Pharmaceutics · 2018 · 34 citations · 23 references
PharmacyPharmaceuticsPharmacologyBioavailabilityDrug DeliveryPharmaceutical FormulationDrug Delivery SystemsDrug FormulationDrug SolubilityPh-responsive Drug DeliverySelf-emulsifying Drug Delivery SystemsSolubility EnhancementAqueous Solubility ImprovementDissolution-induced Drug ReleaseDrug Dissolution KineticsPh OptimaPh-dependent Drug SolubilitySolubilitySolubility - Dissolution RelationshipSupersaturating Drug Delivery Systems
Raloxifene hydrochloride (RLH) was formulated into a pH-modified supersaturatable self-microemulsifying drug delivery system (S-SMEDDS) to increase drug solubility and dissolution rate. Optimal formulations of pH-modified S-SMEDDSs were developed by incorporating hydroxypropyl-cellulose-L as a precipitation inhibitor and phosphoric acid as a pH modifier (an acidifier). RLH was dissolved to greater extents by all pH-modified S-SMEDDSs compared with non-pH-modified S-SMEDDSs. In particular, phosphoric acid afforded greater drug dissolution than did the other acidifiers tested, perhaps because phosphoric acid better controlled the pH. More than 50% of the RLH was released from the pH-modified S-SMEDDS at pH 2.5 compared with only ~5% of the drug into aqueous buffer (pH 1.2 or 6.8) after dissolution of a conventional tablet. pH-modified S-SMEDDSs with a hydrophilic polymer and phosphoric acid improved the dissolution behavior of a drug exhibiting poor aqueous solubility.
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Crystallization of hydrocortisone acetate: influence of polymers
S. Raghavan, A Trividic, A.F Davis et al. · International Journal of Pharmaceutics · 2001 · 402 citations