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Mesalazine is widely used in the management of inflammatory bowel disease. Previous studies reported that mesalazine-induced cardiotoxicity is a rare, potentially fatal complication. Mitochondria play an important role in myocardial tissue homeostasis. Deterioration in mitochondrial function will eventually lead to cardiomyocyte death and consequently cardiovascular dysfunction. The aim of the current study was to investigate the effects of mesalazine on rat heart mitochondria. Rat heart mitochondria were isolated by mechanical lysis and differential centrifugation. Parameters of mitochondrial toxicity including succinate dehydrogenase (SDH) activity, reactive oxygen species (ROS) formation, mitochondrial membrane potential (MMP) collapse, mitochondrial swelling, and cytochrome c release were evaluated. Results revealed that mesalazine induced a concentration- and time-dependent rise in mitochondrial ROS formation, inhibition of SDH, MMP collapse, mitochondrial swelling, and cytochrome c release in rat heart mitochondria. These results indicate that the cardiotoxic effects of mesalazine are most likely associated with mitochondrial dysfunction and ROS formation, which finally ends in cytochrome c release signaling and induction of apoptosis. [ABSTRACT FROM AUTHOR]

A review has been supposed to be arranged on the literature published between 1996 and 2019 concerning applications of suppositories in clinical practice. The rectal route of drug administration has been in use for centuries particularly in children, elderly and comatose patients as well as in palliative care and preterm infants undergoing painful procedures. Morphine, salbutamol, methadone, lidocaine, propranolol, theophylline, and mianserin, which allow avoiding the hepatic first-pass effect, are examples of preference of rectal route over oral one. Only two main classes of antibiotics (,-lactams and macrolides) have been studied recently after the rectal route of their administration. With the help of modern pharmaceutics and novel RDDS, higher bioavailability and controlled release of the drug have become possible. A number of antiepileptic drugs can be given rectally either for acute seizure control or in maintenance therapy. UC can be effectively treated with topical formulations and is superior to rectal corticosteroids. To suppositories most often used in Europe and the United States for their local treatments belong: bisacodyl, glycerol, mesalazine, diclofenac, glyceryl trinitrate, budesonide, prednisolone, and hydrocortisone. Suppositories applied for the treatment of systemic conditions are more numerous. [ABSTRACT FROM AUTHOR]

Background: Oral 5-aminosalicylic acid (5-ASA, mesalazine) is the first choice therapeutic agent for treating mild-to-moderate ulcerative colitis (UC). Unfortunately a significant group of patients fail to respond. Therapeutic drug monitoring might help to maintain or induce remission by providing a tool for optimization of 5-ASA therapy. However, plasma and urine concentrations of 5-ASA reflect systemic uptake and are not useful to evaluate therapeutic effect. Objectives: To explore if mucosal and faecal 5-ASA values correlate with disease activity and/or therapeutic effects in patients with inflammatory bowel disease, especially UC. Method: We identified studies that analysed 5-ASA in faeces or mucosa of humans using an oral 5-ASA formulation, using PubMed and Embase. Results: In total, 39 studies (n = 939) were included, 27 on faecal 5-ASA, 9 on mucosal concentrations, and 3 on both faecal and mucosal values. We included 33 cross-sectional studies, 3 randomised clinical trials, 2 longitudinal cohorts and 1 randomized cross-over study. Mucosal 5-ASA concentrations in healthy subjects and patients on equivalent doses of 5-ASA were not found to differ remarkably. In the sub-analysis of mucosal 5-ASA concentrations in patients with active or quiescent UC, a higher concentration was seen during remission. Faecal concentrations were associated with 5-ASA doses but not with disease activity. Differences in faecal or mucosal 5-ASA values could not be ascribed to different 5-ASA formulations. Conclusions: An increase of the mucosal 5-ASA concentrations was observed during remission in patients with UC. No clear relationship between the faecal 5-ASA excretion and the therapeutic efficacy was identified. [ABSTRACT FROM AUTHOR]

A glassy carbon electrode modified with a nanocomposite consisting of carbon dots, hexadecyltrimethyl ammonium bromide and chitosan showed excellent electrocatalytic activity toward oxidation of mesalazine (MSA). Under optimal experimental conditions, hydrodynamic amperometry was used for sensitive determination of MSA. Calibration curve was obtained in the range of 0.1–10 μM with a detection limit of 0.05 μM. The repeatability of the method was studied for 5 replicate measurements of MSA (50 μM) and the calculated relative standard deviation (RSD %) was 0.74%. The reproducibility for 5 different electrodes (expressed as RSD %) was 1.96% for MSA (50 μM). The amperometric determination of the drug was successfully performed in spiked blood serum samples with recoveries ranging from 96 to 99%. [ABSTRACT FROM AUTHOR]

Photoexcited TiO2 dispersed in a de-aerated acetonitrile/2-propanol (CH3CN/2-PrOH) reaction mixture catalyzes the quick and selective reduction of 5-nitrosalicylic acid methyl ester to the corresponding aniline, an immediate precursor of the drug mesalazine. The transformation is selective also when the starting concentration of nitro compound is increased by orders of magnitude and occurs at room temperature and atmospheric pressure. The photocatalyst can be reused. The photocatalytic reaction can be carried out also under aerated conditions without any loss in selectivity and efficiency. All these factors point out the feasibility of this important synthesis under mild conditions. [ABSTRACT FROM AUTHOR]

Green TLC‐densitometric and RP‐HPLC methods were developed and validated for the determination of the active prodrug sulfasalazine (SZ), its active metabolite mesalazine (MZ) and the major active metabolite of mesalazine, N‐acetyl‐5‐aminosalicylic acid (AS). In the developed TLC‐densitometric method, chromatographic separation was carried out on TLC silica gel plates 60 F254 using a developing system consisting of ethyl acetate–methanol–ammonia solution 33% (8:2.5:0.3, by volume) and then scanning the separated bands at 215 nm using hydrochlorothiazide as an internal standard with linearity ranges of 0.4–3, 0.4–2.4 and 0.3–2 for SZ, MZ and AS, respectively. The developed RP‐HPLC method depended on chromatographic separation using a C18 column with a solvent mixture of methanol–aqueous acetic acid solution (pH 5) as a mobile phase with gradient elution mode and UV scanning at 243 nm using pyrazinamide as internal standard with linearity ranges of 5–50, 5–40, and 3–20 for SZ, MZ and AS, respectively. US Food and Drug Administration guidelines were followed during validation of the methods. The greenness of the developed methods was estimated using the greenness profile and the Eco‐Scale approach. Both methods passed the four quadrants of the greenness profile and had Eco‐Scale score ˃75, thus they were considered to be green according to these approaches. [ABSTRACT FROM AUTHOR]

