A new soluble and bioactive polymorph of praziquantel

Zanolla, Debora; Perissutti, Beatrice; Passerini, Nadia; Chierotti, Michele R.; Hasa, Dritan; Voinovich, Dario; Gigli, Lara; Demitri, Nicola; Geremia, Silvano; Keiser, Jennifer; Vioglio, Paolo Cerreia; Albertini, Beatrice

doi:10.1016/j.ejpb.2018.01.018

Cited by 51 publications

(90 citation statements)

References 47 publications

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“…Such solid dispersions, however, presented a diminished drug recovery, which was found to be dependent on the polymer used [23,24]. Conversely, when PZQ is processed alone by neat grinding maintains a conspicuous residual crystallinity and does not degrade [19,20].…”

Section: Introductionmentioning

confidence: 94%

“…PZQ polymorphic Form B was prepared using a method already reported in the literature [19]. Briefly, 850 mg of PZQ Form A was milled in neat conditions for 4 h at 20 Hz, and the conversion of PZQ Form A into PZQ Form B was eventually assessed by powder X-ray diffraction, differential scanning calorimetry and FT-IR spectroscopy, using the same conditions previously applied [19].…”

Section: Praziquantel Hemihydrate Preparationmentioning

confidence: 99%

“…The optical rotations of the samples dissolved in ethanol (1 g/100 mL) were recorded at 25 • C, λ = 589 nm using a Jasco P2000 Polarimeter (Lecco, Italy), according to a method already reported [9,19,32]. The use of ethanol instead of CHCl 3 permitted an easier preparation of the samples without air bubbles in the cell.…”

Section: Polarimetry and Drug Recoverymentioning

confidence: 99%

“…The two new polymorphs are also available in CSD (indexed as TELCEU01 and GOYZOM, respectively). Both PZQ Form B and Form C preserve the activity against Schistosoma and have an improved water solubility [19,20]. Very recently, other authors have proposed a further solid form, not indexed in the CSD, reported as a pink powder; however, the performed characterizations neither allowed to solve the structure nor to validate it [21].…”

Section: Introductionmentioning

confidence: 99%

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Mechanochemical Formation of Racemic Praziquantel Hemihydrate with Improved Biopharmaceutical Properties

et al. 2020

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Praziquantel (PZQ) is the first-line drug used against schistosomiasis, one of the most common parasitic diseases in the world. A series of crystalline structures including two new polymorphs of the pure drug and a series of cocrystals of PZQ have been discovered and deposited in the Cambridge Structural Database (CSD). This work adds to the list of multicomponent forms of PZQ a relevant example of a racemic hemihydrate (PZQ-HH), obtainable from commercial PZQ (polymorphic Form A) through mechanochemistry. Noteworthy, the formation of the new hemihydrate strongly depends on the initial polymorphic form of PZQ and on the experimental conditions used. The new PZQ-HH has been fully characterized by means of HPLC, Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), Hot-Stage Microscopy (SEM), Powder X-Ray Diffraction (PXRD), Scanning Electron Microscopy (SEM), FT-IR, polarimetry, solid-state NMR (SS-NMR), solubility and intrinsic dissolution rate (IDR), and in vitro tests on Schistosoma mansoni adults. The crystal structure was solved from the powder X-ray diffraction pattern and validated by periodic-DFT calculations. The new bioactive hemihydrate was physically stable for three months and showed peculiar biopharmaceutical features including enhanced solubility and a double intrinsic dissolution rate in water in comparison to the commercially available PZQ Form A.

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Section: Introductionmentioning

confidence: 94%

Section: Praziquantel Hemihydrate Preparationmentioning

confidence: 99%

Section: Polarimetry and Drug Recoverymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Mechanochemical Formation of Racemic Praziquantel Hemihydrate with Improved Biopharmaceutical Properties

et al. 2020

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“…Praziquantel Novel praziquantel form B was compared with the form A by shake-flask and intrinsic dissolution in distilled water at 20 °C and 37 °C consequently. It has been found two times more soluble by both of them (140.3 and 281.3 mg·mL -1 by shake-flask and 31.2 and 62.2 by mg·cm -2 ·min -1 by IDR) (ZANOLLA et al, 2018).…”

Section: Drug Methodology and Observations Yearmentioning

confidence: 93%

Polymorph screening and solubility characterization of lercanidipine hydrochloride

Repin¹

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Better and greener: sustainable pharmaceutical manufacturing technologies for highly bioavailable solid dosage forms

Bertoni

Hasa

Albertini

et al. 2022

Drug Deliv. and Transl. Res.

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A new soluble and bioactive polymorph of praziquantel

Cited by 51 publications

References 47 publications

Mechanochemical Formation of Racemic Praziquantel Hemihydrate with Improved Biopharmaceutical Properties

Mechanochemical Formation of Racemic Praziquantel Hemihydrate with Improved Biopharmaceutical Properties

Polymorph screening and solubility characterization of lercanidipine hydrochloride

Better and greener: sustainable pharmaceutical manufacturing technologies for highly bioavailable solid dosage forms

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