The form II of the antihypertensive drug chlorthalidone

Martins, Felipe Terra; Bonfílio, Rudy; Rosa, Iara M. L.; Santos, Leandro Marcos; Santos, Olimpia Maria Martins; Araújo, Magali Benjamim

doi:10.1039/c3ce40303c

Cited by 14 publications

(10 citation statements)

References 16 publications

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“…Single-crystal and powder X-ray diffraction techniques are the most suitable and commonly utilized tools to study and characterize polymorphs in pharmaceutical solids because they provide unequivocal proof of polymorphism existence [18]. Following our ongoing research to determine the crystal structures of APIs [21,22,23,24,25,26,27,28,29,30], we report here for the first time two crystalline structures of ORBI. The first ORBI crystal structure, which was determined by single-crystal X-ray diffraction, shows the ORBI molecule in a zwitterionic form.…”

Section: Introductionmentioning

confidence: 99%

Structure, Solubility and Stability of Orbifloxacin Crystal Forms: Hemihydrate versus Anhydrate

et al. 2016

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Orbifloxacin (ORBI) is a widely used antimicrobial drug of the fluoroquinolone class. In the official pharmaceutical compendia the existence of polymorphism in this active pharmaceutical ingredient (API) is reported. No crystal structure has been reported for this API and as described in the literature, its solubility is very controversial. Considering that different solid forms of the same API may have different physicochemical properties, these different solubilities may have resulted from analyses inadvertently carried out on different polymorphs. The solubility is the most critical property because it can affect the bioavailability and may compromise the quality of a drug product. The crystalline structure of ORBI determined by SCXRD is reported here for the first time. The structural analysis reveals that the ORBI molecule is zwitterionic and hemihydrated. ORBI hemihydrated form was characterized by the following techniques: TG/DTA, FTIR-ATR, and PXRD. A second crystalline ORBI form is also reported: the ORBI anhydrous form was obtained by heating the hemihydrate. These ORBI solid forms were isomorphous, since no significant change in unit cell and space group symmetry were observed. The solid-state phase transformation between these forms is discussed and the equilibrium solubility data were examined in order to check the impact of the differences observed in their crystalline structures.

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Section: Introductionmentioning

confidence: 99%

Structure, Solubility and Stability of Orbifloxacin Crystal Forms: Hemihydrate versus Anhydrate

et al. 2016

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“…Fexofenadine hydrochloride is an antihistamine used to treat asthma or seasonal allergies and it has several identified polymorphs; however, only form I (anhydrous) is used in the commercial pharmaceutical formulation. [1][2][3] The most commonly used technique to characterise polymorphisms is X-ray diffraction; 4 however, there are many other alternative techniques that can be used in polymorphism analysis, such as vibrational spectroscopy (infrared, Raman and solid-state nuclear magnetic resonance) [5][6][7][8][9] and thermal analysis. 10,11 Near infrared chemical imaging (NIR-CI) is a powerful extension of conventional spectroscopy and is considered interesting technology in pharmaceutical research.…”

Section: Introductionmentioning

confidence: 99%

Mapping the Polymorphic Forms of Fexofenadine in Pharmaceutical Tablets Using near Infrared Chemical Imaging

Brondi

Terra

Sabin

et al. 2014

Journal of Near Infrared Spectroscopy

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This study presents a comparison of partial least squares (PLS) and multivariate curve resolution (MCR-ALS) in the quantification of polymorphic forms I and II of fexofenadine.HCl in pharmaceutical tablets using near infrared chemical imaging (NIR-CI). The PLS model built using a standard normal variate (SNV) pre-processing method resulted in satisfactory fits between the reference and predicted values, with a root mean square error of prediction (RMSEP) for both polymorphic forms below 1.5% (w/w). The MCR-ALS results were obtained using an augmented matrix and SNV pre-processing method. The lack of fit value for decomposition was 0.13%, the correlation coefficient between the pure spectra and the obtained spectral profiles was 99.94% and the RMSEP was below 6% (w/w). The MCR-ALS model efficiently quantified the polymorphic forms and generated distribution maps; however, the PLS model exhibited better recovery of the concentrations.

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“…Esta velocidade com que ocorre a dissolução do fármaco pode ser influenciada por certas características da formulação e/ou da forma farmacêutica, entre elas: tamanho e forma das partículas, polimorfismo, excipientes, tecnologia utilizado preparo, tempos de mistura entre outros 22 . Para os produtos S1 e S2 sugere-se que a diferença nos perfis de dissolução deve-se ao polimorfismo, uma vez que segundo Martins Leal et al 24 …”

Section: Discussionunclassified

Avaliação da qualidade de medicamentos contendo clortalidona

et al. 2017

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ResumoOs diuréticos são a classe de fármacos mais utilizados no tratamento da hipertensão devido a sua eficácia terapêutica e ao baixo custo. Isto faz com que uma grande variedade de medicamentos esteja disponível no comercio e atrelado a este fator muitas empresas tem seus lotes de medicamentos suspensos devido a desvios de qualidade e das modificações realizadas nas formulações após o seu registro. A clortalidona é um diurético tiazídico indicada para o tratamento de hipertensão arterial leve ou moderada e com normalidade das funções cardíacas e renal. Este trabalho teve como objetivo verificar a qualidade de comprimidos de clortalidona comercializados no município de Sinop/ MT. O controle de qualidade foi realizado como estabelecido na Farmacopeia Brasileira quinta edição (ensaios de identificação, pureza, doseamento, ensaios referentes a forma farmacêutica de comprimidos e perfil de dissolução), de cinco produtos contendo clortalidona 25 mg sendo um produto de medicamento referência, dois de medicamentos genéricos e dois de medicamentos similares. Verificou-se que todos os produtos foram aprovados, cumprindo com todos os requisitos exigidos nos ensaios de qualidade e que estudos referentes ao perfil de dissolução nos lotes de produção de medicamentos são importantes para prever a absorção adequada do princípio ativo. Palavras AbstractDiuretics are the most used class of drugs that are used to treat hypertension because of their therapeutic efficiency and low cost. This makes a wide variety of medicines commercially available and, linked to this factor, many companies have their batches of medicines suspended due to deviations of quality and modifications made in the formulas after their registration. Chlorthalidone, is a thiazide diuretic drug indicated for treatment of hypertension of patients with mild or moderate hypertension, and with normal cardiac and renal function. This work aimed to assess and compare the quality of medicines containing chlorthalidone commercialized in Sinop-MT. The quality control was performed as established in the fifth edition of the Brazilian Pharmacopoeia (identification, purity and dosage assays, tests referring to the pharmaceutical form of the tablets and their dissolution profile). Among five products containing 25 mg of chlortalidone, one was a reference drug product, two were generic and two were similar drugs. It was found that all products were approved, meeting all the requirements required in the quality tests, and that studies concerning the dissolution profile in batches of drug production are important to predict adequate absorption of the active principle.

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The form II of the antihypertensive drug chlorthalidone

Abstract: Racemic mixtures of chlorthalidone (CTD) have been structurally elucidated in three crystal forms (space group P1 ¯), namely, Form I,

Cited by 14 publications

References 16 publications

Structure, Solubility and Stability of Orbifloxacin Crystal Forms: Hemihydrate versus Anhydrate

Structure, Solubility and Stability of Orbifloxacin Crystal Forms: Hemihydrate versus Anhydrate

Mapping the Polymorphic Forms of Fexofenadine in Pharmaceutical Tablets Using near Infrared Chemical Imaging

Avaliação da qualidade de medicamentos contendo clortalidona

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