This study aimed to simultaneously determine mesalazine (5‐ASA) and its major metabolite N‐Ac‐5‐ASA in the plasma and to evaluate the impact of different food patterns on the relative bioavailability and pharmacokinetics of a single oral dose of 5‐ASA in healthy subjects. In this single‐dose, open‐label, 3‐period, 3‐treatment crossover study, the subjects received a single, oral dose of 500‐mg enteric‐coated mesalazine tablet together with either a low‐fat or a high‐fat breakfast or under fasting condition (reference). The pharmacokinetic parameters were determined by noncompartmental methods and analyzed with a linear mixed‐effect model. The geometric least squares mean ratio for the area under the plasma concentration–time curve from zero to infinity of N‐Ac‐5‐ASA was 1.05 (90% confidence interval [CI], 0.70‐1.58) for high‐fat/fasted condition and 1.06 (90%CI, 0.82‐1.36) for low‐fat/fasted condition. The least squares mean ratio of 5‐ASA was 0.86 (90%CI, 0.65‐1.14) for high‐fat/fasted condition and 0.78 (90%CI, 0.60‐1.02) for low‐fat/fasted condition. All P values were >.05. The mean maximum plasma concentration and the time to reach the maximum plasma concentration of N‐Ac‐5‐ASA were 2084 ng/mL, 8 hours; 2639 ng/mL, 11 hours, and 2409 ng/mL, 9 hours for fasted, high‐fat, and low‐fat, respectively. The values of 5‐ASA were 1950 ng/mL, 7 hours; 2869 ng/mL, 9 hours; and 2837 ng/mL, 8 hours for fasted, high‐fat, and low‐fat condition. 5‐ASA was well tolerated under all 3 conditions. Food delayed the absorption of 5‐ASA, especially a high‐fat meal. Therefore, enteric‐coated mesalazine tablets should be taken before meals to avoid causing patients slow response and any effect of food on its efficacy. [ABSTRACT FROM AUTHOR]

The article presents case study of 11-year-old boy with a 16-month history of ulcerative colitis (UC) treated with mesalazine, who was admitted with a 2-week history of dry cough and dyspnea. It mentions diagnosis of mesalazine-induced lung injury; and also mentions treatment is initially discontinuation of mesalazine, often with clinical improvement.

Preparations of 5-aminosalycil acid (Mesalazine) are used as the first-line therapy to induce remission if the UC activity is minimal and as the priority drugs for anti-recurrence therapy of patients with UC and are included in the Russian recommendations on the therapy of the colitis of the slight and moderate activity. The choice of the drug and its form requires individual approach, it must be based on the UC duration, activity of the inflammatory process as of the moment of the treatment decision taking, the drug safety profile, its effectiveness and tolerability.

Preparations of 5-ASA are the first line treatment of ulcerative colitis (UC). Today, in the market of drugs 5-ASA available for the treatment of UC, there are many dosage forms, varying in the coating, method of delivery of active substance and dosing regimens of the drug. The aim of this review is to compare these dosage forms by the main parameters: efficiency, safety and adherence to treatment.

Inflammatory bowel diseases are chronic relapsing immune-mediated diseases affecting the gastrointestinal tract. The goal of therapy of ulcerative colitis (one of the IBD variants) is the achievement and maintenance of steroid-free remission, prevention of UC complications, prevention of surgeries and the timely use of surgical treatment when the process progresses and lifethreatening complications develop. It Is predominantly diagnosed in young people and leads to a significant reduction of quality of life. The peculiarity of the UC is its chronic recurrent course. Work on the choice of the most rational schemes of therapy continues goes on. New data from clinical studies on the efficacy and safety of modern methods of pharmacotherapy in addition to data on pharmacoepidemiology and pharmacoeconomics should help the medical community to develop the most optimal treatment strategies based on clinical and socio-economic factors. The standard therapy in the first phase is 5-ASA preparations, such as sulfasalazine and mesalazine. Given the efficacy and safety of each of these preparations it is possible to predict the frequency of transition of patients to more difficult treatment options systemic corticosteroids and biological agents arising in connection with this the possible side effects and additional economic load on the healing process. The article presents economic assessment of the use of two alternative first-line drugs for therapy - mesalazine and sulfasalazine; it shows a possible burden on the budget and subsequent benefit when switching to the most optimal treatment option.

The article is devoted to the classification and treatment of diverticular disease of the colon, which is by its prevalence, nature, clinical manifestations, complications is not only a medical but also a huge socio-economic problem. The article elaborates various domestic and foreign classification approaches with the reflection of the merits and costs requiring appropriate changes in the modern Russian guidelines for the diagnosis and treatment of adult patients with diverticular disease of the colon for the development of treatment and preventive measures in different forms of the disease. The place and the analysis of the effectiveness of different therapy regimens with the use of the effect of rifaximin-α (Alfa Normix), mesalazine, dietary fiber, particularly psyllium in the treatment of diverticular disease without clinical manifestations (asymptomatic diverticulosis); DB with clinical manifestations, including recurrent form (symptomatic uncomplicated diverticulosis); in the treatment of acute uncomplicated diverticulitis and for prevention of recurrence of acute diverticulitis (term and permanent treatment) are established.

