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At least 397 records · Page 22Linked to original sources
PubMed1984

Is N-acetylation of 5-aminosalicylic acid reversible in man?

In two healthy male subjects the disposition of deuterated N-(2H3) acetyl-5-aminosalicylic acid (d3-ac-5-AS) was investigated after a single rectal dose of 500 mg d3-ac-5-AS. Urine and plasma were analysed by h.p.l.c. and gas chromatography mass-spectrometry. Peak concentrations of around 0.5 microgram/ml occurred within 6 h and plasma concentrations declined thereafter with a half-life (t1/2) of about 6 h which was confirmed by urinary excretion data. Renal clearance of d3-ac-5-AS ranged between 200 and 300 ml/min and only 4.4-11.2% of the dose could be recovered in the 48 h urine. Since no undeuterated ac-5-AS could be detected in any of the plasma and urine samples an irreversible acetylation of 5-AS is assumed in man.

Acetylation↗
PubMed2002

FT-IR, FT-Raman and FT-SERS spectra of 4-aminosalicylic acid sodium salt dihydrate.

FT-IR, FT-Raman and FT-SERS spectra of 4-aminosalicylic acid sodium salt dihydrate (4ASAS) have been recorded and analysed. The vibrational bands due to NH2, OH, carboxyl group, and the benzene ring are identified. The CX ipb(17a, 17b), CC ipb(6,18a) and CH ipb (3,14a, 14b) bands are more enhanced in SERS. Broadening of the inplane carboxyl bend indicates interaction with the silver surface. Further the vC=O, v(C-O)c and v(C-O)h are intense in the SERS spectrum. The rocking and wagging modes of NH2 also show up in SERS. The molecule (O, N donor ligand) is thought to adsorb through the carboxyl oxygen atom with the benzene ring in a 'perpendicular side on orientation' with respect to the silver surface.

Aminosalicylic Acid↗
PubMed1980

A simple method for the purification of 5-aminosalicylic acid. Application of the product as substrate in enzyme-linked immunosorbent assay (ELISA).

Commercially available 5-aminosalicylic acid (5-AS) was recrystallised in the presence of Na2S2O5. A completely colourless solution was obtained when the purified product was dissolved at a concentration of 1 mg/ml in a phosphate buffer containing EDTA and H2O2. No significant increase in absorption was found upon storage for 18 h at 4 degrees C. A 8-fold increase in sensitivity of an enzyme-linked immunosorbent assay for the detection of rotavirus antigens was demonstrated by using the modified substrate solution instead of the conventional substrate solution of crude 5-AS. In addition, P/N values did not significantly change between 2 and 18 h after addition of the substrate, thus rendering the time of reading less critical. No difference in sensitivity of the assay was found between modified 5-AS solution and ortho-phenylenediamine (OPD). However, since OPD requires special care in handling the modified 5-AS solution is preferred for use in routine ELISAs.

Aminosalicylic Acids↗
PubMed2001

Pharmacokinetics of para-aminosalicylic acid granules under four dosing conditions.

OBJECTIVE: To determine the pharmacokinetics and relative bioavailability of para-aminosalicylic acid (PAS) granules. DESIGN: Phase I pharmacokinetics study. SETTING: University of Arizona School of Pharmacy. PARTICIPANTS: Sixteen healthy male and female volunteers aged 36 +/- 8 years. INTERVENTIONS: Subjects received single doses of PAS granules (6 g) combined with cycloserine 500 mg, clofazimine 200 mg, ethionamide 500 mg, and pyridoxine 100 mg. Drugs were given on an empty stomach after an overnight fast (reference) with high-fat food, with orange juice, and with antacids. MEASUREMENTS AND RESULTS: Four subjects did not complete all four treatments due to adverse events or personal reasons. Plasma and urine samples were collected for 48 hours and measured by a validated HPLC assay. Pharmacokinetic data analysis was performed with WinNonlin using noncompartmental methods and a one-compartmental model. Bioequivalence testing was performed using the mean ratios of the maximum concentrations (Cmax) and AUC(0-infinity) of PAS, with 90% confidence intervals. Compared with the fasted condition, food increased Cmax 1.5-fold and AUC(0-infinity) 1.7-fold, and it doubled the time to maximum concentration (tmax). The least-squares mean ratios (treatment/reference) for Cmax were 0.90 (58% to 139% CI), 1.16 (75% to 179% CI), and 0.82 (52% to 127% CI) with orange juice, food, or antacid treatment, respectively. Corresponding ratios for AUC(0-infinity) were 1.05 (71% to 155% CI), 1.52 (103% to 224% CI), and 0.84 (57% to 125% CI), respectively. CONCLUSIONS: Food significantly enhanced the absorption of PAS, while orange juice and antacids had minor effects.

Adult↗
PubMed2003

[5-aminosalicylic acid in the treatment of ulcerative colitis and Crohn's disease].

BACKGROUND: Ulcerative colitis and Cohn's disease are characterised by exacerbations and remissions. Their aetiology is not known and treatment modalities are therefore focused on the inflammation. MATERIAL AND METHODS: A review is given of the literature on the clinical efficacy and safety of treatment with 5-aminosalicylates. RESULTS: Aminosalicylic acid has a well-documented efficacy in the acute treatment of mild and moderate ulcerative colitis as well as in maintaining remission in these patients. Its value for patients with Cohn's disease is at the best modest. There are several possible explanations: the variability of disease location, drug disposition and topical availability of the active drug. The usefulness of aminosalicylates has been demonstrated in the long-term treatment of ulcerative colitis for the prevention of colorectal cancer. 5-aminosalicylates have side effects that are comparable with placebo. INTERPRETATION: The benefit of 5-aminosalicylic acid is well documented in the treatment of active ulcerative colitis and for maintaining remission. The opposite is seen in relation to Cohn's disease.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1987

[Unwanted side-effects in using mesalazine (5-aminosalicylic acid) during radiotherapy].

