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Biocatalysts: The Different Classes and Applications for Synthesis of APIs
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
The members of the monoamine oxidases family are flavoenzymes catalyzing the oxidative deamination of a variety of compounds via the formation of an imine (oxidation of C–N → C=N) to aldehydes. Monoamine oxidases (MAOs) have been evolved for use in kinetic resolutions or (oxidative) desymmetrizations (see Green and Turner, 2016, and literature cited therein). Ghislieri et al. (2013) described the development of MAO variants from Aspergillus niger (MAO-N) with the aim to expand their substrate scope by mutations in the small active site pocket and in the substrate entrance channel to accommodate amine substrates containing bulky aryl substituents such as 4-chlorobenzhydrylamine; the R-enantiomer was used to synthesize Levocetirizine (opposite scheme), an antihistamine used for treating allergy symptoms and chronic hives; similarly the authors employed the engineered MAO-N for deracemization of phenyltetrahydroisoquinoline to synthesize Solifenacin from the respective (S)-enantiomer; the drug is prescribed to patients suffering from an overactive bladder.
Application of a proposed reliability analysis multivariate capability index on manufacturing processes
Published in Quality Engineering, 2022
Rister Barreto, Herrera Acosta Roberto
Levocetirizine is an antihistamine, used for treating the symptoms of allergic diseases such as Seasonal Allergic Rhinitis (including ocular symptoms) and Chronic Idiopathic Rhinitis in patients from six months old on. The development of analytic tests for determining pH levels, density, active ingredient assessment and sucrose content in product manufacturing aim to determine the compliance level with the specifications set for each of these variables, according to preestablished standards. An evaluative research was conducted, where data for each of the studied variables were collected to evaluate the performance of the Levocetirizine manufacturing process. The data sample is summarized in Table 1.
Tribo-electrification of pharmaceutical powder blends
Published in Particulate Science and Technology, 2019
Antonella Rescaglio, Frederic De Smet, Luc Aerts, Geoffoy Lumay
Levocetirizine and Cetirizine are Cetirizine dihydrochloride (racemic mixture of (±)-[2-[4-[(4-chlorophenyl)phenylmethyl]-1- piperazinyl]ethoxy]acetic acid), sold under the brand name Zyrtec® among others, is a second generation antihistamine used in the treatment of hay fever, allergies, angioedema, and urticaria, Baltes, De Lannoy, and Rodriguez (1985).