COMBILOSE: A novel lactose-based co-processed excipient for direct compression
Published:  Jan 03, 2023DOI: 10.7324/JAPS.2023.37613
Lactose is the commonly used diluent in the manufacturing of tablets dosage form. However, the poor flowability and compressibility of lactose limit its use as a directly compressible filler binder. In this research work, composite excipient COMBILOSE was developed as a directly compressible filler binder by coprocessing technique. Lactose monohydrate was co-processed with maltose monohydrate and maize starch by co-freezing and co-drying techniques. Physical blends of lactose monohydrate and maize starch were prepared in the ratio of 20:1. Prepared physical blends were dispersed in 5% w/v, 10% w/v, and 15% w/v aqueous solutions of maltose monohydrate. Dispersions were subjected to co-freezing followed by co-drying. Microfine granules of COMBILOSE were obtained by comminution and sifting of the dried composites. The developed composite excipients were evaluated for various excipient functionalities. The results of studies showed that coprocessing of lactose monohydrate with maize starch and maltose monohydrate can improve flowability and tabletability. COMBILOSE containing 10% w/v of maltose monohydrate showed better dilution potential and reduced lubricant sensitivity. Improvement in compressibility was observed, which could be due to the pre-gelatinization of maize starch during the development process. In conclusion, a blend of lactose monohydrate and maize starch in a ratio of 20:1 when processed with 10% of maltose monohydrate could provide good compressibility and better dilution potential with a reduced lubricant sensitivity.
Somnache SN, Pai KV, Godbole AM, Gajare PS, Pednekar AS. Combilose: A novel lactose-based co-processed excipient for direct compression. J Appl Pharm Sci, 2023. https://doi.org/10.7324/JAPS.2023.37613
Akram M, Naqvi SBS, Gauhar S. Development of co-processed micro granules for direct compression. Int J Pharm Pharm Sci, 2011; 3(Suppl 2):64-9.
Chang CK, Alvarez-Nunez FA, Rinella JV Jr, Magnusson LE, Sueda K. Roller compaction, granulation and capsule product dissolution of drug formulations containing a lactose or mannitol filler, starch, and talc. AAPS PharmSciTech, 2008; 9(2):597-604. https://doi.org/10.1208/s12249-008-9088-y
Crouter A, Briens L. The effect of moisture on the flowability of pharmaceutical excipients. AAPS PharmSciTech, 2014; 15:65-74. https://doi.org/10.1208/s12249-013-0036-0
Daraghmeh N, Rashid I, Al Omari MM, 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. https://doi.org/10.1208/s12249-010-9523-8
Deshkar D, Gupta RN, Jayaram Kumar K. Studies on effect of co-processing on palmyrah and maize starch mixtures using DOE approach. Int J Biol Macromol, 2019; 122:417-24. https://doi.org/10.1016/j.ijbiomac.2018.10.079
Dominik M, Vraníková B, Sva?inová P, Elbl J, Pavloková S, Prudilová BB, Šklubalová Z, Franc A. Comparison of flow and compression properties of four lactose-based co-processed excipients: Cellactose® 80, CombiLac®, MicroceLac® 100, and StarLac®. Pharmaceutics, 2021; 13(9):1486. https://doi.org/10.3390/pharmaceutics13091486
Fuentes-González KI, Villafuerte-Robles L. Powder flowability as a functionality parameter of the excipient GalenIQ 720. Int J Pharm Pharm Sci, 2014; 1:66-74.
