Separation of nadolol racemates by high pH reversed-phase preparative chromatography

Abstract

The separation of nadolol racemates under high pH reversed-phase preparative chromatography is presented for the first time.Three Waters C18 adsorbents (XBridge, Shield and XSelect) are compared for the separation of nadolol racemates using ethanol:water:diethylamine solvent mixtures. Experimental and simulation results are presented to compare the separation performances at preparative scale using both the fixed-bed and the simulated moving bed operations.The Waters XBridge C18 adsorbent and an ethanol:water:diethylamine solvent mixture are selected as a good option for the separation of nadolol racemates. The validated methodology allows the separation of a multicomponent nadolol feed mixture composed by four stereoisomers into two pure racemates (two pairs of enantiomers). This work introduces the potential of using an initial achiral separation step in the global strategy for the complete multicomponent separation of the four nadolol stereoisomers.

Holothuria Leucospilota polysaccharides alleviate hyperlipidemia via alteration of lipid metabolism and inflammation‐related gene expression

“…Nadolol is a non‐selective β‐adrenoceptor blocking drug with angina and hypertension suppressing effects (Heel et al, 1980). Currently, nadolol is widely used to relieve cardiovascular disease (Arafah et al, 2020). It is a highly water‐soluble substance that is not entirely metabolized by metabolic enzymes and is mainly excreted in the urine (Misaka et al, 2013).…”

“…Currently, nadolol is widely used to relieve cardiovascular disease (Arafah et al, 2020). It is a highly water-soluble substance that is not entirely metabolized by metabolic enzymes and is mainly excreted in the urine (Misaka et al, 2013).…”

Strategies for Simulated Moving Bed Model Parameter Estimation Based on Minimal System Minimal Knowledge: Adsorption Isotherm Equation Screening and Estimability Analysis

“…5 Finally, the two methodologies can be compared for the case study so that one can decide which one better suits a certain case. The comparison is given by (11) (12) where Δ M and Δ L are the absolute deviation of the model and literature, and δ Md i d ,j and δ Ld i d ,j are the deviations between the present model and experimental points and literature and experimental points, respectively, that should be calculated for both methodologies.…”

“…Aniceto; Cardoso; Silva (2016) applied a modified Linear + Langmuir AIE for the separation of (S,S)-(−) and (R,R)-(+)- trans -stilbene oxide enantiomers in Chiralcel OD adsorbent . Arafah et al (2016, 2018, and 2020) studied the separation of nadolol stereoisomers using Chiralpak IA and adopted a Linear + Langmuir adsorption isotherm equation to describe the adsorption behavior. − Huthmann and Juza (2005) also applied the Linear + Langmuir AIE for less common simulated moving bed chromatography applications in the pharmaceutical industry . Cunha (2021) studied the separation via SMB of medicine against schistosomiasis, the praziquantel, and considered a Langmuir AIE .…”

Novel Chiral Drug Recovery and Enantioseparation Method: Hollow Fiber Membrane Extraction and In Situ Coupling of Back-Extraction with Crystallization

“…However, although many separation technologies have been explored, a mature enantioseparation method is still lacking in industrial application . The reported enantioseparation technologies include crystallization, , enzymatic kinetic resolution, , chromatographic separation, , membrane separation, − and LLE. − The enzymatic kinetic resolution has a high chiral separation effect, but each enzyme has a narrow range of applications. The chromatographic separation method also exhibits good enantioseparation ability, but it is usually only suitable for enantioanalysis.…”