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AAPS PharmSciTech

, Volume 19, Issue 2, pp 866–880 | Cite as

Development and Optimization of a Starch-Based Co-processed Excipient for Direct Compression Using Mixture Design

  • Yonni E. Apeji
  • Avosuahi R. Oyi
  • Adamu B. Isah
  • Teryila S. Allagh
  • Sameer R. Modi
  • Arvind K. BansalEmail author
Research Article
  • 215 Downloads

Abstract

The development of novel excipients with enhanced functionality has been explored using particle engineering by co-processing. The aim of this study was to improve the functionality of tapioca starch (TS) for direct compression by co-processing with gelatin (GEL) and colloidal silicon dioxide (CSD) in optimized proportions. Design of Experiment (DoE) was employed to optimize the composition of the co-processed excipient using the desirability function and other supporting studies as a basis for selecting the optimized formulation. The co-processed excipient (SGS) was thereafter developed by the method of co-fusion. Flow and compaction studies of SGS were carried out in comparison to its parent component (TS) and physical mixture (SGS-PM). Tablets were prepared by direct compression (DC) containing ibuprofen (200 mg) as a model for poor compressibility using SGS, Prosolv®, and StarLac® as multifunctional excipients. The optimized composition of SGS corresponded to TS (90%), GEL (7.5%), and CSD (2.5%). The functionality of SGS was improved relative to SGS-PM in terms of flow and compression. Tablets produced with SGS were satisfactory and conformed to USP specifications for acceptable tablets. SGS performed better than Prosolv® in terms of disintegration and was superior to StarLac with respect to tensile strength and disintegration time. The application of DoE was successful in optimizing and developing a starch-based co-processed excipient that can be considered for direct compression tableting.

KEY WORDS

design of experiment co-processing functionality tablet direct compression 

Notes

Acknowledgements

This work was supported by the Research Training Fellowship for Developing Country Scientists (RTF-DCS) awarded by the Centre for Science and Technology of the Non-Aligned and Other Developing Countries (NAMS-TCT), India. We will also like to thank Quality Starch Chemicals (Tamil Nadu, India) for providing tapioca starch as a gift sample, Cabot Corporation for colloidal silicon dioxide, JRS Pharma (Germany) for Prosolv®, and Roquette Pharma (France) for StarLac®.

