scholarly journals Enhancing solubility and antibacterial activity using multi-component crystals of trimethoprim and malic acid

2021 ◽  
pp. 296-304
Author(s):  
Yori Yuliandra ◽  
Limson Jaya Hutabarat ◽  
Resty Ardila ◽  
Maria Dona Octavia ◽  
Erizal Zaini

Aim: To improve the solubility and antibacterial activity of trimethoprim (TMP) by preparing its multicomponent crystals with malic acid (MA). Methods: Multicomponent crystals of TMP-MA were prepared by solvent co-evaporation. The solid-state properties were characterised by powder X-ray diffraction (PXRD), differential thermal analysis (DTA), Fourier transform infrared (FT-IR) spectroscopy, and scanning electron microscopy (SEM) analyses. The solubility was investigated in an aqueous medium, while the antibacterial activity against Escherichia coli was investigated using the agar disk diffusion method. Results: The PXRD pattern of the TMP-MA binary system differed from the starting materials, supporting the formation of a new crystalline phase (equimolar ratio). The DTA thermogram showed a single, sharp, endothermic peak at 212.5 °C attributable to the TMP-MA multicomponent crystal's melting point. FT-IR spectroscopy showed a solid-state interaction involving proton transfer between TMP and MA. The multicomponent crystal displayed a 2.5-fold higher solubility and had increased antibacterial activity compared to TMP alone. Conclusions: The TMP-MA binary system forms salt-type multicomponent crystals that significantly increase solubility and antibacterial activity. Multicomponent crystal formation is a viable technique for modifying the physicochemical properties of active pharmaceutical ingredients.

Author(s):  
Emilia Bramanti ◽  
Donata Catalano ◽  
Claudia Forte ◽  
Mario Giovanneschi ◽  
Massimo Masetti ◽  
...  

2016 ◽  
Vol 9 (6) ◽  
pp. 2483-2495 ◽  
Author(s):  
Chris Reed ◽  
Charlotte A. Brumby ◽  
Leigh R. Crilley ◽  
Louisa J. Kramer ◽  
William J. Bloss ◽  
...  

Abstract. Nitrous acid (HONO) has been quantitatively measured in situ by differential photolysis at 385 and 395 nm, and subsequent detection as nitric oxide (NO) by the chemiluminescence reaction with ozone (O3). The technique has been evaluated by Fourier transform infrared (FT-IR) spectroscopy to provide a direct HONO measurement in a simulation chamber and compared side by side with a long absorption path optical photometer (LOPAP) in the field. The NO–O3 chemiluminescence technique is robust, well characterized, and capable of sampling at low pressure, whilst solid-state converter technology allows for unattended in situ HONO measurements in combination with fast time resolution and response.


1988 ◽  
Vol 110 (6) ◽  
pp. 1801-1810 ◽  
Author(s):  
Thomas. Bein ◽  
Stephan J. McLain ◽  
David R. Corbin ◽  
Rodney D. Farlee ◽  
Karin. Moller ◽  
...  

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