Dissolution properties of praziquantel–PVP systems

El-Arini, Silvia Kocova; Leuenberger, Hans

doi:10.1016/s0031-6865(97)00051-4

Cited by 50 publications

(20 citation statements)

References 16 publications

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“…Over the last 25 years, many scientists have employed a modified form of this equation that contains the latency time (l), which marks the beginning of drug release from the system (El-Arini & Leuenberger, 1998;Ford et al, 1991;Kim & Fassihi, 1997;Pillay & Fassihi, 1999): (5.23) or the logarithmical version: Over the last 25 years, many scientists have employed a modified form of this equation that contains the latency time (l), which marks the beginning of drug release from the system (El-Arini & Leuenberger, 1998;Ford et al, 1991;Kim & Fassihi, 1997;Pillay & Fassihi, 1999): (5.23) or the logarithmical version:…”

Section: Ritger-peppas and Korsmeyer-peppas Model (Power Law)mentioning

confidence: 99%

Mathematical models of drug release

2015

Strategies to Modify the Drug Release From Pharmaceutical Systems

238

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Section: Ritger-peppas and Korsmeyer-peppas Model (Power Law)mentioning

confidence: 99%

Mathematical models of drug release

2015

Strategies to Modify the Drug Release From Pharmaceutical Systems

238

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“…Foi desenvolvida uma forma modificada desta última equação (El Arini, Leuenberger, 1998;Ford et al, 1991;Harland et al, 1988;Kim, Fassihi, 1997a, 1997bPillay, Fassihi, 1999) para considerar o tempo de espera (l) no início da liberação do fármaco a partir da forma farmacêutica:…”

Section: Modelo De Korsmeyer-peppasunclassified

A dissolução in vitro na previsão da absorção oral de fármacos em formas farmacêuticas de liberação modificada

Manadas¹,

Pina²,

Veiga³

2002

Rev. Bras. Cienc. Farm.

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Pretende-se com o presente trabalho abordar os aspectos teóricos e práticos dos estudos de dissolução das formas farmacêuticas sólidas orais de liberação modificada, em três partes. Na primeira parte faz-se referência à classificação, interesse terapêutico e teoria da liberação do fármaco. Na segunda parte abordam-se as teorias de dissolução, os modelos de liberação, os sistemas de dissolução e sua validação, as especificações e critérios de aceitação dos ensaios de dissolução e ainda os fatores condicionantes da dissolução, liberação e absorção. Na terceira parte confrontamse as condições em que são efetuados os ensaios de dissolução com os parâmetros fisiológicos, fazendo referência aos meios de dissolução e composição do lume do trato gastrintestinal e aos modelos hidrodinâmicos.

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“…Currently, praziquantel (PZQ) represents the drug of choice against all species of Schistosoma, with a therapeutic regimen of 20 mg/kg three times a day at intervals of 4 to 6 h or as a single dose of 40 mg/kg (depending on the parasite and whether used for individual patient management or mass drug administration) [3,4]. Such a high dosage is mainly due to the poor water solubility and bioavailability and extensive first-pass metabolism [5]. Very minor and transient side effects [6] and low toxicity in animals [7] are reported for PZQ.…”

Section: Introductionmentioning

confidence: 99%

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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Dissolution properties of praziquantel–PVP systems

Cited by 50 publications

References 16 publications

Mathematical models of drug release

Mathematical models of drug release

A dissolução in vitro na previsão da absorção oral de fármacos em formas farmacêuticas de liberação modificada

Mechanochemical Formation of Racemic Praziquantel Hemihydrate with Improved Biopharmaceutical Properties

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