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Results for “AMINOSALICYLIC ACID”

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At least 505 records · Page 28Linked to original sources
PubMed2004

Fluorescence spectroscopy studies on 5-aminosalicylic acid and zinc 5-aminosalylicylate interaction with human serum albumin.

The interaction between 5-aminosalicylic acid (5-ASA) or zinc 5-aminosalylicylate (5-ASZ) and human serum albumin (HSA) was studied by fluorescence spectroscopic technique. The binding constants of 5-ASA or 5-ASZ with HSA were determined at different temperatures under the optimum conditions. The binding sites were obtained and the acting force were suggested to be mainly hydrophobic. The effect of common ions on the binding constants was also investigated. A fluorescence spectroscopy assay of the proteins is presented in the paper. The determination results of the proteins in human serum by this method are very close to those obtained using Coomassie Brilliant Blue G-250 colorimetry, with relative standard deviations of 0.8-2.9%. A practical method was proposed for the determination of 5-ASA or 5-ASZ in human serum samples.

Humans↗
PubMed2003

Dendrimers conjugates for colonic delivery of 5-aminosalicylic acid.

The water-soluble polyamidoamine (PAMAM) dendrimer conjugates for colonic delivery of 5-aminosalicylic acid (5-ASA) were designed. The drug was bound to the dendrimer using two different spacers containing azo-bond, p-aminobenzoic acid (PABA) and p-aminohippuric acid (PAH). Incubation of PAMAM dendrimer conjugates containing PABA and PAH spacers with rat cecal contents at 37 degrees C gradually released 5-ASA with time and the amount of drug released was 45.6 and 57.0% of the dose in 24 h, respectively. The release of the drug from the commercial prodrug, sulfasalazine was significantly faster than both conjugates (80.2% of the dose in 6 h). No 5-ASA was detected from the incubation of dendrimer conjugates with the homogenate of the stomach or phosphate buffer, pH 1.2 and 6.8. Only a small amount of 5-ASA was found after incubation of both conjugates with the homogenate of the small intestine for 12 h. It appears that this PAMAM dendrimer can be developed for use as a carrier for colon-specific drug delivery.

4-Aminobenzoic Acid↗
PubMed1994

Effectiveness of 5-aminosalicylic acid for maintaining remission in patients with Crohn's disease: a meta-analysis.

OBJECTIVES: We conducted a meta-analysis of the published randomized clinical trials to evaluate the effectiveness of 5-aminosalicylic acid (5-ASA) for maintaining remission in inactive Crohn's disease. METHODS: The trials were identified by standard computerized techniques for literature search. All studies included in the meta-analysis were aimed at evaluating the effectiveness of 5-ASA in comparison with a control group receiving either no treatment or placebo. RESULTS: Our meta-analysis of five clinical trials published as full-length articles indicates that 5-ASA significantly reduces the relapse frequency in patients with inactive Crohn's disease [odds-ratios (95% CI): 0.56 (0.37-0.84) at 6 months, 0.47 (0.33-0.67) at 12 months, 0.53 (0.38-0.73) at 24 months]. The pooled relapse-free rates in the treatment group were 91% at 6 months, 84% at 12 months, and 72% at 24 months; the corresponding rates in the control group were 77%, 60%, and 52%. A second meta-analysis, conducted using the additional information deriving from four randomized trials published as abstracts, gave essentially the same results. CONCLUSIONS: Whereas our meta-analysis shows that the effectiveness of 5-ASA is statistically significant, a simple pharmacoeconomic assessment indicates that the cost for preventing each relapse can lie between $4,000 and $10,000. This cost compares favorably with the average cost for treating a relapse.

Aminosalicylic Acids↗
PubMed1992

Oral 5-aminosalicylic acid (Asacol) in the maintenance treatment of Crohn's disease.

A randomized, placebo-controlled multicenter trial was conducted to evaluate the efficacy and safety of a delayed-release formulation of 5-aminosalicylic acid (5-ASA) (Asacol; Giuliani & Bracco, Milan, Italy) for prevention of clinical relapse in 125 patients with inactive Crohn's disease. Patients in remission [Crohn's Disease Activity Index (CDAI) less than 150] between 3 months and 2 years were randomly allocated to receive either 800 mg 5-ASA three times daily (n = 64) or placebo (n = 61) for up to 12 months or until relapse of symptoms. Relapse was defined by a CDAI greater than 150, with a minimum increase of 100 points over the baseline value. The cumulative relapse rates were 12% in the 5-ASA group and 22% in the placebo group at 3 months [95% confidence interval (CI) for the difference, -4 to 24]; 28% and 41%, respectively, at 6 months (95% CI, -4 to 30); and 34% and 55%, respectively, at 12 months (95% CI, 3-39; P = 0.02, log rank test). Significant decrease in the risk of relapse was found in patients with ileitis, in those with previous bowel resection and, in those with prolonged prestudy remission. Eight patients (5 on 5-ASA, 3 on placebo) withdrew from the study because of adverse reactions, but no major clinical or laboratory adverse effect was observed. It is concluded that oral 5-ASA coated with Eudragit S (Rohn Pharma GmbH, Wieterstadt, Germany), 2.4 g daily, is safe and seems superior to placebo in preventing or delaying clinical relapse in Crohn's disease, especially in milder cases and in ileal disease.

