scholarly journals Combined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1923
Author(s):  
Marzia Cirri ◽  
Natascia Mennini ◽  
Giulia Nerli ◽  
Jessica Rubia ◽  
Enrico Casalone ◽  
...  

Cefixime (CEF) is a cephalosporin included in the WHO Model List of Essential Medicines for Children. Liquid formulations are considered the best choice for pediatric use, due to their great ease of administration and dose-adaptability. Owing to its very low aqueous solubility and poor stability, CEF is only available as a powder for oral suspensions, which can lead to reduced compliance by children, due to its unpleasant texture and taste, and possible non-homogeneous dosage. The aim of this work was to develop an oral pediatric CEF solution endowed with good palatability, exploiting the solubilizing and taste-masking properties of cyclodextrins (CDs), joined to the use of amino acids as an auxiliary third component. Solubility studies indicated sulfobutylether-β-cyclodextrin (SBEβCD) and Histidine (His) as the most effective CD and amino acid, respectively, even though no synergistic effect on drug solubility improvement by their combined use was found. Molecular Dynamic and 1H-NMR studies provided insight into the interactions of binary CEF:His and ternary CEF:His:SBEβCD systems used to prepare CEF solutions, which resulted stable and maintained unchanged antimicrobial activity during the two-weeks-use in therapy. The ternary solution was superior in terms of more tolerable pH (5.6 vs. 4.7) and better palatability, being resulted completely odorless by a panel test.

Author(s):  
Maithili Pramod Joshi ◽  
Ameya Chaudhari ◽  
Prashant S. Kharkar ◽  
Shreerang V. Joshi

: Historically, the use of Iodinated Contrast Media (ICM) for diagnostic purposes, particularly radiography and computed tomography (CT), is well-known. Many of the ICM are included in the World Health Organization (WHO)’s List of Essential Medicines. Depending on the chemotype and the presence of ionizable functional group(s), the ICM are categorized in the ionic/nonionic monomers/dimers. The lipophilicity, aqueous solubility, viscosity and osmolality are major characteristics dictating their use for one procedure versus the other. Over last several decades, substantial advancement occurred in the design and development of novel ICM, solely to reduce their propensity to cause adverse effects. Given the nature of their acute usage, some of the agents with appreciable toxicity are still used. Understanding their chemistry aspects is crucial to appreciate, acknowledge and justify the usage of these extremely important torch-bearers of diagnostic agent’s class. The present review article presents an in-depth overview of the synthetic methods, therapeutic indications, potential adverse effects along with the commercial and environmental aspects of ICM. The safety and tolerability of these agents is a field that has gained significant importance, which is given due importance in the discussion.


2013 ◽  
Vol 89 (2) ◽  
pp. 171-178
Author(s):  
Helena Lutéscia L. Coelho ◽  
Luís Carlos Rey ◽  
Marina S.G. de Medeiros ◽  
Ronaldo A. Barbosa ◽  
Said G. da Cruz Fonseca ◽  
...  

ACS Nano ◽  
2018 ◽  
Vol 12 (12) ◽  
pp. 12247-12254 ◽  
Author(s):  
Kim-A. Saal ◽  
Frank Richter ◽  
Peter Rehling ◽  
Silvio O. Rizzoli

2018 ◽  
Vol 20 (18) ◽  
pp. 12664-12677 ◽  
Author(s):  
Nad'a Špačková ◽  
Zuzana Trošanová ◽  
Filip Šebesta ◽  
Séverine Jansen ◽  
Jaroslav V. Burda ◽  
...  

Water molecules can interact with the π-face of tryptophan either forming an O–H⋯π hydrogen bond or by a lone-pair⋯π interaction. Surrounding amino acids can favor the one or the other interaction type.


Author(s):  
Frank E. Scully, Jr ◽  
Barbara Conyers

Over the past 20 years, gas chromatography/mass spectroscopy (GC/MS) has been widely used to identify trace organic environmental contaminants and to study the mechanisms of the formation or transformation of organic compounds either by natural or man-made processes. In the area of water and wastewater disinfection, GC/MS has been highly successful in identifying numerous volatile organic chlorination by-products, some of which may pose undesirable health risks to humans and aquatic organisms at concentrations found in some waters. However, despite a considerable amount of research in this area much of the chemistry continues to be poorly understood. Analysis of trace organics by GC/MS relies on the assumption that the compounds to be analyzed are (1) volatile and (2) thermally stable to GC temperatures as high as 300 °C. Because nuclear magnetic resonance spectroscopy (NMR) is a mild and nondestructive method of analysis, it can reveal reactions that occur in water that cannot be observed by GC/MS. Until recently the reactions of amino acids with two or more equivalents of aqueous chlorine were believed to produce aldehydes and nitriles according to equation (1). LeCloirec and Martin have reported that the formation of nitriles in such situations may come in part from the reaction of monochloramine with aldehydes (equation (2)). Because reaction (2) may affect the distribution of products in reaction (1), it was important to determine the relationship between these two reactions. This chapter will review the applications of NMR we have used in studies of the products formed upon chlorination of amino acids.


Author(s):  
Martha Mherekumombe ◽  
John J. Collins

Persisting pain in the context of medical illness has been recognized recently as a global problem by the World Health Organization (WHO, 2012). Whilst the epidemiology of medical illness varies throughout the world, the general principles of pain management are applicable to most medical illnesses in children and are effective. Successful pain management for most children is contingent on the availability of the WHO model list of essential medicines for children (WHO, 2011), although regrettably not all medicines are available in every country in the world.


2013 ◽  
Vol 89 (2) ◽  
pp. 171-178 ◽  
Author(s):  
Helena Lutéscia L. Coelho ◽  
Luís Carlos Rey ◽  
Marina S.G. de Medeiros ◽  
Ronaldo A. Barbosa ◽  
Said G. da Cruz Fonseca ◽  
...  

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