Tartaric acid pellets as a core for extended release of sildenafil citrate: development via solid dispersion and factorial design
Abstract
Abstract Introduction Pulmonary arterial hypertension (PAH) is a progressive disorder characterized by elevated pulmonary arterial pressure, causing vascular remodeling and eventual right heart failure. Sildenafil citrate (SC), a selective phosphodiesterase-5 inhibitor, used in PAH management; however, its clinical utility is limited by poor aqueous solubility and low oral bioavailability (38 - 42%). Objective This study aimed to develop an extended-release sildenafil citrate formulation using tartaric acid pellets as the core, with a solid dispersion system incorporating Soluplus® and Tween® 80 to enhance solubility and sustain release. Method A spray-drying technique was employed to prepare the solid dispersion, and a factorial design was used to optimize the formulation parameters. The optimized dispersion was layered onto inert tartaric acid and subsequently coated with 7% ethylcellulose and hypromellose (80:20) to achieve sustained drug release. Results The optimized formulation (DS03), comprising a 1:1 ratio of Soluplus®: to SC with 10% Tween® 80, increased SC solubility by 50% in FaSSIF (pH 6.5), from 0.04 to 0.06 mg/mL. Incorporation into coated tartaric acid pellets further enhanced solubility to 0.51 mg/mL, representing a 1,175% improvement over pure SC (a 12.75-fold increase). The formulation provided sustained drug release for up to 12 h, with a mean dissolution time (MDT) of 190 min, compared to less than 20 min for the immediate-release reference (Revatio®).…
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