ERRATUM: Enhancing the Pharmaceutical Properties of Ibuprofen through Spherical Agglomeration-Co-Crystallization with Nicotinamide: A Comprehensive Study of Micromeritic, Tabletability, and Dissolution Characteristics
Main Article Content
Abstract
Developing efficient methods for cocrystal production is crucial to improving drug solubility and bioavailability. This study utilized the spherical agglomeration-co-crystallization (SA-CC) method to produce spherical ibuprofen-nicotinamide (IBU-NICO) cocrystals. This method used ethanol (ETA) as a solvent and a mixture of deionized water and PEG-4000 as an anti-solvent, enhancing the micromeritic properties of the cocrystal. The addition of dichloromethane (DCM) facilitated the formation of spherical particles via rapid viscous phase transition. Fourier-transform infrared (FTIR) spectroscopy identified significant molecular interactions, such as hydrogen bonding between the ibuprofen carboxyl and nicotinamide acylamino groups, ensuring cocrystal stability. Hot-stage microscopy (HSM) and scanning electron microscopy (SEM) analyses demonstrated that cocrystals exhibited lower thermal stability but improved dissolution rates due to their amorphous-crystalline structures and rough, porous surfaces. Differential scanning calorimetry (DSC) showed altered thermal profiles with a reduction of 7.21oC, indicating modified crystal lattice structures. Powder X-ray diffraction (PXRD) confirmed the formation of new crystalline phases. Micromeritic evaluations revealed favorable particle size distribution (PSD) with an average size of 5 mm, enhanced flowability, and compressibility, with cocrystals showing superior tensile strength (2.36 MPa at 207.97 MPa) and dissolution rates 2.82 times higher than pure IBU at pH 6.8. These findings highlight the potential of the SA-CC method to produce cocrystals with enhanced drug properties, paving the way for improved pharmaceutical formulations.
Downloads
Article Details
This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.
How to Cite
References
Chen H, Xu H, Wang C, Kang H, Haynes CL, Mahanthappa MK, Sun CC. Novel Quasi-Emulsion Solvent Diffusion-Based Spherical Cocrystallization Strategy for Simultaneously Improving the Manufacturability and Dissolution of Indomethacin. Cryst Growth Des. 2020;20(10):6752–62.
Rojas J, Buckner IS, Kumar V. Co-Proccessed Excipients With Enhanced Direct Compression Functionality for Improved Tableting Performance. Drug Dev Ind Pharm. 2012;38(10):1159–70.
Haruna F, Apeji YE, Oparaeche C, Oyi AR, Gamlen M. Compaction and Tableting Properties of Composite Particles of Microcrystalline Cellulose and Crospovidone Engineered for Direct Compression. Futur J Pharm Sci. 2020;6(1).
Bolla G, Nangia A. Pharmaceutical Cocrystals: Walking the Talk. Chem Commun. 2016;52(54):8342–60.
Nugraha YP, Unique IGANP, Miyake T, Rahmah R, Indra I, Soewandhi SN, Uekusa H. Structural Characterization and Pharmaceutical Evaluation of Telmisartan Hydrochloride Salts. Crystals. 2024;14(2):151.
Izutsu K, Koide T, Takata N, Ikeda Y, Ono M. Characterization and Quality Control of Cocrystals. Chem Pharm Bull. 2016;64(10):1421–30.
Indra I, Wikarsa S, Nugraha YP, Suendo V, Uekusa H, Soewandhi SN. Utilizing hot-stage polarized microscopy and ATR-FTIR for ramipril co-crystal screening, supported by principal component analysis and cluster analysis. J Pharm Pharmacogn Res. 2023;11(6):1137–48.
Machado TC, Kavanagh ON, Cardoso SG, Rodrı́guez-Hornedo N. Synchronization of Cocrystal Dissolution and Drug Precipitation to Sustain Drug Supersaturation. Mol Pharm. 2022;19(8):2765–75.
Yuliandra Y, Zaini E, Syofyan S, Pratiwi W, Putri LN, Pratiwi YS, Arifin H. Cocrystal of ibuprofen–nicotinamide: Solid-state characterization and in vivo analgesic activity evaluation. Sci Pharm. 2018;86(2).
Chen H, Guo Y, Wang C, Dun J, Sun CC. Spherical Cocrystallization - An Enabling Technology for the Development of High Dose Direct Compression Tablets of Poorly Soluble Drugs. Cryst Growth Des. 2019;19(4):2503–10.
Pagire SK, Korde SA, Whiteside BR, Kendrick J, Paradkar A. Spherical crystallization of carbamazepine/saccharin co-crystals: Selective agglomeration and purification through surface interactions. Cryst Growth Des. 2013;13(10):4162–7.
Wang X, Li Z, Zhang C, Wen T, Zhou Y, Ouyang J. Designing Spherical Particles of Arbidol Hydrochloride via Spherical Crystallization: Preparation and Characterization. Ind Eng Chem Res. 2024;63(12):5249–60.
Wu S, Li K, Zhang T, Gong J. Size Control of Atorvastatin Calcium Particles Based on Spherical Agglomeration. Chem Eng Technol. 2015;38(6):1081–7.
Peña R, Nagy ZK. Process Intensification Through Continuous Spherical Crystallization Using a Two-Stage Mixed Suspension Mixed Product Removal (MSMPR) System. Cryst Growth Des. 2015;15(9):4225–36.
