Physical-chemical characterization and quality control of spironolactone raw material samples

Brandão, F. C.; Tagiari, M. P.; Silva, M. A. S.; Berti, Lucas Freitas; Stulzer, Hellen Karine

doi:10.1007/s11094-008-0129-3

Cited by 9 publications

(4 citation statements)

References 20 publications

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“…The DSC thermograms reported in the literature [24], for both polymorphs and amorphous indomethacin, are characteristic, with the sharp endothermic peak above 160 • C being attributed to the γ form, as in our case. The obtained spironolactone DSC curves show a single sharp endothermic peak at the melting temperature of 213 • C, confirming the purity and crystallinity of the SPIR [25].…”

Section: Discussionsupporting

confidence: 61%

Thermal Analysis in the Evaluation of Solid Lipid Microparticles in the Form of Aqueous Dispersion and Fine Powder

Wolska,

Regdon

2023

Applied Sciences

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In the presented study, an attempt was made to investigate the most important attributes of solid lipid microparticles (SLM) using thermal analysis (DSC/TG) in order to determine the importance of this technique in the research and development of lipid microparticles. Particularly interesting in our studies were drug–lipid interactions and modifications of the SLM matrix structure induced by the production method (the hot emulsification method) and further processing (e.g., spray drying), as well as changes occurring during the stability studies. Cyclosporine A, indomethacin and spironolactone were used as model active substances incorporated into SLM. The conducted research demonstrated the significant potential of DSC/TG, especially for the analysis of SLM in the form of fine powder. The method of sample preparation, consisting of evaporation of water at room temperature, turned out to be crucial for the DSC/TG analysis of SLM dispersion. In the case of the tested SLM, the basic and usually the only observed thermal transformation in the DSC spectrum was the endothermic peak associated with the lipid forming a microsphere matrix. This peak is the main source of information about the properties and stability of the tested SLM. The obtained results show that glyceryl behenate (Compritol) is a significantly better lipid for forming lipid microparticles than stearic acid. Although thermal transformations of the incorporated drug substances are not directly visible in the DSC spectra, their impact on the SLM properties can be assessed indirectly, based on changes in the lipid melting point and the shape of the DSC and TG peaks and curves. DSC/TG studies confirmed the lack of an effect of the spray drying process on the properties of drug-loaded SLM with Compritol. Studies have also shown up to a 2-year stability of SLM with CsA.

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Section: Discussionsupporting

confidence: 61%

Thermal Analysis in the Evaluation of Solid Lipid Microparticles in the Form of Aqueous Dispersion and Fine Powder

Wolska,

Regdon

2023

Applied Sciences

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“…No caso do BNZ, deve haver um controle rigoroso do tamanho de partícula, uma vez que este parâmetro físico possui influência direta em sua velocidade de dissolução, um fator crítico para sua biodisponibilidade. 24 Os dados de tamisação do BNZ se ajustaram a uma distribuição logaritmo normal, o que permitiu determinar os valores de diâmetro médio de partícula e desvio padrão geométrico em 192,2 e 0,12 µm, respectivamente. Conforme se observa no histograma da Figura 4, a distribuição do tamanho de partícula do BNZ é relativamente fechada e com tamanhos de partícula consideráveis.…”

