Application of the quality by design principles for the development of the crystallization process for a piperazinyl-quinoline and definition of the control strategy for form 1

Organic Process Research and Development

Volumn 16, Issue 10, 2012, Pages 1598-1606

  Cimarosti, Zadeo ^a   Rossi, Sara ^a   Tramarin, Davide ^a   Laval, Gilles ^a   Stabile, Paolo ^a   Giubellina, Nicola ^a   Maton, William ^a   Allieri, Brigida ^a   Campi, Francesca ^a   Cooke, Jason ^b   Westerduin, Pieter ^a  

^a GSK   (Italy)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CONTROL STRATEGIES; CRYSTALLIZATION PROCESS; PROCESS ANALYTICAL TECHNOLOGY; PROCESS UNDERSTANDING; QUALITY BY DESIGNS;

DRUG PRODUCTS PLANTS;

QUALITY CONTROL;

EID: 84870883057     PISSN: 10836160     EISSN: 1520586X     Source Type: Journal    
DOI: 10.1021/op300126e     Document Type: Article

References (24)

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8. It is worth noting that this work is related to a process developed to support the initial toxicology and clinical requirements, and therefore, it might not be seen as ready for technical transfer or regulatory submission. What is stressed here is the help that the application of the QbD principles has given to achieve process understanding and control and to define a robust control strategy for the solvate.
9. ICH Q8 Pharmaceutical Development, (R2); U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER): Rockville, MD, Aug 2009.
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14. Each of the elements of control can be categorised into three control modes, as follows:(i) attribute controls, which include in-process controls (IPCs), and specifications for starting materials, intermediates, solvents, and drug substance (ii) parametric controls, which involve operation within proven acceptable ranges (PARs) for critical process parameters (CPPs) which are linked to CQAs, it is worth noting that, in this case the PARs were not defined due to the early phase of the project (iii) procedural controls, which describe operations linked to CQAs such as facilities setup, equipment configuration, order of addition, reagent, and solvent choice, sequence of events, etc.
15. Cimarosti, Z.; Giubellina, N.; Stabile, P.; Laval, G.; Tinazzi, F.; Maton, W.; Pachera, R.; Russo, P; Moretti, R.; Rossi, S; Cooke, J.; Westerduin, P. Org. Process Res. Dev. 2011, 15, 1287-1296.
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17. The HPLC method used in the solubility screening is a generic HPLC gradient method with Phenomenex Luna C18 column. Mobile phases: A1 = TFA -0.05% vol/vol in water, B1 = TFA -0.05% vol/vol in acetonitrile. Gradient from 0% B1 to 95% B1 in 8 min. UV detection at 220 nm.
18. Ethanol was initially considered, but it was decided not to test it as its water affinity (water activity) was considered an additional risk with respect to the formation of a monohydrate form; this aspect is discussed in the paper cited in reference 9.
19. A.polymorph study was carried out, after the selection of npropanol as a crystrallization solvent, on 48 solvents and different experiment types; the result of this study highlighted the possible existence of the n-propanolate, but it was decided to continue with the use of this solvent for the initial phases of development.
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23. RAMAN technique uses a very energetic laser that could be generating a significant heating in the solution and this might have process safety implications
24. To develop this quantification model a NIR Bruker Matric-F with a Diffuse Reflectance probe made from Solvias was used. The peculiarity of this probe was the fiber bundle used to make it; in this probe Solvias has used a bundle with seven optical fibers inside rather than one, and this increases, the sensitivity of the instrument a lot. The software used to control the instrument and to develop the model was OPUS build 5, 5, 60 (20050210), version -5.5; Bruker Optics, Inc.