Solid dispersion melt crystallization (SDMC) concept using binary eutectic system for improvement of dissolution rate

Kentaro Atsukawa; Shuntaro Amari; Hiroshi Takiyama

Journal of Industrial and Engineering Chemistry, Vol.101, 21-27, September, 2021

DOI10.1016/j.jiec.2021.05.032 Export Citation

Solid dispersion melt crystallization (SDMC) concept using binary eutectic system for improvement of dissolution rate

Kentaro Atsukawa, Shuntaro Amari, and Hiroshi Takiyama^†

Department of Chemical Engineering, Tokyo University of Agriculture and Technology, 24-16, Nakacho-2, Koganei, Tokyo 184-8588, Japan

E-mail:

From the designs of product and industrial process perspectives, the solubility of a target material is one of the most valuable qualities. We proposed the ‘solid dispersion melt crystallization (SDMC) concept’ as a original strategy for dispersing a target material in a matrix one, in which the target material is naturally dispersed between the crevices formed by the matrix material precipitated first. Furthermore, the effects of introducing some operations, such as cooling, agitation and aeration, to the SDMC concept on the dissolution rate were investigated by a binary eutectic system. According to the experimental results, the dissolution rate was enhanced by the operations (cooling, agitation and aeration). This improvement in the dissolution rate was attributed to the SDMC concept-based enhancement of the nucleation rate. Therefore, it was revealed that an increase in the nucleation rate due to the SDMC concept had effectively improved the dissolution rate.

Keywords:Melt crystallization;Dissolution rate;Nucleation enhancement

[References]

Lipinski CA, J. Pharmacol. Tox. Met., 44, 235 (2000)
Jung MS, Kim JS, Kim MS, Alhalaweh A, Cho W, Hwang SJ, Velaga SP, J. Pharm. Pharmacol., 62, 1560 (2010)
Badgujar BP, Mundada AS, Acta Pharm., 61, 117 (2011)
Urai S, Kudo S, Takiyama H, Food Sci. Technol. Res., 26, 17 (2020)
Gui Y, Chen Y, Chen Z, Jones KJ, Yu L, Pharm. Res., 36, 67 (2019)
Sharma SK, Patel RP, J. Drug Deliv. Ther., 9, 57 (2019)
Nikam VJ, Patil SB, J. Cryst. Growth, 534 (2020)
Ali SF, Joshi M, Akhtar N, Sharma V, Pathak K, Pharm. Biomed. Res., 2, 23 (2016)
Huang S, Mao C, Williams RO, Yang CY, J. Pharm. Sci., 105, 3549 (2016)
Zaini E, Evert A, Octavia MD, Orient. J. Chem., 33, 2080 (2017)
Semjonov K, Kogermann K, Laidmae I, Antikainen O, Strachan CJ, Ehlers H, Yliruusi J, Heinamaki J, Eur. J. Pharm. Sci., 97, 237 (2017)
Peng T, She Y, Zhu C, Shi Y, Huang Y, Niu B, Bai X, Pan X, Wu C, AAPS PharmSciTech, 19, 2620 (2018)
Frank DS, Matzger AJ, Mol. Pharm., 15, 2714 (2018)
Zhu DH, Zograft G, Gao P, Gong YC, Zhang GGZ, J. Pharm. Sci., 105, 2932 (2016)
Liu X, Hu Y, Liu L, Su L, Li N, Yu J, Tang B, Yang Z, Pharm. Res., 35, 125 (2018)
Sousa LAE, Reutzel-Edens SM, Stephenson GA, Taylor LS, Cryst. Growth Des., 16, 737 (2016)
Wilson V, Lou X, Osterling DJ, Stolarik DF, Jenkins G, Gao W, Zhang GGZ, Taylor LS, J. Control. Release, 292, 172 (2018)
Prasad D, Chauhan H, Atef E, J. Pharm. Sci., 103, 3511 (2014)
Liu J, Grohganz H, Rades T, Int. J. Pharm., 588, 119768 (2020)
Sahoo A, Kumar NSK, Suryanarayanan R, J. Control. Release, 311-312, 212 (2019)
Chu KR, Lee E, Jeong SH, Park ES, Arch. Pharm. Res., 35, 1187 (2012)
Sotthivirat S, McKelvey C, Moser J, Rege B, Xu W, Zhang D, Int. J. Pharm., 452, 73 (2013)
Martinez LM, Videa M, Silva TL, Castro S, Caballero A, Lara-Diaz VJ, Castorena-Torres F, Eur. J. Pharm. Biopharm., 119, 243 (2017)
Alshehri SM, Shakeel F, Ibrahim MA, Elzayat EM, Altamimi M, Mohsin K, et al., Saudi Pharm. J., 27, 264 (2019)
Callister WD, Rethwisch DG, Material science and engineering: An introduction, 9th edn., Wiley, New Jersey, 2018.
Jawaid M, Boufi S, Abdul Khalil bin HPS, Cellulose-reinforced nanofibre composites, Massachusetts, 2017.
Wada Y, Matsumoto M, Onoe K, J. Cryst. Growth, 448, 76 (2016)
Ngo AN, Thomas D, Murowchick J, Ayon NJ, Jaiswal A, Youan BC, Int. J. Pharm., 545, 329 (2018)
Nadaf S, Jadhav A, Killedar S, Int. J. Biol. Macromol., 167, 345 (2021)
Perkkalainen P, Halttunen H, Pitkanen I, Thermochim. Acta, 269, 351 (1995)
Atsukawa K, Kudo S, Amari S, Takiyama H, J. Food Eng., 268 (2020)
Mullin JW, Crystallization, 4th ed, Butterworth-Heinemann, Oxford, 2001.
Cosic M, Pazin A, Celan A, Kuzmanic N, Chem. Eng. Trans., 74, 451 (2019)
Davey R, Garside J, From molecules to crystallizers: An introduction to crystallization, Oxford University Press, Oxford, 2000.
Capellades G, Kiil S, Dam-Johansen K, Mealy MJ, Christensen TV, Myerson AS, Cryst. Growth Des., 17, 3287 (2017)

