A NEW ENHANCED SORBITOL: CALCIUM DIPHOSPHATE COMPOSITE AS A DIRECT COMPRESSION EXCIPIENT: A COMPARATIVE STUDY
Abstract
Objective: To evaluate and compare the particle and tableting properties of a new sorbitol (SOR) and anhydrous calcium diphosphate (ACD) composite with common excipients used for the preparation of tablets by direct compression such as polyvinylpyrrolidone (Ludipress®), lactose (Cellactose 80®) and microcrystalline cellulose (Prosolv SMCC 90®).
Methods: All materials were tested for lubricant sensitivity, ejection force, and elastic recovery, dilution potential and reworking ability. Further, compressibility and compactibility were determined using the Heckel and Leuenberger models, respectively.
Results: This new excipient offered more benefits in terms of functionality than commercial direct compressive co-processed excipients and showed better compressibility than other commercial excipients and its compactibility was ranked third after SOR and Prosolv SMCC 90®. However, this composite material was more susceptible to reprocessing than commercial products. Further, it showed a low lubricant sensitivity due to a combination of a plastic and brittle behavior. Moreover, the loading capacity of poorly compressible materials such as gemfibrozil was comparable to that of commercial direct compression excipients. It also showed the fastest in-vitro dissolution of gemfibrozil, whereas commercial products failed to fulfill the US pharmacopoeial requirements.
Conclusion: This new composite material showed potential for use as a direct compression excipient.
Keywords: Agglomeration, Sorbitol, Anhydrous calcium diphosphate, Composites, Direct compression
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References
Jivraj M, Martini LG, Thomson CM. An overview of the different excipients useful for the direct compression of tablets. Pharm Sci Technolo Today 2000;3:58–63.
Allen LV, Popovich NG, Ansel HC. Ansel´s pharmaceutical dosage forms and drug delivery systems. 8th ed. Lippincont W, Wilkins and, editors. Philadelphia; 1999.
Rojas J, Ciro Y, Correa L. Functionality of chitin as a direct compression excipient: a comparative acetaminophen study. Carbohydr Polym 2014;103:134–9.
Rojas J. Excipient functionality enhancement: the cellulose II case. Iowa: Lap Lambert Academic Publishing; 2012. p. 160.
McCormick D. Evolutions in direct compression. Pharm Technol 2005;1:52–62.
Jacob S, Shirwaikar A, Srinivasan K. Novel co-processed excipients of manitol and microcrystalline cellulose for preparaing fast dissolving tablets of glizipide. Indian J Pharm Sci 2007;69:633–9.
Ramya K, Chowdary KPR. Preparation, characterization and evaluation of a new coprocessed excipient as directly compressible vehicle in tablet formulation. J Global Trends Pharm Sci 2013;4:1322-8.
Rojas J. Excipient design by co-processing for direct compression applications. In: Excipient applications in formulation design and drug delivery. Springer; 2015. p. 234-43.
Echeverry E, Rojas J. Functionality enhancement of sorbitol and anhydrous calcium diphosphate composites for direct compression applications. Int J Res Pharm Sci 2014;5:299-303.
Echeverri E, Rojas J, Yepes M. Assessment of the tableting characteristics of a novel sorbitol and calcium diphosphate composites. Int J Pharm Pharm Sci 2015;7:160-4.
Rojas J, Hernadez S, Giraldo A. Crystalline, and amorphous lactoses: Tableting Properties and their Application for the Production of Pharmaceutical Compacts. In: Lactose: Structure, Food Industry Applications, And Role Disorders. NOVA Science Publishers Inc; 2013. p. 87–115.
Rojas J, Hernandez S. Effect of the compaction platform on the densification parameters of tableting excipients with different deformation mechanisms. Chem Pharm Bull 2014;63:281–7.
Paronem P IJ. Pharmaceutical powder compaction technology. Alderborn G NC. Editor. New York: Marcel Dekker Inc; 1996. p. 55-75.
Heckel R. Density-pressure relationships in powder compaction. Trans Metall Soc AIME 1961;221:671–5.
Bolhius GK, Chowhan ZT. Materials for direct compression. In: Alderborn G, Nystrom C. editor. Pharmaceutical Powder Compaction Technology. New York: Marcel Dekker Inc; 1996. p. 419–500.
Jetzwer W, Leuenberger H, Sucker H. The compressibility and compactibility of pharmaceutical powders. Pharm Technol 1983;74:33–9.
Minchom C, Armostrong N. A proposed a technique for expressing the capacity of directly compressible tablet diluents. 124 British Pharmaceutical conference; 1987. p. 69–72.
Bolhius GK, Zuurman K. Tableting properties of experimental and commercially available lactose granulations for direct compression. Drug Dev Ind Pharm 1995;21:2057–71.
Armostrong N, Haines-Nutt R. Elastic recovery and surface-area changes in compacted powder systems. J Pharm Pharmacol 1972;24(Suppl):135–6.
Leuenberger H, Rohera B. Fundamentals of powder compression. I. The compactibility and compressibility of pharmaceutical powders. Pharm Res 1986;3:12–22.
Herting M, Kleinebudde P. Studies on the reduction of tensile strength of tablets after roll compaction/dry granulation. Eur J Pharm Biopharm 2008;70:372–9.
He X, Secreast P, Amidon G. Mechanistic study of the effect of roller compaction and lubricant on tablet mechanical strength. J Pharm Sci 2007;96:1342–55.
Celik M, Mollan M. The effects of lubrication on the compaction and post-compaction properties of directly compressible maltodextrins. Int J Pharm 1996;144:1–9.
Kushner J, Moore F. Scale-up model describing the impact of lubrication on tablet tensile strength. Int J Pharm 2010;399:19–30.