Login Register Cart 0
Generic placeholder image

Current Drug Delivery

Editor-in-Chief

ISSN (Print): 1567-2018
ISSN (Online): 1875-5704

Back
Journal Home About Journal Editorial Board Journal Insight Current Issue Volumes/Issues
Subscribe
Research Article

The Potential Migrated Mechanism of Water-Soluble Components in Pellets Prepared by Wet Extrusion/Spheronization: Effect of Drying Rate

Author(s): Bingwei Wang, Jianping Liu*, Zhenghua Li, Yulong Xia, Shuangshuang Zhang and Ziyi Li

Volume 18, Issue 6, 2021

Published on: 23 November, 2020

Page: [712 - 720] Pages: 9

DOI: 10.2174/1567201817666201124113741

Price: $65

Abstract

Introduction: At present, there are numerous researches on the migration of components in tablets and granules, however, the investigation in the pharmaceutical literatures concerning the effect of drying rate on the migration of water-soluble components of pellets is limited. Temperature and Relative Humidity (RH) are crucial parameters during the drying process, which is an essential step in the preparation of pellets via wet extrusion/spheronization. To quantify these variables, the water loss percentage of pellets per minute is defined as the drying rate.

Aim: The study aimed to investigate the influence of drying rate on the migration of water-soluble components in wet pellets and the potential migrated mechanism.

Methods: The pellets containing tartrazine as a water-soluble model drug and microcrystalline cellulose as a matrix former were prepared by extrusion/spheronization and dried at four different drying temperatures and relative humidity. Afterwards, the extent of migrated tartrazine was assessed regarding appearance, in-vitro dissolution test, Differential Scanning Calorimetry, X-Ray Powder Diffraction, Attenuated total reflectance Fourier transform infrared spectroscopy and Confocal Raman Mapping.

Results: Results demonstrated that red spots of tartrazine appeared on the surface of pellets and more than 40% tartrazine were burst released within 5 minutes when pellets were dried at 60°C/RH 10%. When pellets were dried at 40°C/RH 80%, none of these aforementioned phenomena were observed.

Conclusion: In conclusion, the faster the drying rate was, the more tartrazine migrated to the exterior of pellets. Adjusting drying temperature and relative humidity appropriately could inhibit the migration of water-soluble components within wet extrusion/spheronization pellets.

Keywords: Migration, drying temperature, relative humidity, drying rate, wet extrusion/spheronization, pellets.

