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<p>Co-crystallization is an advanced crystal engineering technique used to improve the physicochemical properties of active pharmaceutical ingredients (APIs) while preserving their molecular integrity. This research presents a novel approach for treating epilepsy by incorporating CBZ-SUC co-crystals into orally disintegrating tablets (ODTs) via direct compression, with the objective of improving patient compliance and enabling rapid therapeutic response. This work involved the co-crystallization of carbamazepine (CBZ), a Biopharmaceutical Classification System (BCS) Class II drug characterized by limited solubility and inadequate compressibility, with succinic acid (SUC) using the solvent-drop grinding technique. The synthesized CBZ-SUC co-crystals were characterized using powder X-ray diffraction (PXRD), Raman spectroscopy, and Fourier transform infrared (FTIR) spectroscopy. PXRD validated the emergence of a novel crystalline phase, characterized by distinct diffraction peaks that distinguish it from pure CBZ. Raman investigation revealed distinctive peaks at 1040&#xa0;cm⁻¹ and 3020–3060&#xa0;cm⁻¹, while FTIR indicated changes in the 3000–3500&#xa0;cm⁻¹ and 1600–1700&#xa0;cm⁻¹ regions, showing hydrogen bonding between CBZ and SUC, confirming significant co-crystal formation and improved solid-state stability. The optimized co-crystals were subsequently formed into orally disintegrating tablets (ODTs) by employing direct compression (DC), utilizing several super disintegrants and excipients to attain rapid disintegration and enhanced mechanical qualities. Among the developed formulations, F-5 demonstrated the most desirable characteristics, featuring an optimal equilibrium of mechanical strength (crushing strength: 3.2&#xa0;kg), rapid disintegration time (oral disintegration: 37.33 ± 1.9&#xa0;s; <i>in vitro</i> disintegration: 23.25 ± 1.2&#xa0;s, <i>n</i> = 6), and improved dissolution rate (80.2% CBZ release within 15&#xa0;min). The optimized formulation adhered to pharmacopeial criteria, exhibiting excellent flavour masking, low friability (0.68%), and strong compressibility. The research highlights the significance of CBZ-SUC co-crystals in overcoming dissolution and compressibility challenges, positioning them as a suitable option for orally disintegrating tablets aimed at seizure management and improved patient compliance.</p>

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Development and Evaluation of Carbamazepine-Succinic Acid Co-Crystal-Based Orally Disintegrating Tablets: A Novel Approach for Enhanced Solubility and Rapid Drug Release

  • 期刊论文

  • 发表日期：

    2026年3月2日

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  • Sana Hayat,
  • Majeed Ullah,
  • Amjad Khan,
  • Sajid Hussain,
  • Sajid Khan Sadozai,
  • Fawad Ali,
  • Abdulwahed Fahad Alrefaei,
  • Atif Ali Khan Khalil,
  • Sajid Ali

摘要

Co-crystallization is an advanced crystal engineering technique used to improve the physicochemical properties of active pharmaceutical ingredients (APIs) while preserving their molecular integrity. This research presents a novel approach for treating epilepsy by incorporating CBZ-SUC co-crystals into orally disintegrating tablets (ODTs) via direct compression, with the objective of improving patient compliance and enabling rapid therapeutic response. This work involved the co-crystallization of carbamazepine (CBZ), a Biopharmaceutical Classification System (BCS) Class II drug characterized by limited solubility and inadequate compressibility, with succinic acid (SUC) using the solvent-drop grinding technique. The synthesized CBZ-SUC co-crystals were characterized using powder X-ray diffraction (PXRD), Raman spectroscopy, and Fourier transform infrared (FTIR) spectroscopy. PXRD validated the emergence of a novel crystalline phase, characterized by distinct diffraction peaks that distinguish it from pure CBZ. Raman investigation revealed distinctive peaks at 1040 cm⁻¹ and 3020–3060 cm⁻¹, while FTIR indicated changes in the 3000–3500 cm⁻¹ and 1600–1700 cm⁻¹ regions, showing hydrogen bonding between CBZ and SUC, confirming significant co-crystal formation and improved solid-state stability. The optimized co-crystals were subsequently formed into orally disintegrating tablets (ODTs) by employing direct compression (DC), utilizing several super disintegrants and excipients to attain rapid disintegration and enhanced mechanical qualities. Among the developed formulations, F-5 demonstrated the most desirable characteristics, featuring an optimal equilibrium of mechanical strength (crushing strength: 3.2 kg), rapid disintegration time (oral disintegration: 37.33 ± 1.9 s; in vitro disintegration: 23.25 ± 1.2 s, n = 6), and improved dissolution rate (80.2% CBZ release within 15 min). The optimized formulation adhered to pharmacopeial criteria, exhibiting excellent flavour masking, low friability (0.68%), and strong compressibility. The research highlights the significance of CBZ-SUC co-crystals in overcoming dissolution and compressibility challenges, positioning them as a suitable option for orally disintegrating tablets aimed at seizure management and improved patient compliance.