Pharmaceutical suspensions of ursodeoxycholic acid for pediatric patients: in vitro and in vivo studies. (28th May 2021)

• Record Type: Journal Article
• Authors: Boscolo, Oriana; Salvo, Leandro; Dobrecky, Cecilia; Fissore, Eliana N.; Buontempo, Fabian; Tripodi, Valeria; Lucangioli, Silvia E.
• Is Part Of: Pharmaceutical development and technology. Volume 26:Number 5(2021)
• Page Start: 599
• Page End: 609
• Publication Date: 2021-05-28
• Subjects: Bioavailability -- formulation vehicle -- pediatric patients -- physicochemical stability -- poorly water-soluble drug -- rheology; Drug delivery systems -- Periodicals; Pharmaceutical technology -- Periodicals; Drugs -- Administration -- Research -- Periodicals; Drug Delivery Systems -- Periodicals; Pharmaceutical Preparations -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615
• DOI: 10.1080/10837450.2021.1905662
• Languages: English
• ISSNs: 1083-7450

Abstract

Abstract: Ursodeoxycholic acid (UDCA) is used in the oral therapy of hepatobiliary cholestatic diseases. Due to UDCA low aqueous solubility, two pediatric oral suspensions (25 mg/mL) were formulated with a few excipients, suspension A (SA) and suspension B (SB) with a vehicle, including two suspending agents. Physical, chemical and microbiological stability and a rheological study were performed at three different conditions (5 °C ± 3 °C, 25 °C ± 2 °C/60% RH ± 5% RH and 40 °C ± 2 °C/75% RH ± 5% RH) for 120 days. Moreover, dissolution study, content uniformity, related substances, and a study of relative oral bioavailability were also carried out. Both suspensions were physically, chemically and microbiologically stable throughout the study. SA and SB can be stored at 25 °C and 5 °C for at least 120 days whereas SA can be kept at 40 °C for at least 90 days and SB for 120 days. They both met USP specifications for dissolution, content uniformity, and related substances. SA and SB showed an improved relative oral bioavailability compared to the solid dosage form and they both displayed similar relative oral bioavailability with no significant differences between them. The developed suspensions proved to be safe and adequate and they are ideal for pediatric use for their acceptability, accurate dose administration and treatment adherence.