ArticlesEffect of Vehicle Amphiphilicity on the Dissolution and Bioavailability of a Poorly Water-Soluble Drug from Solid Dispersions
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2021, Journal of Pharmaceutical SciencesCitation Excerpt :One major reason for incomplete drug release from ASD is that once the water-soluble carrier starts dissolving from near the surface, the liberated water-insoluble drug coats the surface of particles or dosage units, preventing further dissolution of drug from the interior.57 Such a surface coating of ASDs by the water-insoluble drug may be avoided if a surface active carrier is used58 or a surfactant is added to the formulation as the surfactant would facilitate dispersion of the liberated drug in dissolution media.63 It is apparent from the results of dispersion testing presented in Fig. 5 that the possible surface coating by relatively water-insoluble ritonavir might not be a major issue in the release of drugs containing PVPVA as the polymeric carrier, since 80–90% of drug either dissolved or dispersed as fine particles in the aqueous phase even when no additional surfactant was present in the formulation.
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2019, Journal of Pharmaceutical SciencesCitation Excerpt :Lesser hydrophilic P407 and TPGS with the low HLB values of 22 and 13, respectively, provided progressively higher dissolution rates. Serajuddin et al.64,65 reported that water-insoluble liquid or amorphous layers of poorly water-soluble drugs are formed on the surface of solid dispersions during dissolution, thus blocking further release from inside the ASD pellets or particles, and the presence of surfactants in ASDs prevents the formation of such layers by emulsifying or suspending the liberating drug. It is apparent in the present investigation that the lower HLB value of surfactants favors more efficient removal of drug from the dissolving surface.