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Solubility and dissolution studies of tibolone polymorphs BJPS
Bonfilio,Rudy; Souza,Marília Cristina Oliveira; Leal,Jockastta Silva; Viana,Olímpia Maria Martins Santos; Doriguetto,Antônio Carlos; Araújo,Magali Benjamin de.
ABSTRACT Different solid forms of an active pharmaceutical ingredient can have distinct chemical and physical characteristics. In this work, we studied the solubility and dissolution properties of the described tibolone polymorphic forms (I and II). Both forms were successively recrystallized and characterized by powder X-ray diffraction and attenuated total reflection infrared spectroscopy. Equilibrium solubility and dissolution profiles were performed for both forms. Solubility studies demonstrated that form II is statistically more soluble in water, 0.01 mol L-1 HCl and pH 4.5 acetate buffer. The solubility of forms I and II were explained in terms of crystal packing. Dissolution tests of tablets showed a lower release of polymorphic form II than form I...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Tibolone/polymorphs; Powder X-ray diffraction/methods; Infrared spectroscopy/methods; Solubility/drug effects; Dissolution/analysis.
Ano: 2017 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000400607
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Analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profiles BJPS
Resende,Renata Cunha de; Viana,Olímpia Maria Martins Santos; Freitas,Jennifer Tavares Jacon; Bonfilio,Rudy; Ruela,André Luís Morais; Araújo,Magali Benjamim de.
ABSTRACT Spironolactone (SPR) is a steroidal drug administered as a potassium-sparing diuretic for high blood pressure treatment. The drug shows incomplete gastrointestinal absorption due to its poor aqueous solubility. The physicochemical properties of SPR in crystal forms I and II suggest that differences in their aqueous solubility may lead to a lack of bioequivalence between solid-state formulations. In this study, SPR polymorphs in five batches of active pharmaceutical ingredients (APIs) from three manufacturers were characterized using powder X-ray diffraction, infrared spectroscopy, thermal analysis, and solubility measurements. SPR tablets (50 mg) were manufactured in our laboratory using API in pure form II, and API in form II contaminated with...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Spironolactone/dissolution profile; Spironolactone/pharmaceutical equivalence; Spironolactone/solubility; Spironolactone/polymorphism; Drugs/quality assessment..
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000400613
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