Adolescent↗
PubMed1985

Determination of the pK values of 5-aminosalicylic acid and N-acetylaminosalicylic acid and comparison of the pH dependent lipid-water partition coefficients of sulphasalazine and its metabolites.

Sulphasalazine (SASP), used in the treatment of inflammatory bowel disease, is split into sulphapyridine (SP) and 5-aminosalicylic acid (5-ASA) in the colon. Lower plasma levels of SASP and 5-ASA as compared to those of SP may be due to different absorption rates from the colon because of different pK values and pH dependent lipid-water partition coefficients. In this study we determined the pK values of 5-ASA and its major metabolite, N-acetyl amino-salicylic acid (AcASA), by 13C-NMR spectroscopy and compared the pH dependent apparent benzene-water partition coefficients (Papp) of SASP, SP and 5-ASA with respect to their different plasma levels. The COOH group of 5-ASA had a pK value of 3.0, the -NH3+ group had 6.0, the -OH group 13.9; the -COOH group of AcASA had 2.7 and the -OH group 12.9; The Papp of SASP (0.042 +/- 0.004) and 5-ASA (0.059 +/- 0.01) were significantly lower than that of SP (0.092 +/- 0.03) (at pH 5.5).

Aminosalicylic Acids↗
PubMed2006

Colon-specific delivery tablets of sodium 4-aminosalicylic acid.

AIM: To prepare a new oral colon-specific delivery formulation and to investigate the release profile in vitro and the colon-specific delivery property in vivo in dogs. METHODS: Sodium 4-aminosalicylic acid was selected as the model drug. The combination of Eudragit RL30D and RS30D were used as sustained-release film, and Eudragit FS30D used as enteric film, which was expected to release drug depending on pH and time. The release profile of tablets was studied in three phosphate buffers with the pH 6.5, 7.0 or 7.4 for 12 h after a simulated gastric presoak for 2 h in 0.1 mol x L(-1) HCl. The tablets were radiolabelled with 99mTc to make their release times and positions in the gastrointestinal tract be followed using a gamma camera. RESULTS: For the in vitro study, there was no drug released in 0.1 mol x L(-1) HCl for 2 h, and release occurred slowly when pH was above 6.5. Drug was released faster while pH was higher. For the in vivo study, the coated tablets remained intact in the upper gastrointestinal tract, and drug release began after the colonic arrival. The uncoated tablets, however, disintegrated in the stomach of the dogs rapidly. CONCLUSION: The coating could protect the drug until the tablets reached the ascending colon, where drug was released slowly for over 10 h.

Acrylic Resins↗
PubMed1993

A randomized trial to assess the efficacy of 5-aminosalicylic acid for the prevention of radiation enteritis.

Sulphasalazine is an effective treatment for diarrhoea occurring during pelvic radiotherapy. We report the results of a trial to assess the value of its active moiety, 5-aminosalicylic acid, (5-ASA) in a prophylactic setting. Seventy-three patients planned for external beam radiotherapy to the pelvis were randomized on a double-blind basis to receive prophylactic 5-ASA or placebo. The severity of the acute radiation bowel reaction was documented by a weekly questionnaire. Surprisingly, diarrhoea occurred in a higher proportion of patients in the 5-ASA arm than the placebo arm (91.2% versus 73.7%, P = 0.070). The maximum change in both the severity of diarrhoea and the number of days per week on which diarrhoea occurred (from pre-radiotherapy level to the worst level at any time during treatment) were both significantly greater in patients taking 5-ASA than those taking placebo (P = 0.014 and P = 0.026, respectively). The average change (the sum of the weekly scores divided by the number of weeks of treatment, minus the pre-radiotherapy score) for both severity and days per week of diarrhoea were again greater in the 5-ASA than the placebo arm, but failed to reach statistical significance (P = 0.095 and P = 0.079, respectively). The use of anti-diarrhoeal medicines was significantly greater in the 5-ASA arm (P = 0.011). Constipation was more common in the placebo arm but this did not reach significance (P = 0.20). 5-ASA thus has no protective effect against acute radiation enteritis and appears to worsen it. Possible reasons for this surprising finding are discussed.

Aminosalicylic Acids↗