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Masakazu Nagahori, Shuji Kochi, Hiroyuki Hanai, Takayuki Yamamoto, Shiro Nakamura, Soji Omuro, Mamoru Watanabe, Toshifumi Hibi
BACKGROUND: Efficacy of maintenance therapy in ulcerative colitis (UC) in the remission stage has been reported to depend on release profile or dosing regimen of oral 5-aminosalicylic acid (5-ASA) products used. Aim of this study is to investigate real life results in using oral 5-ASA products for maintaining mild to moderate UC patients in Japan. METHODS: Adult UC outpatients treated with oral 5-ASA products were enrolled from 379 sites in Japan between July 2012 and July 2013, and followed for 52 weeks...
April 4, 2017: BMC Gastroenterology
Arie Levine, Baruch Yerushalmi, Michal Kori, Efrat Broide, Yael Mozer-Glassberg, Ron Shaoul, Kaija-Leena Kolho, Eyal Shteyer, Hussein Shamaly, Oren Ledder, Shlomi Cohen, Sarit Peleg, Chen Sarbagili Shabat, Gili Focht, Ebby Shachmon, Mona Boaz, Avi On, Dan Turner
Background: Paediatric ulcerative colitis [UC] is more extensive than adult disease, and more often refractory to mesalamine. However, no prospective trials have evaluated mesalamine enemas for inducing remission in children. Our goal was to evaluate the ability of mesalamine enemas to induce remission in mild to moderate paediatric UC refractory to oral mesalamine. Methods: This was an open-label arm of a previously reported randomised controlled trial of once-daily mesalamine in active paediatric UC [MUPPIT trial]...
August 1, 2017: Journal of Crohn's & Colitis
Alex Yu, Jason R Baker, Ann F Fioritto, Ying Wang, Ruijuan Luo, Siwei Li, Bo Wen, Michael Bly, Yasuhiro Tsume, Mark J Koenigsknecht, Xinyuan Zhang, Robert Lionberger, Gordon L Amidon, William L Hasler, Duxin Sun
As an orally administered, locally acting gastrointestinal drug, mesalamine products are designed to achieve high local drug concentration in the gastrointestinal (GI) tract for the treatment of ulcerative colitis. The aim of this study was to directly measure and compare drug dissolution of three mesalamine formulations in human GI tract and to correlate their GI concentration with drug concentration in plasma. Healthy human subjects were orally administered Pentasa, Apriso, or Lialda. GI fluids were aspirated from stomach, duodenum, proximal jejunum, mid jejunum, and distal jejunum regions...
February 6, 2017: Molecular Pharmaceutics
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
Yongjun Wang, Claire E Parker, Tania Bhanji, Brian G Feagan, John K MacDonald
BACKGROUND: Oral 5-aminosalicylic acid (5-ASA) preparations were intended to avoid the adverse effects of sulfasalazine (SASP) while maintaining its therapeutic benefits. Previously, it was found that 5-ASA drugs in doses of at least 2 g/day, were more effective than placebo but no more effective than SASP for inducing remission in ulcerative colitis. This updated review includes more recent studies and evaluates the efficacy and safety of 5-ASA preparations used for the treatment of mild to moderately active ulcerative colitis...
April 21, 2016: Cochrane Database of Systematic Reviews
Matt Ellington
A 19-year-old woman presented to our emergency department with crampy abdominal pain and per rectal bleeding 2 weeks after falling from a horse. She had been taking regular non-steroidal anti-inflammatory drugs (NSAIDs) for analgaesia. On arrival, she was tachycardic and tachypnoeic, with a lactate of 7.3 mmol/L. 'FAST' ultrasonography was unremarkable and CT scan showed thickened wall of the transverse colon. She underwent flexible sigmoidoscopy, which demonstrated "patchy inflammation and an isolated area of severe deep ulceration with nodularity and oedema"...
August 5, 2015: BMJ Case Reports
Adeyinka Abinusawa, Srini Tenjarla
INTRODUCTION: Oral formulations of 5-aminosalicylic acid (5-ASA) for treatment of ulcerative colitis have been developed to minimize absorption prior to the drug reaching the colon. In this study, we investigate the release of 5-ASA from available oral mesalamine formulations in physiologically relevant pH conditions. METHODS: Release of 5-ASA from 6 mesalamine formulations (APRISO®, Salix Pharmaceuticals, Inc., USA; ASACOL® MR, Procter & Gamble Pharmaceuticals UK Ltd...