Background/Aims: This study compared the efficacy of once-daily administration of multimatrix mesalazine 2.4 g/day with multiple-dose mesalazine for the maintenance of remission.Methods: In this multicenter, randomized, double-blind study, 203 patients with ulcerative colitis in remission received multimatrix mesalazine 2.4 g/day once-daily or time-dependent (controlled-release) mesalazine 2.25 g/day 3 times-daily for 48 weeks. The primary efficacy endpoint was the proportion of patients without rectal bleeding.Results: The proportion of patients without rectal bleeding during the 48-week treatment period in the per protocol set was 84.8% (84/99) in the multimatrix mesalazine 2.4 g/day group and 78.0% (78/100) in the controlled-release mesalazine 2.25 g/day group. The difference between the 2 treatment groups was 6.8% (two-sided 95% confidence interval, −3.9% to 17.6%). The noninferiority margin of −10% was met in the comparison of multimatrix mesalazine 2.4 g/day once-daily with controlled-release mesalazine 2.25 g/day. Multimatrix mesalazine 2.4 g/day once-daily demonstrated consistent efficacy in all subgroups. There was no difference between the 2 treatment groups with regard to safety.Conclusions: A once-daily dose of 2 multimatrix mesalazine tablets (2.4 g) was not inferior to controlled-release mesalazine 2.25 g/day 3 times-daily in maintaining absence of rectal bleeding in ulcerative colitis.

Background/Aims: This study assessed the efficacy and safety of high-dose multimatrix mesalazine once-daily (QD) compared to another form of high-dose mesalazine.Methods: In this multicenter, randomized, double-blind study, 280 patients with mildly to moderately active ulcerative colitis (UC) received multimatrix mesalazine 4.8 g/day QD or pH-dependent-release mesalazine 3.6 g/day three times daily for 8 weeks. The primary endpoint was the change in the UC-Disease Activity Index (UC-DAI) at the end of the treatment period.Results: The change in the UC-DAI (mean±standard deviation) in the per-protocol set was −2.6±2.47 in the multimatrix mesalazine 4.8 g/day group (n=134) and −1.8±2.64 in the pH-dependent-release mesalazine 3.6 g/day group (n=129). The difference in the mean change between the 2 groups was −0.7 (two-sided 95% confidence interval, −1.3 to −0.1). The noninferiority of multimatrix mesalazine 4.8 g/day to pH-dependent-release mesalazine 3.6 g/day was verified within the noninferiority margin (1.1). The superiority of multimatrix mesalazine 4.8 g/day to pH-dependent-release mesalazine 3.6 g/day was also investigated and confirmed in the full analysis set, according to the study protocol. In subgroup analyses, the effectiveness of multimatrix mesalazine 4.8 g/day was consistent in all subgroups. There was no difference in safety between the 2 treatment groups.Conclusions: Multimatrix mesalazine 4.8 g/day has higher efficacy and shows no difference in safety in mildly to moderately active UC, in comparison with pH-dependent-release mesalazine 3.6 g/day.

BACKGROUND Intestinal mast cells may cause gastrointestinal symptoms in patients with diarrhea-dominant irritable bowel syndrome (IBS). The objective of this study was to determine the effect of mesalazine on the number of lamina propria mast cells and clinical manifestations of patients with diarrhea-dominant IBS referred to Shariati Hospital affiliated to Tehran University of Medical Sciences. METHODS This was a randomized placebo-controlled double-blind trial conducted on 49 patients with diarrhea-dominant IBS. The patients were randomly assigned to one of the experiment or control groups. The patients in experiment group took 2400 mg mesalazine daily in three divided doses for 8 weeks and the patient in control group took placebo on the same basis. Our first targeted outcome was an assigned downturn of mast cells number to the safe colonic baseline and the next one was a marked palliation of disease symptoms. Data were analyzed conforming intention-to-treat method. We used MANCOVA test to compare our both assigned outcomes in the two groups. We also compared the data with baseline values in both groups. All statistical tests were performed at the significance level of 0.05. RESULTS There was no significant difference between Mesalazine and placebo groups regarding the number of mast cells (p value=0.396), abdominal pain (p value=0.054), bloating (p value=0.365), defecation urgency (p value=0.212), and defecation frequency (p value=0.702). CONCLUSION Mesalazine had no significant effect either on the number of mast cells or on the severity of disease symptoms. This finding seems to be inconsistent with the hypothesis indicating immune mechanisms as potential therapeutic targets in IBS. The possible difference in this effect of Mesalazine should be evaluated in further studies among populations varying in race, ethnic, and geographical characteristics.

ABSTRACT Lymphoid follicular proctitis (LFP) is an uncommon inflammatory disease that is characterized by rectal bleeding, congested and granular mucosa without ulceration and abnormal and coalescing hyperplastic lymphoid follicles without acute inflammatory changes. The lesions are usually confined to the rectal mucosa. LFP therapy is not well defined. Herein, we present a case of LFP that was resolved with a rapid administration of mesalazine enemas. A 35-year-old male was admitted to our hospital due to intermittent rectal bleeding associated with stools. Total colonoscopy revealed nodular mucosa with top pinpoint-like ulcers from the rectum to the border between the sigmoid flexure and the rectum. The nodules congested together on the lower rectal segment and occupied 2/3 of the rectal lumina. Endoscopic submucosal dissection was performed in order to obtain more specimens for histologic examination, which revealed marked lymphoid follicular hyperplasia with prominent germinal centers and a conserved mantle zone. Treatment was started with mesalazine enemas of 4 g q.d. and the patient was asymptomatic after three days. All the lesions disappeared two months later. Mesalazine enemas could be a promising and effective therapeutic option for LFP therapy.

Abstract Background Myocarditis is a rare complication of therapy with mesalazine, a drug widely prescribed in the treatment of inflammatory bowel disease. Case presentation We report a case of myocarditis occurring in a 49-year-old British man 10 days following initiation of mesalazine therapy for treatment of ulcerative colitis. He presented with troponin-positive chest pain, and the diagnosis of myocarditis was confirmed on the basis of cardiac magnetic resonance imaging, which showed subepicardial delayed gadolinium enhancement in the basal to middle inferior and inferolateral segments of the heart. The patient’s symptoms and condition improved upon stopping mesalazine, and he made a full recovery. Conclusions Mesalazine-induced myocarditis may be more common than first appreciated and is potentially fatal. Therefore, it is imperative that clinicians be aware of this potentially life-threatening adverse effect of mesalazine therapy and warn patients to seek urgent medical attention if cardiac symptoms arise.

