The feasibility of coating by cooling crystallization on ibuprofen naked tablets

doi:10.1007/s11705-017-1619-1

Front. Chem. Sci. Eng.

2017, Vol. 11

Issue (2) : 211-219 https://doi.org/10.1007/s11705-017-1619-1

RESEARCH ARTICLE

The feasibility of coating by cooling crystallization on ibuprofen naked tablets

Fatima Mameri¹(

), Ouahiba Koutchoukali¹(

), Mohamed Bouhelassa¹, Anne Hartwig², Leila Nemdili¹, Joachim Ulrich²

¹. University Constantine 3, Engineering Faculty of Pharmaceutical Processes, 25000 Constantine, Algeria
². Martin Luther University Halle-Wittenberg, Center of Engineering Science, Thermal Process Engineering, D-06099 Halle, Germany

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Abstract

Sugar spray coating is a frequently used process in the pharmaceutical industry. However, this process presents the disadvantage to form an amorphous coating around the active ingredient. A crystalline coating formed on the surface of a tablet is highly desirable. Recently, a new process of coating by cooling crystallization has been developed and applied on bisacodyl pastilles obtained by melt crystallization. In this work, we investigated the feasibility of coating by cooling crystallization on ibuprofen “naked tablets” manufactured by compression. In the first part of this work, the solubility and the metastable zone width have been determined experimentally for the coating solution because they are essential factors for any crystallization process. In the second part, the coating process is investigated on the operating conditions that affect the surface morphology and the crystal growth rate. These experimental conditions include concentration of the coating solution, degree of sub-cooling, agitation speed, retention time, and surface properties of the naked ibuprofen tablets. The results show that naked tablet coating by cooling crystallization is feasible and can be applied in the pharmaceutical industry.

Keywords coating solution crystallization ibuprofen tablets sucrose

Corresponding Author(s): Fatima Mameri,Ouahiba Koutchoukali

Just Accepted Date: 03 January 2017 Online First Date: 15 February 2017 Issue Date: 12 May 2017

Cite this article:

Fatima Mameri,Ouahiba Koutchoukali,Mohamed Bouhelassa, et al. The feasibility of coating by cooling crystallization on ibuprofen naked tablets[J]. Front. Chem. Sci. Eng., 2017, 11(2): 211-219.

URL:

https://academic.hep.com.cn/fcse/EN/10.1007/s11705-017-1619-1
https://academic.hep.com.cn/fcse/EN/Y2017/V11/I2/211

Fig.1 Contact angle between supersaturated sucrose solution and the used seed material

Fig.2 Schematic diagram of experimental setup

Fig.3 (a) Thesolubility of sucrose by refractometer versus temperature and (b) the metastable zone width of the binary system sucrose-water versus temperature by turbidity at an agitation speed of 250 r/min, and a cooling and heating rate of 0.1 K/min

Fig.4 Viscosity of saturated sucrose solutions versus temperature at a shear rate of 100 min^–1 and a cooling rate of 0.1 K/min. (a) Viscosity of supersaturated sucrose solution versus temperature for different degree of sub-cooling starting from saturation concentration at 50 °C; (b) viscosity of saturated sucrose solutions versus different saturation concentrations

Fig.5 Contact angle and surface tension as function of different supersaturated sucrose concentration: (a) Contact angle at different surface characteristics, (b) Surface tension of supersaturated sucrose at a degree of sub-cooling 10 K

Fig.6 Growth rates and surface morphologies of seed particles and their coatings: (a) coated ibuprofen tablet, and (b) coated glass beads. Operating conditions: concentration of coating material 72.36 wt-%, degree of sub-cooling 10 K, agitation speed 200 r/min, retention time 180 min, and spatial resolution (100)

Fig.7 Growth rates of sucrose on ibuprofen naked tablets versus retention time at (a) different concentrations and (b) different degree of sub-cooling

Fig.8 Growth rate versus sucrose supersaturation on the surface of ibuprofen naked tablet

Fig.9 Microscope images of the coated surface versus retention times at optimal operating conditions, spatial resolution (100)

Fig.10 (a) An SEM image of the external surface morphology of a final coated ibuprofen tablet at spatial resolution (100); (b) A microscope image of a coated ibuprofen cross section: (b1) thickness of coating, and (b2) cross section of naked ibuprofen; (c) A microscope image of crystal morphology of coated surface

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