Effect of stearic acid on enalapril stability and dissolution from multiparticulate solid dosage forms

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dc.creatorCunha, Talita de Amorim
dc.creatorSerpa, Raphael Caixeta
dc.creatorOliveira, Ana Paula Martins de
dc.creatorNaves, Leticia Nasser
dc.creatorFreitas, Luis Alexandre Pedro de
dc.creatorTaveira, Stephânia Fleury
dc.creatorDiniz, Danielle Guimarães Almeida
dc.creatorLima, Eliana Martins
dc.creatorMarreto, Ricardo Neves
dc.date.accessioned2022-05-31T12:45:08Z
dc.date.available2022-05-31T12:45:08Z
dc.date.issued2013-09
dc.description.abstractEnalapril maleate (EM) is a widely used anti-hypertensive drug which is unstable when mixed with excipients. Enalaprilate and diketopiperazine (DPK) are the main degradation products of enalapril. The in situ preparation of enalapril sodium salt (NaE) has been used to improve drug stability in dosage forms; however, gas release and product rejection ensue when the chemical reaction for obtaining the sodium salt is not completely finished before packaging. This study evaluated the effect of stearic acid (SA) on enalapril stability in microcrystalline cellulose (MCC) pellets containing EM or NaE. MCC pellets containing SA were prepared by the extrusion–spheronization technique and characterized. Enalapril stability and dissolution were then evaluated. DPK and enalaprilate formation were reduced by the addition of SA in pellets containing EM. The overall enalapril degradation in these formulations was lower when compared with pellets containing EM or even NaE prepared without SA. The immediate release characteristic was maintained by the addition of 5% crospovidone to all the formulations tested. The incorporation of SA into NaE pellets resulted in unexpected enalapril degradation, caused by the interaction of these compounds, as suggested by a thermal analysis of the SA–NaE binary mixture. The findings presented here showed that formulations containing SA could substitute the formation of NaE, since they provide better enalapril stability in solid dosage forms. In addition, it is suggested that the stabilization effects would be observed for other N-carboxyalkyl dipeptide analogs with angiotensin converting enzyme inhibition activity, since these new entities share the same degradation pathway of enalapril.pt_BR
dc.identifier.citationCUNHA, Talita A. et al. Effect of stearic acid on enalapril stability and dissolution from multiparticulate solid dosage forms. AAPS PharmSciTech, New York, v. 14, n. 3, p. 1150-1157, Sept. 2013.pt_BR
dc.identifier.doi10.1208/s12249-013-0006-6
dc.identifier.issne- 1530-9932
dc.identifier.issn1530-9932
dc.identifier.urihttp://repositorio.bc.ufg.br/handle/ri/20818
dc.language.isoengpt_BR
dc.publisher.countryEstados unidospt_BR
dc.publisher.departmentFaculdade de Farmácia - FF (RG)pt_BR
dc.rightsAcesso Abertopt_BR
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectDiketopiperazinept_BR
dc.subjectStearic acid.pt_BR
dc.subjectEnalaprilatept_BR
dc.subjectExtrusion–spheronizationpt_BR
dc.subjectEnalaprilpt_BR
dc.titleEffect of stearic acid on enalapril stability and dissolution from multiparticulate solid dosage formspt_BR
dc.typeArtigopt_BR

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