA) and beclomethasone dipropionate (BDP) have been widely used for the treatment of UC and have yielded satisfactory results. This study compared the effectiveness of 5-ASA and BDP in the treatment of UC. METHODS: The PubMed, Medline, SinoMed, Embase, and Cochrane Librinary databases were searched for eligible studies...
2016: PloS One
Aurelio Romero-Castro, Mara Gutiérrez-Sánchez, José Correa-Basurto, Martha Cecilia Rosales Hernández, Itzia Irene Padilla Martínez, Jessica Elena Mendieta-Wejebe
5-[(4-carboxybutanoyl)amino]-2-hydroxybenzoic acid (C2) is a novel synthetic derivative of 5-aminosalicylic acid (5-ASA), which is currently being evaluated ex vivo as an anti-inflammatory agent and has shown satisfactory results. This study aimed to obtain the pharmacokinetic profiles, tissue distribution and plasma protein binding of C2 in Wistar Rats. Additionally, an HPLC method was developed and validated to quantify C2 in rat plasma. The pharmacokinetic profiles of intragastric, intravenous and intraperitoneal administration routes at singles doses of 100, 50, and 100 mg/kg, respectively, were studied in Wistar rats...
2016: PloS One
Zi Jian Luan, Yue Li, Xin Yu Zhao, Li Wang, Ying Hao Sun, Shi Yao Wang, Jia Ming Qian
OBJECTIVE: To pool the data of studies and to evaluate the efficacy and safety of low-dose azathioprine (AZA) for treating patients with chronic active ulcerative colitis. METHODS: Research subjects were patients with chronic active UC, including steroid-dependent colitis, steroid-refractory colitis patients or patients who couldn't achieve remission after full-dose 5-ASA treatment. The treatment of chronic active UC patients was low-dose AZA (≤1.5 mg/kg/d)...
July 23, 2016: Journal of Digestive Diseases
James M Richter, Nabeela K Arshi, Gerry Oster
Background. Ulcerative proctitis (UP) is typically treated initially with oral 5-aminosalicylate ("5-ASA"), mesalamine suppository, or mesalamine enema ("UP Rx"). Little is known about their effectiveness in practice. Methods. Using a US health insurance database, we identified new-onset UP patients between January 1, 2005, and December 31, 2007, based on the following: (1) initiation of UP Rx; (2) endoscopy in prior 30 days resulting in diagnosis of UP; and (3) no prior encounters for ulcerative colitis or Crohn's disease...
2016: Canadian Journal of Gastroenterology & Hepatology
Brian P Bosworth, William J Sandborn, David T Rubin, Joseph R Harper
BACKGROUND: Rectal budesonide foam is a second-generation corticosteroid efficacious for active mild to moderate ulcerative proctitis and ulcerative proctosigmoiditis. This subgroup analysis examined the impact of baseline oral 5-aminosalicylic acid (5-ASA) on the efficacy and safety of budesonide foam in patients with mild to moderate ulcerative proctitis or ulcerative proctosigmoiditis. METHODS: Patients received budesonide foam 2 mg/25 mL twice daily for 2 weeks, then once daily for 4 weeks, or placebo, with or without continued stable dosing of baseline oral 5-ASAs, for remission induction at week 6 (primary endpoint) in 2 identically designed, randomized, double-blind, phase 3 studies...
August 2016: Inflammatory Bowel Diseases
Andrea L Matthis, Bin Zhang, Lee A Denson, Bruce R Yacyshyn, Eitaro Aihara, Marshall H Montrose
BACKGROUND: 5-aminosalicylic acid (5-ASA) is a classic anti-inflammatory drug for the treatment of ulcerative colitis. N-acetyltransferase (NAT) enzymes convert 5-ASA to its metabolite N-acetyl-5-ASA, and it is unresolved whether 5-ASA or N-acetyl-5-ASA is the effective therapeutic molecule. We previously demonstrated that colonic production of N-acetyl-5-ASA (NAT activity) is decreased in dextran sulfate sodium-induced colitis. Our hypothesis is that 5-ASA is the therapeutic molecule to improve colitis, with the corollary that altered NAT activity affects drug efficacy...
August 2016: Inflammatory Bowel Diseases
Ya-Ting Niu, Yu-Ping Zhao, Yan-Fang Jiao, Jie Zheng, Wen-Li Yang, Ru Zhou, Yang Niu, Tao Sun, Yu-Xiang Li, Jian-Qiang Yu
This study was designed to investigate the anti-inflammatory activity of the pure compound gentiopicroside (Gent) on dextran sulfate sodium (DSS)-induced colitis in a mouse model and to explore the possible related mechanisms. Experimental colitis was induced in ICR mice by dissolving 5% DSS in their drinking water for 7days. Gent (200, 100, and 50mg/kg) and 5-aminosalicylic acid (5-ASA, 100mg/kg) were oral administrated once a day for 7days. Anti-inflammatory effects were evaluated by comparing extend of colonic mucosal injury assessed by disease activity index (DAI), colon length, histopathological examination, and biochemical test...
October 2016: International Immunopharmacology
Abigail R Cannon, Suhail Akhtar, Adam M Hammer, Niya L Morris, Michael J Javorski, Xiaoling Li, Richard H Kennedy, Richard L Gamelli, Mashkoor A Choudhry
Gut barrier disruption is often implicated in pathogenesis associated with burn and other traumatic injuries. In this study, the authors examined whether therapeutic intervention with mesalamine (5-aminosalicylic acid [5-ASA]), a common anti-inflammatory treatment for patients with inflammatory bowel disease, reduces intestinal inflammation and maintains normal barrier integrity after burn injury. Male C57BL/6 mice were administered an approximately 20% TBSA dorsal scald burn and resuscitated with either 1 ml normal saline or 100 mg/kg of 5-ASA dissolved in saline...
September 2016: Journal of Burn Care & Research: Official Publication of the American Burn Association
Elizabeth S John, Kristina Katz, Mark Saxena, Sita Chokhavatia, Seymour Katz
A substantial and growing proportion of patients with inflammatory bowel disease (IBD) are elderly, and these patients require tailored treatment strategies. However, significant challenges exist in the management of this population due to the paucity of data. Establishing the initial diagnosis and assessing the etiology of future symptoms and flares can be challenging as several other prevalent diseases can masquerade as IBD, such as ischemic colitis, diverticular disease, and infectious colitis. Important pharmacologic considerations include reduced glomerular filtration rate and drug-drug interactions in the elderly...
September 2016: Current Treatment Options in Gastroenterology
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