This study was aimed at developing a new, technically simple method for the preparation of a once-daily sustained release matrix formulations, which would enable reproducible release of the active ingredient. Thermoplastic granulation is a new technique in pharmaceutical formulation. Coated particles of an active pharmaceutical ingredient (API) in sustained release matrix are prepared by thermoplastic granulation technique via heating (50 – 75°C) in fluid-bed dryer (FBD) granulator. The FBD creates ideal conditions for the most intense heat and mass transfer by spraying melted liquids onto the granular API. A variety of innovative processes such as granulation, agglomeration, coating and microencapsulation can be realized. Melted mixture of cetyl alcohol, glyceryl monostearate, and polyethylene glycol 4000 (PEG 4000) was used for fluid-bed coating. The present article deals with assessing the influence of rheological properties and hydrophile-lipophile balance (HLB) parameter of thermoplastic granules on the mechanism of drug delivery from sustained release matrix in solid dosage forms. The drug release kinetics model is affected by rheology, HLB of cetyl alcohol, and physicochemical properties of API granules.
Similar content being viewed by others
References
Y. Haramiishi, Y. Kitazawa, M. Sakai, et al., J. Pharm. Soc. Jpn., 111(9), 515 – 523 (1991).
M. Karl, D. Djuric, and K. Kolter, Pharm. Technol., 35(5), 74 – 82 (2011).
J. Kowalski, O. Kalb, Y. M. Joshi, and A. T. Serajuddin, Int. J. Pharm., 381(1), 56 – 61 (2009).
T. Maejima, M. Kubo, T. Osawa, et al., Chem. Pharm. Bull., 46(3), 534 – 536 (1998).
T. Maejima, T. Osawa, K. Nakajima, and M. Kobayashi, Chem. Pharm. Bull., 46(3), 531 – 533 (1998).
N. Passerini, G. Calogera, B. Albertini, and L. Rodriguez, Int. J. Pharm., 391(1 – 2), 177 – 186 (2010).
J. P. Lakshman, J. Kowalski, M. Vasanthavada, et al., J. Pharm. Sci., 100(4), 1553 – 1565 (2011).
R. R. Panda and A. K. Tiwary, Drug Dev. Ind. Pharm., 38(4), 447 – 461 (2012).
J. Kowalski, O. Kalb, Y. M. Joshi, and A. T. Serajuddin, Int. J. Pharm., 381(1), 56–61 (2009).
S. Shah, S. Maddineni, J. Lu, and M. A. Repka, Int. J. Pharm., 453(1), 233–252 (2013).
T. Abberger, Pharmazie, 56(12), 949 – 952 (2001).
T. Abberger and J. O. Henck, Pharmazie, 55(7), 521 – 526 (2000).
B. Van Melkebeke, B. Vermeulen, C. Vervaet, and J. P. Remon, Int. J. Pharm., 326(1 – 2), 89–93 (2006).
K. Dvorácková, M. Rabisková, R. Masteiková, and L. Vocilková, Ceska Slov. Farma., 56(3), 129 – 134 (2007).
X. Chen, H.Wen, and K. Park, in: Oral Controlled Release Formulation Design and Drug Delivery: Theory to Practice, M. Morra (Ed.), John Wiley & Sons: New Jersey: (2010), pp. 257 – 277.
J. S. Grundy and R. T. Foster, Clin. Pharmacokinet., 30(1), 28 – 51 (1996).
M. Levina and A. R. Rajabi-Siahboomi, J. Pharm. Sci., 93(11), 2746 – 2754 (2004).
B. Abrahamsson, T. Albery, A. Eriksson, et al., Eur. J. Pharm. Sci., 22(2 – 3), 165 – 172 (2004).
P. Colombo, Adv. Drug Deliv. Rev., 11(1 – 2), 37 – 57 (1993).
N. A. Peppas, P. Buresa,W. Leobandung, and H. Ichikawa, Eur. J. Pharm. Biopharm., 50(1), 27 – 46 (2000).
J. Siepmann and N. A. Peppas, Pharm. Res., 17(10), 1290 – 1298 (2000).
S. B. Tiwari and A. R. Rajabi-Siahboomi, Pharm. Technol. Eur., 1, 1 – 8 (2008).
Handbook of Pharmaceutical Granulation Technology, D. M. Parikh (Ed.), CRC Press (2016).
M. G. A. Vieira, M. A. da Silva, L. O. dos Santos, and M. M. Beppu, Eur. Polym. J., 47(3), 254 – 263 (2011).
J. Liu, F. Cao, C. Zhang, and Q. Ping, Acta Pharm. Sin. B, 3(4), 263 – 272 (2013).
E. Snejdrova and M. Dittrich, in: Recent Advances in Plasticizers, InTech (2012).
M. Rahman and C.S. Brazel, Progr. Polym. Sci., 29(12), 1223 – 1248 (2004).
S. Pole, S. Maurya, P. Hasnale, et al., Eur. J. Pharm. Med. Res., 3(4), 135 – 144 (2016).
US Pharmacopeia 38 / National Formulary 33, US Pharmacopoeial Convention Inc.: Rockville, MD (2014).
S. Nainar, K. Rajiah, S. Angamuthu, et al., Tropical J. Pharm. Res., 11(2), 319 – 329 (2012)
P. C Sharma, Production Technology (Manufacturing Processes), S. Chand Publishing (2007), pp. 605 – 610.
J. M. Newton, S. Boutel, J. Chatchawalsaisin, and F. Podczeck, Pharm. Technol. Eur., 16(10), 21 – 27 (2004).
R. S. Langer and N. A. Peppas, Biomaterials, 2(4), 201 – 214 (1981).
Applications of Polymers in Drug Delivery, A. Misra (Ed.), Smithers Rapra (2014).
C.S. Brazel and S. L. Rosen, Fundamental Principles of Polymeric Materials, John Wiley & Sons (2012).
C. Maderuelo, A. Zarzuelo, J. M. Lanao, J. Controlled Release, 154, 2 – 19 (2011).
A. Nokhodchi, S. Raja, and P. Patel, Bioimpacts (BI), 2(4), 175 – 187 (2012).
M. U. Ghori and B. R. Conway, Am. J. Pharmacol. Sci., 3(5), 103 – 109 (2015).
Acknowledgments
The author would like to acknowledge FANDA Pharmaceutical Co, for kindly providing gift samples of diclofenac sodium and carbamazepine powder.
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Pourmand, M.R., Shariat, F.P. & Ardjmand, M. Evaluation of Lipophilic Properties of Thermoplastic Granule in Formulation of Sustained Release Matrix in Solid Dosage Forms. Pharm Chem J 53, 660–667 (2019). https://doi.org/10.1007/s11094-019-02058-0
Received:
Published:
Issue Date:
DOI: https://doi.org/10.1007/s11094-019-02058-0