« Previous Next »
Graphical Abstract

[1]
Yokoyama, M.; Tourigny, M.; Moroshima, K.; Suzuki, J.; Sakai, M.; Iwamoto, K.; Takeuchi, H. A novel rapid quantitative analysis of drug migration on tablets using laser induced breakdown spectroscopy. Chem. Pharm. Bull. (Tokyo), 2010, 58(11), 1521-1524.
[http://dx.doi.org/10.1248/cpb.58.1521] [PMID: 21048347]
[2]
Kapsidou, T.; Nikolakakis, I.; Malamataris, S. Agglomeration state and migration of drugs in wet granulations during drying. Int. J. Pharm., 2001, 227(1-2), 97-112.
[http://dx.doi.org/10.1016/S0378-5173(01)00788-8] [PMID: 11564544]
[3]
Ansari, M.A.; Stepanek, F. Design of granule structure: Computational methods and experimental realization. AIChE J., 2006, 52(11), 3762-3774.
[http://dx.doi.org/10.1002/aic.10990]
[4]
Ansari, M.; Stepanek, F. The evolution of microstructure in three- component granulation and its effect on dissolution. Particul. Sci. Technol., 2007, 26(1), 55-66.
[http://dx.doi.org/10.1080/02726350701759274]
[5]
Dyer, A.; Khan, K.; Aulton, M. Effect of the drying method on the mechanical and drug release properties of pellets prepared by extrusion-spheronization. Drug Dev. Ind. Pharm., 1994, 20(20), 3045-3068.
[http://dx.doi.org/10.3109/03639049409041968]
[6]
Kataria, A.; Oka, S.; Smrčka, D.; Grof, Z.; Štěpánek, F.; Ramachandran, R. A quantitative analysis of drug migration during granule drying. Chem. Eng. Res. Des., 2018, 136, 199-206.
[http://dx.doi.org/10.1016/j.cherd.2018.05.001]
[7]
Huang, X.; Brazel, C.S. On the importance and mechanisms of burst release in matrix-controlled drug delivery systems. J. Control. Release, 2001, 73(2-3), 121-136.
[http://dx.doi.org/10.1016/S0168-3659(01)00248-6] [PMID: 11516493]
[8]
Li, G.; Han, D.; Guan, T.; Zhao, X.; He, H.; Tang, X. Isosorbide-5-mononitrate (5-ISMN) sustained-release pellets prepared by double layer coating for reducing 5-ISMN migration and sublimation. Int. J. Pharm., 2010, 400(1-2), 138-144.
[http://dx.doi.org/10.1016/j.ijpharm.2010.08.046] [PMID: 20826202]
[9]
Poutiainen, S.; Honkanen, M.; Becker, J.; Nachtweide, D.; Järvinen, K.; Ketolainen, J. X-ray microtomography analysis of intragranular drug migration during fluidized bed and oven tray drying. J. Pharm. Sci., 2012, 101(4), 1587-1598.
[http://dx.doi.org/10.1002/jps.23051] [PMID: 22228230]
[10]
Oka, S.; Smrčka, D.; Kataria, A.; Emady, H.; Muzzio, F.; Štěpánek, F.; Ramachandran, R. Analysis of the origins of content non-uniformity in high-shear wet granulation. Int. J. Pharm., 2017, 528(1-2), 578-585.
[http://dx.doi.org/10.1016/j.ijpharm.2017.06.034] [PMID: 28627457]
[11]
Armstrong, N.A.; March, G.A. Quantitative assessment of factors contributing to mottling of colored tablets II: Formulation variables. J. Pharm. Sci., 1976, 65(2), 200-204.
[http://dx.doi.org/10.1002/jps.2600650207] [PMID: 1255449]
[12]
Frohoff-Hülsmann, M.A.; Schmitz, A.; Lippold, B.C. Aqueous ethyl cellulose dispersions containing plasticizers of different water solubility and hydroxypropyl methylcellulose as coating material for diffusion pellets. I. Drug release rates from coated pellets. Int. J. Pharm., 1999, 177(1), 69-82.
[http://dx.doi.org/10.1016/S0378-5173(98)00327-5] [PMID: 10205604]
[13]
Warren, J.W., Jr; Price, J.C. Drug migration during drying of tablet granulations I: Effect of particle size of major diluent. J. Pharm. Sci., 1977, 66(10), 1406-1409.
