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PubMed2005

A validated HPLC method with electrochemical detection for simultaneous assay of 5-aminosalicylic acid and its metabolite in human plasma.

A high-performance liquid chromatographic method was developed, validated and applied to the simultaneous determination of 5-aminosalicylic acid (5-ASA) and its acetylated metabolite (acetyl-5-ASA) in human plasma. The method involves liquid-liquid extraction with methanol followed by isocratic reversed-phase chromatography on a Kromasil KR100 C(18) column with electrochemical detection. The recovery, selectivity, linearity, precision and accuracy of the method were evaluated from spiked human plasma samples. The effects of mobile phase composition, buffer concentration, mobile phase pH and concentration of organic modifiers on retention of 5-ASA, acetyl 5-ASA and internal standard were investigated. Limits' of detection were 5 ng/mL for 5-ASA and 10 ng/mL for acetyl-5-ASA, respectively. The method can be used for supporting therapeutical drug monitoring and pharmacokinetic studies.

Aminosalicylic Acids↗
PubMed1990

Therapeutic effectiveness and tolerance of 5-aminosalicylic acid in short term treatment of patients with ulcerative colitis at a low or medium phase of activity.

The therapeutic effectiveness and tolerance of 5-aminosalicylic acid (5ASA), compared with Salazosulphapyridine (SASP) in treatment of ulcerative colitis have been evaluated in 86 patients with the disease at a low or medium phase of activity. After a treatment of six weeks, an improvement was noted in 63.6% (5ASA) and 61.3% (SASP) of these patients. However in no case was a complete remission of the disease observed on the basis of endoscopic inspection. In patients with pancolitis the improvement was lower (37.5% with 5ASA, 40% with SASP). The only side-effect was gastric intolerance, which occurred in 18.1% of the 5ASA and in 19% of the SASP patients. In conclusion we can assume that 5ASA and SASP largely overlap each other as regards both therapeutic effectiveness and occurrence of side-effects.

Aminosalicylic Acids↗
PubMed1975

Colorimetric determination of 5-aminosalicylic acid and its N-acetylated metabolite on urine and feces.

A simple and convenient colorimetric method is described for the quantitative determination of 5-aminosalicylic acid (5-ASA) and N-acetyl-5-ASA in urine and feces after oral administration of salicylazosulfa-pyridine (SASP), the drug of choice in the treatment of ulcerative colitis. N-acetyl-5-ASA is extracted directly from the acidified biological specimen, deacetylated, and the liberated 5-ASA subjected to a modified Bratton-Marshall reaction. The 5-ASA present in the specimen must be acetylated with acetic anhydride prior to extraction. The violet colored product of the Bratton-Marshall reaction has a lambdamax of 560 nm and conforms to Beer's law over the concentration range of 0-70 umg/ml. Average recoveries (+/- S.D., N = 6) OF 5-ASA added to rat and human urine and rat fecal homogenates were 91.6 +/- 4.9%, 102 +/- 6.0%, and 71.0 +/- 4.8%, respectively. Interference by SASP and its sulfapyridine metabolities is negligible. As demonstrated, the colorimetric method is of sufficient sensitivity for application in most metabolic and pharmacokinetic studies conducted with SASP in laboratory animals and man.

Acetylation↗
PubMed1990

Pharmacokinetics of a 5-aminosalicylic acid enteric-coated tablet in patients with Crohn's disease or ulcerative colitis and in healthy volunteers.

