This paper evaluates and compares the properties of directly compressible tabletting materials and matrix tablets containing a combination of α-lactose monohydrate and microcrystalline cellulose in the 3:1 ratio in a physical mixture and in a coprocessed dry binder. Tested parameters include flow properties, compressibility, compactibility and the rate of drug release from tablets. Compressibility is evaluated by means of the energy profile of the compression process. Compactibility is evaluated by means of the tensile strength of the tablets. Dissolution testing is done using the rotating basket method. Dissolution profiles are evaluated by non-linear regression analysis.
Total energy of compression and plasticity values were higher in tabletting materials with the coprocessed dry binder. Increasing additions of polyvinyl alcohol decreased the values of total energy of compression, plasticity, tensile strength of tablets and drug release rate. Dissolution behaviour of tablets, which contained the physical mixture or coprocessed dry binder and the same amount of polyvinyl alcohol, was comparable.
1. P. Gupta, S. K. Nachaegari and A. K. Bansal, Improved Excipient Functionality by Coprocessing, in Excipient Development for Pharmaceutical Biotechnology and Drug Delivery Systems (Eds. K. A. Katdare, M. V. Chaubal) Informa Healthcare USA 2006, pp. 109–126.
2. K. Satish, S. K. Nachaegari and A. K. Bansal, Coprocessed excipients for solid dosage forms, Pharm. Tech.28 (2004) 52–64.
4. P. M. Belda and J. B. Mielck, The tabletting behavior of Cellactose compared with mixtures of celluloses with lactoses, Eur. J. Pharm. Biopharm.42 (1996) 325–330.
5. J. D. Allen, Improving DC with SMCC, Manuf. Chemist.67 (1996) 19–20.
6. B. E. Sherwood and J. W.Becker, A new class of high-functionality excipients: Silicified microcrystalline cellulose, Pharm. Technol. 22 (1998) 78–88.
7. P. C. Schmidt and C. J. Rubensdorfer, Evaluation of Ludipress as a multipurpose excipient for direct compression. Part 1. Powder characteristics and tabletting properties, Drug Dev. Ind. Pharm.20 (1994) 2899–2925; https://doi.org/10.3109/03639049409042687
8. K. G. Wagner and J. A. Dressler, A corn starch/alpha -lactose monohydrate compound as a new directly compressible excipient, Pharm. Ind.64 (2002) 992–999.
9. J. Mužíková, P. Svačinová and A. Srbová, A study of a novel coprocessed dry binder composed of α-lactose monohydrate, microcrystalline cellulose and corn starch. Pharm. Dev. Technol.22 (2017) 964–971; https://doi.org/10.3109/10837450.2015.1131717
10. H. Kathpalia and K. Jogi, Coprocessed excipients – a review, WJPR3 (2014), 3863–3885.
23. V. A. Belousov, Choice of optimal pressure values in tabletting medicinal powders, Khim. Farm. Zh. 10 (1976) 105–111.
24. Y. Lei, Q. Zhou, Y. Zhang, J. Chen, S. Sun and I. Noda, Analysis of crystallized lactose in milk powder by Fourier-transform infrared spectroscopy combined with two-dimensional correlation infrared spectroscopy, J. Mol. Struct. 974 (2010) 88–93; https://doi.org/10.1016/j.molstruc.2009.12.030
25. H. S. Mansur, C. M. Sadahira, A. N. Souza and A. A. P. Mansur, FTIR spectroscopy characterization of poly (vinyl alcohol) hydrogel with different hydrolysis degree and chemically crosslinked with glutaraldehyde, Mater. Sci. Eng. C28 (2008) 539–548; https://doi.org/10.1016/j.msec.2007.10.088
26. A. Michoel, P. Rombaut and A. Verhoye, Comparative evaluation of co-processed lactose and microcrystalline cellulose with their physical mixtures in the formulation of folic acid tablets, Pharm. Dev. Technol. 7 (2002) 79–87; https://doi.org/10.1081/PDT-120002233
27. A. T. M. Serajuddin and C. I. Jarowski, Effect of diffusion layer pH and solubility on the dissolution rate of pharmaceutical bases and their hydrochloride salts. II: salicylic acid, theophylline and benzoic acid, J. Pharm. Sci.74 (1985) 148–154; https://doi.org/10.1002/jps.2600740209