[http://dx.doi.org/10.1002/jps.2600661014] [PMID: 925895]
[14]
Warren, J.W., Jr; Price, J.C. Drug migration during drying of tablet granulations II: Effect of binder solution viscosity and drying temperature. J. Pharm. Sci., 1977, 66(10), 1409-1412.
[http://dx.doi.org/10.1002/jps.2600661015] [PMID: 925896]
[15]
Kiekens, F.; Zelkó, R.; Remon, J.P. Influence of drying temperature and granulation liquid viscosity on the inter- and intragranular drug migration in tray-dried granules and compacts. Pharm. Dev. Technol., 2000, 5(1), 131-137.
[http://dx.doi.org/10.1081/PDT-100100528] [PMID: 10669927]
[16]
Katari, A. An analysis of drug migration during drying of granules as an underlying cause of content non-uniformity in wet granulation; Rutgers University-School of Graduate Studies, 2018.
[17]
Schrank, S.; Hodzic, A.; Zimmer, A.; Glasser, B.J.; Khinast, J.; Roblegg, E. Ibuprofen-loaded calcium stearate pellets: Drying-induced variations in dosage form properties. AAPS PharmSciTech, 2012, 13(2), 686-698.
[http://dx.doi.org/10.1208/s12249-012-9791-6] [PMID: 22552931]
[18]
Schrank, S.; Kann, B.; Saurugger, E.; Hainschitz, M.; Windbergs, M.; Glasser, B.J.; Khinast, J.; Roblegg, E. The effect of the drying temperature on the properties of wet-extruded calcium stearate pellets: Pellet microstructure, drug distribution, solid state and drug dissolution. Int. J. Pharm., 2015, 478(2), 779-787.
[http://dx.doi.org/10.1016/j.ijpharm.2014.12.030] [PMID: 25526671]
[19]
Kowalski, S.J. Toward a thermodynamics and mechanics of drying processes. Chem. Eng. Sci., 2000, 55(7), 1289-1304.
[http://dx.doi.org/10.1016/S0009-2509(99)00400-5]
[20]
Scherer, G.W. Theory of drying. J. Am. Ceram. Soc., 1990, 73(1), 3-14.
[http://dx.doi.org/10.1111/j.1151-2916.1990.tb05082.x]
[21]
Balaxi, M.; Nikolakakis, I.; Kachrimanis, K.; Malamataris, S. Combined effects of wetting, drying, and microcrystalline cellulose type on the mechanical strength and disintegration of pellets. J. Pharm. Sci., 2009, 98(2), 676-689.
[http://dx.doi.org/10.1002/jps.21454] [PMID: 18548618]
[22]
Schrank, S.; Kann, B.; Saurugger, E.; Ehmann, H.; Werzer, O.; Windbergs, M.; Glasser, B.J.; Zimmer, A.; Khinast, J.; Roblegg, E. Impact of drying on solid state modifications and drug distribution in ibuprofen-loaded calcium stearate pellets. Mol. Pharm., 2014, 11(2), 599-609.
[http://dx.doi.org/10.1021/mp4005782] [PMID: 24400735]
[23]
Kathe, K.; Kathpalia, H. Film forming systems for topical and transdermal drug delivery. Asian J Pharm Sci, 2017, 12(6), 487-497.
[http://dx.doi.org/10.1016/j.ajps.2017.07.004] [PMID: 32104362]
[24]
Sanghvi, S.P.; Nairn, J.G. A method to control particle size of cellulose acetate trimellitate microspheres. J. Microencapsul., 1993, 10(2), 181-194.
[http://dx.doi.org/10.3109/02652049309104384] [PMID: 8331492]
[25]
Diamante, L.; Munro, P. Mathematical modelling of hot air drying of sweet potato slices. Int. J. Food Sci. Technol., 1991, 26(1), 99-109.
[http://dx.doi.org/10.1111/j.1365-2621.1991.tb01145.x]
[26]
Doymaz, I.; Pala, M. Hot-air drying characteristics of red pepper. J. Food Eng., 2002, 55(4), 331-335.
[http://dx.doi.org/10.1016/S0260-8774(02)00110-3]
[27]
Fundueanu, G.; Nastruzzi, C.; Carpov, A.; Desbrieres, J.; Rinaudo, M. Physico-chemical characterization of Ca-alginate microparticles produced with different methods. Biomaterials, 1999, 20(15), 1427-1435.