An Eudragit-L coated oral 5-aminosalicylic acid (5-ASA; mesalazine) product (Mesasal), has been formulated to deliver 5-ASA to the distal small bowel and colon for the treatment of inflammatory bowel disease. The purpose of this study was to compare the pharmacokinetic profile of this drug between two patient groups, with either inflamed small or large bowel and with volunteers. Two carefully selected patient groups (one with nine patients suffering from Crohn's disease restricted to the small intestine, and one with ten patients suffering from total ulcerative colitis) and a group of ten volunteers received two 250 mg Mesasal tablets in the morning, on a fasting stomach. Plasma 5-ASA and acetyl-5-ASA concentrations were followed for 48 h, and urine and faecal excretion for 72 h. There was a great variation in most pharmacokinetic parameters within each group. Numerically, however, the data suggests a somewhat higher systemic absorption in patients with Crohn's disease than in healthy volunteers or patients with ulcerative colitis. The location of the inflammatory process might have some influence on the pharmacokinetics of 5-ASA in inflammatory bowel disease.

Adolescent↗
PubMed1987

5-Aminosalicylic acid in the treatment of Crohn's disease. A 16-week double-blind, placebo-controlled, multicentre study with Pentasa.

The response to 5-aminosalicylic acid (5-ASA) in mild and moderately active Crohn's disease localized in the small bowel was studied in a randomized, double-blind, placebo-controlled trial in four centres. Sixty-seven patients were included, of whom 30 were treated with 1500 mg slow-release 5-ASA/day (Pentasa) for a scheduled period of 16 weeks. In the 5-ASA group 40% of the patients improved, versus 30% of the placebo-treated group ('intent to treat' basis; p greater than 0.1). Four of the patients treated with 5-ASA left the study owing to disease deterioration, versus 10 of the placebo-treated patients (p greater than 0.2). Seventeen patients were secondarily excluded, and the remaining 50 patients (23 receiving 5-ASA) were reevaluated in greater detail. No statistically significant differences in outcome were shown. Three patients (one given 5-ASA) were withdrawn from the study because of presumed side effects, but no serious adverse reactions were recorded. The present results indicate that 5-ASA, at least in the dosage used, is not superior to placebo. Nevertheless, trends towards a beneficial effect in Crohn's disease in the small bowel justify further clinical trials with a larger dosage of 5-ASA.

Adolescent↗
PubMed1994

Long-term therapy with 5-aminosalicylic acid in Crohn's disease: is it useful? Our four years experience.

At present it is not clear if long-term therapy with 5-aminosalicylic acid (5-ASA) is useful in the prevention of relapses of Crohn's disease (CD) in remission. Long-lasting randomized studies are necessary to gauge the efficacy of a long-term therapy, but actually the trials are rarely longer than 12 months. The aim of our study was therefore to evaluate the efficacy of 5-ASA in maintaining the remission in inactive CDs followed up for 4 years. Sixty-six patients, 41 males, mean age 35 +/- 8, having a definitive diagnosis of CD made at least 2 years before, with ileum localization in 39 and ileocolic in 27, entered the study when Crohn's disease activity index (CDAI) and a laboratory index (LI) values were lower than 150 and 100 respectively for at least 6 weeks. Subjects with previous surgical treatment or with an endoscopic index severity (CDEIS) more than 4 were excluded. The patients were randomly divided into two groups: 33 received 5-ASA at 2.4 g/day in a delayed-release formulation (Eudragit-S-coated Mesaline) while another 33 as a control group received non-specific therapy. CDAI and LI were evaluated every 6 months, relapse being defined by a CDAI > or = 150 and LI > or = 100. To confirm the clinical and laboratory diagnosis of relapse, all the patients with CDAI > or = 150 and LI > or = 100 underwent X-ray and/or endoscopic examination. Statistical analysis was made at the end of the study.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed2004

The folate pathway is a target for resistance to the drug para-aminosalicylic acid (PAS) in mycobacteria.

