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Aim: Colorectal cancer is an extremely aggressive form of cancer that often leads to death. Lactoferrin shows potential for targeting and treating colorectal cancer; however, oral delivery faces hurdles hampering clinical applications. We engineered dual-responsive lactoferrin nanostructured microbeads to overcome delivery hurdles and enhance drug targeting., Methods: The hydrophobic drug mesalazine (MSZ) was coupled to lactoferrin to form amphiphilic conjugate nanoparticles, dispersed in water. The lipid-soluble polyphenolic drug resveratrol (RSV) was then encapsulated into the hydrophobic core of LF-MSZ nanoparticles. To impart thermoresponsive properties, the dual-payload NPs were coupled with a PNIPAAm shell; finally, to further endow the nanoparticles with gastrointestinal resistance and pH responsiveness, the nanoparticles were microencapsulated into ionically cross-linked pectin-alginate beads., Results: The nanoparticles showed enhanced internalization and cytotoxicity against HCT colon cancer cells via LF-receptor-mediated endocytosis. Thermal triggering and tuned release were conferred by the temperature-sensitive polymer. The coatings protected the drugs from degradation. Orally delivered microbeads significantly reduced tumor burden in a mouse colon cancer model, lowering carcinoembryonic antigen and elevating antioxidant enzymes. Apoptotic pathways were stimulated, indicated by heightened Bax/Bcl2 ratio and caspase-3/9 expression., Conclusion: Overall, we propose the innovative lactoferrin nanostructured microbeads as a paradigm shift in oral colorectal cancer therapeutics.

Background: Currently, traditional Chinese medicine (TCM) formulas are commonly being used as adjunctive therapy for ulcerative colitis in China. Network meta-analysis, a quantitative and comprehensive analytical method, can systematically compare the effects of different adjunctive treatment options for ulcerative colitis, providing scientific evidence for clinical decision-making., Aim: To evaluate the clinical efficacy and safety of commonly used TCM for the treatment of ulcerative colitis (UC) in clinical practice through a network meta-analysis., Methods: Clinical randomized controlled trials of these TCM formulas used for the adjuvant treatment of UC were searched from the establishment of the databases to July 1, 2022. Studies that met the inclusion criteria were screened and evaluated for literature quality and risk of bias according to the Cochrane 5.1 standard. The methodological quality of the studies was assessed using ReviewManager (RevMan) 5.4, and a funnel plot was constructed to test for publication bias. ADDIS 1.16 statistical software was used to perform statistical analysis of the treatment measures and derive the network relationship and ranking diagrams of the various intervention measures., Results: A total of 64 randomized controlled trials involving 5456 patients with UC were included in this study. The adjuvant treatment of UC using five TCM formulations was able to improve the clinical outcome of the patients. Adjuvant treatment with Baitouweng decoction (BTWT) showed a significant effect [mean difference = 36.22, 95% confidence interval (CI): 7.63 to 65.76]. For the reduction of tumor necrosis factor in patients with UC, adjunctive therapy with BTWT (mean difference = -9.55, 95%CI: -17.89 to -1.41), Shenlingbaizhu powder [SLBZS; odds ratio (OR) = 0.19, 95%CI: 0.08 to 0.39], and Shaoyao decoction (OR = -23.02, 95%CI: -33.64 to -13.14) was effective. Shaoyao decoction was more effective than BTWT (OR = 0.12, 95%CI: 0.03 to 0.39), SLBZS (OR = 0.19, 95%CI: 0.08 to 0. 39), and Xi Lei powder (OR = 0.34, 95%CI: 0.13 to 0.81) in reducing tumor necrosis factor and the recurrence rate of UC., Conclusion: TCM combined with mesalazine is more effective than mesalazine alone in the treatment of UC., Competing Interests: Conflict-of-interest statement: The authors declare that there is no conflict of interest regarding the publication of this paper., (©The Author(s) 2024. Published by Baishideng Publishing Group Inc. All rights reserved.)

Objective: The recommendations of the Spanish Ministry of Health on vaccination in risk groups include mesalazine among the treatments with a possible negative effect on its effectiveness. However, this is not the recommendation of most experts. Our objective was to evaluate the effect of mesalazine on the humoral response to the SARS-CoV-2 vaccine in patients with inflammatory bowel disease (IBD)., Methods: VACOVEII is a Spanish, prospective, multicenter study promoted by GETECCU, which evaluates the effectiveness of the SARS-CoV-2 vaccine in patients with IBD. This study includes IBD patients who have recieved the full vaccination schedule and without previous COVID-19 infection. Seroconversion was set at 260BAU/mL (centralized determination) and was assessed 6 months after full vaccination. In this subanalysis of the study, we compare the effectiveness of the vaccine between patients treated with mesalazine and patients without treatment., Results: A total of 124 patients without immunosuppressive therapy were included, of which 32 did not receive any treatment and 92 received only mesalazine. Six months after full vaccination, no significant differences are observed in the mean concentrations of IgG anti-S between both groups. In the multivariate analysis, antibody titers were independently associated with the use of mRNA vaccines and with SARS-CoV-2 infection., Conclusion: Mesalazine does not have a negative effect on the response to SARS-CoV-2 vaccines in IBD patients., (Copyright © 2024 Elsevier España, S.L.U. All rights reserved.)

Background: The benefits and risks of Xileisan (XLS) in the treatment of ulcerative colitis (UC) remain unclear., Aim: The present study aimed to evaluate the efficacy and safety of the combination of XLS and mesalazine when treating UC., Methods: We searched eight databases for clinical trials evaluating the combination of XLS and mesalazine in the treatment of UC, up to January 2024. Meta-analysis and trial sequential analysis (TSA) were performed using Revman 5.3 and TSA 0.9.5.10 beta, respectively., Results: The present study included 13 clinical studies involving 990 patients, of which 501 patients received XLS combined with mesalazine while 489 patients received mesalazine alone. The meta-analysis showed that, in terms of efficacy, the combination of XLS and mesalazine significantly improved the clinical efficacy rate by 22% [risk ratio (RR) = 1.22; 95%CI: 1.15-1.28; P < 0.00001] and mucosal improvement rate by 25% (RR = 1.25; 95%CI: 1.12-1.39; P = 0.0001), while significantly reducing the duration of abdominal pain by 2.25 days [mean difference (MD) = -2.25; 95%CI: -3.35 to -1.14; P < 0.0001], diarrhea by 2.06 days (MD = -2.06; 95%CI: -3.92 to -0.20; P = 0.03), hematochezia by 2.32 days (MD = -2.32; 95%CI: -4.02 to -0.62; P = 0.008), tumor necrosis factor alpha by 16.25 ng/mL (MD = -16.25; 95%CI: -20.48 to -12.01; P < 0.00001), and interleukin-6 by 14.14 ng/mL (MD = -14.14; 95%CI: -24.89 to -3.39; P = 0.01). The TSA indicated conclusiveness in the meta-analysis of the efficacy endpoints. In terms of safety, the meta-analysis revealed that the combination of XLS and mesalazine did not increase the occurrence of total and gastrointestinal adverse events, abdominal distension, and erythema ( P > 0.05). The TSA showed non conclusive findings in the meta-analysis of the safety endpoints. Harbord's test showed no publication bias ( P = 0.734)., Conclusion: Treatment with XLS alleviated the clinical symptoms, intestinal mucosal injury, and inflammatory response in patients with UC, while demonstrating good safety., Competing Interests: Conflict-of-interest statement: All the authors report no relevant conflicts of interest for this article., (©The Author(s) 2024. Published by Baishideng Publishing Group Inc. All rights reserved.)

