Enantiotropically Related Albendazole Polymorphs

Pranzo, Marco B.; Cruickshank, Dyanne L.; Coruzzi, Massimo; Caira, Mino R.; Bettini, Ruggero

doi:10.1002/jps.22072

Cited by 60 publications

(76 citation statements)

References 28 publications

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“…The solubility data and the melting point data both suggest that type I crystal is more stable than type II. The enthalpy of solution (ΔH s ) can be calculated from the equation InC S = −ΔH S /R*(1000/T) + β by plotting the logithium of molar concentration against 1000/T as shown in Figure 10(b) [10]. The ΔH s values for type I and II crystals are calculated to be 25.87 and 23.63 J/mol, respectively.…”

Section: Solubility In Methanol and Stability Of Azilsartan Type I Anmentioning

confidence: 99%

“…The ΔH s values for type I and II crystals are calculated to be 25.87 and 23.63 J/mol, respectively. The difference in Gibbs free energy of the two crystal types, ΔG T , has been calculated using the reported method [10]. The value ΔG T initially decreases and then increases with rising temperature but stays negative (Figure 11).…”

Section: Solubility In Methanol and Stability Of Azilsartan Type I Anmentioning

confidence: 99%

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Crystal Type Iof Azilsartan Polymorphs: Preparation and Analysis

Ge¹,

Li²,

Cheng³

2016

JCPT

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Azilsartan (2-ethoxy-1-([2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl)-1H-benzimidazole-7-carboxylic acid) is a new angiotensin II receptor antagonist used in the treatment of hypertension. This paper describes the preparation of type I crystal and its single crystal diffraction data, the comparison of the powder diffraction data for both type I and II crystals as well as their stability and solubility in methanol.

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Section: Solubility In Methanol and Stability Of Azilsartan Type I Anmentioning

confidence: 99%

Section: Solubility In Methanol and Stability Of Azilsartan Type I Anmentioning

confidence: 99%

Crystal Type Iof Azilsartan Polymorphs: Preparation and Analysis

Ge¹,

Li²,

Cheng³

2016

JCPT

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“…Crystal morphology analysis by SEM ( Figure 6) showed uniformity among the 3 batches, ABZ01, ABZ02 and ABZ03, and a crystalline structure in accordance to the XRD diffractogram, with crystals of different sizes and shapes showing a strong tendency to aggregate (Pranzo et al, 2010).…”

Section: Granulometric and Crystal Morphology Analysismentioning

confidence: 56%

“…Consistent with Pranzo et al, (2010), the 3 batches (ABZ01, ABZ02, and ABZ03) were not Form II polymorphs.…”

Section: X-ray Diffractionmentioning

confidence: 84%

Assay and physicochemical characterization of the antiparasitic albendazole

Cavalcanti

Sousa²,

Tabosa

et al. 2012

Braz. J. Pharm. Sci.