This study evaluates various techniques for producing mesalamine (5ASA)-loaded particles employing chitosan as a biopolymer: (1) the polyelectrolyte complexation of chitosan with phthalate hypromelose (HP), (2) the chemical crosslinking of chitosan with genipin and (3) the water-in-oil emulsion method associated with chemical crosslinking with genipin. Systems were characterized by dynamic light scattering, zeta potential (ζ), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR) and a drug release profile. Method (1) was efficiently produced unloaded nanoparticles (491 nm, PdI=0.26 and ζ = 23.2), but the conditions for chitosan and HP cross-linking enhanced the precipitation of 5ASA. Method (2) caused the degradation of the drug. Method 3 produced sub-micron and microparticles, thereby varying the agitation method; 3 h magnetic agitation resulted in 2692 nm, Pdi = 0.6 and ζ = 46, while Ultra-Turrax, 5 min produced submicron particles (537 nm, PdI = 0.6). The percentage yield was approximately 50%, which is very satisfactory considering the impossibility of encapsulating 5ASA using other methods. FTIR showed the covalent interaction of chitosan and genipin. The drug release was rapid in acidic fluid, but in neutral pH a slower release was obtained in the initial stage, followed by rapid release, which may ensure the controlled release of 5ASA in the colon.

A key challenge for the effective treatment of intestinal diseases, including inflammatory bowel disease (IBD), is to develop an oral drug delivery system that can resist gastric acid erosion and efficiently release drugs after rapid entry into the intestine. In the present work, we developed oral composite nanoparticles (MSZ@PRHS) consisting of a rough mesoporous silica (RHS) loaded with Mesalazine (MSZ) and a CAP polymer membrane for targeted relief of inflammation in colitis. At the pH values of the simulated stomach and small intestine, the release rate of MSZ from MSZ@PRHS was low, while at the pH values of the simulated colon, the release rate of MSZ was high. In dextran sulfate sodium salt (DSS)-induced acute colitis mouse model, compared with oral administration of the drug Mesalazine in the equivalent solution form, oral administration of PRHS loaded with drug-loaded nanoparticles can significantly alleviate the symptoms of inflammatory bowel disease, and improve the therapeutic effect. We propose that the intestinal microenvironment provides an interface for nanocomposites switch and a promising drug delivery platform for the management and treatment of many intestinal diseases, where controlled drug release and prolonged residence time are required., 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 Zhao, Xu, Liu, Lei, Deng, Wang and Yang.)

Background: Mesalazine, a preparation of 5-aminosalicylic acid, is a medication widely used in clinical practice as a first-line therapy in the treatment of mild and moderate inflammatory bowel disease. However, the long-term safety of mesalazine in large sample population was unknown. The current study was to assess mesalazine -related adverse events of real-world through data mining of the US Food and Drug Administration Adverse Event Reporting System (FAERS). Methods: Disproportionality analyses, including the reporting odds ratio (ROR), the proportional reporting ratio the Bayesian confidence propagation neural network and the multi-item gamma Poisson shrinker (MGPS) algorithms were employed to quantify the signals of mesalazine -associated AEs. Results: Out of 14,149,980 reports collected from the FDA Adverse Event Reporting System database, 24,284 reports of mesalazine -associated AEs were identified. A total of 170 significant disproportionality preferred terms conforming to the four algorithms simultaneously were retained. The most common AEs included colitis ulcerative, diarrhoea, condition aggravated, crohn's disease, fatigue, abdominal pain, nausea, haematochezia, which were corresponding to those reported in the specification and clinical trials. Unexpected significant AEs as dizziness, drug ineffective, drug hypersensitivity, infection, off label use, weight decreased, decreased appetite, arthralgia, rash might also occur. The median onset time of mesalazine -related AEs was 1,127 days (interquartile range [IQR] 1,127-1,674 days), and most of the cases occurred 2 years later (n = 610, 70.93%) and within the first 1 month (n = 89, 10.35%) after mesalazine initiation. Conclusion: Results of our study were consistent with clinical observations. We also found potential new and unexpected AEs signals for mesalazine, suggesting prospective clinical studies were needed to confirm these results and illustrate their relationship. Our results could provide valuable evidence for further safety studies of mesalazine., 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 Liu, Gu, Zhang, Zhou, Wang and Xu.)

Symptomatic Uncomplicated Diverticular Disease (SUDD) is the most common clinical form of Diverticular Disease (DD). The therapy should be aimed at reducing both the intensity and frequency of symptoms as well as preventing complications. The pharmacological treatments include fibers, not absorbable antibiotics (for example rifaximin), anti-inflammatory drugs (for example 5-amino-salycilic acid) and probiotics, alone or in combination with other drugs. Although some of these treatments seem to be effective in treating SUDD, but their efficacy in preventing complications of the disease is still uncertain. It has been hypothesized that microbial imbalance associated with bacterial overgrowth of the colon, may be the key to the development of diverticular disease (DD). Therefore, drugs that can manipulate gut microbiota such as probiotics or rifaximine are considered as a potential key therapy. Rifaximine is able to modulate the intestinal ecosystem, restoring eubiosis. Traditionally, DD of the colon is thought to be related to low grade of inflammation. By analogy with other inflammatory bowel diseases mesalazine has been studied also in DD. There are several evidences that may support the use of mesalazine in the SUDD. Unfortunately, mesalazine cannot be used to prevent diverticulitis because of the paucity of high-quality studies. Currently, mesalazine has a limited place for the management of SUDD. In SUDD probiotics have been proven as an effective therapy in reducing abdominal symptoms, but unfortunately there has been limited number of relevant studies regarding efficacy of this therapy. [ABSTRACT FROM AUTHOR]

