Development of Nifedipine Amorphous Solid Dispersion Composed of Surface-Active Agents

Article Preview

Abstract:

The amorphous solid dispersions (ASDs) containing amino methacrylate copolymer and surface-active agents were prepared to improve the nifedipine (NDP) dissolution. The different types of surface-active agent i.e., polysorbates 80, sodium lauryl sulfate (SLS) and polyethylene glycol (PEG) 400 were used. In order to evaluate the ASDs formulation,powder X-ray diffractometry and thermal analysis to characterize NDP crystallinity in ASDs and the dissolution study of NDP have been performed to compare the dissolution profiles. The ASDs were kept for 6 months to investigate the stability. In the X-ray diffraction pattern, no peak was observed in all samples of ASDs. No peak was found in sample of all ASDs from the thermograms. These results suggest that the drug may be molecularly dispersed in matrix of amino methacrylate copolymer. The drug dissolution at 120 min, from ASDs without surface-active agent and NDP powder were 58.31% and 17.95%, respectively. The dissolved NDP from ASDs composed of SLS, polysorbate 80 and PEG400 were 96.25%, 88.86% and 75.32%, respectively. These results may occur due to the reduction of surface tension, the addition of the low amount of high efficiency of surface-active agent e.g., SLS (compared with PEG400 and polysorbate 80) provided the higher NDP dissolution. The content analysis of NDP in selected ASDs was studied at the end of 3 and 6 months, the NDP content remained unchanged after storage.

You might also be interested in these eBooks

Info:

Periodical:

Pages:

35-39

Citation:

Online since:

October 2021

Export:

Price:

Permissions CCC:

Permissions PLS:

Сopyright:

© 2021 Trans Tech Publications Ltd. All Rights Reserved

Share:

Citation:

* - Corresponding Author

[1] X. Ma, R. O. Williams, Characterization of amorphous solid dispersions: An update, J. Drug. Deliv. Sci. Technol. 50 (2019) 113–124.

Google Scholar

[2] D.J. Jang, T. Sim, E. Oh, Formulation and optimization of spray-dried amlodipine solid dispersion for enhanced oral absorption, Drug Dev. Ind. Pharm. 39 (2013) 1133–1141.

DOI: 10.3109/03639045.2012.723218

Google Scholar

[3] P. Tran, Y.C. Pyo, D.H. Kim, S.E. Lee, J.K. Kim, J.S. Park, Overview of the manufacturing methods of solid dispersion technology for improving the solubility of poorly water-soluble drugs and application to anticancer drugs, Pharmaceutics. 11 (2019).

DOI: 10.3390/pharmaceutics11030132

Google Scholar

[4] J. Akbari, M.Saeedi, K. Morteza-Semnani, H. R. Kelidari, F. S. Moghanlou, G. Zareh, S. Rostamkalaei, F. Sadegh Moghanlou, G. Zareh, S. Rostamkalaei, The effect of tween 20, 60, and 80 on dissolution behavior of sprionolactone in solid dispersions prepared by PEG 6000, Adv. Pharm. Bull. 5 (2015) 435–441.

DOI: 10.15171/apb.2015.059

Google Scholar

[5] D. Feng, T. Peng,Z. Huang,V. Singh, Y. Shi, T. Wen, M. Lu, G. Quan, X. Pan, C. Wu, Polymer–surfactant system based amorphous solid dispersion: Precipitation inhibition and bioavailability enhancement of itraconazole, Pharmaceutics.10 (2018).

DOI: 10.3390/pharmaceutics10020053

Google Scholar

[6] A. Raha, A. Bagchi, P. Mukherjee, M. Paul, Study of the Effect of co-solvent on the critical micelle concentration (CMC) of sodium lauryl sulphate study of the effect of co-solvent on the critical micelle concentration (CMC) of sodium lauryl sulphate, Int. J. Recent Adv. Pharm. Res. 6 (2016) 122–127.

DOI: 10.1039/tf9555100728

Google Scholar

[7] L.B. Vieira, M.W. Casimiro, R.G. Santos, Surface tension of aqueous amoxicillin + peg systems, Colloids Interface Sci. Commun. 24, (2018) 93–97.

DOI: 10.1016/j.colcom.2018.04.006

Google Scholar

[8] S.C. Kothekar, A.M. Ware, J.T. Waghmare, S.A. Momin, Comparative analysis of the properties of Tween-20, Tween-60, Tween-80, Arlacel-60, and Arlacel-80, J. Dispers. Sci. Technol. 28 (2007) 477–484.

DOI: 10.1080/01932690601108045

Google Scholar

[9] M. Minhaz, M. Rahman, M. Ahsan, A. Khalipha, M. Chowdhury, Dissolution enhancement of poorly soluble drug by solvent evaporation method using hydrophilic polymer: a solid dispersion technique, Int. J. Pharm. Life Sci. 1 (2012).

DOI: 10.3329/ijpls.v1i2.12952

Google Scholar

[10] M.H.G. Dehghana, J. Mohammad, Improving dissolution of meloxicam using solid dispersions, Iran. J. Pharm. Res. 5 (2006) 231–238.

Google Scholar

[11] D.Q.M. Craig, The mechanisms of drug release from solid dispersions in water-soluble polymers, Int. J. Pharm. 231 (2002) 131–144.

DOI: 10.1016/s0378-5173(01)00891-2

Google Scholar