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The aim of this study was to characterize three batches of albendazole by pharmacopeial and complementary analytical techniques in order to establish more detailed specifications for the development of pharmaceutical forms. The ABZ01, ABZ02, and ABZ03 batches had melting points of 208 °C, 208 °C, and 209 °C, respectively. X-ray diffraction revealed that all three batches showed crystalline behavior and the absence of polymorphism. Scanning electron microscopy showed that all the samples were crystals of different sizes with a strong tendency to aggregate. The samples were insoluble in water (5.07, 4.27, and 4.52 mg mL -1 , respectively) and very slightly soluble in 0.1 M HCl (55.10, 56.90, and 61.70 mg mL -1 , respectively) and additionally showed purities within the range specified by the Brazilian Pharmacopoeia 5th edition (F. Bras. V; 98% to 102%). The pharmacopeial assay method was not reproducible and some changes were necessary. The method was validated and showed to be selective, specific, linear, robust, precise, and accurate. From this characterization, we concluded that pharmacopeial techniques alone are not able to detect subtle differences in active pharmaceutical ingredients; therefore, the use of other complementary techniques is required to ensure strict quality control in the pharmaceutical industry.Uniterms: Albendazole/characterization. Antiparasitics/quality control.O objetivo do trabalho foi caracterizar três lotes de albendazol com técnicas analíticas farmacopéicas e complementares a fim de estabelecer especificações mais detalhadas para o desenvolvimento de formas farmacêuticas. Os lotes ABZ01, ABZ02 e ABZ03 apresentaram fusão em 208 °C, 208 °C e 209 °C. Foi possível evidenciar, por difração de raios X, que os três lotes apresentaram comportamento cristalino e ausência de polimorfismo. Através da microscopia eletrônica de varredura verificou-se que todas as amostras apresentaram cristais com diferentes tamanhos e forte tendência de agregação. As amostras foram insolúveis em água (5,07; 4,27 e 4,52 µg mL -1 ) e muito pouco solúveis em HCl 0,1M (55,10; 56,90 e 61,70 µg mL -1 ) e, ainda, apresentaram pureza dentro da faixa especificada pela F.Bras.V (98% a 102%). O método farmacopéico de doseamento não foi reprodutível, e algumas mudanças foram necessárias. O método foi validado e demonstrou ser seletivo, específico, linear, robusto, preciso e exato. A partir dessa caracterização, pode-se concluir que apenas técnicas farmacopéicas não são capazes de detectar diferenças sutis entre os ingredientes farmacêuticos ativos, necessitando, portanto, de uso de outras técnicas complementares para garantir um rígido controle de qualidade na indústria farmacêutica.Unitermos: Albendazol/caracterização. Antiparasitários/controle de qualidade.

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“…Albendazole is commercialized in form I (metastable), which is the most soluble form. Both forms I and II are stable under storage conditions; however, much care is required to control the form because of the possibility of undesirable polymorphic phase conversion in this API (Pranzo et al, 2010).…”

Section: Albendazole and Mebendazolementioning

confidence: 99%

Polymorphism: an evaluation of the potential risk to the quality of drug products from the Farmácia Popular Rede Própria

Santos

Reis

Jacon

et al. 2014

Braz. J. Pharm. Sci.

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Polymorphism in solids is a common phenomenon in drugs, which can lead to compromised quality due to changes in their physicochemical properties, particularly solubility, and, therefore, reduce bioavailability. Herein, a bibliographic survey was performed based on key issues and studies related to polymorphism in active pharmaceutical ingredient (APIs) present in medications from the Farmácia Popular Rede Própria. Polymorphism must be controlled to prevent possible ineffective therapy and/or improper dosage. Few mandatory tests for the identification and control of polymorphism in medications are currently available, which can result in serious public health concerns.Uniterms: Polymorphism. Medicines/quality control. Medicines/solubility. Medicines/bioavailability.O polimorfismo em sólidos é um fenômeno frequente em fármacos e pode levar a problemas na qualidade dos medicamentos por alterar suas propriedades físico-químicas, em especial a solubilidade e, consequentemente, a biodisponibilidade. Nesse trabalho realizou-se levantamento bibliográfico sobre os principais estudos e problemas relacionados ao polimorfismo em fármacos presentes nos medicamentos disponibilizados pela Farmácia Popular do Brasil. O polimorfismo deve ser controlado a fim de evitar possível ineficácia terapêutica e/ou dosagem inapropriada dos medicamentos. Destacamos que são poucos os ensaios obrigatórios para identificação e controle desse fenômeno em medicamentos, o que pode acarretar grande problema de saúde pública. Unitermos:Polimorfismo. Medicamentos/controle de qualidade. Medicamentos/solubilidade. Medicamentos/biodisponibilidade.

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Enantiotropically Related Albendazole Polymorphs

Cited by 60 publications

References 28 publications

Crystal Type Iof Azilsartan Polymorphs: Preparation and Analysis

Crystal Type Iof Azilsartan Polymorphs: Preparation and Analysis

Assay and physicochemical characterization of the antiparasitic albendazole

Polymorphism: an evaluation of the potential risk to the quality of drug products from the Farmácia Popular Rede Própria

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