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[Display omitted] • Aminosalicylates are the most common drugs administered to inflammatory bowel disease patients. • Oral 5-aminosalicylic acid formulations are prescribed more often than topical formulations, despite having a lower efficacy. • pH-triggered drug delivery systems are the most effective approach for colon-targeted release. • Nanoparticles present a promising approach for Crohn's disease therapy due to selective uptake by inflamed tissue. Inflammatory bowel disease incidence has been constantly rising for the past few decades. Current therapies attempt to mitigate its symptoms since no cure is established. The most commonly prescribed drug for these patients is 5-aminosalicylic acid (5-ASA). Due to the low rate and seriousness of side effects compared to other therapies, 5-ASA is still largely prescribed in many stages of inflammatory bowel disease, including scenarios where evidence suggests low effectiveness. Although commercialized formulations have come a long way in improving pharmacokinetics, it is still necessary to design and develop novel delivery systems capable of increasing effectiveness at different stages of the disease. In particular, micro- and nano-sized particles might be the key to its success in Crohn's disease and in more serious disease stages. This review provides an overview on the clinical significance of 5-ASA formulations, its limitations, challenges, and the most recent micro- and nanoparticle delivery systems being designed for its controlled release. Emergent alternatives for 5-ASA are also discussed, as well as the future prospects for its application in inflammatory bowel disease therapies. [ABSTRACT FROM AUTHOR]

Mesalazine, also known as 5-aminosalicylic acid (5-ASA), is a synthetic drug from the family of nonsteroidal anti-inflammatory drugs (NSAIDs) used for inflammatory diseases of the gastrointestinal tract. However, 5-ASA has also been used for various other diseases due to its pharmacological effects, but they are usually scattered across various publications, which may limit further research and clinical use of this drug. This review is a summary of published information on the biological and pharmacological effects of 5-ASA with the aim of identifying its anti-oxidant role and medicinal use. 5-ASA data have been collected from 1987 to February 2021 using major databases such as Web of Science, PubMed, Elsevier, Wiley Online Library, Springer, Google Scholar, etc. According to research, the pharmacological and biological effects of 5-ASA include treatment of inflammatory bowel disease, and anti-oxidant, anti-inflammatory, antibacterial, antifungal, anticancer, anti-amyloid, gastric protection (gastroprotective), and antidiverticulosis properties. Numerous pharmacological studies have shown that 5-ASA is an anti-oxidant and anti-ulcer compound with high therapeutic potential that, if the appropriate dose is discovered, its chemical structure changes and its effectiveness is optimized, 5-ASA has been used experimentally for other diseases. [ABSTRACT FROM AUTHOR]

The 2021 National report from IBD UK included responses from over 10 000 patients with inflammatory bowel disease, over 70% of whom reported having at least one flare in the last 12 months. As the first-line treatment for patients with mild and moderate ulcerative colitis, the action and delivery mechanisms of mesalazine are crucial for successful management of the disease. The choice of the most appropriate formulation of mesalazine and securing patient concordance and adherence to treatment remains a challenge for healthcare professionals. This article details the outcome of a roundtable discussion involving a group of gastroenterology consultants and specialist nurses which considered the importance of ensuring that patients have individualised mesalazine therapy before escalation to other treatments and gives recommendations for the management of patients with mild or moderate ulcerative colitis. [ABSTRACT FROM AUTHOR]

Scorpion venom has anti-microbial, anti-cancer, and anti-malarial activities. Also, it has an effective role in the treatment of autoimmune disease and as a pain-relieving agent. Ulcerative colitis (UC) is a chronic deteriorating inflammatory bowel disease. It is urgent to find new and safe products with lesser side effects. This study aimed to use scorpion Leiurus quinquestriatus venom (L.Q venom) for the first time as an anti-inflammatory agent to ameliorate the colon condition after UC induction. Also, to detect the effect of the combinatorial treatment of L.Q venom and Meslazine (Mes) drug. Fifty male albino mice were divided into 5 groups (n = 10); the first group (Gp1) served as a negative control. UC was induced in Gp2, Gp3, Gp4 and Gp5 by 4% acetic acid. Gp2 served as a positive control. After 24 h of UC induction, Gp3 was injected with L.Q venom (3.12 µg/kg) inter peritoneal (i.p), and Gp4 was administered orally by Mes (100 mg/kg). Gp5 was treated with L.Q venom and Mes as in Gp3 and Gp4. All treatments were taken for 7 consecutive days. Disease activity index (DAI), the macroscopic and microscopic investigations, TREM-1, MMP-9, caspase-3, NO, MPO levels were measured. Moreover, COX-2 and IL-22 were investigated in colonic tissue and TLR-9 expression was determined by RT-PCR. The results showed that all previous mentioned parameters were increased in the positive control group (Gp2), however, treatment with L.Q venom (Gp3) decreased these parameters. Interestingly, the combinatorial treatment with L.Q venom/Mes showed an additive effect that was able to ameliorate the physiological, biochemical and histopathological changes that were induced in UC-mice. Collectively, the L.Q venom showed a promising anti-inflammatory effect, which could be used to ameliorate the side effects of UC, either alone or in combination with Mes.

Ulcerative colitis (UC) is a complex inflammatory bowel disorder that can induce colonic and rectal dysfunction. Mesalazine, a first-line medicine, is routinely prescribed for UC treatment. However, the pharmacological targets of mesalazine against UC are not detailed in current publications. In the current study, a transcriptomics strategy was applied to reveal the therapeutic targets and molecular mechanisms of mesalazine for treating dextran sulfate sodium (DSS)-induced UC in mice. Compared with the UC group, a total of 1,663 differentially expressed genes were identified in mesalazine-treated mice, of which 262 were upregulated and 1,401 were downregulated. GO and KEGG enrichment analyses indicated that the protective actions of mesalazine for treating UC were related to the functional regulation of immune inflammatory response, such as the regulation of T cells, white blood cells, and cytokine receptor pathways. In addition, ingenuity pathway analysis of the gene network further revealed the inhibitory action of mesalazine on C–C motif chemokine ligands (CCL11 and CCL21) and C–X–C motif chemokine ligands (CXCL3 and CXCR2). Taken together, the current transcriptomic findings revealed anti-UC pharmacological targets, including the newly discovered biotargets CCL11, CCL21, CXCL3, and CXCR2, of mesalazine against DSS-induced intestinal inflammation.

The solubility of mesalazine in {acetonitrile + water} mixtures was reported at T = (293.2–313.2) K and correlated with some cosolvency models namely van't Hoff, Apelblat, Jouyban-Acree, Jouyban-Acree-van't Hoff, combined nearly ideal binary solvent/Redlich-Kister, modified Wilson, NRTL and UNIQUAC models. The Yalkowsky and extended Yalkowsky models were employed to predict the solubility data. The apparent thermodynamic quantities of dissolution and mixing for mesalazine in aqueous acetonitrile solutions were computed. Finally, preferential solvation analysis demonstrates that mesalazine is preferentially solvated by water in almost all the mixtures, except in the region 0.19 < x1 < 0.29. [ABSTRACT FROM AUTHOR]

