Solubility and dissolution studies of tibolone polymorphs

Bonfílio, Rudy; Souza, Marília Cristina Oliveira; Leal, Jockastta Silva; Viana, Olímpia Maria Martins Santos; Araújo, Magali Benjamim

doi:10.1590/s2175-97902017000400233

Cited by 8 publications

(3 citation statements)

References 8 publications

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“…However, tibolone form II tablets have a lower release than tablets containing form I. These forms also differ in interactions with pharmaceutical excipients [25]. Our study confirms the importance of polymorphism studies and emphasizes the problem of varieties of physicochemical properties in different conditions.…”

Section: Resultssupporting

confidence: 79%

Structural Polymorphism of Sorafenib Tosylate as a Key Factor in Its Solubility Differentiation

et al. 2021

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The presence of active pharmaceutical ingredients (APIs) in the forms of different polymorphic states can induce differences in their physicochemical properties. In the case of poorly soluble APIs, like the oncological drug sorafenib tosylate, small variations in solubility may result in large bioavailability differences. The control of its therapeutic dose is crucial from the effective pharmacotherapy point of view and the reduction of side effects. Therefore, this study aimed to assess the influence of sorafenib tosylate polymorphic forms on its solubility and, consequently, permeability, based on passive diffusion through membranes simulating the gastrointestinal tract (GIT) conditions. In the first part of the work, two crystalline forms of sorafenib tosylate were identified using the X-ray powder diffraction, FT-IR, and Raman spectroscopy. Subsequently, solubility studies were carried out. Both forms of sorafenib tosylate were insoluble in 0.1 N hydrochloric acid (HCl), in acetate buffer (pH 4.5), and in phosphate buffer (pH 6.8). Solubility (mg/mL) of form I and III of sorafenib tosylate in 0.1 N HCl + 1.0% SDS was 0.314 ± 0.006 and 1.103 ± 0.014, respectively, in acetate buffer pH 4.5 + 1.0% SDS it was 2.404 ± 0.012 and 2.355 ± 0.009, respectively, and in phosphate buffer pH 6.8 + 1.0% SDS it was 0.051 ± 0.005 and 1.805 ± 0.023, respectively. The permeability study was assessed using the parallel artificial membrane permeability assay (PAMPA) model. The apparent permeability coefficient (Papp—cm s−1) of form I and III in pH 1.2 was 3.01 × 10−5 ± 4.14 × 10−7 and 3.15 × 10−5 ± 1.89 × 10−6, respectively, while in pH 6.8 it was 2.72 × 10−5 ± 1.56 × 10−6 and 2.81 × 10−5 ± 9.0 × 10−7, respectively. Changes in sorafenib tosylate concentrations were determined by chromatography using the high-performance liquid chromatography (HPLC)–DAD technique. As a result of the research on the structural polymorphism of sorafenib tosylate, its full spectral characteristics and the possibility of using FT-IR and Raman spectroscopy for the study of polymorphic varieties were determined for the first time, and the HPLC method was developed, which is appropriate for the assessment of sorafenib solubility in various media. The consequences of various physicochemical properties resulting from differences in the solubility of sorafenib tosylate polymorphs are important for pre-formulation and formulation studies conducted with its participation and for the safety of oncological sorafenib therapy.

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Section: Resultssupporting

confidence: 79%

Structural Polymorphism of Sorafenib Tosylate as a Key Factor in Its Solubility Differentiation

et al. 2021

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“…This determination is achieved by adding an excess of a compound in a fixed volume (25–50 ml), followed by agitation at room temperature that can last several days. This study is conducted using water and different buffers to fully characterize the solubility of a said active ingredient ( Bonfilio et al, 2018 ). In our research, we evaluated the antimicrobial properties of the BG extract based on the evidence of its wound healing properties ( Backhouse et al, 2008 ; Bustamante et al, 2015 ).…”

Section: Discussionmentioning

confidence: 99%

Formulation of water-soluble Buddleja globosa Hope extracts and characterization of their antimicrobial properties against Pseudomonas aeruginosa

Araya

Leiva-Soto²,

Bruna³

et al. 2022

Front. Pharmacol.

