A study of the heat-mediated phase transformations of praziquantel hydrates. Evaluation of their impact on the dissolution rate

Salazar-Rojas, Duvernis; Kaufman, Teodoro S.; Maggio, Rubén M.

doi:10.1016/j.heliyon.2022.e11317

Cited by 3 publications

(3 citation statements)

References 25 publications

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“…Considering these two above-discussed new hydrated forms, both PZQ-MH and PZQ-HH solid-state transformations under heat stress were monitored through hot-stage attenuated total reflectance coupled to mid infrared spectroscopy (HS-ATR-MIR) empowered by multivariate curve resolution coupled to alternating least squares (MCR-ALS) and DSC in a study reported by Salazar-Rojas et al [ 103 ]. The monitoring setup involved heating the samples on the ATR stage at a rate of 5 °C/min (30–145 °C), while acquiring MIR spectra (3500–600 cm −1 ) every minute.…”

Section: Pzq Multicomponent Solid Formsmentioning

confidence: 99%

Praziquantel Fifty Years on: A Comprehensive Overview of Its Solid State

D’Abbrunzo,

Procida,

Perissutti

2023

Pharmaceutics

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This review discusses the entire progress made on the anthelmintic drug praziquantel, focusing on the solid state and, therefore, on anhydrous crystalline polymorphs, amorphous forms, and multicomponent systems (i.e., hydrates, solvates, and cocrystals). Despite having been extensively studied over the last 50 years, new polymorphs and the greater part of their cocrystals have only been identified in the past decade. Progress in crystal engineering science (e.g., the use of mechanochemistry as a solid form screening tool and more strategic structure-based methods), along with the development of analytical techniques, including Synchrotron X-ray analyses, spectroscopy, and microscopy, have furthered the identification of unknown crystal structures of the drug. Also, computational modeling has significantly contributed to the prediction and design of new cocrystals by considering structural conformations and interactions energy. Whilst the insights on praziquantel polymorphs discussed in the present review will give a significant contribution to controlling their formation during manufacturing and drug formulation, the detailed multicomponent forms will help in designing and implementing future praziquantel-based functional materials. The latter will hopefully overcome praziquantel’s numerous drawbacks and exploit its potential in the field of neglected tropical diseases.

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Section: Pzq Multicomponent Solid Formsmentioning

confidence: 99%

Praziquantel Fifty Years on: A Comprehensive Overview of Its Solid State

D’Abbrunzo,

Procida,

Perissutti

2023

Pharmaceutics

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“…The generation of multicomponent solid forms of active pharmaceutical ingredients (APIs) such as salts, cocrystals, hydrates, and solvates to improve the physicochemical properties of pharmaceutical compounds has been well established, enhancing the solubility and/or dissolution rate of many APIs. , While each of these strategies has proven successful for a range of APIs, it is not a “one size fits all” arrangement. Salts require the presence of ionizable groups on reactant molecules, while cocrystals require molecular complementarity (MC) and a relatively high degree of hydrogen bond propensity (HBP), requirements that are not met by all API and coformer pairs.…”

Section: Introductionmentioning

confidence: 99%

“…The generation of multicomponent solid forms of active pharmaceutical ingredients (APIs) such as salts, 1 cocrystals, 2 hydrates, 3 and solvates 4 to improve the physicochemical properties of pharmaceutical compounds has been well established, enhancing the solubility and/or dissolution rate of many APIs. 5 , 6 While each of these strategies has proven successful for a range of APIs, it is not a “one size fits all” arrangement.…”

Section: Introductionmentioning

confidence: 99%