Background/Aims: Thiopurines are key drugs in maintenance therapy for treating inflammatory bowel disease (IBD). Time-dependent 5-aminosalicylates (5-ASA) releasing preparations (time-dependent 5-ASA) increase 6-thioguanine nucleotide (6-TGN), an active metabolite of thiopurines. However, the effects of pH-dependent 5-ASA releasing preparations (pH-dependent 5-ASA) on thiopurine metabolism were not reported. Methods: We conducted a retrospective study of 134 IBD patients who received thiopurine treatment. The 6-methylmercaptopurine (6-MMP)/6-TGN values after taking the same dose of thiopurine preparations for at least 28 days were included. Results: There was a significant decrease in the 6-MMP/6-TGN ratio in time-dependent 5-ASA compared with group without 5-ASA preparations and the pH-dependent 5-ASA group (p = 0.008 and < 0.001 respectively). Spearman's rank correlation coefficient indicated a negative relationship between the daily oral dose of time-dependent 5-ASA and the 6-MMP/6-TGN ratio (r = –0.362, p = 0.003). Multivariate logistic regression analysis was performed in the groups with 6-MMP/6-TGN ratios of 1 or more and less than 1. The use of time-dependent 5-ASA and concomitant allopurinol negatively affected the independent 6-MMP/6-TGN ratio (p = 0.006 and 0.007 respectively). Conclusion: Our study revealed that time-dependent but not pH-dependent 5-ASA decreases the 6-MMP/6-TGN ratio. We also confirmed that concomitant allopurinol results in a low 6-MMP/6TGN ratio. [ABSTRACT FROM AUTHOR]

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Copyright of Journal of Education & Science is the property of Republic of Iraq Ministry of Higher Education & Scientific Research (MOHESR) 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.)

Mesalazine is the gold standard drug for treatment of ulcerative colitis (UC). Here, we describe 4 cases of familial adenomatous polyposis (FAP) patients with UC that showed reduction of intestinal polyp diameter by mesalazine treatment. Of note, the effects of mesalazine on the development of intestinal polyps in FAP patients have not been reported, and we further investigated whether the short-term use of high-dose mesalazine (4 g/day) has harmful effects on FAP patients or not. The authors found that the treatment showed slightly adverse events in FAP patients. However, mesalazine tended to reduce the number of colon polyps in male subjects with FAP. This report provides basic information for planning a double-blind, randomized, clinical trial that aims to show mesalazine's potential to suppress intestinal polyp development in FAP. [ABSTRACT FROM AUTHOR]

OBJECTIVE: The aim of this study was to investigate the regulatory mechanism of mesalazine (MSLZ) on microRNA-21, microRNA-31 and Toll-like receptor 4/myeloid differentiation primary response 88 (TLR4/MyD88)-dependent pathway in 2,4,6-trinitrobenzene sulfonic acid (TNBS)/ethanol-induced ulcerative colitis (UC) model in mice. MATERIALS AND METHODS: The UC model was constructed by coloclysis of TNBS/ethanol in mice. 60 male mice were randomly assigned into control group, model group, MSLZ group and Azathioprine (AZA) group, with 15 mice in each. Corresponding drug or saline was i.g. injected in mice for consecutive 14 days. Pathological lesions in colon tissues were observed by hematoxylin and eosin (HE) staining under the microscope. The expression levels of microRNA-21 and microRNA-31 in mouse colon tissues were determined by quantitative Real Time-Polymerase Chain Reaction (qRT-PCR). The mRNA and protein levels of relative genes in TLR4/MyD88-dependent pathway in mouse colon tissues were detected by qRT-PCR and Western blot, respectively. RESULTS: A mouse UC model was successfully constructed based on scores of DAI, colonic damage and pathological lesions under the microscope. MSLZ markedly improved clinical symptoms and mucosal healing. Meanwhile, the protective effect of MSLZ was similar or even stronger than that of AZA. The expression levels of microRNA-21 and microRNA-31 in mouse colon tissues in the model group were significantly higher than those of the control group (p<0.01). Compared with the model group, both MSLZ and AZA treatment could remarkably inhibit the expressions of microRNA-21 and microRNA-31 (p<0.01). The mRNA and protein levels of relative genes in TLR4/MyD88-dependent pathway in mouse colon tissues were markedly upregulated in the model group when compared with those of the control group. The inhibitory effect of MSLZ on the expressions of upstream factors in TLR4/MyD88-dependent pathway (including TLR4, MyD88, TRAF-6 and NF-κB) was slightly stronger than AZA, which was weaker in inhibiting downstream factors (including TNF-α and IL-1β). However, no significant difference in the inhibition of TLR4/MyD88-dependent pathway was found between MSLZ and AZA (p>0.05). CONCLUSIONS: In the TNBS/ethanol-induced UC mouse model, MSLZ could inhibit the expressions of microRNA-21 and microRNA-31 in colon tissues. Furthermore, MSLZ also inhibited the release of inflammatory factors by inhibiting the TLR4/MyD88-dependent pathway in UC mice. [ABSTRACT FROM AUTHOR]

Ulcerative colitis is a continual and proximal spread of inflammation affecting most frequently the distal part of the colon. Among other things, therapies containing mesalazine are used. The following text discusses its therapeutic potential in the given context and at the same time highlights the obvious differences in pharmacokinetics in the Czech Republic available medicinal products given by their different technological processes. [ABSTRACT FROM AUTHOR]

Crocin, as a carotenoid compound of saffron, exerts a potent antioxidant property. Mesalazine is frequently used in the treatment of ulcerative colitis. This study investigated the effects of separated and combination treatments with crocin and mesalazine in a rat model of ulcerative colitis. Ulcerative colitis was induced by intra-colonic administration of acetic acid (4.00%, 1.00 mL) at 8 cm proximal of the anus. Normal saline, acetic acid, crocin (5.00, 10.00 and 20.00 mg kg-1), mesalazine (100 and 300 mg kg-1) and crocin (5.00 mg kg-1) plus mesalazine (100 mg kg-1) were administered after induction of colitis for eight days. Body weight, organosomatic index (OSI), macroscopic and microscopic evaluations of colon and measurement of malondialdehyde (MDA), superoxide dismutase (SOD), tumor necrosis factor-alpha (TNF-α) contents of colon tissue were determined on day eight after induction of colitis. Crocin (10.00 and 20.00 mg kg-1), mesalazine (300 mg kg-1) and crocin (5.00 mg kg-1) plus mesalazine (100 mg kg-1) significantly (p < 0.05) improved body weight and OSI and reduced macroscopic and microscopic scores. These treatments also significantly (p <0.05) recovered the increased levels of MDA and TNF-α as well as the decreased level of SOD in colon tissue. Crocin and mesalazine did not produce significant effects in intact rats. Based on the results, it is concluded that crocin and mesalazine produced protective effects on colon tissue via antioxidant and anti-inflammatory actions. In addition, a synergistic effect was observed between crocin and mesalazine in attenuating ulcerative colitis. [ABSTRACT FROM AUTHOR]

