Colonic spreading of a non‐chlorofluorocarbon mesalazine rectal foam enema in patients with quiescent ulcerative colitis

Abstract

S U M M A R YBackground: Rectal foam enemas provide for drug delivery to the distal colon for treatment of left sided ulcerative colitis. However, currently available formulations contain chlorofluorocarbons which are due to be phased out in the near future. The objective of this study was therefore to determine the degree of dispersion of a newly developed nonchlorofluorocarbon rectal foam preparation in ulcerative colitis patients. Methods:This was an open label non-controlled study of a single administration of a mesalazine foam enema (two actuations containing 2 g of mesalazine in approximately 120 mL foam) in 10 patients with quiescent ulcerative colitis. Spreading of the 99mTclabelled foam enema was assessed over a 4-h period by the non-invasive technique of gamma scintigraphy. Results: All patients retained the enema for the full 4-h imaging period. In nine out of the 10 patients, the enema was observed to spread as far as the descending colon and on average 2 3 % of the dose was present in the descending colon at 4 h post-dose. Conclusions : The extent of spreading observed in the study supports the use of the formulation in the treatment of left sided ulcerative colitis.

Foam Preparations for the Treatment of Ulcerative Colitis

“…In an open-label non-controlled study 10 patients with quiescent UC were given 2g/120ml radiolabelled 5-ASA foam and assessed by scintigraphy over 4 hours. In 9 of 10 patients the extent of spread was at least to the descending colon and on average 23% of the dose remained present at 4 hours [7]. From these data it has been extrapolated that the physical properties of the foam including greater surface coating, mucosal adhesion, and volumetric expansion may make it a preferable delivery system compared to liquid enemas.…”

“…Scintigraphy studies using radiolabelled *Address correspondence to this author at the Inflammatory Bowel Disease Center, Section of Gastroenterology and Hepatology, Dartmouth-Hitchcock Medical Center, Lebanon, NH 03756, USA; Tel: (603) 650 8101; Fax: (603) 650 5225; E-mail: corey.a.siegel@hitchcock.org 5-ASA have consistently demonstrated that suppositories stay in the rectum, foam enemas reach the proximal sigmoid and descending colon, and liquid enemas extend to the splenic flexure [5][6][7] Fig. (1).…”

Review article: aminosalicylates for distal colitis

“…Enemas, foams and gel, thanks to their proximal spread, 5–7 should be the treatment of choice for proctosigmoiditis and left‐sided colitis. Regarding liquid enemas, the volume instilled and the viscosity of the enema seem the most important determinants of the proximal spread: a larger volume has a more consistent proximal spread 8 .…”

“…Regarding liquid enemas, the volume instilled and the viscosity of the enema seem the most important determinants of the proximal spread: a larger volume has a more consistent proximal spread 8 . Foams and gel may offer the advantage of a more prolonged retention and a more homogeneous coating of the inflamed mucosa 5, 8 . A randomized comparison of 5‐ASA foam vs. liquid 5‐ASA enemas reported that patients found foam was easier to retain and was more comfortable 9 .…”

Colonic spread and serum pharmacokinetics of budesonide foam in patients with mildly to moderately active ulcerative colitis

“…Because of the mostly small foam volume (10 mL), however, they show limited spread and therefore cover only the mucosa of the rectum and distal sigmoid colon 17, 18 . In contrast, a higher spreading capacity has been demonstrated for foams with a larger volume 19, 20 …”