title: New metastable form of glibenclamide prepared by redispersion from ternary solid dispersions containing polyvinylpyrrolidone-K30 and sodium lauryl sulfate.
abstract: Modification of polymorphic forms of poorly water-soluble drugs is one way to achieve the desirable properties. In this study, glibenclamide (GBM) particles with different polymorphic forms, including a new metastable form, were obtained from redispersion of ternary solid dispersion systems. The ternary solid dispersion systems, consisting of GBM, polyvinylpyrrolidone-K30 (PVP-K30) and sodium lauryl sulfate (SLS), were prepared by solvent evaporation method and subsequently redispersed in deionized water. The precipitated drug particles were then collected at a given time period. The drug particles with different polymorphic forms could be achieved depending on the polymer/surfactant ratio. Amorphous drug nanoparticles could be obtained by using a high polymer/surfactant ratio, whereas two different crystalline forms were obtained from the systems containing low polymer/surfactant ratios. Interestingly, a new metastable form IV of GBM with improved dissolution behavior could be obtained from the system of GBM:PVP-K30:SLS with the weight ratio of 2:2:4. This new polymorphic form IV of GBM was confirmed by differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy, powder X-ray diffractometry (PXRD) and solid state13C nuclear magnetic resonance (NMR) spectroscopy. The molecular arrangement of the new polymorphic form IV of GBM was proposed. The GBM particles with polymorphic form IV also showed an improved dissolution behavior. In addition, it was found that the formation of the new polymorphic form IV of GBM by this process was reproducible.
authors.affiliation: a Department of Manufacturing Pharmacy, Faculty of Pharmacy , Mahidol University , Bangkok , Thailand and.
authors.forename: Thanu
authors.initials: T
authors.lastname: Thongnopkoon
authors.affiliation: a Department of Manufacturing Pharmacy, Faculty of Pharmacy , Mahidol University , Bangkok , Thailand and.|b Center of Excellence in Innovative Drug Delivery and Nanomedicine, Faculty of Pharmacy, Mahidol University , Bangkok , Thailand.
authors.forename: Satit
authors.initials: S
authors.lastname: Puttipipatkhachorn
mesh_terms: D002152:Calorimetry, Differential Scanning; D003460:Crystallization; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D005905:Glyburide / Q000008:administration & dosage / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D053758:Nanoparticles / Q000737:chemistry; D011205:Povidone / Q000737:chemistry*; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D013501:Surface-Active Agents / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D012997:Solvents; D013501:Surface-Active Agents; D012967:Sodium Dodecyl Sulfate; D011205:Povidone; D005905:Glyburide
keywords: Dissolution; glibenclamide; metastable form; polymorphic form; solid dispersion