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Insight into the Dissolution Molecular Mechanism of Ternary Solid Dispersions by Combined Experiments and Molecular Simulations.
Han, Run; Huang, Tianhe; Liu, Xinyang; Yin, Xunqing; Li, Haifeng; Lu, Jiahong; Ji, Yuanhui; Sun, Huimin; Ouyang, Defang.
Afiliação
  • Han R; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese, Medical Sciences (ICMS), University of Macau, Macau, China.
  • Huang T; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese, Medical Sciences (ICMS), University of Macau, Macau, China.
  • Liu X; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese, Medical Sciences (ICMS), University of Macau, Macau, China.
  • Yin X; Institute of Applied Physics and Materials Engineering, University of Macau, Macau, China.
  • Li H; Institute of Applied Physics and Materials Engineering, University of Macau, Macau, China.
  • Lu J; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese, Medical Sciences (ICMS), University of Macau, Macau, China.
  • Ji Y; Jiangsu Province Hi-Tech Key Laboratory for Bio-medical Research, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, 211189, China.
  • Sun H; National Institute for Food and Drug Control, No. 2, Tiantan Xili Road, Beijing, 100050, China.
  • Ouyang D; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese, Medical Sciences (ICMS), University of Macau, Macau, China. defangouyang@umac.mo.
AAPS PharmSciTech ; 20(7): 274, 2019 Aug 05.
Article em En | MEDLINE | ID: mdl-31385095
With the increase concern of solubilization for insoluble drug, ternary solid dispersion (SD) formulations developed more rapidly than binary systems. However, rational formulation design of ternary systems and their dissolution molecular mechanism were still under development. Current research aimed to develop the effective ternary formulations and investigate their molecular mechanism by integrated experimental and modeling techniques. Glipizide (GLI) was selected as the model drug and PEG was used as the solubilizing polymer, while surfactants (e.g., SDS or Tween80) were the third components. SD samples were prepared at different weight ratio by melting method. In the dissolution tests, the solubilization effect of ternary system with very small amount of surfactant (drug/PEG/surfactant 1/1/0.02) was similar with that of binary systems with high polymer ratios (drug/PEG 1/3 and 1/9). The molecular structure of ternary systems was characterized by differential scanning calorimetry (DSC), infrared absorption spectroscopy (IR), X-ray diffraction (XRD), and scanning electron microscope (SEM). Moreover, molecular dynamic (MD) simulations mimicked the preparation process of SDs, and molecular motion in solvent revealed the dissolution mechanism of SD. As the Gordon-Taylor equation described, the experimental and calculated values of Tg were compared for ternary and binary systems, which confirmed good miscibility of GLI with other components. In summary, ternary SD systems could significantly decrease the usage of polymers than binary system. Molecular mechanism of dissolution for both binary and ternary solid dispersions was revealed by combined experiments and molecular modeling techniques. Our research provides a novel pathway for the further research of ternary solid dispersion formulations.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Polietilenoglicóis / Polissorbatos / Modelos Moleculares / Glipizida Idioma: En Revista: AAPS PharmSciTech Assunto da revista: FARMACOLOGIA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: China País de publicação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Polietilenoglicóis / Polissorbatos / Modelos Moleculares / Glipizida Idioma: En Revista: AAPS PharmSciTech Assunto da revista: FARMACOLOGIA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: China País de publicação: Estados Unidos