Your browser doesn't support javascript.
loading
Amorphous Solid Dispersions of Felodipine and Nifedipine with Soluplus®: Drug-Polymer Miscibility and Intermolecular Interactions.
Sarpal, Kanika; Munson, Eric J.
Afiliação
  • Sarpal K; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536, USA.
  • Munson EJ; Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY 40536, USA. Electronic address: munsone@purdue.edu.
J Pharm Sci ; 110(4): 1457-1469, 2021 04.
Article em En | MEDLINE | ID: mdl-33359813
The objective of this study was to investigate thermodynamic and kinetic miscibility for two structurally similar model compounds nifedipine (NIF) and felodipine (FEL) when formulated as amorphous solid dispersions (ASDs) with an amphiphilic polymer Soluplus®. Thermodynamic miscibility was studied via melting point depression approach for the two systems. The Flory Huggins theory was used to calculate the interaction parameter and generate the phase diagrams. It was shown that NIF was more miscible in Soluplus® than FEL. The nature of drug polymer interactions was studied by fourier transform infra-red spectroscopy (FTIR) and solid-state nuclear magnetic resonance spectroscopy (ssNMR). The data from spectroscopic analyses showed that both the drugs interacted with Soluplus® through hydrogen bonding interactions. Furthermore, 13C ssNMR data was used to get quantitative estimate of the extent of hydrogen bonding for ASDs samples. Proton relaxation measurements were carried out on ASDs in order to evaluate phase heterogeneity on two different length scales of mixing. The data suggested that better phase homogeneity in NIF:SOL systems especially for lower Soluplus® content ASDs on smaller domains. This could be explained by understanding the extent of hydrogen bonding interactions for these two systems. This study highlights the need to consider thermodynamic and kinetic mixing, when formulating ASDs with the goal of understanding phase mixing between drug and polymer.
Assuntos
Palavras-chave

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Preparações Farmacêuticas / Felodipino Idioma: En Ano de publicação: 2021 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Preparações Farmacêuticas / Felodipino Idioma: En Ano de publicação: 2021 Tipo de documento: Article