[http://dx.doi.org/10.1016/S0142-9612(99)00050-2] [PMID: 10454015]
[28]
Shariff, A.; Pk, M.; Klk, P.; M, M. Entrapment of andrographolide in cross-linked alginate pellets: I. Formulation and evaluation of associated release kinetics. Pak. J. Pharm. Sci., 2007, 20(1), 1-9.
[PMID: 17337420]
[29]
Talukder, R.; Fassihi, R. Gastroretentive delivery systems: Hollow beads. Drug Dev. Ind. Pharm., 2004, 30(4), 405-412.
[http://dx.doi.org/10.1081/DDC-120030935] [PMID: 15132183]
[30]
Siepmann, J.; Siepmann, F.; Paeratakul, O.; Bodmeier, R. Process and formulation factors affecting drug release from pellets coated with Ethylcellulose pseudolatex Aquacoat. In: Aqueous Polymeric Coatings for Pharmaceutical Dosage Forms; CRC Press, UK, 2008, pp. 223-256.
[31]
Schrank, S.; Kann, B.; Windbergs, M.; Glasser, B.J.; Zimmer, A.; Khinast, J.; Roblegg, E. Microstructure of calcium stearate matrix pellets: A function of the drying process. J. Pharm. Sci., 2013, 102(11), 3987-3997.
[http://dx.doi.org/10.1002/jps.23707] [PMID: 23983150]
[32]
Chen, Q.; Bi, J.; Wu, X.; Yi, J.; Zhou, L.; Zhou, Y. Drying kinetics and quality attributes of jujube (Zizyphus jujuba Miller) slices dried by hot-air and short-and medium-wave infrared radiation. Lebensm. Wiss. Technol., 2015, 64(2), 759-766.
[http://dx.doi.org/10.1016/j.lwt.2015.06.071]
[33]
Liu, J.; Cao, F.; Zhang, C.; Ping, Q. Use of polymer combinations in the preparation of solid dispersions of a thermally unstable drug by hot-melt extrusion. Acta Pharm. Sin. B, 2013, 3(4), 263-272.
[http://dx.doi.org/10.1016/j.apsb.2013.06.007]
[34]
Davis, T.D.; Peck, G.E.; Stowell, J.G.; Morris, K.R.; Byrn, S.R. Modeling and monitoring of polymorphic transformations during the drying phase of wet granulation. Pharm. Res., 2004, 21(5), 860-866.
[http://dx.doi.org/10.1023/B:PHAM.0000026440.00508.cf] [PMID: 15180346]
[35]
Bondeson, D.; Mathew, A.; Oksman, K. Optimization of the isolation of nanocrystals from microcrystalline cellulose by acid hydrolysis. Cellulose, 2006, 13(2), 171.
[http://dx.doi.org/10.1007/s10570-006-9061-4]
[36]
Berggren, J.; Alderborn, G. Effect of drying rate on porosity and tabletting behaviour of cellulose pellets. Int. J. Pharm., 2001, 227(1-2), 81-96.
[http://dx.doi.org/10.1016/S0378-5173(01)00787-6] [PMID: 11564543]
[37]
Melegari, C.; Bertoni, S.; Genovesi, A.; Hughes, K.; Rajabi-Siahboomi, A.R.; Passerini, N.; Albertini, B. Ethylcellulose film coating of guaifenesin-loaded pellets: A comprehensive evaluation of the manufacturing process to prevent drug migration. Eur. J. Pharm. Biopharm., 2016, 100, 15-26.
[http://dx.doi.org/10.1016/j.ejpb.2015.12.001] [PMID: 26686647]
[38]
Ciolacu, D.; Ciolacu, F.; Popa, V.I. Amorphous cellulose—structure and characterization. Cellul. Chem. Technol., 2011, 45(1), 13.
[39]
Yu, Y.; Wu, H. Significant differences in the hydrolysis behavior of amorphous and crystalline portions within microcrystalline cellulose in hot-compressed water. Ind. Eng. Chem. Res., 2010, 49(8), 3902-3909.
[http://dx.doi.org/10.1021/ie901925g]
[40]
Prakash, S.; Jha, S.; Datta, N. Performance evaluation of blanched carrots dried by three different driers. J. Food Eng., 2004, 62(3), 305-313.
[http://dx.doi.org/10.1016/S0260-8774(03)00244-9]

Rights & Permissions Print Cite
Article Metrics
16
© 2024 Bentham Science Publishers | Privacy Policy