Graphical abstract Highlights • Mesalazine was efficiently encapsulated in chitosan microparticles. • The microsystems are characterized by significant bio-adhesion. • The formulation promoted significant anti-inflammatory activity. • Microencapsulated mesalazine may be used for the treatment of IBDs. Abstract The development of innovative strategies for the efficacious treatment of inflammatory bowel diseases (IBD) still remains a goal for pharmaceutical research. Targeting the lower section of the intestine is the main aim of therapy because it is the compartment primarily affected by IBDs. Mesalazine was microencapsulated in chitosan particles in order to modulate its unfavorable pharmacokinetic profile exploiting the bioadhesive feature of the polysaccharide and increase the anti-inflammatory effect of the drug following its rectal administration in an in vivo model of induced IBD. The chitosan microparticles (1–4 μm mean size) allowed efficient retention of the mesalazine and a prolonged drug release lasting up to 48 h. In vitro and in vivo experiments confirmed the significant mucoadhesion feature of the formulation by means of mucin assay and CLSM experiments and demonstrated its therapeutic efficacy at a drug concentration 2-fold lower than the commercial formulation Asamax® (13 mg/kg vs 26 mg/kg). [ABSTRACT FROM AUTHOR]

Crohn’s Disease (CD), one of the types of inflammatory bowel disease, poses a significant challenge to modern healthcare. This condition severely impacts patients’ quality of life, and its incidence is continuously rising. Despite constant research, current treatment options are limited and largely unsuccessful and result in serious side effects, therefore new therapy alternatives are needed. Liposomal formulation provides a new hope for disease management. In our study, we characterized the anti-inflammatory activity of mesalazine (5-ASA) and chlorogenic acid (CGA) encapsulated in liposomal formulation in the animal model of CD. Liposomes were obtained by thin film hydration method and characterized in terms of suspension stability and particle size and distribution. Colitis was induced in mice by intracolonic (i.c.) administration of 2,4,6-trinitrobenzenesulfonic acid (TNBS). The effect of treatment with liposomal suspensions of 5-ASA and CGA was evaluated macroscopically and by measuring myeloperoxidase (MPO) activity. We observed that liposome-encapsulated 5-ASA (5 mg/kg), but not CGA (20 mg/kg) attenuated colitis as evidenced by a decreased macroscopic and microscopic scores. It may be hypothesized that the composition of liposomal lipid bilayer as well as the switch in macrophage populations leading to unfavorable accumulation of anti-inflammatory agents in the cells may underly the efficiency of obtained liposomes and need to be taken into consideration in further studies on drug delivery. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Education & Science is the property of Republic of Iraq Ministry of Higher Education & Scientific Research (MOHESR) 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.)

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.)

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.)

Graphical abstract Abstract Carbopol® 971 and poly(2-ethyl-2-oxazoline) form hydrogen-bonded interpolymer complexes in aqueous solutions and their complexation is strongly dependent on solution pH. This work investigated the complexation between these polymers in aqueous solutions. The compositions of interpolymer complexes as well as the critical pH values of complexation were determined. The structure of these complexes was studied in solutions using transmission electron microscopy and in solid state using elemental analysis, FTIR spectroscopy and differential scanning calorimetry. Solid compacts were prepared based on interpolymer complexes and physical blends of these polymers and their swelling behaviour was studied in aqueous solutions mimicking the fluids present in the gastrointestinal tract. These materials were used to prepare oral formulations of mesalazine and its release from solid matrices was studied in vitro. It was demonstrated that the complexation between Carbopol® 971 and poly(2-ethyl-2-oxazoline) has a profound effect on the drug release from matrix tablets. [ABSTRACT FROM AUTHOR]

The application of clay minerals in therapeutics is becoming important due to their structural and surface physicochemical properties. 5-aminosalicylic acid (5-ASA) is a very common pharmaceutical drug and is used worldwide. The interactions between the 5-ASA molecule and both the aluminol and siloxane surfaces of kaolinite are studied by means of atomistic calculations using force fields based on empirical interatomic potentials and quantum mechanics calculations based on density functional theory. A conformational analysis of 5-ASA has been performed and the anion of 5-ASA was also studied. The calculated adsorption energy values indicate that 5- ASA is likely to be adsorbed on the kaolinite surfaces with greater affinity to the aluminol surface. Hence, kaolinite may be considered as a promising pharmaceutical carrier of 5-ASA. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

Ulcerative colitis (UC) considers one of inflammatory disorders which affect colon mucosa cause a substantial burden on human day life. In the past, treatment of UC depended on aminosalicylates and antibiotics but due to their adverse side effects and incomplete effectiveness, antioxidant anti-inflammatory agents are used nowadays to ameliorate UC. The aim of this work is to evaluate the modulatory effect of Lactobacillus and/or Spirulina oral administration in acetic acid induced colitisin albino rats. Rats were divided randomly into (6) groups. 1st group (negative control), 2nd group (acetic acid), 3rd group (Mesalazine) at dose 20mg/kg orally was used as positive drug control. 4th group (Lactobacillus) at dose1×109 CFU/rat daily. 5th group (Spirulina) at dose500mg/kg daily. 6thgroup (Lactobacillus at dose 1×109 CFU/rat + Spirulina at dose 500mg/kg). Results revealed that the experimental colitis group showed significant increase in DAI, macroscopic damage, colon weight, colonic MDA, NO, molecular expressions (iNOS and COX-2) and significant decrease in colon length, GSH level and CAT activity. Lactobacillus and/or Spirulina supplementation revealed significant improvement in macroscopic and microscopic finding, increase antioxidant biomarkers, significant inhibitions of MDA and nitric oxide. Furthermore, significant decline in COX-2 and iNOS expressions were reported. In conclusion, the protective effects of Lactobacillus and/or Spirulina in UC are due to their ability to reduce iNOS and COX-2 expressions, increase antioxidant biomarkers and significant inhibition of lipid peroxidations. Furthermore, Lactobacillus and Spirulina have synergistic protective effect on colon tissue and could be used in combination to ameliorate UC. [ABSTRACT FROM AUTHOR]