Ulcerative colitis (UC) is a complex inflammatory bowel disorder that can induce colonic and rectal dysfunction. Mesalazine, a first-line medicine, is routinely prescribed for UC treatment. However, the pharmacological targets of mesalazine against UC are not detailed in current publications. In the current study, a transcriptomics strategy was applied to reveal the therapeutic targets and molecular mechanisms of mesalazine for treating dextran sulfate sodium (DSS)-induced UC in mice. Compared with the UC group, a total of 1,663 differentially expressed genes were identified in mesalazine-treated mice, of which 262 were upregulated and 1,401 were downregulated. GO and KEGG enrichment analyses indicated that the protective actions of mesalazine for treating UC were related to the functional regulation of immune inflammatory response, such as the regulation of T cells, white blood cells, and cytokine receptor pathways. In addition, ingenuity pathway analysis of the gene network further revealed the inhibitory action of mesalazine on C–C motif chemokine ligands (CCL11 and CCL21) and C–X–C motif chemokine ligands (CXCL3 and CXCR2). Taken together, the current transcriptomic findings revealed anti-UC pharmacological targets, including the newly discovered biotargets CCL11, CCL21, CXCL3, and CXCR2, of mesalazine against DSS-induced intestinal inflammation. [ABSTRACT FROM AUTHOR]

Background: Ulcerative colitis is a common non-specific chronic disease. Supplementing probiotics has become an important method for the treatment of ulcerative colitis. This study aimed to explore the effect of supplementing bifid triple viable capsules on background mesalazine plus somatostatin on plasma inflammatory factors and T cell frequency in ulcerative colitis patients.Methods: A total of 130 ulcerative colitis patients admitted to our hospital from August 2018 to March 2020 were included and divided into the experimental group (65 patients with mesalazine plus somatostatin and bifid triple viable capsules for treatment) and the control group (65 patients treated with mesalazine plus somatostatin) using the random number table method. Bifid triple viable bacteria capsules were given orally, 420 mg each time, with 3 times a day for 2 months.Results: Before treatment, the plasma levels of IL-6, IL-8, hs-CRP, TNF-α, D-lactic acid, and endotoxin (ET), CD4+, CD8+, CD4/CD8 ratio, diamine oxidase (DA0), emotional ability, social ability, intestinal and systemic symptoms were not significantly different between the two groups (all P > 0.05). After treatment, the plasma levels of IL-6, IL-8, hs-CRP, and TNF-α decreased in both groups, and were lower in the experimental group than those in the control group (all P < 0.05). The levels of CD4+ and CD4/CD8 ratio increased, and were higher in the experimental group than those in the control group (P < 0.05); the CD8+ levels were reduced, and were lower in the experimental group than those in the control group (P < 0.05). The plasma D-lactic acid, ET, and DA0 levels were decreased, and were lower in the experimental group than those in the control group; emotional ability, social ability, intestinal and systemic symptoms were improved, and were higher in the experimental group than those in the control group (all P < 0.05). During the course of treatment, 2 cases of abdominal discomfort and 1 case of rash occurred in the experimental group, with an adverse event rate of 4.62% (3/65); 3 cases of abdominal discomfort and 2 cases of rash occurred in the control group, with an adverse event rate of 7.69% (5/65).Conclusion: The supplementary treatment of bifid triple viable capsules can effectively enhance the curative effect in ulcerative colitis patients, reduce plasma inflammatory factors, and regulate T cell frequency, which is worthy of clinical application. [ABSTRACT FROM AUTHOR]

Background and Aim: Thiopurines are often used in combination with mesalazine for the treatment of ulcerative colitis (UC). Mesalazine formulations are delivered to the digestive tract by various delivery systems and absorbed as 5‐aminosalicylic acid (5‐ASA). 5‐ASA is known to inhibit thiopurine S‐methyltransferase (TPMT) activity and to affect thiopurine metabolism. There have been no studies comparing TPMT inhibition by multimatrix mesalazine (MMX) with other formulations. We investigated the difference in TPMT inhibition by different mesalazine formulations and prospectively confirmed the clinical relevance. Methods: Plasma concentrations of 5‐ASA, N‐acetyl‐5‐aminosalicylic acid (N‐Ac‐5‐ASA), and TPMT activities were measured in UC patients receiving various mesalazine formulations (time‐dependent or pH‐dependent mesalazine or MMX) as monotherapy. Patients already on both time‐dependent or pH‐dependent mesalazine and thiopurines switched their mesalazine to MMX, examining 6‐thioguanine nucleotide (6‐TGN) and 6‐methylmercaptopurine (6‐MMP) 0 and 8 weeks after switching. Clinical relapse after switching was also monitored for 24 weeks. Results: Plasma 5‐ASA and N‐Ac‐5‐ASA levels were significantly higher in patients receiving time‐dependent mesalazine (n = 12) compared with pH‐dependent mesalazine (n = 12) and MMX (n = 15), accompanied by greater TPMT inhibition. Prospective switching from time‐dependent mesalazine to MMX decreased 6‐TGN levels, increased those of 6‐MMP, and increased 6‐MMP/6‐TGN ratios. Furthermore, this resulted in significantly more relapses than switching from pH‐dependent mesalazine to MMX. Conclusions: Time‐dependent mesalazine has higher plasma 5‐ASA and N‐Ac‐5‐ASA levels and greater TPMT inhibition than MMX. Therefore, switching from time‐dependent mesalazine to MMX may lead to an increase of 6‐MMP/6‐TGN, which may reduce the clinical effectiveness of thiopurines, warranting close monitoring after switch. [ABSTRACT FROM AUTHOR]

Objective　To evaluate the pharmacokinetics of the new mesalazine enteric-coated sustained-release granules in SD rats and their distribution in the gastrointestinal tract, and to understand the preclinical pharmacokinetics and gastrointestinal distribution characteristics of the preparation. Methods　Rats were administered orally to determine the drug concentrations in plasma samples and in the gastrointestinal tract. The commercially available mesalazine sustained-release granule was used as a reference to self-developed one to evaluate the process of absorption and elimination in vivo, relative bioavailability, and distribution in the gastrointestinal tract. Results　The relative bioavailability of mesalazine enteric-coated sustained-release granule and non-enteric-coated one characterized by mesalazine was 89.62% ± 9.36%. After oral administration of mesalazine entericcoated sustained-release granules, the drug has a high concentration distribution in the stomach within 2-8 hours, and gradually enters and remains in the jejunum, ileum and colon over time for 6-12 hours and then reaching a high concentration distribution in the colon. This help for the absorption of mesalazine, as well as the fixed-point release of the drug to produce a therapeutic effect. Conclusion　The absorption and elimination process of mesalazine enteric sustained-release granule showed linear kinetic characteristics. There was no significant difference in pharmacokinetic parameters from the commercially available formulations, and it had a certain fluidity in the gastrointestinal tract. Good gastrointestinal distribution characteristics help the absorption of drugs in the body and the targeted release of the site of action. [ABSTRACT FROM AUTHOR]

An anti-inflammatory medication termed Mesalazine (MLZ) is generally recommended to prevent inflammatory bowel diseases (IBD). However, its prolonged usage has been associated with the risk of kidney failure. Therefore, there is a pressing need for the development of effective electrocatalysts to enable rapid detection of MLZ in the environment. Layered double hydroxides (LDHs) have emerged as promising candidates in the realm of sensor technology due to their adjustable interlayer spacing and large surface area. In this study, we utilized the hydrothermal method to synthesize cobalt aluminum-layered double hydroxide (CoAl-LDH) and evaluated its suitability as an active electrocatalyst for MLZ detection. The prepared CoAl-LDH was characterized for its physicochemical attributes employing XRD, FT-IR, XPS, FESEM, and TEM analysis. Subsequent examination of its electrochemical properties via voltammetric techniques revealed that the CoAl-LDH-modified glassy carbon electrode (GCE) exhibited enhanced electrocatalytic activity. Notably, the CoAl-LDH/GCE demonstrated a lower detection limit of 0.029 µM and a linear detection range spanning from 0.049 to 665.1 µM. Furthermore, the modified electrode demonstrated favorable attributes such as good repeatability, reproducibility, and stability. Real-time application of the modified electrode in the spiked water and urine samples yielded satisfactory recovery results, indicating its potential for practical use in environmental monitoring. [Display omitted] • Facile synthesis of CoAl-LDH via hydrothermal approach. • Fabrication of CoAl-LDH/GCE sensor for the detection of mesalazine. • The sensor displays good selectivity, repeatability, and reproducibility. • The proposed sensor was used to detect mesalazine in real samples and obtained acceptable results. [ABSTRACT FROM AUTHOR]

