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Disposition of 5-Aminosalicylic Acid by Olsalazine and Three Mesalazine Preparations in Patients with Ulcerative Colitis

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Disposition of 5-Aminosalicylic Acid by Olsalazine and Three Mesalazine Preparations in Patients with Ulcerative Colitis Gut, 1990, 31, 1271-1276 1271 Disposition of5-aminosalicylic acid by olsalazine and Gut: first published as 10.1136/gut.31.11.1271 on 1 November 1990. Downloaded from three mesalazine preparations in patients with ulcerative colitis: comparison of intraluminal colonic concentrations, serum values, and urinary excretion L Sterk Laursen, M Stokholm, K Bukhave, J Rask-Madsen, K Lauritsen Abstract foundation of rational pharmacotherapy with To compare the disposition of5-aminosalicylic this drug, whether it depends on the activity of acid (5-ASA) and its acetylated metabolite bacterial azoreductases or the physicochemical during treatment with olsalazine and mesala- properties of the drug. Thus, knowledge of the zine, 14 patients with inactive ulcerative colitis disposition is mandatory for exploring dose were randomly assigned to olsalazine (1 g twice response effects, in addition to being ofpotential daily) and the mesalazines, Asacol (800+400+ toxicological interest. The purpose ofthe present 800 mg daily), Pentasa (750+500+750 mg study was, therefore, to compare the efficiency of daily), and Salofalk (750+500+750 mg daily) in delivery of the active principle 5-ASA to the a crossover design trial so that all received colon and the systemic load as a basis for each drug for seven days. Intraluminal colonic potential long term toxicity during treatment concentrations of 5-ASA were estimated after with olsalazine and three controlled release five days by the method of equilibrium in vivo mesalazine preparations (Asacol, Pentasa, and dialysis offaeces. A predose serum sample and Salofalk) in patients with inactive ulcerative a 24 hour urine collection were obtained on day colitis. seven. The 5-ASA and acetyl-5-aminosalicylic acid (Ac-5-ASA) values were determined by high performance liquid chromatography. Methods Olsalazine almost doubled the colonic concen- trations (mean 23*7 (SEM) (1.9) mmol/l) of its PATIENTS therapeutically active ingredient (5-ASA) com- Fourteen patients with ulcerative colitis in http://gut.bmj.com/ pared with equimolar doses of Pentasa (12.6 remission took part in the study (Table I). Apart (2.2) mmol/l; p<0.0003) and Salofalk (15.0 from the study drugs, and in some cases oral (2.0) mmol/l; p<0003). At the same time, contraceptives, no medication was given during olsalazine treatment was associated with lower the study. The diagnosis of ulcerative colitis had serum concentrations and urinary excretions previously been established on the basis of (p<005) of 5-ASA and Ac-5-ASA compared symptoms, sigmoidoscopic appearance, histo- with the mesalazine preparations. The low logy of the rectal mucosa, and radiologic appear- on September 24, 2021 by guest. Protected copyright. systemic load of 5-ASA provided by olsalazine ance. 8 Patients were considered in remission reduces the potential risk of nephrotoxicity when they were symptom free - that is, stool during long term treatment. frequency less than two a day, no discharge of blood, pus, or mucus from the rectum, normal sigmoidoscopic appearance, and no appreciable Department of Medical Since it became clear that 5-aminosalicylic acid inflammation seen on rectal biopsy specimen. Gastroenterology, (5-ASA) is the therapeutically active moiety of Each participant gave informed consent. The Odense University Hospital, Odense, sulphasalazine in treating ulcerative colitis and study was done in accordance with the Helsinki Denmark that sulphapyridine simply acts as a carrier to Declaration II and was approved by the regional L Sterk Laursen ensure that the active part is released within the ethics committee. M Stokholm K Lauritsen bowel,' 2 a 'second generation of sulphasalazine' Before entry and on each study day laboratory has emerged.3 Orally ingested plain 5-ASA is screening was done. This included blood haemo- Department of rapidly and completely absorbed from the upper globin concentration, reticulocyte count, Biochemistry and Nutrition, The Technical gastrointestinal tract.' By contrast, it is poorly erythrocyte sedimentation rate, leucocyte count, University of Denmark, absorbed in the colon, where it probably acts leucocyte differential count, platelet count, Copenhagen, Denmark from the luminal side.47 Independent of serum concentrations of Na, K, Ca, albumin, K Bukhave acetylator phenotype, 5-ASA is subsequently orosomucoid, creatinine, urea, alanine amino- Department of acetylated, mainly in the gut wall,8-0 to N-acetyl- Gastroenterology G, 5-aminosalicylic acid (Ac-5-ASA). This meta- Bispebjerg Hospital, bolite is considered to be therapeutically inert." TABLE I Patients' details University of A number of 5-ASA Copenhagen, Denmark delivery systems has, Sex, male/female 7/7 J Rask-Madsen therefore, been developed. These are either Age (yrs), mean (range) 44 (25-69) Correspondence to: sulphapyridine-free azobond analogues of Height (cm), mean (range) 169 (152-191) Dr K Lauritsen, Department Weight (kg), mean (range) 74(53-97) of Medical Gastroenterology, sulphasalazine, such as olsalazine,'2 13 or enteric Duration ofdisease (yrs), mean (range) 9 (2-17) Odense University Hospital, coated (delayed release) or slow release 5-ASA Duration of remission (mths), mean (range) 16(1-50) DK-5000 Odense C, Location ofdisease: Denmark. (mesalazine) preparations, such as Asacol,'4 Proctosigmoiditis 7 Left sided colitis 4 Accepted for publication Pentasa,'6 and Salofalk.'7 Pancolitis 3 18 December 1989 Control of the disposition of 5-ASA is the 1272 StErk Laursen, Stokholm, Bukhave, Rask-Madsen, Lauritsen transferase, lactate dehydrogenase, alkaline water during each treatment period after five phosphatase, bilirubin, and plasma prothrom- days using the method of equilibrium in vivo Gut: first published as 10.1136/gut.31.11.1271 on 1 November 1990. Downloaded from bin, in addition to urine analyses for protein and dialysis of faeces (see below). Faeces were glucose and microscopy for erythrocytes, leuco- collected until the dialysis bags had been cytes, and casts. recovered and the stool output was quantified. The 24 hour faecal excretion of 5-ASA and Ac-5- ASA was estimated as the 24 hour stool outputx FORMULATION OF OLSALAZINE AND MESALAZINE concentration in free faecal waterx0x 8 (this Olsalazine (disodium azodisalicylate; Dipentum; fraction20 being used to approximate free faecal Pharmacia AB, Uppsala, Sweden), which is one water). On day seven, a morning predose serum molecule of 5-ASA diazotised to another, was sample and a 24 hour urine collection were provided either in enteric coated tablets contain- obtained for determination of 5-ASA and Ac-5- ing 500 mg of the drug or in gelatin capsules, ASA and for calculation of their 24 hour urinary each of which contained 250 mg of the drug.'2 excretions. Olsalazine has been shown to be poorly absorbed Patient compliance was checked after each from the small intestine and reaches the colon treatment period by counting the amount of intact,'9 where it is activated into two molecules unused study drug. A diary had been pro- of 5-ASA. 12 vided for recording the number of bowel move- Asacol (Tillotts Laboratories, Henlow, UK) ments, the presence or absence of blood, and was provided as tablets containing 400 mg of 5- unexpected events, ifany. ASA coated by a 120 pim thick acrylic based Olsalazine enteric coated tablets versus olsalazine resin (Eudragit S). Asacol has been designed to capsules. After the above four treatment periods disintegrate at a pH above 7, and most has been had been completed the patients were assigned in shown to break up in the terminal ileum or the random order to each of two olsalazine formula- ascending colon.'5 tions for 21 days: 500 mg enteric coated tablets, Pentasa (Ferring A/S, Copenhagen, Den- one tablet in the morning and one in the evening mark) was provided as tablets containing 250 mg and 250 mg gelatin capsules, two capsules in the of 5-ASA in microgranules coated with a semi- morning and two in the evening. At the end of permeable membrane of ethylcellulose. 16 each study period in vivo dialysis of faeces, the Because of the amphoionic properties of ethyl- quantity of stool output, a morning predose cellulose, 5-ASA is slowly released from the serum sample, and a 24 hour urine collection granules into the intestine continuously over were obtained for analyses and calculations as time, but enhanced with pH above 6.'6 described above. Furthermore, the serum Salofalk (Dr Falk GmbH & Co, Freiburg, samples were analysed for olsalazine and olsala- FRG; in some countries marketed as Claversal or zine sulphate. http://gut.bmj.com/ Mesasal) was provided as tablets containing 250 mg of 5-ASA in a buffer system of sodium- carbonate and glycine protected by ethyl- EQUILIBRIUM IN VIVO DIALYSIS OF FAECES cellulose and an outer coating of the resin In vivo dialysis of faeces was done as previously Eudragit-L.'7 Salofalk has been shown to break described in detail'3 by pooling the contents of up at pH above 5 5, delivering its contents five swallowed dialysis bags after their intestinal mainly to the distal part of the ileum and the transit (faecal dialysates). The bags had been on September 24, 2021 by guest. Protected copyright. colon. made by tying off 4 cm segments of Visking seamless cellulose tubing 8/32 filled with Rheomacrodex (Pharmacia) containing 10% EXPERIMENTAL DESIGN dextran (mean mol wt 40000) in saline. The Olsalazine versus mesalazine. In the first part of faecal dialysates were stored immediately at the study olsalazine was compared with each of -20°C. The samples were analysed for concen- the three mesalazine preparations - Asacol, trations of5-ASA, Ac-5-ASA, and olsalazine (the Pentasa, and Salofalk. A crossover design was latter only performed on samples obtained applied. According to a computer generated during the two three week regimens on olsala- randomisation list, all patients received each of zine). The validations to ensure that these the following regimens in random order for compounds had reached an equlibrium have seven days: previously been described.
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