Abstract Background Although very common in Western countries, poor epidemiological data on diverticular disease (DD) is available from the family practice. Aims To evaluate the behavior of Italian General Practitioners (GPs) on approaching DD. Methods Health Search Database was analyzed retrospectively. Results On a population of 975,523 individuals, 33,597 patients had a registered diagnosis of DD ("lifetime" prevalence = 3.4%, M = 3.2%, F = 3.7%; higher values are found in females over-65 years old; low rates of complications: diverticulitis = 0.3%, bleeding = 0.002%). As risk factors, NSAIDs and ASA were taken by 14.8% and 26.5% respectively, opioids by 7.5%, corticosteroids by 5.2%; as protective factors, 30.4% were under statins and 17.7% under calcium-antagonists. Approximately 13% of patients were referred to specialists. Colonoscopy and abdominal CT were prescribed to 48.5% and to 13% of already diagnosed patients. Among DD sufferers, 27% experienced hospitalization, but only 3.4% of cases were for a DD-linked problem. Treatment included rifaximin (61%), mesalazine (14.7%), probiotics (12.4%), ciprofloxacin (7.6%). Conclusion DD has a large impact in general practice with a higher prevalence in the elderly. GPs are required to pay particular attention to risk factors both for disease development and for its complications in order to reduce the costs deriving from diagnostic procedures, referral and hospitalization. [ABSTRACT FROM AUTHOR]

The elimination of superoxide radical anions (O2•−) by 5-amino-2-hydroxybenzoic acid (mesalazine, 5-ASA), 4-amino-2-hydroxybenzoic acid (4-ASA), and related compounds used for ulcerative colitis treatment was investigated using cyclic voltammetry and electron spin resonance (ESR) analyses aided by density functional theory (DFT) calculations. Quasi-reversible O2/O2•− redox was found to be modified by the compounds, suggesting that an acid–base reaction in which a hydroperoxyl radical (HO2•) is formed from O2•− occurs. However, the deprotonated 5-ASA anion can eliminate O2•− through proton-coupled electron transfer (PCET), forming a radical product. This electron transfer (ET) was confirmed by ESR analysis. The 4-aminophenol moiety in 5-ASA plays an important role in the PCET, involving two proton transfers and one ET based on π-conjugation. The electrochemical and DFT results indicated that O2•− elimination by 5-ASA proceeds efficiently through the PCET mechanism after deprotonation of the 1-carboxyl group. Thus, 5-ASA may act as an anti-inflammatory agent in the alkali intestine through PCET-based O2•− elimination.

A novel green, straightforward, and precise spectrophotometric method for determination of mesalazine drug has been developed. This method relies on an oxidative coupling reaction between mesalazine and the environmentally friendly phenoxazine reagent in an acidic medium within the presence of potassium iodate as an oxidizing agent. The resulting colored product exhibits maximum absorbance at 549 nm. The calibration graph was rectilinear over the range of 0.2-30 µg mL-1 (1.31×10-6-1.96×10-4 mol L-1) with determination Coefficient (R2) of 0.9994 and molar absorptivity of 4.8×103 L mol-1 cm-1. The limits of detection and quantitation were found to be 0.191 and 0.638 µg mL-1, respectively. The average recovery percentage was 100.9 with a relative standard deviation less than 3.1. The proposed method was effectively applied to determine mesalazine in tablet dosage forms from three different sources, yielding highly satisfactory results that closely align with the standard method outlined in the British Pharmacopeia. [ABSTRACT FROM AUTHOR]

• The Co-Mordenite/Mesoporous Carbon modified Glassy Carbon Electrode (Co-MOR/MC-GCE) was presented. • The voltammetric method for the ultrasensitive determination of mesalazine (MES) was developed. • The nanomolar level of LOD was achieved without any preconcentration step. • The method was applied for the determination of MES in pharmaceutical, environmental, and biological samples. In this paper, an ultrasensitive and highly selective analytical method for the voltammetric determination of the anti-inflammatory drug mesalazine (MES) at the Co-exchanged mordenite/mesoporous carbon modified glassy carbon electrode (Co-MOR/MC-GCE) is presented. The combination of unique properties of zeolite and mesoporous carbon, affirmed by conducting morphology and textural parameters studies, resulted in the fabrication of the unique platform sensing, which exhibited a significant enhancement effect of MES oxidation peak current. In the voltammetric determination of mesalazine by the means of differential pulse voltammetry (DPV), univariate optimization stage of the instrumental parameters and the pH value of the supporting electrolyte was performed. In 0.04 mol L−1 Britton-Robinson buffer solution (pH 2.0), the oxidation peak of MES at 0.41 V vs. Ag | AgCl | 3 M KCl reference electrode revealed a linear response in the range of 0.99 – 99.01 µg L−1 (6.47·10−9 – 6.47·10−7 mol L−1) with the limit of detection (LOD) equal to 0.27 µg L−1 (1.76·10−9 mol L−1). The developed protocol was successfully applied for the direct determination of mesalazine in pharmaceuticals, environmental waters, and biological fluids (human urine and serum) with recovery of 103.4 – 119.3%. [Display omitted] [ABSTRACT FROM AUTHOR]

The article is devoted to the comparative characterization of different derivatives of 5-aminosalicylic acid. Researches of the past decades have changed the presentation of the potential use of aminosalicylates in the therapy of various inflammatory bowel diseases. In connection with unknown etiology of Crohn’s disease and ulcerative colitis, there is no causal treatment of these diseases. The essence of treatment is reduced to inhibition of inflammatory activity during exacerbations and a course of preventive treatment. Numerous studies over the past 20 years have shown that the basis of basic treatment for nonspecific chronic inflammatory bowel diseases is 5-aminosalicylic acid drugs, or salicylates. When choosing the dosage form, you should take into account the differences between mesalazine preparations depending on the type of the coat. It is shown that in terms of pharmacokinetics, the most effective mesalazine dosage forms for the treatment of ulcerative colitis and Crohn’s disease with lesions of the colon are enteric coated tablets that provides a pH-dependent gradual release of 5-aminosalicylic acid throughout the entire colon. 5-aminosalicylic acid drugs available today on the pharmaceutical market are able to control the course of ulcerative colitis and Crohn’s disease with lesions of the colon in the majority of patients. The use of 5-aminosalicylic acid preparations is not limited to the treatment of ulcerative colitis and Crohn’s disease. The drug is widely used in other diseases of the bowel, such as diverticular disease of the colon, colitis banal, radiation damages of the colon, as well as to treat common diseases, such as irritable bowel syndrome. The study, which was conducted in the department bowel disease of the State Institution «Institute of Gastroenterology» for 2 years, showed a positive effect of 20-day treatment with Mesacol in uncomplicated diverticular disease. The use of Mesacol at a dose of 1,600 mg per day resulted in complete relief of abdominal symptoms in 68.7 % of patients.