Objective of this study was to observe the clinical effect of mesalazine combined with bifid triple viable (BTV) on ulcerative colitis. One hundred sixty patients with ulcerative colitis were divided into the experimental group accepting mesalazine combined with BTV and the control group accepting mesalazine alone. It was found that the overall treatment effective rate was 93.75%, in the experimental group as against 77.50% in the control group, p<0.05. Comparing the levels of inflammatory factors (IL-6,IL-8,TNF-a) before and after treatment in the two groups, the improvement degree of the experimental group after treatment was significantly better than that of the control group, p<0.05. The overall nursing satisfaction of the research group was 97.50%, which was significantly higher than the 75.00% of the control group, p<0.05. To conclude that combined therapy of mesalazine and BTV can significantly improve the therapeutic effect in patients with ulcerative colitis, and the scientific nursing mode is an important guarantee to improve the therapeutic results. [ABSTRACT FROM AUTHOR]

A simple and accurate spectrophotometric method has been suggested for the determination of Mesalazine (MES), carbamazepine (CAM) and diclofenac sodium (DFS) in pure and pharmaceutical dosages. The method is based on the oxidation of drugs in acidic medium with known excess of N-bromosuccinimide (in case of MES), or bromate-bromide mixture (in case of CAM and DCF) and subsequent determination of unreacted oxidant by decolorization of nile blue dye (NB) and measure the absorbance of unoxidized dye at 640 nm. Calibration curves of the dye in the presence of studied drugs were rectilinear over the ranges 0.1-2.2, 0.4-2.4 and 0.6-2.8 µg ml-1 with molar absorptivity of 6.21×104, 1.05×105 and 1.21×105 l.mol-1.cm-1 for MES, CAM and DCF respectively. The common excipients and additives didn’t interfere in their determination. The suggested method was successfully applied for determination of the studied drugs in their pharmaceutical forms resulted in a good agreement with standard British pharmacopeia method and standard addition procedure.

Aim of the study. To compare the efficacy of treatment of patients with moderate left-sided and overall affection ulcerative colitis (UC) receiving equivalent doses of mesalazines – Mesacol and Salofalk.Materials and methods. 90 UC patients of medium severity who received mesalazine Salofalk (group 1) were included, of which 41 (45.5%) were males and 49 (54.5%) females, mean age 35.8 ± 2.5 years, and 96 UC patients of medium severity who received mesalazine Mesacol (group 2), of whom 42 (43.75%) were males and 54 (56.25%) females, mean age 37.1 ± 3.1 years. Patient follow-up time was 12 weeks. The efficacy of the therapy was assessed taking into account 1) response to therapy in 2 weeks from the beginning of therapy; 2) achievement and maintenance of clinical remission (persistent remission) within 12 weeks after the beginning of therapy. Results and discussions. After 2 weeks 78 (86,7%) patients of the 1st group responded to the therapy with mesalazine Salofalc (stool frequency decreased to 4–6 t/day, presence of pathological impurities in the stool decreased, according to laboratory indices anemia and leukocytosis decreased, and the level of CRP and ESR decreased). Twelve patients (13.3%) did not have a proper response to therapy. In the 2nd group of patients receiving Mesacol mesalazine, 80 (83,4%) out of 96 patients responded to the therapy, and 16 patients (16,6%) did not respond. After 12 weeks, 78 (86.7%) of the 90 UC Group 1 patients who responded to mesalazine Salofalk treatment still had clinical remission. The Mayo index in the group decreased from an average of 7.98 ±0.11 to 2.9 ±0.24 points. After 12 weeks, in group 2 UC patients (n = 96), 80 patients (83.4%) who responded to Mesalazine Mesacol therapy also had clinical remission. The Mayo Index in Group 2 decreased on average from 7.8 ± 0.1 to 2.8 ± 0.25 points. One year after the start of Salofalk mesalazine therapy, clinical remission remained in 76 (84.4%) of the 90 UC patients who responded to therapy, of whom 32 (35.5%) had clinical endoscopic remission. In the second group of UC patients receiving Mesacol, clinical remission remained in 78 (82.0%) out of 96 patients who responded to therapy, clinical endoscopic remission in 32 (35.5%) patients with UC. When comparing the duration of remission among UC patients receiving mesalazine Salofalk and patients receiving mesalazine Mesacol, there was no statistically significant difference (p = 0.45).Conclusion. Mesalazines remain the first line of treatment for mild and moderate UC patients. Treatment of moderately active UC should start with oral mesalazine >2 g/day in combination with local mesalazine. Prolonged continuous use of Mesacol and Salofalk mesalazines for a year is comparable in efficacy.

In this research, the electrochemical oxidation of mesalazine was investigated in presence and absence of benzenesulfinic acid and 4-toluenesulfinic acid as a nucleophile using cyclic voltammetry and controlled-potential coulometry. The results indicate that quinoneimine generated by oxidation of mesalazine, participates in reaction with arylsulfinic acids via Michael addition reaction in a ECC electrochemical mechanism pattern. To approve the proposed ECC mechanism, electrochemical synthesis of oxidation of mesalazine was also performed in the presence of benzenesulfinic acid and the obtained product, was identified by of FT-IR and mass spectrometry spectra. Homogenous rate constants (kobs) of Michael addition reaction for quinoneimine generated by oxidation of mezalasine with arylsulfinic acids, were estimated by cyclic voltamogram digital simulation method.

Ulcerative colitis is a chronic inflammatory disease affecting mainly the colon and presenting with diarrhea, bloody defecation andabdominal pain. Although cardiac and/or pulmonary involvement has been reported in patients with ulcerative colitis, it rarelyinvolves both the pleura and pericardium at the same time. Also, it is difficult to determine whether pulmonary or cardiac diseaseis secondary to the ulcerative colitis drugs or to the underlying disease process. Here we present a rare case of pleuropericardialeffusion in a patient newly diagnosed with ulcerative colitis. In ulcerative colitis, the simultaneous involvement of the respiratoryand cardiovascular systems is uncommon yet potentially dangerous.

Simple, sensitive and rapid spectrophotometric method for the determination of mesalazine in pure form and pharmaceutical preparations is described. The method is based on the reaction of mesalazine with p-bromanil in the presence of borate buffer solution of pH9 to form a pink color charge transfer complex of maximum absorption peak (λmax) at 346 nm. Under the optimized reaction conditions, Beer’s law correlating the absorbance with mesalazine concentration was obeyed in the range of 0.48-12 μg ml-1. The molar absorptivity was 6.5×103 L.mol−1cm−1. The limits of detection was 0.053μg ml-1. The accuracy and precision of the method were satisfactory; the average recovery was 98.04% and values of relative standard deviations better than 1.70 %. The stoichiometry of the reaction was studied, and the reaction mechanism was postulated. The proposed method was successfully applied to the determination of mesalazine in its pharmaceutical tablet and capsule with good accuracy and precisions. The results obtained by the proposed method were compared with those obtained by the official method.