Section: Análise Granulométrica E Morfológicaunclassified

Caracterização físico-química do fármaco antichagásico benznidazol

Maximiano¹,

Costa²,

Souza³

et al. 2010

Quím. Nova

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Recebido em 5/1/10; aceito em 18/4/10; publicado na web em 9/8/10 PHYSICOCHEMICAL CHARACTERIZATION OF ANTICHAGASIC BENZNIDAZOLE. Currently, benznidazole (BNZ) is a unique therapeutic alternative available in Brazil to treat Chagas disease. Despite its traditional medical use, little is known about the chemical nature of this drug. A detailed study of the physicochemical properties of BNZ was performed using multiple assays. Thermal, diffractometric, morphological and reological drug profiles were obtained. The partition coefficient and solubility results allowed this drug to be classified as a class IV drug according to the biopharmaceutical classification system. This information will be useful for the development of more effective BNZ formulations and for establishing the quality profile of BNZ.Keywords: benznidazole; preformulation; biopharmaceutical classification. INTRODUÇÃOA pesquisa e o desenvolvimento de medicamentos inovadores têm sido uma empreitada cada vez mais cara e complexa, o que torna mais escassa a introdução de novas moléculas no mercado. Estima-se que de cada 30.000 compostos sintetizados, apenas 0,003% chegam a se tornar fármacos disponíveis no comércio. 2Dentre as causas que explicam estes inúmeros fracassos estão problemas derivados de sua biodisponibilidade e toxicidade, que podem estar relacionados ao escasso conhecimento acerca da natureza da molécula em estudo. 3Neste contexto, os estudos de pré-formulação, realizados nas etapas de pesquisa pré-clínica e clínica de fármacos inovadores, e que visam acumular o máximo de informação sobre o comportamento das novas entidades químicas, constituem um valioso instrumento para traçar estratégias de desenvolvimento racional de formulações mais eficazes e seguras e, portanto, com maiores possibilidades de êxito. 4,5 Diversos aspectos concernentes à substância ativa, como a biodisponibilidade a partir da forma farmacêutica, ou ao medicamento, como seu prazo de validade, e até mesmo seu processamento industrial são afetados pelas propriedades físico-químicas dos fármacos.O Benznidazol [BNZ] (N-benzyl-2-nitro-1-imidazole-acetamide) (Figura 1), constitui um dos únicos recursos terapêuticos disponíveis no combate à doença de Chagas há décadas. Este medicamento é bastante efetivo na fase aguda da doença, mas existem relatos de baixa ou nenhuma eficácia na fase crônica. Efeitos secundários severos associados à utilização desse fármaco têm sido reportados, tendo como consequência, a interrupção do tratamento medicamentoso. Apesar de ser um fármaco já consolidado no mercado e bastante estudado do ponto de vista farmacológico, as propriedades físico-químicas do BNZ são praticamente desconhecidas. Estudos de pré-formulação poderiam propiciar uma maior compreensão das suas características biofarmacêuticas e permitir vislumbrar alternativas para melhorar sua ação terapêutica.Desta forma, o objetivo deste estudo foi traçar o perfil físico-químico do BNZ através de diferentes ensaios de caracterização, como forma de estabelecer parâmetros de qualidade para est...

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“…Different polymorphs of the same drug or biologically active substance may have different physicochemical properties, which directly influence the process of synthesis and production of the drug, as well as the dissolution, stability and bioavailability process, among other characteristics that affect the quality, efficacy and safety of the drug. Thus, the identification, characterization and control of polymorphs are fundamental, both in the product development phase and during the marketing period …”

Section: Introductionmentioning

confidence: 99%

Polymorphic characterization and implications on biopharmaceutics properties of potential anti-inflammatory drug candidate eremantholide C from Lychnophora trichocarpha (Brazilian Arnica)

Caldeira

Saúde-Guimarães

Lacerda

et al. 2019

Journal of Pharmacy and Pharmacology

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Objectives To perform the polymorphic and physicochemical characterization of the potential anti‐inflammatory drug, eremantholide C (EREC), as well as to evaluate the influence of these characteristics on its biopharmaceutics classification. Methods Eremantholide C was obtained from chloroformic extract of Lychnophora trichocarpha and crystallized in two distinct solvents: chloroform (EREC 1) and ethyl acetate (EREC 2). To evaluate the polymorphism, EREC samples were submitted to melting point, purity, infrared spectroscopy, differential scanning calorimetry (DSC), X‐ray powder diffraction, optical microscopy and scanning electron microscopy analysis. In addition, EREC samples crystallized after intrinsic dissolution study were submitted to DSC and X‐ray powder diffraction analysis. Key findings EREC 1 showed fusion at 234.7–241.6 °C, while EREC 2 showed fusion at 238.6–243.7 °C. No polymorphic transitions were observed during the intrinsic dissolution experiment. A single sharp endothermic peak was obtained for the EREC samples. X‐ray diffraction showed no crystallographic differences between the EREC samples. EREC 1 and EREC 2 showed birefringence under polarized light and indefinite morphology; however, the shape of the crystals was common to the two samples. Conclusions Eremantholide C does not present classical or morphological polymorphism; therefore, there is no influence of crystalline transitions in the solubility and consequently in its biopharmaceutics classification and oral absorption process.

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Physical-chemical characterization and quality control of spironolactone raw material samples

Cited by 9 publications

References 20 publications

Thermal Analysis in the Evaluation of Solid Lipid Microparticles in the Form of Aqueous Dispersion and Fine Powder

Thermal Analysis in the Evaluation of Solid Lipid Microparticles in the Form of Aqueous Dispersion and Fine Powder

Caracterização físico-química do fármaco antichagásico benznidazol

Polymorphic characterization and implications on biopharmaceutics properties of potential anti-inflammatory drug candidate eremantholide C from Lychnophora trichocarpha (Brazilian Arnica)

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