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Successful treatment of ulcerative colitis (UC) is highly dependent on several parameters, including dosing regimen and the ability to deliver drugs to the disease site. In this study two strategies for delivering mesalazine (5-aminosalicylic acid, 5-ASA) to the colon were compared in an advanced in vitro model of the human gastrointestinal (GI) tract, the SHIME® system. Herein, a prodrug strategy employing bacteria-mediated drug release (sulfasalazine, Azulfidine®) was evaluated alongside a formulation strategy that utilised pH and bacteria-mediated release (5-ASA, Octasa® 1600 mg)...

No abstract text is available yet for this article.

No abstract text is available yet for this article.

No abstract text is available yet for this article.

Drug targeting is necessary to deliver drugs to a specific site of action at a rate dictated by therapeutic requirements. The pharmacological action of a drug can thereby be optimised while minimising adverse effects. Numerous colonic drug delivery systems have been developed to avoid such undesirable side effects; however, these systems lack site specificity, leaving room for further improvement. The objective of the present study was to explore the potential of amino-alkoxycarbonyloxymethyl (amino-AOCOM) ether prodrugs as a general approach for future colonic delivery...

The purpose of this study was to develop a bicarbonate buffer flow-through cell (FTC) dissolution test. Mesalazine colon targeting tablets of a generic development product (test formulation, TF; Mesalazine 400 mg tablet) and the original product (reference formulation, RF; Asacol® 400 mg tablet) were used as model formulations. A clinical bioequivalence (BE) study was conducted on 48 healthy male subjects under fasting conditions. The oral absorption time profiles were calculated by point-area deconvolution...

BACKGROUND: Enteric-coated medications are supposed to pass intact through the gastric environment and to release the drug content into the small intestine or the colon. Before dissolution of the enteric coating, they may appear hyperdense on computed tomography (CT). Unfortunately, few reports have been published on this topic so far. In this case report, the hyperdense appearance on contrast-enhanced CT of an enteric-coated mesalamine tablet was initially misinterpreted as a jejunal gastrointestinal stromal tumor (GIST)...

Providing healthcare workers with cost information about the medications they prescribe can influence their decisions. The current study aimed to analyse the impact of two nudges that presented cost information to prescribers through a hospital's electronic prescribing system. The nudges were co-created by the research team: four behavioural scientists and the lead hospital pharmacist. The nudges were rolled out sequentially. The first nudge provided simple cost information (percentage cost-difference between two brands of mesalazine: Asacol® and Octasa® )...

Targeted drug delivery to the colon offers a myriad of benefits, including treatment of local diseases, direct access to unique therapeutic targets and the potential for increasing systemic drug bioavailability and efficacy. Although a range of traditional colonic delivery technologies are available, these systems exhibit inconsistent drug release due to physiological variability between and within individuals, which may be further exacerbated by underlying disease states. In recent years, significant translational and commercial advances have been made with the introduction of new technologies that incorporate independent multi-stimuli release mechanisms (pH and/or microbiota-dependent release)...

No abstract text is available yet for this article.

Ulcerative colitis (UC) is one of the most well-known types of inflammatory bowel disease that manifests as recurrent inflammation of rectum and colon. The goal of this study is to evaluate the protective effects of shark liver oil (SLO) on acetic acid-induced ulcerative colitis in rats. Eighty induced UC rats were randomly divided into ten equal groups and received the following treatments for seven days: 1 ml of normal saline rectally, 1 ml of gel base (carboxymethyl cellulose) rectally, 10 mg/kg of Asacol rectally, 10 mg/kg of mesalazine orally, 5% gel form of SLO rectally, 10% gel form of SLO rectally, 200 mg of SLO orally, and 400 mg of SLO orally...

The aim of this article is to introduce the basic design of used medicinal products with controlled drug release for the treatment of inflammatory bowel diseases and to clarify their behaviour in gastrointestinal tract from the perspective of pharmaceutical technology. Specifically, it focuses on pharmaceutical drugs containing 5-aminosalicylic acid (Asacol®, Pentasa®, Salofalk®) and budesonide (Budenofalk®, Cortiment®, Entocort®). As a part of this paper, basic recommendations and practical information that can be used in clinical practice are also given...

BACKGROUND: Oral 5-aminosalicylic acid (5-ASA; also known as mesalazine or mesalamine) preparations were intended to avoid the adverse effects of sulfasalazine (SASP) while maintaining its therapeutic benefits. In an earlier version of this review, we found that 5-ASA drugs were more effective than placebo for maintenance of remission of ulcerative colitis (UC), but had a significant therapeutic inferiority relative to SASP. In this version, we have rerun the search to bring the review up to date...

BACKGROUND: Oral 5-aminosalicylic acid (5-ASA) preparations were intended to avoid the adverse effects of sulfasalazine (SASP) while maintaining its therapeutic benefits. It was previously 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 (UC). This review is an update of a previously published Cochrane Review. OBJECTIVES: To assess the efficacy, dose-responsiveness and safety of oral 5-ASA compared to placebo, SASP, or 5-ASA comparators (i...

AIMS: Mesalamine is the first-line therapy for treating mild-to-moderate ulcerative colitis. Multiple mesalamine formulations are available, with similar safety and efficacy profiles. Mesalamine is commonly administered as divided dosing, although once-daily dosing may provide benefits for patients. We evaluated pharmacokinetics of three dosing regimens of two oral delayed-release mesalamine formulations in healthy adult volunteers. METHODS: Randomised, open-label, parallel-group study of mesalamine pharmacokinetics following Lialda 2× 1...

Purpose: Mesalazine formulations are the drug of choice in the treatment of ulcerative colitis (UC). They are released at alkaline pH in order to deliver 5-aminosalicylic acid to the colon. The colonic pH is significantly lower in UC patients than in normal patients. This study was conducted for the first time to evaluate the clinical efficacy of co-administration of pantoprazole and Asacol in the treatment of ulcerative colitis patients who excrete intact Asacol tablets in the feces...

BACKGROUND: 5-aminosalicylic acid (5-ASA) is the first-line therapy for ulcerative colitis (UC). 5-ASA acts locally in the colonic mucosa by numerous proposed mechanisms, and is metabolised by N-acetyltransferase (NAT). Large variations in mucosal 5-ASA concentrations have been reported, but the underlying mechanisms are not understood. AIM: To study the relationship between 5-ASA concentration, 5-ASA formulation, NAT genotype and bacterial microbiome in patients with UC...

BACKGROUND: Inflammatory bowel diseases contain two digestive system diseases, ulcerative colitis (UC) and Crohn's disease with unclear causes. The aim of present study was to investigate the therapeutic effects of administration of the Sesame oil (SO) and grape seed oil (GSO) as enema route in rats suffering from experimental acetic acid induced UC. METHODS: Eighty male rats were randomly allocated into 8 equal groups as health control (HC1 ) without any disease treated with 1 ml of normal saline as enema; HC2 received SO; HC3 received GSO; negative control (NC) with induced UC receiving 1 ml of normal saline as enema; and positive control (PC) with induced UC treated by asacol...

BACKGROUND: Antitumor immunotherapy has become a major player in cancer therapy. Ipilimumab is a humanized monoclonal antibody against the cytotoxic T lymphocyte-associated antigen 4 (CTLA-4), an important downregulator of T-cell activation. Ipilimumab has demonstrated tumor regression and improvement in overall survival in patients with metastatic melanoma. Unfortunately, immune activation induced by this drug has been associated with several immune-mediated adverse effects, namely diarrhea and colitis...

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...