title: Physicochemical and mechanical properties of paracetamol cocrystal with 5-nitroisophthalic acid.
abstract: We report novel pharmaceutical cocrystal of a popular antipyretic drug paracetamol (PCA) with coformer 5-nitroisophhthalic acid (5NIP) to improve its tabletability. The cocrystal (PCA-5NIP at molar ratio of 1:1) was synthesized by solvent evaporation technique using methanol as solvent. The physicochemical properties of cocrystal were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetry analysis (TGA), fourier transform infrared spectroscopy (FTIR), hot stage polarized microscopy (HSPM) and scanning electron microscopy (SEM). Stability of the cocrystal was assessed by storing them at 40°C/75% RH for one month. Compared to PCA, the cocrystal displayed superior tableting performance. PCA-5NIP cocrystal showed a similar dissolution profile as compared to PCA and exhibited good stability. This study showed the utility of PCA-5NIP cocrystal for improving mechanical properties of PCA.
authors.affiliation: Dexa Laboratories of Biomolecular Sciences, Cikarang 17550, West Java, Indonesia; School of Pharmacy, Bandung Institute of Technology, Bandung 40132, West Java, Indonesia.
authors.forename: Stevanus
authors.initials: S
authors.lastname: Hiendrawan
authors.affiliation: Dexa Laboratories of Biomolecular Sciences, Cikarang 17550, West Java, Indonesia.
authors.forename: Bambang
authors.initials: B
authors.lastname: Veriansyah
authors.affiliation: Dexa Laboratories of Biomolecular Sciences, Cikarang 17550, West Java, Indonesia.
authors.forename: Edward
authors.initials: E
authors.lastname: Widjojokusumo
authors.affiliation: School of Pharmacy, Bandung Institute of Technology, Bandung 40132, West Java, Indonesia.
authors.forename: Sundani Nurono
authors.initials: SN
authors.lastname: Soewandhi
authors.affiliation: School of Pharmacy, Bandung Institute of Technology, Bandung 40132, West Java, Indonesia.
authors.forename: Saleh
authors.initials: S
authors.lastname: Wikarsa
authors.affiliation: Dexa Laboratories of Biomolecular Sciences, Cikarang 17550, West Java, Indonesia. Electronic address: raymond@dexa-medica.com.
authors.forename: Raymond R
authors.initials: RR
authors.lastname: Tjandrawinata
mesh_terms: D000082:Acetaminophen / Q000737:chemistry*; D055598:Chemical Phenomena; D003460:Crystallization; D018360:Crystallography, X-Ray; D065546:Drug Liberation; D004355:Drug Stability; D055595:Mechanical Phenomena; D010795:Phthalic Acids / Q000737:chemistry*; D012995:Solubility
chemical_list: D010795:Phthalic Acids; D000082:Acetaminophen; C527944:5-nitroisophthalic acid
keywords: 5-Nitroisophhthalic acid; 5-Nitroisophthalic acid (PubChem CID: 12069); Acetonitrille (PubChem CID: 6342); Cocrystal; Dissolution rate; Mechanical properties; Methanol (PubChem CID: 887); Paracetamol; Paracetamol (PubChem CID: 1983); Potassium dihydrogen phosphate (PubChem CID: 516951); Sodium hydroxide (PubChem CID: 14798)