The increasing rate of multidrug-resistant tuberculosis has led to more use of second-line antibiotics such as para-aminosalicylic acid (PAS). The mode of action of PAS remains unclear, and mechanisms of resistance to this drug are undefined. We have isolated PAS-resistant transposon mutants of Mycobacterium bovis BCG with insertions in the thymidylate synthase (thyA) gene, a critical determinant of intracellular folate levels. BCG thyA mutants have reduced thymidylate synthase activity and are resistant to known inhibitors of the folate pathway. We also find that mutations in thyA are associated with clinical PAS resistance. We have identified PAS-resistant Mycobacterium tuberculosis isolates from infected patients, which harbour mutations in thyA and show reduced activity of the encoded enzyme. Thus, PAS acts in the folate pathway, and thyA mutations probably represent a mechanism of developing resistance not only to PAS but also to other drugs that target folate metabolism.

Aminosalicylic Acid↗
PubMed2002

Evaluation of renal function following treatment with 5-aminosalicylic acid derivatives in patients with ulcerative colitis.

BACKGROUND: A number of cases of nephrotoxicity have been reported in patients with inflammatory bowel disease taking oral 5-aminosalicylic acid (5-ASA). AIM: To evaluate the effects of 9 months of therapy with mesalazine or olsalazine on renal function in patients with ulcerative colitis in remission. METHODS: Forty patients with ulcerative colitis in complete remission for 6 months were randomized to either olsalazine (n=20) or mesalazine (n=20 for nine months). Thirty-six of the 40 patients were on prior salicylate therapy. Disease activity was the measure ofclinical efficacy and was assessed by the Harvey-Bradshaw Index (HBI). Laboratory efficacy measurements included glomerular filtration rate (GFR), microalbuminuria, urinary gluthathione S-transferase (GST) and serum C-reactive protein (CRP). Safety analysis consisted of documentation of adverse events and laboratory values. RESULTS: There was no significant reduction in the GFR overall on therapy. The levels of GFR adjusted for baseline were similar in the two treatment groups after 3, 6 and 9 months. A significantly higher percentage of mesalazine-treated patients experienced drug related adverse events, all of a minor nature. The incidence of adverse events causing early withdrawal was similar in the two treatment groups. CONCLUSION: Treatment with mesalazine or olsalazine for 9 months had no significant impact on GFR.

Adult↗
PubMed2002

Chitosan capsules for colon-specific drug delivery: enhanced localization of 5-aminosalicylic acid in the large intestine accelerates healing of TNBS-induced colitis in rats.

The objective of this study was to achieve the colon-specific delivery of an anti-ulcerative colitis drug using chitosan capsules and to accelerate healing of 2,4,6-trinitrobenzene sulfonic acid sodium salt (TNBS)-induced colitis in rats. 5-Aminosalicylic acid (5-ASA) was used as a model of an anti-inflammatory drug. The gastrointestinal transit of chitosan capsules was determined by counting the number of capsules in the gastrointestinal lumen by celiotomy at certain times after their oral administration to rats. The chitosan capsules reached the large intestine 3.5 h after oral administration in rats. We studied the release of 5-ASA from chitosan capsule by the Japan Pharmacopoeia (JP) rotating basket method. The release of 5-ASA from the chitosan capsule markedly increased in the presence of rat cecal contents. After oral administration of chitosan capsules containing 5-ASA, the concentrations of 5-ASA in the large intestinal mucosa were higher than those in the CMC suspension. For the treatment of colitis in rats, 5-ASA was orally administered using chitosan capsules or a carboxy methyl cellulose (CMC) suspension to TNBS-induced rats. The colonic injury and inflammation were assessed by measuring the myeloperoxidase (MPO) activities, colon wet weight/body weight (C/B) ratio and the damage score, respectively. When 5-ASA was orally administered using chitosan capsules in TNBS-induced colitis rats, we found better therapeutic effects with 5-ASA than with a 5-ASA CMC suspension, as evaluated by the MPO activities, C/B ratio and the damage score. In conclusion, chitosan capsules may be useful carriers for the colon-specific delivery of anti-inflammatory drugs including 5-ASA and the healing of TNBS-induced colitis in rats.

Administration, Oral↗
PubMed1989

Coated mesalazine (5-aminosalicylic acid) versus sulphasalazine in the treatment of active ulcerative colitis: a randomised trial.

