For Libraries For Publication Open Access Downloads About Us Contact Us
Paper Titles
Magnetocaloric Effect of Ni44Co6Mn40CuxSn10-x Quinary Alloy Comes from the Martensitic Transformation
p.17
First-Principle Study of Effect of Strain on the Band Structure of Germanane Monolayer
p.25
Temperature Dependence of Commensurate Magnetic Resonance in Cuprate Superconductors
p.31
V-Defect and Dislocation Analysis in InGaN Multiple Quantum Wells on Patterned Sapphire Substrate
p.37
The Effect of Compression Force on Alteration of Desloratadine and its Multicomponent Crystal Crystallinities Using X-Ray Diffraction and ATR-FTIR Techniques
p.43
First Principles Study on Magnetic and Optical Properties of Single Layer CrSi2
p.53
Input Interface for all Spin Logic
p.61
Proposal and Demonstration of GaN-Based Normally-Off Vertical Field-Effect Transistor with a Design of Back Current Block Layer
p.69
The Unique Property in Magnetic Noise of Spin Modulated Atomic Magnetometer
p.75

The Effect of Compression Force on Alteration of Desloratadine and its Multicomponent Crystal Crystallinities Using X-Ray Diffraction and ATR-FTIR Techniques

Article Preview

Abstract:

This work studied the effect of compression force on the desloratadine (DES) and its multi-component crystal (MCC) formulation and focused on the molecular crystal behavior of DES and MCC after compression. Crystallinity behavior of drugs in a mechanical process is to be interesting manner. In this research, DES and MCC were compressed using hydraulic presser equipped with 13 mm flat-face punch under different compression pressures in a range of 25 – 350 MPa. The solid state of DES and its MCC was evaluated using powder X-ray diffraction (XRD) and attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy. Single XRD was carried out to confirm the molecular structure of crystal lattice. Powder XRD diffractogram under different compression forces was compared to the crystallinity degree, crystallite size and peak broadening. Those parameters were processed using Origin software. Crystallinity degree was calculated using Ruland’s methods, meanwhile, the crystallinity size was calculated using Scherrer’s equation after corrected to the broadening (full width at half maximum; FWHM) and diffraction baseline. As increasing the compression force, degree and size of crystallinity and FWHM were altered. In addition, the degree of crystallinity and crystallite size of DES and MCC decreased, while the FWHM increased. Furthermore, alteration of PXRD in DES was higher than that of MCC which had no alteration as increase as the compression force. FTIR result showed that neither DES nor MCC had no significant alteration after compression. However, the tabletability of MCC was better than DES owing to the potential slip plane of MCC.

You might also be interested in these eBooks
Recent Advances in Condensed Matter Physics View Preview

Info:

Periodical:

Key Engineering Materials (Volume 787)

Pages:

43-51

DOI:

https://doi.org/10.4028/www.scientific.net/KEM.787.43

Citation:

Cite this paper

Online since:

November 2018

Authors:

Ahmad Ainurofiq*, Rachmat Mauludin, Diky Mudhakir, Arif Budi Setianto, Sundani Nurono Soewandhi

Keywords:

Compression Force, Crystallinity Determination, Desloratadine, FTIR, Multicomponent Crystal, XRD

Export:

RIS, BibTeX

Price:

Permissions CCC:

Request Permissions

Permissions PLS:

Request Permissions

Сopyright:

© 2018 Trans Tech Publications Ltd. All Rights Reserved

Share:

Citation:

* - Corresponding Author

References

[1] R.Bandyopadhyay, J. Selbo, G. E. Amidon and M. Hawley, Application of Powder X-ray Diffraction in Studying the Compaction Behavior of Bulk Pharmaceutical Powders, J. Pharm. Sci. 94 (2005) 2520–2530.

DOI: 10.1002/jps.20415

Google Scholar

[2] T. Feng, R. Pinal and M. T. Carvajal, Process Induced Disorder in Crystalline Materials:Differentiating Defective Crystals from the Amorphous Form of Griseofulvin, J. Pharm. Sci. 97 (2008) 3207–3221.

DOI: 10.1002/jps.21219

Google Scholar

[3] I. Tho and A. Bauer-Brandl, Quality by design (QbD) approaches for the compression step of tableting, Expert Opin. Drug Deliv. 8 (2011) 1631–1644.