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Buddleja globosa Hope (BG) extracts are traditionally used to treat skin and gastric ulcers due to their healing properties. Non-aqueous solvents such as ethanol and DMSO are usually used to extract naturally occurring compounds. However, the cytotoxicity of these solvents and the low water solubility of the extracted compounds can hinder their biomedical applications. To overcome the limited solubility of the BG extracts, we aimed to enhance the solubility by processing a standardized hydroalcoholic extract (BG-126) through spray drying (SD), with and without two solubility enhancers. Spray-dried BG (BG-SD) extracts and spray-dried BG extracts plus polyvinylpyrrolidone (BG-SD PVP) and Soluplus® (BG-SD SP) were developed starting from BG-126 (containing 53% ethanol). These four formulations were characterized by total phenolic content, water solubility at 25°C and 37°C, and antimicrobial properties against Pseudomonas aeruginosa. All the SD formulations presented a solubility that allowed them to reach maximum concentrations of 1,024 μg/ml catechin for BG-SD and 2,048 μg/ml catechin for BG-SD PVP and BG-SD SP for antimicrobial testing. BG-SD showed the highest antimicrobial potency with a minimum inhibitory concentration (MIC) of 512 μg/ml catechin, followed by BG-126 with a MIC of 1,024 μg/ml catechin and SP. BG-126 was also shown to inhibit biofilm formation, as well as the excipients PVP and SP. The spray-dried BG (BG-SD) extract represents a promising natural active component with enhanced antimicrobial properties against P. aeruginosa for further research and the development of novel phytopharmaceuticals.

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“…Owing to its low solubility in water (Bonfilio et al, 2018), it could be detected in very low concentration in surface waters.…”

Section: Introductionmentioning

confidence: 99%

Avaliação Da Remoção De Alumínio De Água Utilizando Adsorvente Produzido a Partir De Folhas De Persea Americana Mill

Tomassoni¹,

Giroletti²,

Hassemer³

2022

Meio Ambiente E Sustentabilidade: Formação Interdisciplinar E Conhecimento Científico 2

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Editora Direitos para esta edição cedidos à Atena Editora pelos autores. Open access publication by Atena Editora Todo o conteúdo deste livro está licenciado sob uma Licença de Atribuição Creative Commons. Atribuição-Não-Comercial-NãoDerivativos 4.0 Internacional (CC BY-NC-ND 4.0). O conteúdo dos artigos e seus dados em sua forma, correção e confiabilidade são de responsabilidade exclusiva dos autores, inclusive não representam necessariamente a posição oficial da Atena Editora. Permitido o download da obra e o compartilhamento desde que sejam atribuídos créditos aos autores, mas sem a possibilidade de alterála de nenhuma forma ou utilizá-la para fins comerciais.Todos os manuscritos foram previamente submetidos à avaliação cega pelos pares, membros do Conselho Editorial desta Editora, tendo sido aprovados para a publicação com base em critérios de neutralidade e imparcialidade acadêmica.A Atena Editora é comprometida em garantir a integridade editorial em todas as etapas do processo de publicação, evitando plágio, dados ou resultados fraudulentos e impedindo que interesses financeiros comprometam os padrões éticos da publicação. Situações suspeitas de má conduta científica serão investigadas sob o mais alto padrão de rigor acadêmico e ético.

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Solubility and dissolution studies of tibolone polymorphs

Cited by 8 publications

References 8 publications

Structural Polymorphism of Sorafenib Tosylate as a Key Factor in Its Solubility Differentiation

Structural Polymorphism of Sorafenib Tosylate as a Key Factor in Its Solubility Differentiation

Formulation of water-soluble Buddleja globosa Hope extracts and characterization of their antimicrobial properties against Pseudomonas aeruginosa

Avaliação Da Remoção De Alumínio De Água Utilizando Adsorvente Produzido a Partir De Folhas De Persea Americana Mill

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