OBJECTIVE: To assess the safety and efficacy of a preparation of mesalazine (5-aminosalicylic acid) coated with a pH dependent resin (Eudragit L) as compared with sulphasalazine in patients with active mild to moderate ulcerative colitis. DESIGN: Eight week randomised double blind parallel group study. SETTING: Forty six gastroenterology outpatient clinics in seven countries. PATIENTS: Two hundred and twenty patients aged 18-70 who met the following criteria: clinical activity index greater than or equal to 6 and endoscopic index greater than or equal to 4; no concomitant treatment for ulcerative colitis; no hypersensitivity to salicylates or sulphonamides. Of the 164 patients eligible for efficacy analysis, 87 received the coated preparation of mesalazine and 77 sulphasalazine. Most of the remaining patients (28 in each group) were ineligible for the efficacy analysis because of treatment with steroid enemas. All pretrial characteristics were comparable in the two treatment groups. INTERVENTIONS: Coated mesalazine (Mesasal) 1.5 g daily or sulphasalazine 3.0 g daily for eight weeks. Compliance monitored by pill counts. END POINT: Clinical and endoscopic remission. MEASUREMENTS AND MAIN RESULTS: Clinical activity measured by daily diary cards, assessment by investigators, and laboratory findings. Endoscopic evaluation at week 8. After four weeks 50 of 70 patients (71%) taking coated mesalazine and 38 of 58 (66%) taking sulphasalazine had achieved remission of their disease by eight weeks remission rates were 74% (37/50 patients) and 81% (35/43) in the two treatment groups respectively. Endoscopic remission at eight weeks was recorded in 20 of 41 patients (49%) taking coated mesalazine and 18 of 38 (47%) taking sulphasalazine. There was a higher incidence of adverse events among patients taking sulphasalazine (25/105; 24%) than among those taking coated mesalazine (16/115; 14%). CONCLUSION: Mesalazine coated with Eudragit L is a safe, logical alternative to sulphasalazine.

Adolescent↗
PubMed1995

Comparison between high dose 5-aminosalicylic acid and 6-methylprednisolone in active Crohn's ileocolitis. A multicenter randomized double-blind study. German 5-ASA Study Group.

BACKGROUND: The value of 5-aminosalicylic acid (5-ASA) in Crohn's disease (CD) is still under discussion. In a previous study 2 g 5-ASA per day were inferior to a standard glucocorticoid treatment with 6-methylprednisolone (6-MPred) (Can J Gastroenterol 1990; 4: 446-51). In the present study we tested whether in active CD response rates to 4.5 g 5-ASA/day were not different from those to 6-MPred. METHODS: Multicenter randomized double-blind double-dummy trial. 34 patients with active CD (CDAI > 150) were included. 17 patients were in the 5-ASA group (Salofalk, 4.5 g/day), 17 patients in the 6-MPred group (Urbason, initial dose 48 mg/day, weekly tapering). Duration of treatment was 8 weeks. Main outcome measure was remission of CD (CDAI < 150) and decrease of at least 60 points. RESULTS: Both groups were comparable with respect to demographic and clinical parameters. The median CDAI decrease in the 5-ASA group was 85, in the 6-MPred group 122 (p = 0.7437). The median AUC of the CDAI in the 5-ASA group was 1027, in the 6-MPred group 950 (p = 0.137). The median AUC of the CDAI per treatment day was 22.94 in the 5-ASA group, and 17.33 in the 6-MPred group (p = 0.0555). On an intention-to-treat basis remission rates after 8 weeks were 40.0% in the 5-ASA group and 56.3% in the 6-MPred group (p = 0.5867). CONCLUSIONS: Response rates to 5-ASA or 6-MPred were not significantly different although there was a trend towards a higher efficacy of 6-MPred. 5-ASA may be considered as alternative treatment in patients with activer CD who are intolerant to or refuse glucocorticoids.