DOI: 10.1517/17425247.2011.633506

Google Scholar

[4] N. K. Thakral, S. Mohapatra, G. A. Stephenson and R. Suryanarayanan, Compression-Induced Crystallization of Amorphous Indomethacin in Tablets: Characterization of Spatial Heterogeneity by Two-Dimensional X-ray Diffractometry, Mol. Pharm. 12 (2015).

DOI: 10.1021/mp5005788

Google Scholar

[5] M. Morita and S. Hirota, Estimation of the Degree of Crystallinity and the Disorder Parameter in a Drug by an X-Ray Diffraction Method with a Single Sample, Chem. Pharm. Bull. (Tokyo) 30 (1982) 3288–3296.

DOI: 10.1248/cpb.30.3288

Google Scholar

[6] M. Otsuka, F. Kato and Y. Matsuda, Comparative evaluation of the degree of indomethacin crystallinity by chemoinfometrical fourie-transformed near-infrared spectroscopy and conventional powder X-ray diffractiometry, AAPS PharmSci 2 (2000) 80–87.

DOI: 10.1208/ps020109

Google Scholar

[7] K. Nikowitz, A. Domján, K. Pintye-Hódi and G. Regdon, Multivariate calibration of the degree of crystallinity in intact pellets by X-ray powder diffraction, Int. J. Pharm. 502 (2016) 107–116.

DOI: 10.1016/j.ijpharm.2016.02.018

Google Scholar

[8] P. Kommavarapu, A. Maruthapillai, R. Allada, K. Palanisamy and P. Chappa, Simultaneous estimation of degree of crystallinity in combination drug product of abacavir, lamivudine and neverapine using X-ray powder diffraction technique, J. Young Pharm. 5 (2013).

DOI: 10.1016/j.jyp.2013.10.003

Google Scholar

[9] M. Colombo, S. Orthmann, M. Bellini, S. Staufenbiel and R. Bodmeier, Influence of Drug Brittleness, Nanomilling Time, and Freeze-Drying on the Crystallinity of Poorly Water-Soluble Drugs and Its Implications for Solubility Enhancement, AAPS PharmSciTech 18 (2017).

DOI: 10.1208/s12249-017-0722-4

Google Scholar

[10] T. D. Davis, K. R. Morris, H. Huang, G. E. Peck, J. G. Stowell, B. J. Eisenhauer, J. L. Hilden, D. Gibson and S. R. Byrn, In situ Monitoring of Wet Granulation Using Online X-Ray Powder Diffraction, Pharm. Res. 20 (2003) 1851–1857.

DOI: 10.1023/b:pham.0000003385.20030.9a

Google Scholar

[11] E. Räsänen, J. Rantanen, A. Jørgensen, M. Karjalainen, T. Paakkari and J. Yliruusi, Novel identification of pseudopolymorphic changes of theophylline during wet granulation using near infrared spectroscopy, J. Pharm. Sci. 90 (2001) 389–396.

DOI: 10.1002/1520-6017(200103)90:3<389::aid-jps13>3.0.co;2-9

Google Scholar

[12] J. C. Anthes, H. Gilchrest, C. Richard, S. Eckel, D. Hesk, R. E. West, S. M. Williams, S. Greenfeder, M. Billah, W. Kreutner and R. E. Egan, Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor, Eur. J. Pharmacol. 449 (2002).

DOI: 10.1016/s0014-2999(02)02049-6

Google Scholar

[13] A. Ainurofiq, R. Mauludin, D. Mudhakir and S. N. Soewandhi, Synthesis, characterization, and stability study of desloratadine multicomponent crystal formation, Res. Pharm. Sci. 13 (2018) 93–102.

DOI: 10.4103/1735-5362.223775

Google Scholar

[14] A. Ainurofiq, R. Mauludin, D. Mudhakir, D. Umeda, S. N. Soewandhi, O. D. Putra and E. Yonemochi, Improving mechanical properties of desloratadine via multicomponent crystal formation, Eur. J. Pharm. Sci. 111 (2018) 65–72.

DOI: 10.1016/j.ejps.2017.09.035

Google Scholar

[15] S.-Y. Chang and C. C. Sun, Superior Plasticity and Tabletability of Theophylline Monohydrate, Mol. Pharm. 14 (2017) 2047–(2055).

