The Role And Importance Of Solid Dispersions In Improving The Bioavailability Profile Of Drugs
Poor aqueous solubility
remains a significant barrier to the bioavailability and therapeutic efficacy
of many active pharmaceutical ingredients (APIs). Solid dispersion (SD)
technology has emerged as a promising formulation strategy to overcome this
limitation by converting crystalline APIs into amorphous forms, thereby
enhancing dissolution rates and systemic absorption. SDs are classified into
four generations based on formulation complexity, ranging from simple eutectic
mixtures to advanced polymer-surfactant systems offering controlled release.
Preparation methods such as melting, solvent evaporation, spray drying, freeze
drying, hot-melt extrusion, supercritical fluid processing, and Kinetisol®
play a critical role in determining the physicochemical stability and
performance of the final product. Each technique offers distinct advantages
depending on the thermal and chemical properties of the API and excipients.
Despite demonstrated improvements in solubility and pharmacokinetic profiles,
commercial application of SDs remains limited due to scalability and stability
challenges, particularly regarding recrystallization of amorphous forms. Recent
advances, especially solvent-free and high-energy technologies like Kinetisol®,
offer significant potential to address these issues. Overall, SD technology is
considered an effective approach to improve the oral bioavailability of poorly
water-soluble drugs and increase patient compliance, and is gaining increasing
importance in the development of dosage forms.
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