Analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profiles
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 dif...
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doaj-bcaa941258374b0bbca8c0c06664c08f2020-11-24T23:10:02ZengUniversidade de São PauloBrazilian Journal of Pharmaceutical Sciences2175-979052461362110.1590/s1984-82502016000400005S1984-82502016000400613Analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profilesRenata Cunha de ResendeOlímpia Maria Martins Santos VianaJennifer Tavares Jacon FreitasRudy BonfilioAndré Luís Morais RuelaMagali Benjamim de AraújoABSTRACT 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 form I, which was found in a commercial batch. Physicochemical quality evaluations of the manufactured tablets, along with five SPR tablets marketed in Brazil, were performed, and results indicated differences in their dissolution profiles. In the manufactured tablets, differences were associated with the increased solubility of API in form II contaminated with form I compared to API in pure form II. In the marketed SPR tablets, the formulation composition demonstrated an important role in the dissolution rate of the drug, leading to lack of pharmaceutical equivalence among the drug products.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000400613&lng=en&tlng=enSpironolactone/dissolution profileSpironolactone/pharmaceutical equivalenceSpironolactone/solubilitySpironolactone/polymorphismDrugs/quality assessment. |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Renata Cunha de Resende Olímpia Maria Martins Santos Viana Jennifer Tavares Jacon Freitas Rudy Bonfilio André Luís Morais Ruela Magali Benjamim de Araújo |
spellingShingle |
Renata Cunha de Resende Olímpia Maria Martins Santos Viana Jennifer Tavares Jacon Freitas Rudy Bonfilio André Luís Morais Ruela Magali Benjamim de Araújo Analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profiles Brazilian Journal of Pharmaceutical Sciences Spironolactone/dissolution profile Spironolactone/pharmaceutical equivalence Spironolactone/solubility Spironolactone/polymorphism Drugs/quality assessment. |
author_facet |
Renata Cunha de Resende Olímpia Maria Martins Santos Viana Jennifer Tavares Jacon Freitas Rudy Bonfilio André Luís Morais Ruela Magali Benjamim de Araújo |
author_sort |
Renata Cunha de Resende |
title |
Analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profiles |
title_short |
Analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profiles |
title_full |
Analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profiles |
title_fullStr |
Analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profiles |
title_full_unstemmed |
Analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profiles |
title_sort |
analysis of spironolactone polymorphs in active pharmaceutical ingredients and their effect on tablet dissolution profiles |
publisher |
Universidade de São Paulo |
series |
Brazilian Journal of Pharmaceutical Sciences |
issn |
2175-9790 |
description |
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 form I, which was found in a commercial batch. Physicochemical quality evaluations of the manufactured tablets, along with five SPR tablets marketed in Brazil, were performed, and results indicated differences in their dissolution profiles. In the manufactured tablets, differences were associated with the increased solubility of API in form II contaminated with form I compared to API in pure form II. In the marketed SPR tablets, the formulation composition demonstrated an important role in the dissolution rate of the drug, leading to lack of pharmaceutical equivalence among the drug products. |
topic |
Spironolactone/dissolution profile Spironolactone/pharmaceutical equivalence Spironolactone/solubility Spironolactone/polymorphism Drugs/quality assessment. |
url |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000400613&lng=en&tlng=en |
work_keys_str_mv |
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1725608449927020544 |