An enema containing beclomethasone dipropionate (BDP), with a strong anti-inflammatory action and few systemic side effects, was prepared and a pharmaceutical study of this enema was performed regarding its clinical application for the treatment of ulcerative colitis patients.
The enemas were prepared by adding BDP ethanol to an aqueous solution consisting of 1% methylcellose, and this was divided into 50 ml (containing 1 mg of BDP) doses in plastic syringes. The pH, osmolarity and specific gravity of these enemas were approximately 5, 100 mOsm/kg·H20 and 1.0, respectively. The mean residual concentration of BDP in these enemas (n=6), preserved in dark under refrigeration at 4°C, declined to 93.4% after one week and 85.6% after four weeks, when compared, to the concentration determined immediately after preparation. Although the residual concentration of BDP enemas, preserved in light at 40°C, declined to 93.9% after one week and remained almost constant thereafter, the crystallization of BDP was observed the first day after preparation. Furthermore, the stability of BDP in the enemas was reduced by adjusting the pH of the enemas to 3 and 7, but it was improved by adding methyl p-hydroxybenzoate to these solutions.
These BDP enemas were administered to three patients with ulcerative colitis. An improvement was seen in all three subjects regarding both the clinical symptoms and blood data (values related to inflammatory: white blood cells and C-reactive protein). In addition, the disappearance of side effects was also confirmed after administration of BDP enemas to two of the subjects who had developed such side effects as moon face and edema with prednisolone enemas.
Based on these results, BDP enemas were thus suggested to be effective for of ulcerative colitis.