Ursodeoxycholic Acid for Oral Administration: A Formulatory Study of a Suspension

Ursodeoxycholic acid (UDCA), a hydrophilic bile acid effective in dissolving cholesterol gallstones, is usually administered by capsules and tablets. However, oral solid dosage forms are generally inadequate for pediatric needs, since, in order to individualize the preparations, hospitals have to prepare, from capsules, doses corresponding to age and weight of the children. Aim of the present paper was to produce and characterize UDCA suspensions for a personalized regimen of therapy. Four different suspensions were prepared by dissolving preservatives, sodium chloride sweeteners and/or rheology modifiers in hot pure water. After cooling 2.5% (w/v) of UDCA powder was added. After production the formulations were subjected to UDCA content analysis by HPLC, rheological measurements and stability test. The physical and chemical stability of UDCA containing suspensions were investigated for 28 days after production. For physical stability the rate of sedimentation, the height of the sediment and the ease of redispersion, were measured. Particularly, the sedimentation volumes of the four suspensions were between 88 and 95%. The results demonstrated that all UDCA suspensions are characterized by good chemical stability (nominal concentration over 96%). The results indicated that suspensions could be proposed as alternative formulations for the pediatric administration of UDCA.