Mesalazine suppositories are widely used to treat ulcerative colitis and have a guaranteed safety profile, but although rare, they can cause pulmonary toxicity. A 35-year-old woman with ulcerative colitis was diagnosed to have acute eosinophilic pneumonia after 29 days of oral mesalazine use and improved after mesalazine and corticosteroid were withdrawn. Reintroduction of mesalazine suppositories resulted in acute eosinophilic pneumonia recurrence after 28 days. Mesalazine re-administration (even via a different route) in patients with a history of mesalazine-induced eosinophilic pneumonia should be undertaken cautiously, because eosinophilic pneumonia may recurrence.

Abstract Background Cronkhite-Canada syndrome is a rare disease of unknown etiology and the optimal treatment for this syndrome is unknown. Case presentation We present the case of a man who at the age of 66.0 years was diagnosed with Cronkhite-Canada syndrome (CCS). In addition to watery diarrhea, alopecia, and a complete loss of toenails and fingernails, the patient had been suffering from dysgeusia and rapid weight loss of more than 10.0 kg within a few months. The patient had recently incurred a distal radius fracture. During the initial endoscopy an extensive polyposis of the stomach and jejunum was found. The diagnosis of CCS was made and after initiation of a steroid therapy his diarrhea improved immediately. A discontinuation of the steroid therapy was not possible and mesalazine (1000 mg t.i.d.) was added to prednisolone (10.0 mg/d). This therapy led to a remission within 6.0 months with weight gain and normalization of serum albumin levels. The prednisolone dose was reduced to 7.5 mg/d. During the following year, the steroids could be further reduced and nails had regrown again. Within three years, all polyps had disappeared and the steroid therapy was finished while the dosage of mesalazine was reduced in a stepwise fashion. Four years later, the mesalazine was stopped and more than 14.0 years after the initial diagnosis the patient is still in complete remission without any treatment. Conclusion The optimal treatment for CCS is unknown. In our case, the initial combination therapy of corticosteroids plus mesalazine followed by a mesalazine monotherapy has led to a remarkable long-lasting remission with complete resolution of all intestinal polyps.

Currently, the number of patients treated with immune-checkpoint inhibitor involving nivolumab is increasing. Nevertheless, it causes various immune-related adverse events (irAEs). Here, we report the case of a patient who underwent long-term follow-up after suffering from nivolumab-associated colitis. The patient was a 57-year-old man who underwent resection of a bladder tumor. Following surgery, lymph node metastasis was detected, and he was treated by nivolumab. Two months after treatment with nivolumab, the patient complained of bloody diarrhea. Colonoscopy revealed pancolitis with erosions, loss of vascular pattern and erythema. Pathological findings indicated a disease state of pan-ulcerative colitis. As an irAE by nivolumab, the patient was started with 30 mg of prednisolone. Prednisolone treatment successfully induced clinical remission and mucosal healing. Nevertheless, eight months after stopping the steroid treatment, the colitis relapsed with diarrhea following elevation of fecal immunochemical test (FIT) and fecal calprotectin (CPT). The relapsed colitis was treated by mesalazine, and then diarrhea was improved. Nivolumab-associated colitis relapsed following mucosal healing suggesting that it is necessary to consider maintenance therapy as well as remission induction for long-term survivor. The present case also demonstrates that the FIT and CPT would be effective biomarker to assess the disease activity of nivolumab-associated colitis.

Background: We aimed to evaluate the therapeutic effect of additional ursodeoxycholic acid (UDCA) with mesalazine, compared to mesalazine alone in patients with ulcerative colitis (UC). The mechanism was evaluated by monitoring the changes of IL-23-IL-17 axis and the intestinal microflora. Methods: In this prospective, single center study, patients with UC were randomly assigned to the Mesalazine group (n=20) or the UDCA + Mesalazine group (n=20). Mayo score and Inflammatory Bowel Disease Questionnaire (IBDQ), and fecal samples for 16S rRNA sequencing and blood samples for IL-23 and IL-17 ELISA were collected for analysis. Results: Mayo scores and IBDQ score of the UDCA + Mesalazine group were significantly better than those of the Mesalazine group (P = 0.015 and P < 0.001, respectively). At post-treatment week 4, IL-23 and IL-17 levels were significantly lower in the UDCA + Mesalazine group compared to those in the Mesalazine group (both P < 0.038). In patients with UC after treatment, Firmicutes in the UDCA + Mesalazine group was higher than those in the Mesalazine group (P < 0.001). The UDCA + Mesalazine group showed lower percentage of Proteobacteria compared to those in the Mesalazine group (P < 0.001). Conclusion: Additional UDCA could provide better therapeutic effects than mesalazine alone, possibly due to the change of IL-23 and IL-17 and the proportional distribution of intestinal microflora. [ABSTRACT FROM AUTHOR]

We prepared, for the first time, carbon aerogels support on Pd–WO3 nanorods (CAs/Pd–WO3) hybrid nanocomposite via sol-gel and microwave-assisted methods. The as-prepared CAs/Pd–WO3-modified electrode was used as effective electrocatalyst for nanomolar level detection of mesalazine (MSA). The typical porous nature of carbon aerogels effectively prevented the aggregation of Pd-doped WO3 nanorods and increased the electrochemically active surface area. In addition, the Pd–WO3 nanointerface provides intrinsic improvement of the electrocatalytic activity and stability for the electrochemical oxidation process, and the interconnected conducting network of the porous surfaces of CAs accelerated rapid electron transport at the working electrode. The synergistic effect of the CAs/Pd–WO3 architecture has excellent electrocatalytic activity for the detection of MSA with high sensitivity of 2.403 ± 0.004 μA μM−1 cm−2, low detection limit of 0.8 ± 0.3 nM and wide linear response from 0.003–350 μM at a low applied potential of 0.30 V vs. Ag|AgCl. Satisfactory results were observed for its analytical performance in detecting MSA in human blood serum and urine samples, and recoveries ranged from 98.8 to 100.4%. We believe that the architecture of the modified CAs/Pd–WO3 electrocatalysts can be effectively used in clinical applications for the detection of MSA. [ABSTRACT FROM AUTHOR]

A 57-year-old woman with Crohn's disease (ulcerative proctitis) treated with mesalazine (5-ASA) developed worsening respiratory distress and cough. The lack of response to antibiotics and the results of bronchoalveolar lavage led to the diagnosis of mesalazine-related hypersensitivity pneumonitis, an infrequent entity. Symptoms improved after discontinuation of mesalazine and the administration of corticosteroid therapy. The authors discuss the diagnosis and management of this rare condition.

