scholarly journals Flow Synthesis Kinetics for Lomustine, an Anti-Cancer Active Pharmaceutical Ingredient

Author(s):  
Samir Diab ◽  
Mateen Raiyat ◽  
Dimitrios I. Gerogiorgis

Continuous flow synthesis of Active Pharmaceutical Ingredients (APIs) can offer access to process conditions that are otherwise hazardous when operated in batch mode, resulting in improved mixing and heat transfer,...

2020 ◽  
Vol 5 (9) ◽  
pp. 1527-1555 ◽  
Author(s):  
Zsolt Fülöp ◽  
Péter Szemesi ◽  
Péter Bana ◽  
János Éles ◽  
István Greiner

This review focuses on the flow-oriented design (FOD) in the multi-step continuous-flow synthesis of active pharmaceutical ingredients.


Author(s):  
Cloudius Sagandira ◽  
Sinazo Nqeketo ◽  
Kanysile Mhlana ◽  
Thembela Sonti ◽  
Paul Watts ◽  
...  

Continuous flow chemistry has opened a new paradigm in both the laboratory and pharmaceutical industry. This review details the recently reported literature on continuous multistep telescoped synthesis of active pharmaceutical...


2021 ◽  
pp. 37-54
Author(s):  
Roman Petrovich Terekhov ◽  
Denis Igorevich Pankov ◽  
Ekaterina Aleksandrovna Anfinogenova ◽  
Irina Anatolievna Selivanova

Рolymorphism is receiving increasing attention due to its influence on the physicochemical and pharmacological properties of the active pharmaceutical ingredients (API) while maintaining the molecular structure. This review is devoted to the problem of APIs phase state control both at the development stage and during the circulation of the drug. The term «polymorphism» has different definitions depending on the branch of science. There is no unambiguous solution to this issue in the regulatory documentation of pharmaceutical industry either. Based on the analysis of literary sources, the article presents a comparison of pharmacopeia methods, recommended in Russian and foreign regulatory documents for the analysis of polymorphism of medicinal substances, including state pharmacopeias of Russia, Belarus, Kazakhstan, the USA, and Japan, as well as international pharmacopeias of the European Economic Union and the Eurasian Economic Union. The trend on using a complex of high-tech equipment is revealed. A systematic approach to analysis based on X-ray diffraction, thermal, spectral, microscopic, biological, and physical methods for determining constants makes it possible not only to identify the polymorphic modification of API, but also to characterize its structure, morphology, physicochemical properties and pharmacological activity. In the Russian Federation, the phenomenon of polymorphism is being studied especially intensively, and some control methods, such as biological methods, are validated only in Russian pharmacopeia. A promising direction for further research is the improvement and harmonization of regulatory documentation within the framework of this chemical and technological field of pharmacy. A global approach will help to reduce not only the probability of poor-quality products entering the market, but also the costs of establishing the authenticity of the active pharmaceutical ingredient produced.


2020 ◽  
Vol 5 (7) ◽  
pp. 1186-1197 ◽  
Author(s):  
Victor R. L. J. Bloemendal ◽  
Mathilde A. C. H. Janssen ◽  
Jan C. M. van Hest ◽  
Floris P. J. T. Rutjes

This review highlights a selection of multistep continuous flow (one-flow) processes leading to the synthesis of active pharmaceutical ingredients (APIs).


1970 ◽  
Vol 7 (6) ◽  
pp. 6-10
Author(s):  
Mukhtar Gambo Lawal ◽  
Muhammad Dauda Mukhtar ◽  
Abdulkadir Magaji Magashi

There are increasing reports on the high incidence of substandard drugs, especially in developing countries.Pharmaceutical products have been reported to contain either no, low, or excessive amounts of the active pharmaceutical ingredient (API). Inview of the above, 112 samples of six different antibiotic oral drug formulations were evaluated for chemical quality by assessing the presence and the percentage content of the stated active pharmaceutical ingredients using validated HPLC assay as described in the official monograph of the British and United Stated pharmacopoeia. The result indicates that 43 (38.4%) had active ingredients outside the set pharmacopoeial limit and therefore were non-compliant to the BP and the USP specifications for percentage content.  Ampiclox and Cotrimoxazole had the highest proportion of samples with active ingredient outside the pharmacopoeial limit, and in three samples (one Augmentin and two Ampiclox), no active ingredient was detected. The presence of API lower than the claimed content declared on the packaging was the primary cause of non-compliance. The potential implications of the use of substandard drugs are treatment failure and the development of drug-resistance.  


2019 ◽  
Vol 21 (16) ◽  
pp. 4422-4433 ◽  
Author(s):  
Romain Morodo ◽  
Romaric Gérardy ◽  
Guillaume Petit ◽  
Jean-Christophe M. Monbaliu

A robust continuous flow procedure for the transformation of bio-based glycerol into high value-added β-amino alcohol active pharmaceutical ingredients.


2019 ◽  
Vol 17 (6) ◽  
pp. 1552-1557 ◽  
Author(s):  
Renata M. Aguiar ◽  
Raquel A. C. Leão ◽  
Alejandro Mata ◽  
David Cantillo ◽  
C. Oliver Kappe ◽  
...  

Continuous-flow production of chiral intermediates plays an important role in the development of building blocks for Active Pharmaceutical Ingredients (APIs), being α-amino acids and their derivatives widely applied as building blocks.


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