In a prospective randomized placebo controlled double blind study, the prophylactic effect of mesalazine (5-aminosalicylic acid. 5-ASA) as suppositories (3 x 250 mg/day) on radiation induced proctitis during radiotherapy for prostatic carcinoma was studied. The study ended when 16 patients had been included (5-ASA: eight, placebo: eight) because of severe side effects in the 5-ASA group. 75% of patients treated with 5-ASA reported symptoms of a severe proctitis while only one patient in the placebo group had similar complaints. The application of mesalazine as suppositories is not useful in preventing radiation induced proctitis during radiotherapy of prostate carcinoma.

Aged↗
PubMed1992

Hemolytic activity of a dental adhesive monomer (N-methacryloyloxy-5-aminosalicylic acid, MASA) and its interaction with phospholipid liposomes as studied by NMR and DSC.

N-methacryloyloxy-5-aminosalicylic acid (MASA) has recently been used as an adhesive primer in restorative resin systems. To monitor the biological activity of MASA, we studied changes in NMR-chemical shifts (delta H) and the differential scanning calorimetry (DSC) phase transition temperature (Tm) of dipalmitoylphosphatidylcholine (DPPC)/MASA liposomes with or without the presence of albumin and collagen. The delta H and the Tm did not alter significantly and the interaction of MASA with DPPC was found to be small. Hemolytic activity of MASA was markedly smaller than that of the phosphate monomer (MDP) in bonding agents widely used. These findings suggest that using a MASA primer in resin systems has an acceptable biocompatibility for dentin-pulp, involving its adsorption and adhesion to hard tooth tissues.

1,2-Dipalmitoylphosphatidylcholine↗
PubMed1996

The anti-oxidant properties of 5-aminosalicylic acid.

Oxidative damage to biological membranes is an important cause of tissue injury in inflammatory bowel disease. 5-Aminosalicylic Acid (5ASA) has therapeutic efficacy in Ulcerative colitis, which may be based on its antioxidant properties. We used Parinaric acid as a fluorescent marker of oxidation in an intestinal microvillous brush border membrane preparation. Various concentrations of the antioxidants 5ASA, ascorbate, and tocopherol were added, and oxidation was initiated from within the membrane by 2,2' azobis (2.4-dimethylvaleronitrile) (AMVN) and from solution by 2,2' azobis (2-amidinopropane) hydrochloride (AAPH). Tocopherol was able to inhibit oxidation from either source. Ascorbate was only able to inhibit oxidation initiated from solution. 5ASA was able to inhibit oxidation initiated from either site, and was more effective than tocopherol against AAPH, but similarly effective against AMVN. We postulate that water soluble 5ASA preferentially associates with membrane surface, allowing chain-breaking antioxidant activity when peroxidation is initiated within the membrane. Likewise, it is effective against aqueous oxidants because its position allows it to interact with AAPH before lipid peroxidation can be initiated as well as breaking the lipid peroxidation chain once it is initiated. This dual capacity may be important for therapeutic effect of 5ASA and may suggest other candidate antioxidants for clinical trials.

Amidines↗
PubMed1988

Comparison of delayed release 5 aminosalicylic acid (mesalazine) and sulphasalazine in the treatment of mild to moderate ulcerative colitis relapse.

Oral formulations of 5-aminosalicylic acid (mesalazine) appear less toxic than sulphasalazine. We have therefore compared sulphasalazine, low dose mesalazine and high dose mesalazine in the treatment of mild to moderate relapse of ulcerative colitis. Sixty one patients (32 men, aged 20-78 years) were randomly allocated to sulphasalazine 2 g daily, mesalazine 800 mg daily, or mesalazine 2.4 g daily in a double blind, double dummy, four week trial. Groups were comparable for age, sex, extent of disease, and pretrial sulphasalazine intake. Four patients were unable to complete the study because of treatment failure (two taking sulphasalazine and two high dose mesalazine). A further two patients taking sulphasalazine developed side effects necessitating withdrawal. Within treatment comparisons revealed significant improvement of: sigmoidoscopic grade in the sulphasalazine group; rectal bleeding, sigmoidoscopic and histological grade in the low dose mesalazine group; stool frequency, rectal bleeding and sigmoidoscopic grade in the high dose mesalazine group. Greater improvement in rectal bleeding (p less than 0.05) and sigmoidoscopic appearances (p less than 0.05) occurred in patients taking high dose mesalazine than in those taking sulphasalazine. In two patients taking high dose mesalazine minor rises of plasma creatinine concentrations occurred, suggesting the need to monitor renal function.

Adult↗
PubMed1999

Antiulcer effect of the N- and O-beta-D-glucopyranosides of 5-aminosalicylic acid.

Starting from methyl 5-nitrosalicylate (20) the N- and O-beta-glucopyranosyl derivatives (24, 28) of 5-aminosalicylic acid were prepared. The LD50 values of these compounds were determined on mice, and the inhibitory effect of 24 (0.83 mmol/kg) and 28 (1.2 mmol/kg) on gastric ulcer on rats, induced by indomethacin was investigated.

Aminosalicylic Acids↗