Yunjian Zhang,1 Ling Luo,1 Xiaofang Wang,1 Xiaoyang Liu,1 Xiaoyan Wang,1 Yi Ding2 1Division of Pulmonary and Critical Care Medicine, Department of Medicine, 2Department of Pathology, Jishuitan Hospital, Fourth Medical College of Peking University, Beijing, People’s Republic of China Abstract: Mesalazine-induced eosinophilic pneumonia has been rarely reported. We reported a case of mesalazine-induced eosinophilic pneumonia in a 56-year-old female who took mesalazine without a prescription for suspected ulcerative colitis. She had an elevated eosinophil count in peripheral blood and bronchoalveolar lavage fluid. Eosinophil infiltration was also noted in bone marrow aspirates. Chest radiograph and computed tomography demonstrated bilateral upper lung predominant infiltrates and spirometry showed a restrictive ventilatory defect with a reduced diffusion capacity. The patient recovered after cessation of mesalazine therapy. Mesalazine-induced lung damage should be considered in patients who develop unexplained respiratory symptoms while taking this agent. Keywords: mesalazine, pneumonia, eosinophil, colitis

Background: There is no published data on changes in the endoscopic activity index within first weeks of treatment with various pharmaceutical forms of mesalazine.Aim: Comparative assessment of clinical efficacy and safety of various pharmaceutical forms of mesalazine (tablets, enemas and foam) in the treatment of left-sided ulcerative colitis.Materials and methods: Thirty patients with chronic relapsing left-sided moderate ulcerative colitis participated in the study. They were administered mesalazine either orally (group 1, n = 10) or rectally in micro-enemas (group 2, n = 10) and as foam (group 3, n = 10). Activity of ulcerative colitis was accessed before and after the treatment, along with collecting of patient responses regarding the ease of their use.Results: The mean index of ulcerative colitis activity among all patients before treatment was 7.2 ± 0.8 points. After 1 week of treatment with oral mesalazine, the index of ulcerative colitis activity decreased to 5.2 points and in those patients who were using microenemas and foam, to 4.6 and 3.4 points, respectively, with the difference before/after treatment being significant only in the group 3 (p < 0.05). At 2 weeks of treatment, the activity index decreased more than 2-fold in all groups (p < 0.05). According to the questionnaire, 83.3% of patients accepted the oral intake of the agent as the most convenient one. The highest proportion of compliant patients was in the group using the foam. Conclusion: Mesalazine is highly effective, as shown by a 2-fold decrease in the ulcerative colitis activity index after 2 weeks of treatment. The endoscopic activity index shows more rapid decrease after the use of mesalazine foam (already at 1 week of treatment).

The literature review gives an update on the frequency and risk factors of complications of colonic diverticular disease, the results of recent investigations, which suggest the success and safety of outpatient treatment for uncomplicated acute diverticulitis. It evaluates the efficacy of pharmacological agents from different groups in preventing complications of colonic diverticular disease.

Targeted drug delivery systems are a very convenient method of treating inflammatory bowel disease. The properties of pectin make this biopolymer a suitable drug carrier. These properties allow pectin to overcome the diverse environment of the digestive tract and deliver the drug to the large intestine. This investigation proposed bipolymeric formulations consisting of the natural polymer pectin and a synthetic polymer containing the drug 5-aminosalicylic acid. Pectin beads were prepared via ionotropic gelation involving the interaction between the hydrophilic gel and calcium ions. The obtained formulations consisted of natural polymer, 5-aminosalicylic acid (5-ASA) and one of the synthetic polymers, such as polyacrylic acid, polyvinylpyrrolidone, polyethylene glycol or aristoflex. The release of the drug was carried out employing a basket apparatus (USP 1). The acceptor fluid was pH = 7.4 buffer with added enzyme pectinase to reflect the colon environment. The amount of the released drug was determined using UV-Vis spectrophotometry at a wavelength of λ = 330 nm. The kinetics of the drug dissolution revealed that none of the employed models was appropriate to describe the release process. A kinetic analysis of the release profile during two release stages was carried out. The fastest drug release occurred during the first stage from a formulation containing pectin and polyethylene glycol. However, according to the applied kinetic models, the dissolution of 5-ASA was rather high in the formulation without the synthetic polymer during the second stage. Depending on the formulation, 68–77% of 5-ASA was released in an 8-hour time period. The FTIR and DSC results showed that there was no interaction between the drug and the polymers, but interactions between pectin and synthetic polymers were found.

Inflammatory bowel disease is a common name for Crohn’s disease and ulcerative colitis. These inflammatory states cause damage in the sidewalls of the gastrointestinal tract, resulting in malabsorption of food and vitamins. Folic acid (Vitamin B9) is often associated with inflammatory bowel diseases since reduced overall folate concentration in the human body may lead to the development of colorectal cancer and megaloblastic anaemia. However, its deficiency is easily compensated by taking an additional folic acid pill during regular therapy. At the moment, there are no studies that have examined the compatibility of folic acid with 5-aminosalicylate drugs used in the treatment of inflammatory bowel diseases. In this work, differential scanning calorimetry, forced degradation studies, isothermal stress testing and dissolution stability testing were used to determine the stability of folic acid and one of the most commonly used 5-aminosalicylates, mesalazine, when present in the same solution or blend. To monitor the assay of folic acid, mesalazine and nine of its related impurities, a single HPLC method was developed. Results of compatibility studies showed that no physicochemical interaction between mesalazine and folic acid occurs when combined, opening the path to the development of new formulations, such as a mesalazine/folic acid fixed-dose combination.