Gohel MC, Jogani PD, Bariya SH. Development of agglomerated directly compressible diluent consisting of brittle and ductile materials. Pharm Dev Technol, 2003; 8(2):143-51. https://doi.org/10.1081/PDT-120018481
Gohel MC, Patel TM, Parikh RK, Parejiya PB, Barot BS, Ramkishan A. Exploration of novel co-processed multifunctional diluent for the development of tablet dosage form. Indian J Pharm Sci, 2012; 74(5):381-6. https://doi.org/10.4103/0250-474X.108412
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(35):9. https://doi.org/10.1186/s43094-020-00055-9
Hasan MM, Chowdhury SS, Lina SM, Bhoumik NC, Ashab I. Comparative evaluation of Zea mays (L.) and Ipomoea batatas (L.) as a pharmaceutical excipient. IOSR-JPBS, 2012; 3:31-6. https://doi.org/10.9790/3008-0363136
Hauschild K, Picker KM. Evaluation of a new coprocessed compound based on lactose and maize starch for tablet formulation. AAPS J, 2004; 6(2):27-38. https://doi.org/10.1208/ps060216
Kudo Y, Yasuda M, Matsusaka S. Effect of particle size distribution on flowability of granulated lactose. Adv Powder Technol, 2020; 31(1):121-7. https://doi.org/10.1016/j.apt.2019.10.004
Lamy B, Serrano DR, O'connell P, Couet W, Marchand S, Healy AM, Tewes F. Use of leucine to improve aerodynamic properties of ciprofloxacin-loaded maltose microparticles for inhalation. EJPR, 2019; 1(1):2-11. https://doi.org/10.34154/2019-EJPR.01(01).pp-02-11/euraass
Malamataris S, Goidas P, Dimitriou A. Moisture sorption and tensile strength of some tableted direct compression excipients. Int J Pharm, 1991; 68(1-3):51-60. https://doi.org/10.1016/0378-5173(91)90126-9
Mizumoto T, Masuda Y, Yamamoto T, Yonemochi E, Terada K. Formulation design of a novel fast-disintegrating tablet. Int J Pharm, 2005; 306(1-2):83-90. https://doi.org/10.1016/j.ijpharm.2005.09.009
Moondra S, Maheshwari R, Taneja N, Tekade M, Tekade RK. Bulk level properties and its role in formulation development and processing. In: Tekadle RK (ed.). Advances in pharmaceutical product development and research, dosage form design parameters. vol. II. Academic Press, London, UK, pp 221-56, 2018. https://doi.org/10.1016/B978-0-12-814421-3.00006-3
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. https://doi.org/10.1016/j.ejpb.2008.04.011
Olorunsola EO, Akpan GA, Adikwu MU. Evaluation of chitosan-microcrystalline cellulose blends as direct compression excipients. J Drug Deliv, 2017; 2017:8. https://doi.org/10.1155/2017/8563858
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. IJPRI, 2011; 2:39-45.
Patel P, Telange D, Sharma N. Comparison of different granulation techniques for lactose monohydrate. Int J Pharm Sci Drug Res, 2011; 3(3):222-5.
Patel S, Kaushal AM, Bansal AK. Compression physics in the formulation development of tablets. Crit Rev Ther Drug Carrier Syst, 2006; 23(1):1-65 https://doi.org/10.1615/CritRevTherDrugCarrierSyst.v23.i1.10
Rani U, Begum N. Overview of co processed excipients used to improve tabletting performance. JADD, 2014; 1(6):8.
Sandhan SB, Derle DV. A review on functionality assessment of multifunctional excipients. IJPSR, 2019; 10(9):4078-89.
Schwarz E, Fichtner V, Luhn O, Häusler O. Case study: properties of a co-processed compound versus the physical blend based on lactose and starch. Available via https://www.roquette.com/media-center/resources/ pharma-poster-properties-of-a-co-processed-compound-vs-blend-lactose-starch (Accessed 08 May 2022). Tomar M, Kumar SA, Raj SA. Effect of moisture content of exicipient (microcrystalline cellulose) on direct compressible solid dosage forms. IJPSR, 2017; 8(1):282.
Tye CK, Sun CC, Amidon GE. Evaluation of the effects of tableting speed on the relationships between compaction pressure, tablet tensile strength, and tablet solid fraction. J Pharm Sci, 2005; 94(3):465-72. https://doi.org/10.1002/jps.20262
Ugoeze KC, Idris MEJ. Development of co-processed powders containing lactose, Mucuna flagellipes seed gum and Ipomoea batatas tuber starch. Int J Appl Biol Pharm, 2020; 11(4):256-75.
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