Objectives To analyze the clinical effect of Feng-Liao-Chang-Wei-Kang Granule combined with mesalazine on chronic colitis. Methods 120 patients with chronic enteritis admitted to Qionghai Hospital of Traditional Chinese Medicine from October 2020 to March 2022 were selected as the research objects, and were randomly divided into combined group (62 cases) and conventional group (58 cases). Patients in the conventional group were treated with oral mesalazine on the bais of conventional treatment, while patients in the combined group were treated with Feng-Liao-Chang-Wei-Kang Granule combined with mesalazine. The clinical efficacy, inflammatory factor level, colonic mucosal lesion degree, quality of life and TCM syndrome scores of the two groups were compared. Results The total clinical effective rate in the combined group was higher than that in the conventional group (P <0. 05). After treatment, the levels of inflammatory factors in the two groups were lower than those before treatment, and the levels of interleukin-6 (IL-6), C-reactive protein (CRRP) and tumor necrosis factor- (TNF-a) in the combined group were lower than those in the conventional group ( P < 0. 001 ). Ater treatment, the Baron and Geboes scores of the two groups were lower than those before treatment, and the Baron and Geboes scores of the combined group were lower than those of the conventional group ( P < 0.001 ). Ater treatment, the scores of quality of life in the two groups were higher than those before treatment, while the scores of TCM syndromes were lower than those before treatment. The scores of quality of life in the combined group were higher than those in the conventional group (P <0.001). Conclusions Feng-Liao-Chang-Wei-Kang Granule combined with mesalazine can obviously improve the curative eefect, reduce the level of in-flammatory factors, improve the degree of colonic mucosal lesions and improve the quality of life of patients with chronic colitis, which is worthy of popularization and application in clinical practice. [ABSTRACT FROM AUTHOR]

Background Mesalazine is a well-established 1st line treatment for inflammatory bowel disease (IBD). Cardiotoxicity following 5-aminosalicyclic-acid therapy remains a rare yet serious complication and can often be challenging to distinguish from myocarditis presenting as an extra-intestinal manifestation of IBD. Case summary We present a case of a 22-year-old man with a background of ulcerative colitis commenced on a mesalazine preparation for disease progression. He presented to our hospital 12 days following drug initiation with acute chest pain, peak troponin-T of 242 ng/L, dynamic electrocardiogram changes, and severe left ventricular systolic dysfunction on transthoracic echocardiogram. The clinical diagnosis of myopericarditis was suspected and mesalazine was stopped shortly after. Outpatient cardiac magnetic resonance performed 2 weeks following mesalazine cessation demonstrated a recovery of cardiac function with associated symptom and biochemical resolution. Discussion Clinicians should be aware of this potentially fatal adverse effect of a commonly prescribed medication. Symptoms of myocarditis often occur within the early stages of mesalazine initiation, which aids the clinical diagnosis. The mainstay of treatment is to simply discontinue the drug with rapid resolution of symptoms seen without any permanent or long-term cardiac dysfunction. Close liaison with the gastroenterology team is key, as 2nd line IBD therapies are often required for the ongoing management of the patient's colitis. [ABSTRACT FROM AUTHOR]

Objective: To explore the effect of compound Kushen Decoction combined with mesalazine on the treatment of ulcerative colitis and the level of inflammatory factors. Methods: Taking 206 patients with ulcerative colitis admitted to the Department of Integrated Traditional Chinese and Western Medicine and Gastroenterology in our hospital from January 2017 to December 2019 as the research subjects, the subjects were divided into a control group and a study group according to a random sampling method. 103 cases in each group, the control group received mesalazine treatment, and the study group was treated with Compound Kushen Decoction on the basis of the control group. The total effective rate of treatment of the two groups was compared, and the mucosal lesions, disease activity index and various inflammations were compared before and after treatment. Factor level changes and medication safety. Results: The total effective rate of treatment in the study group was higher than that in the control group (P<0.05); after treatment, the mucosal lesions and disease activity index under colonoscopy in the two groups were significantly improved compared with before treatment, and the study group was significantly better than the control group (P<0.05) ); After treatment, the two groups of interleukine (IL)-6, IL-8, tumor necrosis factor (TNF)-α, C-reactive protein (CRP) and procalcitonin (Procallcitonin, PCT) and other inflammatory factors were significantly lower than before treatment, and the study group was lower than the control group (P<0.05); there was no statistical difference in the incidence of adverse reactions caused by the two groups of drugs (P>0.05). Conclusion: Compound Kushen Decoction combined with mesalazine can effectively relieve clinical symptoms, improve intestinal mucosal lesions, reduce intestinal inflammatory response, control the progress of the disease, and have significant efficacy and safety. It has positive significance in promoting the recovery of patients with ulcerative colitis. [ABSTRACT FROM AUTHOR]

This study reports the experimental mesalazine solubility data in the binary mixtures of ethanol and water at temperature ranges of 293.2–313.2 K. The generated data are correlated with six co-solvency mathematical models including the van't Hoff, the mixture response surface, the Yalkowsky, the Jouyban–Acree, the Jouyban–Acree–van't Hoff, and the modified Wilson models, and the mean relative deviations (MRD%) of the back-calculated solubility for each investigated model are reported. Density of the mesalazine saturated solutions as another physicochemical property are also fitted by the Jouyban–Acree model. Moreover, standard enthalpy, entropy and Gibbs free energy changes for mesalazine dissolution process are obtained by using the van't Hoff and Gibbs equations. Furthermore, by means of inverse Kirkwood-Buff integrals is observed that mesalazine is preferentially solvated by water in almost all the mixtures studied. [ABSTRACT FROM AUTHOR]

Background: The efficacy data on treatment in older adults are scarce, while the greatest increase in ulcerative colitis (UC) prevalence is observed in age groups of individuals 40 to 65 years of age and ≥65 years of age., Aim: We assessed the difference in rates of clinical and endoscopic response and remission in UC adults (≤60 years) and older adults (>60 years) treated with mesalazine., Methods: We performed a post hoc analysis of data from a phase 3 noninferiority trial of 817 UC patients treated with mesalazine for 8 and additional 26 weeks in a double-blind and open-label study, respectively. We used Wilcoxon rank sum or chi-square test to analyze differences between groups and multivariable logistic regression to determine the associations between endoscopic remission as outcome (Mayo endoscopic subscore [MES] = 0 or ≤1) and independent variables including disease duration, baseline MES, age, sex, comedications, and comorbidities., Results: Older adults had a longer disease duration, a higher number of comorbidities, concomitant medications, and higher baseline MES (2.38 ± 0.486 in older adults vs 2.26 ± 0.439 in adults; P = .008) compared with adults. We observed no difference in rates of combined clinical and endoscopic remission, clinical remission and response, and endoscopic remission and response at week 8 and 38 post-treatment. In addition to other well-known predictors of worse outcome, patients with ≥3 comedications were less likely to achieve an MES = 0 at week 8 and 38 and an MES ≤1 at week 38., Conclusions: We observed similar efficacy of mesalazine in adult and older adult UC patients. The increased comedication number rather than age may decrease effectiveness of UC medications, highlighting the importance of healthy aging., (© 2024 Crohn’s & Colitis Foundation. Published by Oxford University Press on behalf of Crohn’s & Colitis Foundation.)

Background: Faecal calprotectin (FC) shows an excellent correlation with endoscopic and histological activity of ulcerative colitis (UC) and it is the best predictor of clinical relapse. Our aim was to evaluate the usefulness of modifying the dose of mesalazine based on FC levels, in clinical practice., Methods: Retrospective, single-centre study in UC patients in clinical remission while treated with mesalazine which dosage was decreased (DOWN) or increased (UP) according to FC levels. The main endpoint was the long-term maintenance of clinical remission., Results: A total of 56 patients were included (39 DOWN, 17 UP). In the DOWN group, the median baseline dose of mesalazine was 3.6g/day and the median baseline FC was 36μg/g. After a median follow-up of 22 months, 28% required rescue therapy. The cumulative relapse-free survival after tapering was 91% and 82% at 12 and 24 months, respectively. In the UP group, the median baseline dose of mesalazine was 2.4g/day, with a median baseline FC of 524μg/g. After a median follow-up of 12 months, 29% required rescue therapy. The cumulative relapse-free survival after dose increase was 86% and 72% at 12 and 24 months, respectively., Conclusions: Mesalazine dose modification based on FC monitoring seems to be a safe strategy in patients with UC in clinical remission, with a probability of clinical relapse around 20% at two years., (Copyright © 2023 Elsevier España, S.L.U. All rights reserved.)