May 2015: Advances in Therapy
Alvaro Goyanes, Grace B Hatton, Hamid A Merchant, Abdul W Basit
The aminosalicylate mesalazine (mesalamine) forms the mainstay of treatment in ulcerative colitis (UC), a disease for which many commercial modified-release products have been developed with the aim of providing targeted gastrointestinal release. The release profiles of five of these commercial formulations were evaluated in bicarbonate buffer using a novel dissolution model that mimics the dynamic conditions of the gastrointestinal tract. Monolithic and multi-particulate mesalazine formulations with pH-dependent and/or independent release mechanisms were evaluated (Asacol(®) 800, Octasa(®), Mezavant(®) XL, Salofalk(®), Pentasa(®)), and each of the products displayed a distinctive dissolution profile...
April 30, 2015: International Journal of Pharmaceutics
Sumon Chakraborty, Lokesh Yadav, Deepika Aggarwal
Prediction of the in vivo performance of the drug product from the in vitro studies is the major challenging job for the pharmaceutical industries. From the current regulatory perspective, biorelevant dissolution media should now be considered as quality control media in order to avoid the risk associated. Physiological based pharmacokinetic models (PBPK) coupled with biorelevant dissolution medium is widely used in simulation and prediction of the plasma drug concentration and in vivo drug performance. The present investigation deals with the evaluation of biorelevant dissolution media as well as in vivo drug performance by PBPK modelling using STELLA® simulation software...
2015: Drug Development and Industrial Pharmacy
Y Karrout, L Dubuquoy, C Piveteau, F Siepmann, E Moussa, D Wils, T Beghyn, C Neut, M-P Flament, L Guerin-Deremaux, L Dubreuil, B Deprez, P Desreumaux, J Siepmann
The first proof of concept in vivo for a new type of microbiota-sensitive film coatings allowing for colon targeting is presented. The efficacy of these polysaccharide barriers to optimize drug release for the treatment of inflammation is demonstrated in an experimental colitis model with Wister rats. 5-Aminosalicylic acid (5-ASA) pellets were prepared by extrusion-spheronization and coated with Nutriose:ethylcellulose (EC) 1:4 or peas starch:ethylcellulose 1:2 blends. The pellets were mixed with standard chow, and the daily drug dose was 150mg/kg...
January 10, 2015: Journal of Controlled Release: Official Journal of the Controlled Release Society
You Lim Kim, Young Sook Park, Eun Kyoung Park, Dae Rim Park, Gyu Sik Choi, Sang Bong Ahn, Seong Hwan Kim, Yun Ju Jo
Crohn's disease (CD) may involve any part of the gastrointestinal tract, from the mouth to the anus. Approximately >90% of cases occur in the small bowel and colon. Upper gastrointestinal involvement, especially duodenal manifestation, is relatively rare. Therefore, adequate medical treatment for duodenal CD has not yet been established. We report a case of CD with duodenal involvement. A 46-year-old man with Crohn's ileocolitis presented to our hospital with right upper quadrant pain. An endoscopy showed a deep excavated ulcer with deformity at the duodenal bulb, and he was initially treated with azathioprine (1 mg/kg), Pentasa (3...
January 2014: Intestinal Research
Stephan Karl Böhm, Wolfgang Kruis
In 1977, 5-aminosalicylic acid (5-ASA) was discovered as a therapeutically active moiety of sulfasalazine (SASP) and was launched for topical and oral therapy of ulcerative colitis (UC) in 1984. As a first-step, delivery systems had to be developed to protect 5-ASA against absorption in the upper gastrointestinal tract, resulting in different and competing strategies (azo compounds, controlled release, and pH-dependent release). In a second step, at the beginning of the new century, coinciding with the expiration of patent protection for the first 5-ASA formulations, two component composite release mechanisms (pH-dependent and controlled release) were developed...
2014: Clinical and Experimental Gastroenterology
Fuminao Takeshima, Masato Matsumura, Kazuya Makiyama, Kazuo Ohba, Masaki Yamakawa, Hitoshi Nishiyama, Takuji Yamao, Yuko Akazawa, Naoyuki Yamaguchi, Ken Ohnita, Tatsuki Ichikawa, Hajime Isomoto, Kazuhiko Nakao
BACKGROUND: High-dose (4.0 g/day) mesalazine is typically used for induction therapy, but its efficacy as maintenance therapy remains to be determined. We conducted a multicenter retrospective study to investigate the efficacy of continuous treatment with 4.0 g/day of mesalazine. MATERIAL/METHODS: Japanese ulcerative colitis (UC) patients receiving acute induction therapy with 4.0 g/day mesalazine were enrolled and followed. Those who clinically improved or who achieved clinical remission were categorized into 2 sub-groups according to the median duration of treatment with 4...
