Physicochemical and mechanical properties of paracetamol cocrystal with 5-nitroisophthalic acid

[Display omitted] 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 sol...

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Published inInternational journal of pharmaceutics Vol. 497; no. 1-2; pp. 106 - 113
Main Authors Hiendrawan, Stevanus, Veriansyah, Bambang, Widjojokusumo, Edward, Soewandhi, Sundani Nurono, Wikarsa, Saleh, Tjandrawinata, Raymond R.
Format Journal Article
LanguageEnglish
Published Netherlands Elsevier B.V 30.01.2016
Subjects
5-Nitroisophhthalic acid
Acetaminophen - chemistry
Chemical Phenomena
Cocrystal
Crystallization
Crystallography, X-Ray
Dissolution rate
Drug Liberation
Drug Stability
Mechanical Phenomena
Mechanical properties
Paracetamol
Phthalic Acids - chemistry
Solubility
Potassium dihydrogen phosphate (PubChem CID: 516951)
Sodium hydroxide (PubChem CID: 14798)
Paracetamol
5-Nitroisophthalic acid (PubChem CID: 12069)
Dissolution rate
Cocrystal
Mechanical properties
5-Nitroisophhthalic acid
API
Paracetamol (PubChem CID: 1983)
Acetonitrille (PubChem CID: 6342)
Methanol (PubChem CID: 887)
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Abstract [Display omitted] 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.
AbstractList [Display omitted] 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.
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.
Author Wikarsa, Saleh
Tjandrawinata, Raymond R.
Hiendrawan, Stevanus
Veriansyah, Bambang
Soewandhi, Sundani Nurono
Widjojokusumo, Edward
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  givenname: Sundani Nurono
  surname: Soewandhi
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  surname: Tjandrawinata
  fullname: Tjandrawinata, Raymond R.
  email: raymond@dexa-medica.com
  organization: Dexa Laboratories of Biomolecular Sciences, Cikarang 17550, West Java, Indonesia
BackLink https://www.ncbi.nlm.nih.gov/pubmed/26657269$$D View this record in MEDLINE/PubMed
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Keywords Potassium dihydrogen phosphate (PubChem CID: 516951)
Sodium hydroxide (PubChem CID: 14798)
Paracetamol
5-Nitroisophthalic acid (PubChem CID: 12069)
Dissolution rate
Cocrystal
Mechanical properties
5-Nitroisophhthalic acid
API
Paracetamol (PubChem CID: 1983)
Acetonitrille (PubChem CID: 6342)
Methanol (PubChem CID: 887)
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Snippet [Display omitted] We report novel pharmaceutical cocrystal of a popular antipyretic drug paracetamol (PCA) with coformer 5-nitroisophhthalic acid (5NIP) to...
We report novel pharmaceutical cocrystal of a popular antipyretic drug paracetamol (PCA) with coformer 5-nitroisophhthalic acid (5NIP) to improve its...
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SubjectTerms 5-Nitroisophhthalic acid
Acetaminophen - chemistry
Chemical Phenomena
Cocrystal
Crystallization
Crystallography, X-Ray
Dissolution rate
Drug Liberation
Drug Stability
Mechanical Phenomena
Mechanical properties
Paracetamol
Phthalic Acids - chemistry
Solubility
Title Physicochemical and mechanical properties of paracetamol cocrystal with 5-nitroisophthalic acid
URI https://dx.doi.org/10.1016/j.ijpharm.2015.12.001
https://www.ncbi.nlm.nih.gov/pubmed/26657269
https://search.proquest.com/docview/1753230506
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