Imaging Dehydration Kinetics of a Channel Hydrate Form of the HIV-1 Attachment Inhibitor Prodrug BMS-663068

Leane, Michael; Gamble, John F.; Brown, Jonathan; Hughes, Helen; Crull, George B.; Engstrom, Josh D.; Gao, Qi; Bunker, Matt; Rutherford, Sandra A; Parker, Andrew S.; Roberts, Clive J.; Tobyn, Mike

doi:10.1002/jps.23747

Cited by 2 publications

(3 citation statements)

References 42 publications

(72 reference statements)

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“…Form: A stable solid state form is needed because lack of form control (such as conversion to a more stable polymorph) can lead to changes in material properties with associated manufacturing challenges. This can in turn impact the desired final performance and stability 21 . An example of an API with form issues is given under the Class 4 OT section.…”

Section: Developability Parametersmentioning

confidence: 99%

A proposal for a drug product Manufacturing Classification System (MCS) for oral solid dosage forms

Leane

Pitt

Reynolds

2014

Pharmaceutical Development and Technology

204

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This paper proposes the development of a drug product Manufacturing Classification System (MCS) based on processing route. It summarizes conclusions from a dedicated APS conference and subsequent discussion within APS focus groups and the MCS working party. The MCS is intended as a tool for pharmaceutical scientists to rank the feasibility of different processing routes for the manufacture of oral solid dosage forms, based on selected properties of the API and the needs of the formulation. It has many applications in pharmaceutical development, in particular, it will provide a common understanding of risk by defining what the "right particles" are, enable the selection of the best process, and aid subsequent transfer to manufacturing. The ultimate aim is one of prediction of product developability and processability based upon previous experience. This paper is intended to stimulate contribution from a broad range of stakeholders to develop the MCS concept further and apply it to practice. In particular, opinions are sought on what API properties are important when selecting or modifying materials to enable an efficient and robust pharmaceutical manufacturing process. Feedback can be given by replying to our dedicated e-mail address (mcs@apsgb.org); completing the survey on our LinkedIn site; or by attending one of our planned conference roundtable sessions.

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Section: Developability Parametersmentioning

confidence: 99%

A proposal for a drug product Manufacturing Classification System (MCS) for oral solid dosage forms

Leane

Pitt

Reynolds

2014

Pharmaceutical Development and Technology

204

View full text Add to dashboard Cite

show abstract

“…In a computational investigation of the (de)hydration kinetics, an important role is also played by calculation of the solvent-accessible volume, which significantly differs for non-stoichiometric and stoichiometric hydrates [ 88 ]. Resulting from water loss, possible collapse of a void or conformational disorientation has a direct impact on the above discussed H-bonds network.…”

Section: Methods Applied For Analysis Of Hydratesmentioning

confidence: 99%

“…In case of APIs’ hydrates, the most commonly applied theoretical approaches encompass CSP [ 86 , 88 , 116 , 117 ] and NMR crystallography methods [ 83 , 118 , 119 , 120 , 121 , 122 ], not both of them at once [ 123 , 124 ]. Because of the common simultaneous application of various analytical methods by the researchers, it is impossible to review the last decade advances in this field method by method.…”

Section: Hydrates Structural Analysis Selected Cases Within the Lmentioning

confidence: 99%

Pharmaceutical Hydrates Analysis—Overview of Methods and Recent Advances

et al. 2020

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This review discusses a set of instrumental and computational methods that are used to characterize hydrated forms of APIs (active pharmaceutical ingredients). The focus has been put on highlighting advantages as well as on presenting some limitations of the selected analytical approaches. This has been performed in order to facilitate the choice of an appropriate method depending on the type of the structural feature that is to be analyzed, that is, degree of hydration, crystal structure and dynamics, and (de)hydration kinetics. The presented techniques include X-ray diffraction (single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD)), spectroscopic (solid state nuclear magnetic resonance spectroscopy (ssNMR), Fourier-transformed infrared spectroscopy (FT-IR), Raman spectroscopy), thermal (differential scanning calorimetry (DSC), thermogravimetric analysis (TGA)), gravimetric (dynamic vapour sorption (DVS)), and computational (molecular mechanics (MM), Quantum Mechanics (QM), molecular dynamics (MD)) methods. Further, the successful applications of the presented methods in the studies of hydrated APIs as well as studies on the excipients’ influence on these processes have been described in many examples.

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Imaging Dehydration Kinetics of a Channel Hydrate Form of the HIV-1 Attachment Inhibitor Prodrug BMS-663068

Cited by 2 publications

References 42 publications

A proposal for a drug product Manufacturing Classification System (MCS) for oral solid dosage forms

A proposal for a drug product Manufacturing Classification System (MCS) for oral solid dosage forms

Pharmaceutical Hydrates Analysis—Overview of Methods and Recent Advances

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