DOI: 10.1021/acs.molpharmaceut.7b00124

Google Scholar

[16] S. Bhadra and D. Khastgir, Determination of crystal structure of polyaniline and substituted polyanilines through powder X-ray diffraction analysis, Polym. Test. 27 (2008) 851–857.

DOI: 10.1016/j.polymertesting.2008.07.002

Google Scholar

[17] E. Fukuoka, M. Makita and S. Yamamura, Preferred Orientation of Crystallites in Tblets. III. Variations of Crystallinity and Crystallite Size of Pharmaceuticals with Compression, Chem. Pharm. Bull. (Tokyo) 41 (1993) 595–598.

DOI: 10.1248/cpb.41.595

Google Scholar

[18] M. C. Burla, R. Caliandro, M. Camalli, B. Carrozzini, G. L. Cascarano, L. De Caro, C. Giacovazzo, G. Polidori and R. Spagna, SIR2004: an improved tool for crystal structure determination and refinement, J. Appl. Crystallogr. 38 (2005) 381–388.

DOI: 10.1107/s002188980403225x

Google Scholar

[19] G. M. Sheldrick, A short history of SHELX, Acta Crystallogr. A 64 (2008) 112–122.

Google Scholar

[20] C. F. Macrae, I. J. Bruno, J. A. Chisholm, P. R. Edgington, P. McCabe, E. Pidcock, L. Rodriguez-Monge, R. Taylor, J. van de Streek and P. A. Wood, Mercury CSD 2.0 – new features for the visualization and investigation of crystal structures, J. Appl. Crystallogr. 41 (2008).

DOI: 10.1107/s0021889807067908

Google Scholar

[21] S. Park, J. O. Baker, M. E. Himmel, P. A. Parilla and D. K. Johnson, Cellulose crystallinity index: measurement techniques and their impact on interpreting cellulase performance, Biotechnol. Biofuels 3 (2010) 10.

DOI: 10.1186/1754-6834-3-10

Google Scholar

[22] E. Fukuoka, M. Makita and S. Yamamura, Pattern Fitting Procedure for the Characterization of Crystals and/or Crystallities in Tablets, Chem. Pharm. Bull. (Tokyo) 41 (1993) 2166–2171.

DOI: 10.1248/cpb.41.2166

Google Scholar

[23] S. Aitipamula, A. B. H. Wong, P. S. Chow and R. B. H. Tan, Pharmaceutical Salts of Haloperidol with Some Carboxylic Acids and Artificial Sweeteners: Hydrate Formation, Polymorphism, and Physicochemical Properties, Cryst. Growth Des. 14 (2014).

DOI: 10.1021/cg500245e

Google Scholar

[24] P. M. Bhatt and G. R. Desiraju, Form I of desloratadine, a tricyclic antihistamine, Acta Crystallogr. C 62 (2006) o362-363.

DOI: 10.1107/s0108270106012571

Google Scholar

[25] P. P. Bag, M. Chen, C. C. Sun and C. M. Reddy, Direct correlation among crystal structure, mechanical behaviour and tabletability in a trimorphic molecular compound, CrystEngComm 14 (2012) 3865–3867.

DOI: 10.1039/c2ce25100k

Google Scholar

[26] S. Chattoraj, L. Shi and C. C. Sun, Understanding the relationship between crystal structure, plasticity and compaction behaviour of theophylline, methyl gallate, and their 1:1 co-crystal, CrystEngComm 12 (2010) 2466.

DOI: 10.1039/c000614a

Google Scholar

[27] E. Supuk, M. U. Ghori, K. Asare-Addo, P. R. Laity, P. M. Panchmatia and B. R. Conway, The influence of salt formation on electrostatic and compression properties of flurbiprofen salts, Int. J. Pharm. 458 (2013) 118–127.

DOI: 10.1016/j.ijpharm.2013.10.004

Google Scholar

© 2025 Trans Tech Publications Ltd. All rights are reserved, including those for text and data mining, AI training, and similar technologies. For open access content, terms of the Creative Commons licensing CC-BY are applied.
Scientific.Net is a registered trademark of Trans Tech Publications Ltd.