Sowa M, Klapwijk AR, Ostendorf M, Beckmann W. Particle Engineering of an Active Pharmaceutical Ingredient for Improved Micromeritic Properties. Chem Eng Technol. 2017;40(7):1282–92.
Hansen J, Kleinebudde P. Enabling the direct compression of metformin hydrochloride through QESD crystallization. Int J Pharm. 2021;605(March):120796.
Alatas F, Pratiwi GK, Meylifepri H. Multicomponent Crystal Formation of Dexibuprofen-Caffeine to Improve Solubility. Trop J Nat Prod Res. 2023;7(10):4128–32.
Anggraini D, Firmansyah F, Novita G, Audia RA. Improving the Solubility of Fenofibric Acid via Multicomponent Crystal Formation with Theobromine Coformer. Trop J Nat Prod Res. 2024;8(4):6901–5.
Anggraini D, Umar S, Arifin H, Zaini E. Dissolution rate enhancement and physicochemical characterization of a fenofibric acid–nicotinamide eutectic mixture. Trop J Nat Prod Res. 2021;5(9):1614–8.
Zaini E, Marhammah RP, Fitriani L, Hasanah U, Umar S. The Preparation and Characterization of the Solid Dispersion of Piperine with Hydroxypropyl Methylcellulose (HPMC) 2910 Using Spray Drying. Trop J Nat Prod Res. 2022;5(12):2103–7.
Kumara GHAJJ, Hayano K, Ogiwara K. Image Analysis Techniques on Evaluation of Particle Size Distribution of Gravel. Int J GEOMATE. 2012;3(1):290–7.
Thakur A, Thipparaboina R, Kumar D, Sai Gouthami K, Shastri NR. Crystal engineered albendazole with improved dissolution and material attributes. CrystEngComm. 2016;18(9):1489–94.
Pitt K, Peña R, Tew JD, Pal K, Smith R, Nagy ZK, Litster JD. Particle design via spherical agglomeration: A critical review of controlling parameters, rate processes and modelling. Powder Technol. 2018;326:327–43.
Lin SY. Simultaneous screening and detection of pharmaceutical co-crystals by the one-step DSC–FTIR microspectroscopic technique. Drug Discov Today. 2017;22(4):718–28.
Biedrzycka K, Marcinkowska A. The Use of Hot Melt Extrusion to Prepare a Solid Dispersion of Ibuprofen in a Polymer Matrix. Polymers (Basel). 2023;15(13):2912.
Januś E, Ossowicz P, Klebeko J, Nowak A, Duchnik W, Kucharski Ł, Klimowicz A. Enhancement of Ibuprofen Solubility and Skin Permeation by Conjugation With l-Valine Alkyl Esters. RSC Adv. 2020;10(13):7570–84.
Alhadid A, Kefalianakis L, Wendler A, Nasrallah S, Jandl C, Kronawitter SM, Kieslich G, Minceva M. Thermodynamic Approach for Estimating the Melting Enthalpy of Cocrystals. Cryst Growth Des. 2024;24(11):4770–80.
Vasilev NA, Surov AO, Voronin AP, Drozd K V., Perlovich GL. Novel cocrystals of itraconazole: Insights from phase diagrams, formation thermodynamics and solubility. Int J Pharm. 2021;599(March):120441.
Octavia MD, Hasmiwati H, Revilla G, Zaini E. Multicomponent Crystals of Piperine-Nicotinic Acid: The Physicochemical and Dissolution Rate Properties. Trop J Nat Prod Res. 2023;7(8):3701–5.
Chatterjee A, Gupta MM, Srivastava B. Spherical Crystallization: A Technique Use to Reform Solubility and Flow Property of Active Pharmaceutical Ingredients. Int J Pharm Investig. 2017;7(1):4.
Nitsure A, Patel D, Wairkar S. Improved processability of ethambutol hydrochloride by spherical agglomeration. Pharm Dev Technol. 2020;25(3):376–84.
Cui P, Yang W, Yin Q, Zhou L, Zhang M, Bao Y, Xie C, Hou B, Yin Q. Spherulitic Growth Strategy for Agitation-Induced Formation of Spherical Amoxicillin Sodium Products. Ind Eng Chem Res. 2022;61(27):9821–32.
Ravouru N, Penjuri SCB, Damineni S, Muni RL, Poreddy SR. Preparation and in vitro evaluation of ibuprofen spherical agglomerates. Turkish J Pharm Sci. 2018;15(1):7–15.
Karagianni A, Malamatari M, Kachrimanis K. Pharmaceutical cocrystals: New solid phase modification approaches for the formulation of APIs. Pharmaceutics. 2018;10(1):1–30.
Kavanagh ON, Wang C, Walker GM, Sun CC. Modulation of the powder properties of lamotrigine by crystal forms. Int J Pharm. 2021;595(January):120274.
Chow SF, Chen M, Shi L, Chow AHL, Sun CC. Simultaneously improving the mechanical properties, dissolution performance, and hygroscopicity of ibuprofen and flurbiprofen by cocrystallization with nicotinamide. Pharm Res. 2012;29(7):1854–65.
Shin DW, Lee SJ, Ha Y, Choi Y-S, Kim JW, Park S, Park M. Pharmacokinetic and Pharmacodynamic Evaluation According to Absorption Differences in Three Formulations of Ibuprofen. Drug Des Dev Ther. 2017;Volume11:135–41.