References

  1. 1.
    Odeku OA. Potentials of tropical starches as pharmaceutical excipients: a review. Starch/Staerke. 2013;65(1–2):89–106.CrossRefGoogle Scholar
  2. 2.
    Alebiowu G. Studies on the tableting properties of Sorghum Bicolor Linn (Poaceae) starch I: evaluation of binder types and concentrations on the properties of sorghum starch granulations. Discov Innov. 2001;13(1/2):73–7.Google Scholar
  3. 3.
    Odeku OA, Schmid W, Picker-Freyer KM. Material and tablet properties of pregelatinized (thermally modified) Dioscorea starches. Eur J Pharm Biopharm. 2008;70(1):357–71.CrossRefPubMedGoogle Scholar
  4. 4.
    Ochubiojo EM, Rodrigues A. Starch: from food to medicine. INTECH Open Access Publisher. 2012:488 p.Google Scholar
  5. 5.
    Rashid I, Al-Omari MMH, Badwan AA. From native to multifunctional starch-based excipients designed for direct compression formulation. Starch/Starke. 2013;65(Dc):552–71.Google Scholar
  6. 6.
    Kittipongpatana OS, Kittipongpatana N. Preparation and physicomechanical properties of co-precipitated rice starch-colloidal silicon dioxide. Powder Technol. 2011;217:377–82.CrossRefGoogle Scholar
  7. 7.
    Adedokun MO, Itiola OA. Material properties and compaction characteristics of natural and pregelatinized forms of four starches. Carbohydr Polym. 2010;79(4):818–24.CrossRefGoogle Scholar
  8. 8.
    Nachaegari SK, Bansal AK. Co-processed excipients for solid dosage forms. Pharm Technol. 2004;(January):52–64.Google Scholar
  9. 9.
    Saha S, Shahiwala AF. Multifunctional coprocessed excipients for improved tabletting performance. Expert Opin Drug Deliv. 2009 Feb;6(2):197–208.CrossRefPubMedGoogle Scholar
  10. 10.
    Alebiowu G, Itiola OA. The influence of pregelatinized starch disintegrants on interacting variables that act on disintegrant properties. Pharm Technol. 2003;27(August):28–33.Google Scholar
  11. 11.
    Rojas J, Buckner I, Kumar V. Co-processed excipients with enhanced direct compression functionality for improved tableting performance. Drug Dev Ind Pharm. 2012;38(10):1159–70.CrossRefPubMedGoogle Scholar
  12. 12.
    Daraghmeh N, Rashid I, Al Omari MMH, Leharne SA, Chowdhry BZ, Badwan A. Preparation and characterization of a novel co-processed excipient of chitin and crystalline mannitol. AAPS PharmSciTech. 2010;11(4):1558–71.CrossRefPubMedPubMedCentralGoogle Scholar
  13. 13.
    Chauhan SI, Nathwani S V., Soniwala MM, Chavda JR. Development and characterization of multifunctional directly compressible co-processed excipient by spray drying method. AAPS PharmSciTech. 2016;Aug(1):1–9. Google Scholar
  14. 14.
    El-Barghouthi M, Eftaiha A, Rashid I, Al-Remawi M, Badwan A. A novel superdisintegrating agent made from physically modified chitosan with silicon dioxide. Drug Dev Ind Pharm. 2008;34(4):373–83.CrossRefPubMedGoogle Scholar
  15. 15.
    Hamid RAS, Al-Akayleh F, Shubair M, Rashid I, Al-Remawi M, Badwan A. Evaluation of three chitin metal silicate co-precipitates as a potential multifunctional single excipient in tablet formulations. Mar Drugs. 2010;8(5):1699–715.CrossRefPubMedPubMedCentralGoogle Scholar
  16. 16.
    Adeoye O, Alebiowu G. Evaluation of co-processed disintegrants produced from tapioca starch and mannitol in orally disintegrating paracetamol tablets. Acta Pol Pharm ñ Drug Res. 2014;71(5):803–11.Google Scholar
  17. 17.
    Rojas J, Kumar V. Comparative evaluation of silicified microcrystalline cellulose II as a direct compression vehicle. Int J Pharm. 2011;416(1):120–8.CrossRefPubMedGoogle Scholar
  18. 18.
    Singh S, Rao RK V., Venugopal K, Manikandan R. Alteration in dissolution characteristics of gelatin-containing formulations: a review of the problem, test methods, and solutions. Pharm Technol. 2002;April:36–58.Google Scholar
  19. 19.
    Arora V, Gupta VB, Singhal R. Advances in direct compression technology. Pharma Times. 2007;39(2):26–7.Google Scholar
  20. 20.
    Edge S, Steele DF, Chen A, Tobyn MJ, Staniforth JN. The mechanical properties of compacts of microcrystalline cellulose and silicified microcrystalline cellulose. Int J Pharm. 2000;200:67–72.CrossRefPubMedGoogle Scholar
  21. 21.
    Tobyn MJ, Mccarthy GP, Staniforth JN, Edge S. Physicochemical comparison between microcrystalline cellulose and silicified microcrystalline cellulose. Int J Pharm. 1998;169:183–94.CrossRefGoogle Scholar
  22. 22.
    Adeoye O, Alebiowu G. Flow, packing and compaction properties of novel coprocessed multifunctional directly compressible excipients prepared from tapioca starch and mannitol. Pharm Dev Technol. 2014;7450(8):901–10.CrossRefGoogle Scholar
  23. 23.
    Olowosulu AK, Oyi A, Isah AB, Ibrahim MA. Formulation and evaluation of novel coprocessed excipients of maize starch and acacia gum (StarAc) for direct compression tabletting. Int J Pharm Res Innov. 2011;2:39–45.Google Scholar
  24. 24.
    Gamlen MJD, Martini LG, Al Obaidy KG. Effect of repeated compaction of tablets on tablet properties and work of compaction using an instrumented laboratory tablet press. Drug Dev Ind Pharm. 2015;41(1):163–9.CrossRefPubMedGoogle Scholar
  25. 25.
    United States Pharmacopoeial Convention. USP protocol for disintegration. USP/NF: In; 2008.Google Scholar
  26. 26.
    United States Pharmacopoeial Convention. USP protocol for bulk and tapped densities. USP/NF: In; 2012.Google Scholar
  27. 27.
    Sheokand S, Modi SR, Bansal AK. Dynamic vapor sorption as a tool for characterization and quantification of amorphous content in predominantly crystalline materials. J Pharm Sci. 2014;103(11):3364–76.CrossRefPubMedGoogle Scholar
