Solubility Properties Of The Serotonergic Agonist 2,3,4,5-Tetrahydro-8-(Methylsulfonyl)-1h-3-Benzazepin-7-Ol

AbstractThe apparent solubility of S K & F 103829 (2, 3, 4, 5-Tetrahydro- 8-(methyl sulfonyl)-lH-3-benzazepin-7-0l) as a function of pH was determined in the presence of methane sulfonic,acetic and hydrochloric acids. The mesylate salt of S K & F 103829 was observed to be highly soluble in water (solubiity - 441.3 mg/mL). However, the addition of NaCl to solutions of the mesylate salt was observed to cause a dramatic decrease in solubility which was determined to be due to the formation of the poorly soluble hydrochloride salt (saturated solubility in water 1.0 mg/mL). when acetic acid was used in the studies. A plausible explanation for this unique solubility profie and the implication of the solubility data generated on development of a parenteral formulation is discussed.