Adult↗
PubMed1986

Effect of a slow-release 5'-aminosalicylic acid preparation on disease activity in Crohn's disease.

A short-term double-blind controlled trial has been performed comparing a slow-release 5'-aminosalicylic acid (5-ASA) tablet (Pentasa) with placebo in the outpatient treatment of mild and moderate active Crohn's colitis. The disease activity was measured objectively by quantitation of the faecal excretion of 111In-labelled autologous granulocytes, which directly reflects gut inflammation. Twelve patients were randomized to receive either Pentasa or placebo. After 10 days of treatment faecal granulocyte excretion fell in all patients receiving 5-ASA, while no consistent change was found in the placebo group. These results suggest that this slow-release preparation of 5-ASA should be tested in larger controlled therapeutic trials over a longer period of time.

Adult↗
PubMed2003

Determination of 5-aminosalicylic acid in pharmaceutical formulation by differential pulse voltammetry.

The oxidative behaviour of 5-aminosalicylic acid (5-ASA) has been investigated by differential pulse voltammetry using a glassy carbon electrode in different buffer systems. Linear sweep voltammetry was used to study the influence of pH on the peak current and peak potential. The solution conditions and instrumental parameters were optimized to obtain a good sensitivity. The Britton-Robinson buffer of pH 1.81 was selected as a suitable analytical medium in which 5-ASA exhibited a sensitive diffusion controlled oxidative peak at 0.564 V (vs. Ag/AgCl). The peak current varied linearly with drug concentration in the range between 1 x 10(-4) and 2 x 10(-6) M. The proposed voltammetric method has been applied to the determination of the drug in commercial delayed-release tablet forms. A mean recovery of 101.23% with a relative standard deviation of 1.35% was obtained.

Calibration↗
PubMed2005

Colon-specific drug delivery systems based on cyclodextrin prodrugs: in vivo evaluation of 5-aminosalicylic acid from its cyclodextrin conjugates.

AIM: To investigate the release of cyclodextrin-5-aminosalicylic acid (CyD-5-ASA) in cecum and colon. METHODS: An anti-inflammatory drug 5-ASA was conjugated onto the hydroxyl groups of alpha-, beta- and gamma-cyclodextrins (CyDs) through an ester linkage, and the in vivo drug release behavior of these prodrugs in rat's gastrointestinal tract after the oral administration was investigated. RESULTS: The 5-ASA concentration in the rat's stomach and small intestine after the oral administration of CyD-5-ASA conjugate was much lower than that after the oral administration of 5-ASA alone. The lower concentration was attributable to the passage of the conjugate through the stomach and small intestine without significant degradation or absorption, followed by the degradation of the conjugate site-specific in the cecum and colon. The oral administration of CyD-5-ASA resulted in lower plasma and urine concentration of 5-ASA than that of 5-ASA alone. CONCLUSION: CyD-5-ASA conjugates may be used as prodrugs for colon-specific drug delivery system.

Animals↗
PubMed1994

5-Aminosalicylic acid in pregnancy: clinical report.

Ulcerative colitis (UC) is a disease condition which typically affects young people; pregnancy is therefore frequent in women with this disease. 5-aminosalicylic acid (5-ASA) is known to be efficacious in maintaining remission of UC, but its safety in pregnancy has not yet been established. In the present study, the safety of 5-ASA was assessed in 16 women with UC (mean age: 31 years, range 25-35) who had a total of 19 pregnancies over the period from 1988 to 1992. All the patients were in clinical remission of UC at the beginning of pregnancy and were receiving a regular maintenance therapy with 5-ASA (ASACOL tablets, 1.2 g/day). During pregnancy, 4 women had a clinical relapse requiring treatment with higher doses of 5-ASA and, in some cases, with steroids. Our observations confirm that the treatment with 5-ASA does not affect the course of pregnancy nor does it damage the fetus, but it can protect from recurrences of UC.

Adult↗