Study on Mechanism for Amorphous Drug Stabilization Using Gelucire 50/13

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概要

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• Methods of preparation and application of amorphous form are well established but it is equally important to note that devitrification of amorphous drugs has limited their applications. Present study was performed to investigate mechanism for amorphous drug stabilization using Gelucire in comparison with polyvinylpyrrolidone (PVP). Etoricoxib and celecoxib were taken as model drugs for this study, as etoricoxib has only proton accepting site for hydrogen bonding in comparison with celecoxib, which has both proton accepting and donating site. Solid dispersion of celecoxib with polyvinylpyrrolidone and Gelucire was prepared by spray drying and melt-granulation technique respectively. X-ray powder diffractometry and differential scanning calorimetry were used to study the physical state of the drug. Dissolution studies were performed to differentiate dissolution performance. Stability study samples were evaluated for physical state of the drug and dissolution performance. An IR study in correlation with molecular modeling was carried out to study the mechanism for stabilization. Dissolution of melt-granulation of amorphous celecoxib was improved significantly as compared to amorphous celecoxib and Celecoxib-PVP solid dispersion. Melt-granulation with lipid seemed to be more dominant than amorphization of drug for improving dissolution. Stability data revealed that PVP was significantly advantageous for amorphous form stabilization whereas Gelucire failed in case of Celecoxib. In contrast to this, our previous study revealed the stabilization ability of Gelucire for amorphous etoricoxib. Molecular modeling and IR studies revealed that H-bonding was predominant mechanism for stabilization. Out of two proposed mechanism for amorphous drug stabilization by lipids, H-bonding ability is more dominant than immobilization of molecule in lipid matrix.

著者

• Shimpi Shamkant

  Formulation Research Division, APL Research Centre, Aurobindo Pharma Ltd.

• Mahadik Kakasaheb

  Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy

• Paradkar Anant

  Institute of Pharmaceutical Innovation, and IRC in Polymer Science and Technology, University of Bra

• Mahadik Kakasaheb

  Department Of Pharmaceutics Bharati Vidyapeeth University Poona College Of Pharmacy

関連論文

• Study on Mechanism for Amorphous Drug Stabilization Using Gelucire 50/13
• Application of Polyglycolized Glycerides in Protection of Amorphous Form of Etoricoxib during Compression

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