Chapter 17 Regulatory Considerations in Dissolution and Drug Release of BCS Class II and IV Compounds

Nickerson, Beverly; Guo, Michele Xuemei; Norris, Kenneth J.; Zhang, Ling

doi:10.1201/9781315364537-18

Cited by 2 publications

(1 citation statement)

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“…Along with all the above-mentioned benefits, it is also possible to incorporate extra health benefits through the appropriate coformers. Although several properties of the pure drug are improved, the structure will not get al tered, resulting in unchanged pharmacological activity [25][26][27][28][29][30][31][32][33].…”

Section: Introductionmentioning

confidence: 99%

Enhancement of Solubility and Dissolution Rate of Acetylsalicylic Acid via Co-Crystallization Technique: A Novel Asa-Valine Cocrystal

et al. 2021

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Objective: This study aims to synthesize acetylsalicylic acid (ASA) cocrystals using valine as a coformer via a co-crystallization technique to increase the solubility and dissolution rate of ASA. Methods: The ASA-valine cocrystal (1:1 molar ratio) was prepared using the solvent evaporation technique with ethanol: water (50:50). The cocrystal was characterized using Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Scanning electron microscopy (SEM), melting point to confirm the formation of cocrystal. The evaluation of cocrystal was done by drug content determination, solubility and dissolution studies. Results: The prepared cocrystal was successfully confirmed for the formation of a hydrogen bond. The melting point of prepared cocrystal was decreased compared to pure ASA and valine, which indicated the formation of a new crystalline form. The FT-IR studies showed the formation of a new hydrogen bond by shifting the-O-H,-C=O and-N-H functional groups. SEM studies ensured that the prepared cocrystals were in needle-like appearance. Finally, DSC and PXRD studies were also indicated the successful formation of ASA-valine cocrystal. The drug release of cocrystal was found to be 100% at 60th min. Where in the case of pure ASA and marketed product of ASA exhibited the dissolution rate of 59% and 69% at 60th min respectively. Conclusion: The co-crystallization technique can be adopted as the best strategy to increase the solubility and dissolution rate of BCS class 2 drugs. Therefore the prepared ASA-valine cocrystal can be a greater alternative to increase the solubility and dissolution rate compared with pure and marketed ASA.

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