  28. 28.
    Heckel RW. Density-pressure relationships in powder compaction. Trans Metall Soc AIME. 1961;221:671–5.Google Scholar
  29. 29.
    Sonnergaard JM. Quantification of the compactibility of pharmaceutical powders. Eur J Pharm Biopharm. 2006;63(August 2006):270–7.CrossRefPubMedGoogle Scholar
  30. 30.
    USP29-NF24. USP monograph: ibuprofen tablets. 2009.Google Scholar
  31. 31.
    Cornell JA. Experiments with mixtures: designs, models, and the analysis of mixture data, 2nd edition. New York: John Wiley & Sons; 1990. p. 83–9.Google Scholar
  32. 32.
    Nagpal M, Goyal A, Kumar S, Singh I. Starch-silicon dioxide coprecipitate as superdisintegrant: formulation and evaluation of fast disintegrating tablets. Int J Drug Deliv. 2012;4:164–74.Google Scholar
  33. 33.
    Chavan RB, Modi SR, Bansal AK. Role of solid carriers in pharmaceutical performance of solid supersaturable SEDDS of celecoxib. Int J Pharm. 2015;495(1):374–84.CrossRefPubMedGoogle Scholar
  34. 34.
    Zhou Q, Armstrong B, Larson I, Stewart PJ, Morton DAV, Terada K. Improving powder flow properties of a cohesive lactose monohydrate powder by intensive mechanical dry coating. J Pharm Sci. 2010;99(2):969–81.CrossRefPubMedGoogle Scholar
  35. 35.
    Sun CC. Decoding powder tabletability: roles of particle adhesion and plasticity. J Adhes Sci Technol. 2011;25(4–5):483–99.CrossRefGoogle Scholar
  36. 36.
    Andrade RD, Lemus R, Perez CE. Models of sorption isotherms for food: uses and limitations. Rev LA Fac QUÍMICA Farm. 2011;18(3):325–34.Google Scholar
  37. 37.
    Murikipudi V, Gupta P, Sihorkar V. Efficient throughput method for hygroscopicity classification of active and inactive pharmaceutical ingredients by water vapor sorption analysis. Pharm Dev Technol. 2011;18:1–11.Google Scholar
  38. 38.
    Nokhodchi A. An overview of the effect of moisture on compaction and compression. Pharamaceutical Technol. 2005;(January):46–66.Google Scholar
  39. 39.
    Callahan JC, Cleary GW, Elefant M, Kaplan G, Kensler T, Nash RA. Equilibrium moisture content of pharmaceutical excipients. Drug Dev Ind Pharm. 1982;8(3):355–69.CrossRefGoogle Scholar
  40. 40.
    Airaksinen S, Karjalainen M, Shevchenko A, Westermarck S, Leppänen E, Rantanen J, et al. Role of water in the physical stability of solid dosage formulations. J Pharm Sci. 2005;94(10):2147–65.CrossRefPubMedGoogle Scholar
  41. 41.
    Osei-Yeboah F, Chang S, Sun CC. A critical examination of the phenomenon of bonding area—bonding strength interplay in powder tableting. Pharm Res. 2016:1–7.Google Scholar
  42. 42.
    Upadhyay P, Khomane KS, Kumar L, Bansal AK. Relationship between crystal structure and mechanical properties of ranitidine hydrochloride polymorphs. CrystEngComm. 2013;15(19):3959–64.CrossRefGoogle Scholar
  43. 43.
    Ilić I, Govedarica B, Šibanc R, Dreu R, Srčič S. Deformation properties of pharmaceutical excipients determined using an in-die and out-die method. Int J Pharm. 2013;446(1):6–15.PubMedGoogle Scholar
  44. 44.
    Yadav JA, Khomane KS, Modi SR, Ugale B, Yadav RN, Nagaraja CM, et al. Correlating single crystal structure, nanomechanical, and bulk compaction behavior of febuxostat polymorphs. Mol Pharm. 2017;14:866–74.CrossRefPubMedGoogle Scholar
  45. 45.
    Egart M, Ilic I, Jankovic B, Lah N, Srcic S. Compaction properties of crystalline pharmaceutical ingredients according to the Walker model and nanomechanical attributes. Int J Pharm. 2014;472:347–55.CrossRefPubMedGoogle Scholar
  46. 46.
    Lamešic D, Planinšek O, Lavric Z, Ilic I. Spherical agglomerates of lactose with enhanced mechanical properties. Int J Pharm. 2017;516:247–57.CrossRefPubMedGoogle Scholar
  47. 47.
    Zhou D, Qiu Y. Understanding material properties in pharmaceutical product development and manufacturing: powder flow and mechanical properties. J Valid Technol. 2010:65–77.Google Scholar
  48. 48.
    Khomane KS, More PK, Raghavendra G, Bansal AK. Molecular understanding of the compaction behavior of indomethacin polymorphs. Mol Pharm. 2013;10(2):631–9.CrossRefPubMedGoogle Scholar
  49. 49.
    Šantl M, Ilić I, Vrečer F, Baumgartner S. A compressibility and compactibility study of real tableting mixtures: the impact of wet and dry granulation versus a direct tableting mixture. Int J Pharm. 2011;414(1–2):131–9.PubMedGoogle Scholar
  50. 50.
    Sun CC. Microstructure of tablet—pharmaceutical significance, assessment, and engineering. Pharm Res. 2016:1–11.Google Scholar
  51. 51.
    Rumman M. Understanding the functionality of MCC Rapid as an excipient for DC—moving towards QbD: University of Basel; 2009.Google Scholar
  52. 52.
    Singh I, Birender K, Prateek J. Preparation and characterization of starch-metal silicate co-precipitates—evaluation as tablet superdisintegrant. Polim Med. 2014;44(3):157–66.PubMedGoogle Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2017

Authors and Affiliations

  • Yonni E. Apeji
    • 1
    • 2
  • Avosuahi R. Oyi
    • 2
  • Adamu B. Isah
    • 2
  • Teryila S. Allagh
    • 2
  • Sameer R. Modi
    • 1
  • Arvind K. Bansal
    • 1
    Email author
  1. 1.Department of PharmaceuticsNational Institute of Pharmaceutical Education and Research (NIPER)MohaliIndia
  2. 2.Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty of Pharmaceutical SciencesAhmadu Bello UniversityZariaNigeria

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