[1] Lipinski CA, J. Pharmacol. Tox. Met., 44, 235 (2000)

[2] Jung MS, Kim JS, Kim MS, Alhalaweh A, Cho W, Hwang SJ, Velaga SP, J. Pharm. Pharmacol., 62, 1560 (2010)

[3] Badgujar BP, Mundada AS, Acta Pharm., 61, 117 (2011)

[4] Urai S, Kudo S, Takiyama H, Food Sci. Technol. Res., 26, 17 (2020)

[5] Gui Y, Chen Y, Chen Z, Jones KJ, Yu L, Pharm. Res., 36, 67 (2019)

[6] Sharma SK, Patel RP, J. Drug Deliv. Ther., 9, 57 (2019)

[7] Nikam VJ, Patil SB, J. Cryst. Growth, 534 (2020)

[8] Ali SF, Joshi M, Akhtar N, Sharma V, Pathak K, Pharm. Biomed. Res., 2, 23 (2016)

[9] Huang S, Mao C, Williams RO, Yang CY, J. Pharm. Sci., 105, 3549 (2016)

[10] Zaini E, Evert A, Octavia MD, Orient. J. Chem., 33, 2080 (2017)

[11] Semjonov K, Kogermann K, Laidmae I, Antikainen O, Strachan CJ, Ehlers H, Yliruusi J, Heinamaki J, Eur. J. Pharm. Sci., 97, 237 (2017)

[12] Peng T, She Y, Zhu C, Shi Y, Huang Y, Niu B, Bai X, Pan X, Wu C, AAPS PharmSciTech, 19, 2620 (2018)

[13] Frank DS, Matzger AJ, Mol. Pharm., 15, 2714 (2018)

[14] Zhu DH, Zograft G, Gao P, Gong YC, Zhang GGZ, J. Pharm. Sci., 105, 2932 (2016)

[15] Liu X, Hu Y, Liu L, Su L, Li N, Yu J, Tang B, Yang Z, Pharm. Res., 35, 125 (2018)

[16] Sousa LAE, Reutzel-Edens SM, Stephenson GA, Taylor LS, Cryst. Growth Des., 16, 737 (2016)

[17] Wilson V, Lou X, Osterling DJ, Stolarik DF, Jenkins G, Gao W, Zhang GGZ, Taylor LS, J. Control. Release, 292, 172 (2018)

[18] Prasad D, Chauhan H, Atef E, J. Pharm. Sci., 103, 3511 (2014)

[19] Liu J, Grohganz H, Rades T, Int. J. Pharm., 588, 119768 (2020)

[20] Sahoo A, Kumar NSK, Suryanarayanan R, J. Control. Release, 311-312, 212 (2019)

[21] Chu KR, Lee E, Jeong SH, Park ES, Arch. Pharm. Res., 35, 1187 (2012)

[22] Sotthivirat S, McKelvey C, Moser J, Rege B, Xu W, Zhang D, Int. J. Pharm., 452, 73 (2013)

[23] Martinez LM, Videa M, Silva TL, Castro S, Caballero A, Lara-Diaz VJ, Castorena-Torres F, Eur. J. Pharm. Biopharm., 119, 243 (2017)

[24] Alshehri SM, Shakeel F, Ibrahim MA, Elzayat EM, Altamimi M, Mohsin K, et al., Saudi Pharm. J., 27, 264 (2019)

[25] Callister WD, Rethwisch DG, Material science and engineering: An introduction, 9th edn., Wiley, New Jersey, 2018.

[26] Jawaid M, Boufi S, Abdul Khalil bin HPS, Cellulose-reinforced nanofibre composites, Massachusetts, 2017.

[27] Wada Y, Matsumoto M, Onoe K, J. Cryst. Growth, 448, 76 (2016)

[28] Ngo AN, Thomas D, Murowchick J, Ayon NJ, Jaiswal A, Youan BC, Int. J. Pharm., 545, 329 (2018)

[29] Nadaf S, Jadhav A, Killedar S, Int. J. Biol. Macromol., 167, 345 (2021)

[30] Perkkalainen P, Halttunen H, Pitkanen I, Thermochim. Acta, 269, 351 (1995)

[31] Atsukawa K, Kudo S, Amari S, Takiyama H, J. Food Eng., 268 (2020)

[32] Mullin JW, Crystallization, 4th ed, Butterworth-Heinemann, Oxford, 2001.

[33] Cosic M, Pazin A, Celan A, Kuzmanic N, Chem. Eng. Trans., 74, 451 (2019)

[34] Davey R, Garside J, From molecules to crystallizers: An introduction to crystallization, Oxford University Press, Oxford, 2000.

[35] Capellades G, Kiil S, Dam-Johansen K, Mealy MJ, Christensen TV, Myerson AS, Cryst. Growth Des., 17, 3287 (2017)