Albendazole is an effective antihelmintic drug, which has an unpredictable therapeutic response due to its low solubility in biological fluids that limits its oral absorption. In an attempt to improve solubility, albendazole hydrochloride, a soluble pharmaceutical salt, was obtained and characterized by X-ray diffraction together with magic angle spinning solid-state nuclear magnetic resonance spectroscopy, Raman and Fourier transform infrared spectroscopies, thermal analysis, energy-dispersive X-ray spectroscopy, and scanning electron microscopy. These studies revealed that the crystalline habit of albendazole hydrochloride is different from that of the albendazole solid forms previously reported. The full structure was elucidated by performing single-crystal X-ray diffraction. The characterization studies showed the participation of the carbamate moiety in the salt formation. In addition, the solubility studies showed a significant increase in the solubility with respect to forms I and II of albendazole. In conclusion, our results indicate that albendazole hydrochloride can be an auspicious salt to be used as a new product in an attempt to counteract unfavorable pharmaceutical properties.
Aim: A solid self-emulsifying drug delivery systems was developed by using the spray-drying technique, to improve the solubility of resveratrol (RES). Materials & methods: Cod liver oil and three surfactant system were tested: soy phosphatidylcholine (SPC)/Eumulgin® HRE-40 (EU)/Sodium oleate (system A); SPC/Tween®80 (TW) /Sodium oleate (system B) and SPC/EU/TW (system C). Results: The greatest incorporation was obtained with system C (21.26 mg/ml). Solid self-emulsifying drug delivery systems with the highest yield were obtained with colloidal silicon dioxide (CSD) (80.12%), and CSD sodium croscarmelose 9:1 and 5:5. RES dissolution attained 100% at 45 min with CSD:CS 5:5. Discussion: The surface modification to hydrophilic by CSD:sodium croscarmellose reduced the cohesive force among drug particles. Conclusion: The developed systems are a good approximation for the design of strategies that could allow increasing the oral bioavailability of RES.
In order to improve the stability of oxytetracycline hydrochloride, a polymorphic antibiotic set of novel binary systems were developed using β-cyclodextrin and amino acids with different acid-basic characteristics as ligands. The formation constants for each system containing β-cyclodextrin, L-aspartic acid, histidine and N-acetylcysteine were determined by Scott’s method and statistical studies. The structure of the binary systems with β-cyclodextrin and N-acetylcysteine was elucidated by NMR experiments. The effect β-cyclodextrin and N-acetylcysteine on the polymorph’s chemical stability in aqueous and phosphate buffered saline solutions at 25 °C was monitored by an optimized and validated high-performance liquid chromatography method. The combination of N-acetylcysteine with the three polymorphs and the β-cyclodextrin system obtained with the form III demonstrated a reduction in the degradation rate of oxytetracycline hydrochloride in the aqueous solution when compared to each free form, with an increase of 20 h in the half time. It evidences that the use of amino acids as ligands constitutes an interesting alternative for pharmaceutical areas. In conclusion, based on the results obtained, these pharmaceutical systems could be candidates for the development of a pharmaceutical formulation for the administration of the drug through reconstituted solutions using the binary system as a promising tool for improving the stability of oxytetracycline hydrochloride polymorphs in solution.
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