July 27, 2014: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
Asha G Nair, Russell R Cross
Mesalamine-containing products are considered first-line treatment for inflammatory bowel disease. Myocarditis is recognised as a very rare possible side effect of these medications, but has not often been described in the paediatric population. We present a case of an adolescent with Crohn's disease who presented with myopericarditis after recent initiation of Pentasa. Once identified as the causative agent, the drug was discontinued, with subsequent normalisation of troponin and improvement of function. This case identifies the importance of prompt evaluation, diagnosis, and treatment of paediatric patients receiving mesalamine-containing medications that present with significant cardiovascular symptoms...
April 2015: Cardiology in the Young
Alvaro Mitsunori Nishikawa, Luciano Paladini, Régis Delfini, Paulo Gustavo Kotze, Otavio Clark
CONTEXT: Unspecified Ulcerative Rectocolitis is a chronic disease that affects between 0.5 and 24.5/105 inhabitants in the world. National and international clinical guidelines recommend the use of aminosalicylates (including mesalazine) as first-line therapy for induction of remission of unspecified ulcerative rectocolitis, and recommend the maintenance of these agents after remission is achieved. However, multiple daily doses required for the maintenance of disease remission compromise compliance with treatment, which is very low (between 45% and 65%)...
October 2013: Arquivos de Gastroenterologia
Irina Kadiyala, Dylan Jacobs
This patent review focuses exclusively on the oral delivery of mesalamine (5-ASA) and excludes oral mesalamine pro-drug and rectal delivery formulations. The formulation strategies of marketed formulations (Apriso(®), Asacol(®), Lialda(®) and Pentasa(®)) and non-marketed formulations are reviewed and explained by decoding formulation specifics that enable the site specific delivery for the treatment of inflammatory bowel disease.
April 2014: Recent Patents on Drug Delivery & Formulation
B Flourié, H Hagège, G Tucat, D Maetz, X Hébuterne, J P Kuyvenhoven, T G Tan, M J Pierik, A A M Masclee, O Dewit, C S Probert, D Aoucheta
BACKGROUND: Aminosalicylates are first-choice treatment for mild-to-moderately active ulcerative colitis (UC); however, multi-dosing regimens are inconvenient. AIM: To compare the efficacy and safety of once- (OD) vs. twice- (BD) daily prolonged-release mesalazine (Pentasa, Ferring, Saint-Prex, Switzerland) for active mild-to-moderate UC in a non-inferiority study. METHODS: Eligible patients (n = 206) were randomised to 8 weeks of mesalazine (4 g/day), either OD with two sachets of 2 g mesalazine granules in the morning (n = 102) or BD with one 2 g sachet in the morning and one in the evening (n = 104)...
April 2013: Alimentary Pharmacology & Therapeutics
Brian G Feagan, John K Macdonald
BACKGROUND: Oral 5-aminosalicylic acid (5-ASA) preparations were intended to avoid the adverse effects of sulfasalazine (SASP) while maintaining its therapeutic benefits. Previously, it was found that 5-ASA drugs in doses of at least 2 g/day, were more effective than placebo but no more effective than SASP for inducing remission in ulcerative colitis. This updated review includes more recent studies and evaluates the efficacy and safety of 5-ASA preparations used for the treatment of mild to moderately active ulcerative colitis...
2012: Cochrane Database of Systematic Reviews
Jamal El Bakali, Pauline Gilleron, Mathilde Body-Malapel, Roxane Mansouri, Giulio G Muccioli, Madjid Djouina, Amélie Barczyk, Frédérique Klupsch, Virginie Andrzejak, Emmanuelle Lipka, Christophe Furman, Didier M Lambert, Philippe Chavatte, Pierre Desreumaux, Régis Millet
Further on to our earlier work on the 4-oxo-1,4-dihydropyridine, we describe herein our strategy to get access to potent selective CB₂ receptor agonists. Thus, we designed and synthesized 29 compounds, evaluated on both hCB₁ and hCB₂ cannabinoid receptors, and assessed 11 of them in the TNBS-induced colitis model in mice. Compound 48 was found to be the most efficient of our series, exhibiting an exquisite protection against experimental colitis, superior to the one observed after treatment with Pentasa...
October 25, 2012: Journal of Medicinal Chemistry
Wolfgang Kruis, Ludger Leifeld, Julia Morgenstern, Roland Pfützer, Birgitta Reimers, Sabine Ceplis-Kastner
BACKGROUND AND AIMS: The optimal mesalazine dosing strategy for ulcerative colitis (UC) continues to evolve. The current study aimed to explore whether documenting drug use could prompt changes in prescribing habits. METHODS: In a multicenter, prospective, observational study, outpatients with active or quiescent UC were enrolled if they were receiving, or were planned to receive, sustained release mesalazine microgranules (Pentasa). Clinical and prescribing data were collected at study entry, after 2 and 8 weeks...
May 2013: Journal of Crohn's & Colitis
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