02137nas a2200217   4500008004100000245016400041210006900205260000800274300001400282490000700296520127000303100003101573700002301604700002601627700002601653700002101679700002501700700003301725700003001758856013101788       2022                        eng d00aNovel pharmaceutical cocrystal of apalutamide, a nonsteroidal antiandrogen drug: synthesis, crystal structure, dissolution, stress, and excipient compatibility0 aNovel pharmaceutical cocrystal of apalutamide a nonsteroidal ant  cJAN  a1130-11420 v223 aApalutamide (APA), a second-generation nonsteroidal antiandrogen BCS Class II drug with poor solubility and high permeability. A novel 1:1 cocrystal of Apalutamide (APA) with methylparaben (MP) was identified by cooling crystallization during the cocrystal screening and characterized by various solid-state techniques, such as PXRD, DSC, TGA, FT-IR, and 13C solid-state CP-MAS NMR spectroscopy. The crystal structures of APA and its cocrystal (APA-MP) were determined by the SC-XRD technique. The crystal structure analysis of the APA-MP cocrystal revealed that the APA and MP molecules are connected through strong O–H···O hydrogen bonds. The novel cocrystal improves the solubility and dissolution rate in different physiological conditions compared to poorly soluble APA due to strong hydrogen bond between the drug and the coformer. The cocrystal is stable (physically and chemically) under stress conditions, such as exposure to the relative humidity, mechanical grinding, open exposure to atmosphere at cRT (critical room temperature) and compression pressure of 10 tons. In addition, the compatibility of the cocrystal with excipients used in the drug product of APA (ERLEADA) was also investigated, and no disproportionation of cocrystal was observed.1 aSaladi, Venkata, Narasayya1 aKammari, Bal, Raju1 aMandad, Pratap, Reddy1 aKrishna, Gamidi, Rama1 aSajja, Eswaraiah1 aThirumali, Rajan, S.1 aMarutapilli, Arthanareeswari1 aMathad, Vijayavitthal, T.  uhttps://library.ncl.res.in/content/novel-pharmaceutical-cocrystal-apalutamide-nonsteroidal-antiandrogen-drug-synthesis-crystal