Instability in Theophylline and Carbamazepine Hydrate Tablets: Cocrystal Formation Due to Release of Lattice Water

Arora, Kapildev K.; Thakral, Seema; Suryanarayanan, Raj

doi:10.1007/s11095-013-1022-7

Cited by 20 publications

(20 citation statements)

References 56 publications

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“…58,60) Storage of some tablets containing hydrated API or coformer crystals, such as theophylline monohydrate-anhydrous citric acid formulations, have also produced cocrystals. 61) …”

Section: )mentioning

confidence: 99%

Characterization and Quality Control of Pharmaceutical Cocrystals

Izutsu¹,

Koide²,

Takata

et al. 2016

CHEMICAL & PHARMACEUTICAL BULLETIN

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Recent active research and new regulatory guidance on pharmaceutical cocrystals have increased the rate of their development as promising approaches to improve handling, storage stability, and bioavailability of poorly soluble active pharmaceutical ingredients (APIs). However, their complex structure and the limited amount of available information related to their performance may require development strategies that differ from those of single-component crystals to ensure their clinical safety and efficacy. This article highlights current methods of characterizing pharmaceutical cocrystals and approaches to controlling their quality. Different cocrystal regulatory approaches between regions are also discussed. The physical characterization of cocrystals should include elucidating the structure of their objective crystal form as well as their possible variations (e.g., polymorphs, hydrates). Some solids may also contain crystals of individual components. Multiple processes to prepare pharmaceutical cocrystals (e.g., crystallization from solutions, grinding) vary in their applicable ingredients, scalability, and characteristics of resulting solids. The choice of the manufacturing method affects the quality control of particular cocrystals and their formulations. In vitro evaluation of the properties that govern clinical performance is attracting increasing attention in the development of pharmaceutical cocrystals. Understanding and mitigating possible factors perturbing the dissolution and/ or dissolved states, including solution-mediated phase transformation (SMPT) and precipitation from supersaturated solutions, are important to ensure the bioavailability of orally administrated lower-solubility APIs. The effect of polymer excipients on the performance of APIs emphasizes the relevance of formulation design for appropriate use.

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“…58,60) Storage of some tablets containing hydrated API or coformer crystals, such as theophylline monohydrate-anhydrous citric acid formulations, have also produced cocrystals. 61) …”

Section: )mentioning

confidence: 99%

Characterization and Quality Control of Pharmaceutical Cocrystals

Izutsu¹,

Koide²,

Takata

et al. 2016

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…This released water can interact with the other formulation components causing chemical decomposition . It can also alter the functionality of the excipients in the formulation . (ii) The physical form of the anhydrous product will be strongly dictated by the dehydration conditions.…”

Section: Resultsmentioning

confidence: 99%

“…29,30 It can also alter the functionality of the excipients in the formulation. [31][32][33] (ii) The physical form of the anhydrous product will be strongly dictated by the dehydration conditions. It is instructive to recognize that the formulation components as well as the packaging will also play a role in this regard.…”

Section: Solid Oral Dosage Form Of Ad-importance Of the Physical Formmentioning

confidence: 99%

Modulating the Dehydration Conditions of Adefovir Dipivoxil Dihydrate to Obtain Different Physical Forms of Anhydrate

Arora¹,

Bhardwaj²,

Mistry

et al. 2015

Journal of Pharmaceutical Sciences

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“…Namely, they can reveal the existence or non-existence of an intermediate in the dehydration process [ 138 ], as well as define the kinetics of a conversion of an amorphous substance into a crystalline upon the dissolution [ 139 ]. A perfect example of the strong influence of hydration conditions on the received hydrate form is the case of sodium naproxen [ 140 ]. An anhydrous form changes in a one-step process into a dihydrate I, but when the hydration is conducted in two steps, dihydrate II emerges.…”

Section: Mechanism Of (De)hydration Selected Cases Within the Lasmentioning

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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Instability in Theophylline and Carbamazepine Hydrate Tablets: Cocrystal Formation Due to Release of Lattice Water

Abstract: The water released by API dehydration mediated cocrystal formation in intact tablets and affected dissolution behavior.

Cited by 20 publications

References 56 publications

Characterization and Quality Control of Pharmaceutical Cocrystals

Characterization and Quality Control of Pharmaceutical Cocrystals

Modulating the Dehydration Conditions of Adefovir Dipivoxil Dihydrate to Obtain Different Physical Forms of Anhydrate

Pharmaceutical Hydrates Analysis—Overview of Methods and Recent Advances

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