Discovery of a novel and pharmaceutically viable propylene glycol solvate of Idelalisib. (2021)

• Record Type: Journal Article
• Authors: Narasayya, Saladi Venkata; Maruthapillai, Arthanareeswari; Mahapatra, Sudarshan
• Is Part Of: Materials today. Volume 34:Part 2(2021)
• Page Start: 510
• Page End: 515
• Publication Date: 2021
• Subjects: Propylene glycol -- Solvate -- Stability -- Solubility -- Phase transformation; Materials science -- Congresses -- Periodicals; 620.1
• DOI: 10.1016/j.matpr.2020.03.103
• Languages: English
• ISSNs: 2214-7853

Abstract

Abstract: Identification of a right solid form of any active pharmaceutical ingredient (API) has become an integral part of research and development irrespective of innovator or generic companies. This is due to an increased focus on the physicochemical properties of the selected solid forms directly relating to its efficacy, safety and bioavailability. Idelalisib is a BCS class II drug with poor solubility and high permeability. Physicochemical properties of Idelalisib (API) have been modified by synthesing a propylene glycol solvate using antisolvent precipitation crystallization method. PXRD, DSC, TGA, GC and MC. Stress, hygroscopicity, characterize the prepared Propylene Glycol solvate and stability testing of novel propylene glycol solvate has shown physical and chemical stability of Idelalisib propylene glycol solvate. The obtained propylene Glycol solvate is stable for six months at 40 °C and 75% RH. The novel propylene Glycol solvate can endure pharmaceutical process pressure and it has intrinsic dissolution rate advantages over marketed Form.