Purpose: Current pharmacological treatments for Ulcerative Colitis (UC) have limitations. Therefore, it is important to elucidate any available alternative or complementary treatment, and Chinese herbal medicine shows the potential for such treatment. As a traditional Chinese herbal medicine, Danshen-related preparations have been reported to be beneficial for UC by improving coagulation function and inhibiting inflammatory responses. In spite of this, the credibility and safety of this practice are incomplete. Therefore, in order to investigate whether Danshen preparation (DSP) is effective and safe in the treatment of UC, we conducted a systematic review and meta-analysis. Methods: PubMed, Embase, Cochrane Library, Web of Science, China National Knowledge Infrastructure, Wanfang Database and CQVIP Database were searched for this review.The main observation indexes were the effect of DSP combined with mesalazine or DSP on the effective rate, platelet count (PLT), mean platelet volume (MPV) and C-reactive protein (CRP) of UC. The Cochrane risk of bias tool was used to assess the risk of bias. The selected studies were evaluated for quality and data processing using RevMan5.4 and Stata17.0 software. Results: A total of 37 studies were included. Among them, 26 clinical trials with 2426 patients were included and 11 animal experimental studies involving 208 animals were included. Meta-analysis results showed that compared with mesalazine alone, combined use of DSP can clearly improve the clinical effective rate (RR 0.86%, 95% CI:0.83-0.88, p < 0.00001) of UC. Furthermore it improved blood coagulation function by decreasing serum PLT and increasing MPV levels, and controlled inflammatory responses by reducing serum CRP, TNF-α, IL-6, and IL-8 levels in patients. Conclusion: Combining DSP with mesalazine for UC can enhance clinical efficacy. However, caution should be exercised in interpreting the results of this review due to its flaws, such as allocation concealment and uncertainty resulting from the blinding of the study. Systematic Review Registration : http://www.crd.york.ac.uk/PROSPERO/myprospero.php, identifier PROSPERO: CRD42022293287., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2024 Zhang, Xiong, Liu, Hu, Song, Liu and Jia.)

This study demonstrates an effective, simple, and selective method for monitoring mesalazine in pharmaceutical formulations using liquid phase micro-extraction (LPME) and spectrophotometry. Combining LPME with spectrophotometry is an efficient method for analysing various compounds in different matrices. This method is based on extracting the ion-pair formed between the blue indophenol produced by the oxidative reaction of mesalazine and syringic acid in an alkaline medium and a quaternary ammonium salt into a micro-volume of organic solvent. The experimental parameters influencing LPME performance, such as the type and concentration of the quaternary ammonium ion salt and the type and volume of the extractant solvent, were optimised for optimal detection. The linear range and the limit of detection for measuring red species in pharmaceutical formulations were determined to be 0.005-0.080 μg/mL -1 and 0.003 μg/mL -1 , respectively, with a relative standard deviation of 4-6%. The method had a preconcentration factor of 50 at 520nm, making it highly efficient and reliable for monitoring mesalazine in pharmaceutical formulations., (Copyright © 2023 Académie Nationale de Pharmacie. Published by Elsevier Masson SAS. All rights reserved.)

Dapsone (DpS) is an antimicrobial and antiprotozoal agent, especially used to treat leprosy. The drug shares a similar mode of action with sulfonamides. Additionally, it possesses anti-inflammatory activity, useful for treating autoimmune diseases. Here, we developed a “me-better” alternative to sulfasalazine (SSZ), a colon-specific prodrug of mesalazine (5-ASA) used as an anti-inflammatory bowel diseases drug; DpS azo-linked with two molecules of 5-ASA (AS-DpS-AS) was designed and synthesized, and its colon specificity and anti-colitic activity were evaluated. AS-DpS-AS was converted to DpS and the two molecules of 5-ASA (up to approximately 87% conversion) within 24 h after incubation in the cecal contents. Compared to SSZ, AS-DpS-AS showed greater efficiency in colonic drug delivery following oral gavage. Simultaneously, AS-DpS-AS substantially limited the systemic absorption of DpS. In a dinitrobenzene sulfonic acid-induced rat colitis model, oral AS-DpS-AS elicited better efficacy against rat colitis than oral SSZ. Moreover, intracolonic treatment with DpS and/or 5-ASA clearly showed that combined treatment with DpS and 5-ASA was more effective against rat colitis than the single treatment with either DpS or 5-ASA. These results suggest that AS-DpS-AS may be a “me-better” drug of SSZ with higher therapeutic efficacy, owing to the combined anti-colitic effects of 5-ASA and DpS.

Symptomatic ulcerative colitis (UC) can be a chronic, disabling condition. Flares in disease activity are associated with many of the negative impacts of mild-to-moderate UC. Rapid resolution of flares can provide benefits to patients and healthcare systems. i Support Therapy–Access to Rapid Treatment (iSTART) introduces patient-centered care for mild-to-moderate UC. iSTART provides patients with the ability to self-assess symptomology and self-start a short course of second-line treatment when necessary. An international panel of experts produced consensus statements and recommendations. These were informed by evidence from systematic reviews on the epidemiology, mesalazine (5-ASA) treatment, and patient use criteria for second-line therapy in UC. Optimized 5-ASA is the first-line treatment in all clinical guidelines, but may not be sufficient to induce remission in all patients. Corticosteroids should be prescribed as second-line therapy when needed, with budesonide MMX® being a preferred steroid option. Active involvement of suitable patients in management of UC flares has the potential to improve therapy, with patients able to show good accuracy for flare self-assessment using validated tools. There is a place in the UC treatment pathway for an approach such as iSTART, which has the potential to provide patient, clinical and economic benefits.

Background/AimsThis study compared the efficacy of multimatrix mesalazine 2.4 g/day and 4.8 g/day with controlled-release mesalazine 2.25 g/day.MethodsIn this multicenter, randomized, double-blind study, 251 patients with mildly to moderately active ulcerative colitis received multimatrix mesalazine 2.4 g/day once daily (Multimatrix-2.4), 4.8 g/day once daily (Multimatrix-4.8), or controlled-release (time-dependent) mesalazine 2.25 g/day 3 times daily (Time-2.25) for 8 weeks. The primary efficacy endpoint was the change in the ulcerative colitis-disease activity index (UC-DAI) score.ResultsThe mean change in the UC-DAI score and standard deviation in the per protocol set was −1.9±2.5 for Multimatrix-2.4 and −2.4±2.8 for Time-2.25. The difference between Multimatrix-2.4 and Time-2.25 was 0.3 (two-sided 95% confidence interval [CI], −0.5 to 1.1), thus non-inferiority was not demonstrated based on the pre-defined non-inferiority margin (1.0). In the full analysis set, the difference between Multimatrix-4.8 and Time-2.25 was −1.2 (two-sided 95% CI, −2.0 to −0.5), and the mean change in UC-DAI score in the FAS was −3.3 (two-sided 95% CI, −3.9 to −2.8) for Multimatrix-4.8 and −1.9 (two-sided 95% CI, −2.5 to −1.3) for Multimatrix-2.4, indicating that Multimatrix-4.8 was more effective than Time-2.25 and Multimatrix-2.4. There was no difference among the treatment groups in terms of safety.ConclusionsThis study showed that the efficacy of multimatrix mesalazine 2.4 g/day was comparable to controlled release mesalazine 2.25 g/day, although non-inferiority was not demonstrated. Importantly, this was the first study to indicate that multimatrix mesalazine 4.8 g/day was more effective than 2.4g/day with no associated safety concerns.

