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Insight into the Dissolution Molecular Mechanism of Ternary Solid Dispersions by Combined Experiments and Molecular Simulations
Run Han1; Tianhe Huang1; Xinyang Liu1; Xinyang Liu2; Haifeng Li2; Jiahong Lu1; Yuanhui Ji3; Huimin Sun4; Defang Ouyang1
2019-08-05
Source PublicationAAPS PHARMSCITECH
ISSN1530-9932
Volume20Issue:7
Abstract

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.

KeywordSolid Dispersion Dissolution Effect Molecular Modeling Ternary System
DOI10.1208/s12249-019-1486-9
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000478877700002
PublisherSPRINGER, 233 SPRING ST, NEW YORK, NY 10013 USA
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Cited Times [WOS]:1   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorDefang Ouyang
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese, Medical Sciences (ICMS), University of Macau, Macau, China
2.Institute of Applied Physics and Materials Engineering, University of Macau, Macau, China
3.Jiangsu Province Hi-Tech Key Laboratory for Bio-medical Research, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, 211189, China
4.National Institute for Food and Drug Control, No. 2, Tiantan Xili Road, Beijing, 100050, China
First Author AffilicationUniversity of Macau
Corresponding Author AffilicationUniversity of Macau
Recommended Citation
GB/T 7714
Run Han,Tianhe Huang,Xinyang Liu,et al. Insight into the Dissolution Molecular Mechanism of Ternary Solid Dispersions by Combined Experiments and Molecular Simulations[J]. AAPS PHARMSCITECH,2019,20(7).
APA Run Han.,Tianhe Huang.,Xinyang Liu.,Xinyang Liu.,Haifeng Li.,...&Defang Ouyang.(2019).Insight into the Dissolution Molecular Mechanism of Ternary Solid Dispersions by Combined Experiments and Molecular Simulations.AAPS PHARMSCITECH,20(7).
MLA Run Han,et al."Insight into the Dissolution Molecular Mechanism of Ternary Solid Dispersions by Combined Experiments and Molecular Simulations".AAPS PHARMSCITECH 20.7(2019).
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