Fluconazole-tartaric acid co-crystal formation and its mechanical properties

被引:2
作者
Alatas, Fikri [1 ]
Suwartiningsih, Nia [1 ]
Ratih, Hestiary [1 ]
Sutarna, Titta Hartyana [1 ]
机构
[1] Univ Jenderal Achmad Yani, Fac Pharm, Jalan Terusan Jenderal Sudirman, Cimahi, Indonesia
来源
PHARMACY EDUCATION | 2021年 / 21卷 / 02期
基金
英国自然环境研究理事会;
关键词
Flowability; Fluconazole; Tartaric acid; Mechanical properties; Ultrasound-assisted solution co-crystallisation (USSC); Tabletability; SOLID-STATE CHARACTERIZATION; SPHERICAL CRYSTALLIZATION; TABLETING PROPERTIES; COCRYSTAL; COMPRESSIBILITY; FLOWABILITY; DISSOLUTION; ULTRASOUND; FORMS;
D O I
10.46542/pe.2021.212.116122
中图分类号
G40 [教育学];
学科分类号
040101 ; 120403 ;
摘要
Introduction: The formation of co-crystal is widely studied to obtain more favourable physicochemical properties than the pure active pharmaceutical ingredient (API). The co-crystal formation between an anti-fungal drug, fluconazole (FLU), and tartaric acid (TAR) has been investigated and its impact on mechanical properties has also been studied. Methods: The co-crystal of FLU-TAR (1:1) molar ratio was prepared by ultrasound-assisted solution co-crystallization (USSC) method with ethanol as the solvent. Polarization microscopy was used to observe the crystal morphology. Meanwhile, powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC) methods were used to characterise the co-crystal formation. The mechanical properties of the co-crystal, such as flowability and tabletability, were compared with pure FLU. Results: Photomicroscopes revealed the unique crystal morphology of the USSC product was different from the two starting components. The typical PXRD pattern was shown by the USSC product, which indicated the formation of FLU-TAR co-crystal. In addition, the DSC thermogram revealed 169.2 degrees C as the melting point of the FLU-TAR co-crystal, which is between the melting points of FLU and TAR. It indicates that FLU-TAR co-crystal has better flowability and tabletability than pure FLU. Conclusion: FLU-TAR co-crystal is one of the alternative solid forms for a raw material in pharmaceutical tablet preparation because it has better mechanical properties than pure fluconazole.
引用
收藏
页码:116 / 122
页数:7
相关论文
共 29 条
  • [1] Ultrasound assisted cocrystallization from solution (USSC) containing a non-congruently soluble cocrystal component pair: Caffeine/maleic acid
    Aher, Suyog
    Dhumal, Ravindra
    Mahadik, Kakasaheb
    Paradkar, Anant
    York, Peter
    [J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2010, 41 (05) : 597 - 602
  • [2] Relationship between mechanical properties and crystal structure in cocrystals and salt of paracetamol
    Ahmed, Hamzah
    Shimpi, Manishkumar R.
    Velaga, Sitaram P.
    [J]. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2017, 43 (01) : 89 - 97
  • [3] Solid-state characterization of fluconazole
    Alkhamis, KA
    Obaidat, AA
    Nuseirat, AF
    [J]. PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, 2002, 7 (04) : 491 - 503
  • [4] Melting point-solubility-structure correlations in multicomponent crystals containing fumaric or adipic acid
    Batisai, Eustina
    Ayamine, Alban
    Kilinkissa, Ornella E. Y.
    Bathori, Nikoletta B.
    [J]. CRYSTENGCOMM, 2014, 16 (43): : 9992 - 9998
  • [5] Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Fluconazole
    Charoo, Naseem
    Cristofoletti, Rodrigo
    Graham, Alexandra
    Lartey, Paul
    Abrahamsson, Bertil
    Groot, D. W.
    Kopp, Sabine
    Langguth, Peter
    Polli, James
    Shah, Vinod P.
    Dressman, Jennifer
    [J]. JOURNAL OF PHARMACEUTICAL SCIENCES, 2014, 103 (12) : 3843 - 3858
  • [6] Origin of Deteriorated Crystal Plasticity and Compaction Properties of a 1:1 Cocrystal between Piroxicam and Saccharin
    Chattoraj, Sayantan
    Shi, Limin
    Chen, Miles
    Alhalaweh, Amjad
    Velaga, Sitaram
    Sun, Changquan Calvin
    [J]. CRYSTAL GROWTH & DESIGN, 2014, 14 (08) : 3864 - 3874
  • [7] Improvement of fluconazole flowability and its effect on dissolution from tablets and capsules
    Consiglieri, Vladi Olga
    Mourao, Samanta
    Sampaio, Mauricio
    Granizo, Patricia
    Garcia, Pedro
    Martinello, Valeska
    Spricigo, Rodrigo
    Ferraz, Humberto Gomes
    [J]. BRAZILIAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2010, 46 (01) : 115 - 120
  • [8] The influence of polymorphism on the manufacturability and in vitro dissolution of sulindac-containing hard gelatin capsules
    Guadalupe Sanchez-Gonzalez, Elizabeth
    Yepez-Mulia, Lilian
    Hernandez-Abad, Vicente Jesus
    Jung Cook, Helgi
    [J]. PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, 2015, 20 (03) : 306 - 313
  • [9] Physicochemical and mechanical properties of paracetamol cocrystal with 5-nitroisophthalic acid
    Hiendrawan, Stevanus
    Veriansyah, Bambang
    Widjojokusumo, Edward
    Soewandhi, Sundani Nurono
    Wikarsa, Saleh
    Tjandrawinata, Raymond R.
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2016, 497 (1-2) : 106 - 113
  • [10] Implication of microstructure on the mechanical behaviour of an aspirin-paracetamol eutectic mixture
    Jain, Hemant
    Khomane, Kailas S.
    Bansal, Arvind K.
    [J]. CRYSTENGCOMM, 2014, 16 (36): : 8471 - 8478