Background: Diverticular disease (DD) is a common condition, especially in Western countries. In about 80% of patients, colonic diverticula remain asymptomatic (diverticulosis), while approximately 20% of patients may develop abdominal symptoms (symptomatic uncomplicated diverticular disease, SUDD) and, eventually complications as acute diverticulitis (AD). The management of this condition has been improved, and in the last five years European countries and the USA have published guidelines and recommendations. Scope: To summarize the latest evidence and clinical implication in treatment of DD focusing the attention either on the treatment of diverticulosis, SUDD and AD together with the primary and secondary prevention of diverticulitis. Findings: The present review was based on the latest evidence in the treatment of DD in the last 10 years. In the last 5 years, six countries issued guidelines on DD with differences regarding covered topics and recommendations regarding treatments. At present there is a lack of rationale for drug use in patients with asymptomatic diverticulosis, but there are limited indications to suggest an increase in dietary fibre to reduce risk of DD. To achieve symptomatic relief in SUDD patients, several therapeutic strategies with fibre, probiotics, rifaximin and mesalazine have been proposed even if a standard therapeutic approach remained to be defined. Agreement has been reached for the management of AD, since recent guidelines showed that antibiotics can be used selectively, rather than routinely in uncomplicated AD, although use of antibiotics remained crucial in the management of complicated cases. With regard to treatment for the primary and secondary prevention of AD, the efficacy of rifaximin and mesalazine has been proposed although with discordant recommendations among guidelines. Conclusion: Treatment of DD represented an important challenge in clinical practice, especially concerning management of SUDD and the primary and secondary prevention of AD.

Ulcerative colitis (UC) is a chronic disease characterized by immune diffuse inflammation of the mucosa of the colon with mandatory involvement in the inflammatory process of the rectum. The choice of conservative or surgical treatment depends upon the severity of the attack, extent of lesions of the colon, presence of extraintestinal manifestations, duration of disease, efficacy and safety of past therapy and the risk of complications UC. In Russia and abroad for the treatment and prevention of relapses of UC are widely used mesalazine having minimum side effects. Our study shows high adherence of patients to receive drugs 5-ASA and the positive impact of the use of oral medications 5-ASA Salofalk and Asacol for the maintenance of remission in patients UC moderate severity in clinical practice. This study also showed the importance of long-term use (at least 12 months) drugs 5-ASA to maintain remission and reduce the risk of disease recurrence.

Drug-induced acute pancreatitis (DIAP) is an often-neglected entity where the disorder is the consequence of the toxic effects of various agents applied to treat potentially life-threatening conditions, such as inflammatory bowel disease. Here, we present the case of a male patient with ulcerative colitis with a history of two episodes of recurrent acute pancreatitis. After excluding other potential causes, we suspected DIAP since the patient received 5-aminosalycilate (5-ASA) prior to the first episode and, one year later, azathioprine (AZA) prior to the second episode. The causative effect of AZA was confirmed by performing a re-challenge with a reduced dose. While both episodes of DIAP had a mild disease course, they were associated with acute relapse of ulcerative colitis. Last seen, the patient was asymptomatic. With this case, we would like to highlight the importance and diagnostic difficulties of DIAP in the background of recurrent cases when common etiological factors of acute pancreatitis are excluded. [ABSTRACT FROM AUTHOR]

Background There are few recent studies on the use of 5-aminosalicylates (5-ASA) as therapy for Crohn's disease (CD) in routine clinical practice. The aim of this database investigation was to provide real-world evidence on 5-ASA use in CD. Methods Patients with CD, aged ≥18 years when first prescribed 5-ASA (index date) and having received 5-ASA at any time between 01 January 2006 and 07 May 2018, were included for analysis. Outcomes included treatment patterns and resource use. Results Of 21,456 patients with CD, 9492 (44.2%) had been prescribed 5-ASA, with the majority (5606; 59.1%) starting on oral 5-ASA as monotherapy. 58.3% (5537) of patients on 5-ASA did not require dose change, 67.6% (6416) did not require supplementary treatment (e.g., corticosteroids, immunosuppressants, etc.), and 4.6% (436) required a switch to another treatment. Resource use was significantly decreased in the year after vs. year before 5-ASA initiation (including: specialist referrals, hospitalizations and hospital days; all P<0.001). Patients remained on 5-ASA for a median of 4.7 years (interquartile range 1.2-10.1). 25.3% (2406) of patients were still on 5-ASA at 10 years. There was a significant correlation between earlier use of 5-ASA following diagnosis and longer 5-ASA retention (P<0.001). Conclusions 5-ASA is widely used as a long-term treatment for CD, as evidenced by continuation rates extending beyond 10 years in a quarter of patients. CD-related healthcare resource use decreased significantly in the year following 5-ASA initiation. Earlier use was associated with longer retention [ABSTRACT FROM AUTHOR]

Diverticulitis is the most severe form of Diverticular disease (DD). An effective treatment strategy for its prevention has not yet been defined. This review aimed to provide a viewpoint on the role of mesalazine, also note as 5-aminosalicylic acid (5-ASA), in the prevention of diverticulitis. A systematic electronic search of relevant articles was performed using PubMed, Embase, Scopus, and Cochrane. Randomized controlled trials (RCTs), open trials, and retrospective studies, published between January 1999 and January 2020, were identified. Twelve eligible studies that analyzed primary or secondary outcomes of diverticulitis were included. The population included patients with symptomatic uncomplicated diverticular disease (SUDD), or patients with a history of diverticulitis. All studies compared 5-ASA to placebo, rifaximin, or other treatments. Two studies, including 359 patients, assessed the efficacy of 5-ASA in preventing the first appearance of diverticulitis in patients with SUDD. Of these, one showed that 5-ASA was effective, and one did not. Ten studies, including 2.995 patients, assessed the efficacy of 5-ASA treatment in preventing the recurrence of diverticulitis in patients with a history of diverticulitis. Four studies showed that 5-ASA had a certain degree of efficacy. All four RCTs demonstrated that 5-ASA did not significantly reduce the rate of diverticulitis recurrence. In a retrospective trial, 5-ASA was less effective than rifaximin in preventing diverticulitis recurrence. In an open trial, there was no difference between 5-ASA and probiotic treatment. Overall, there is currently conflicting evidence regarding the efficacy of 5-ASA treatment in the prevention of diverticulitis and further RCTs are needed. [ABSTRACT FROM AUTHOR]

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Copyright of Practical Pharmacy & Clinical Remedies is the property of Editorial Department of Practical Pharmacy & Clinical Remedies and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: Modified Sijunzi decoction (SJZD) has been used to treat ulcerative colitis (UC) in remission. However, more rigorous clinical trials are necessary to evaluate its effectiveness. Therefore, a series of single-case randomised controlled trials (N-of-1 trials) is proposed to compare the efficacy of modified SJZD with mesalazine for treating UC in remission.Methods: This is a single-site, hospital-based, double-blind N-of-1 trial for 10 single subjects. Three cycles of N-of-1 trials are planned. There are two treatment periods in each cycle. Modified SJZD combined with mesalazine placebo or mesalazine combined with modified SJZD placebo will be randomised during each 8-week treatment period. There is no washout period in the study. Subjects will be selected by the researcher strictly in accordance with the inclusion and exclusion criteria.Discussion: Paired t tests and mixed-effect models will be used to analyse the visual analogue scale (VAS) for clinical symptoms and the quality of life questionnaire responses. The findings will be interpreted with caution. We anticipate that the results will show that modified SJZD is effective for patients with UC in remission.Trial Registration: Chinese Clinical Trial Register, ID: ChiCTR1900024086. Registered on 24 June 2019. [ABSTRACT FROM AUTHOR]