Construction and Validation of Binary Phase Diagram for Amorphous Solid Dispersion Using Flory–Huggins Theory

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• 作者：Krishna Bansal ; Uttam Singh Baghel ; Seema Thakral
• 刊名：AAPS PharmSciTech
• 出版年：2016
• 出版时间：April 2016
• 年：2016
• 卷：17
• 期：2
• 页码：318-327
• 全文大小：410 KB
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• 作者单位：Krishna Bansal (1)
  Uttam Singh Baghel (2)
  Seema Thakral (1) (3)
  
  1. GVM College of Pharmacy, Sonipat, Haryana, 131001, India
  2. Khalsa College of Pharmacy, Amritsar, Punjab, 143001, India
  3. College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, 55455, USA
  
• 刊物主题：Pharmacology/Toxicology; Biotechnology; Biochemistry, general; Pharmacy;
• 出版者：Springer US
• ISSN：1530-9932

文摘

Drug–polymer miscibility is one of the fundamental prerequisite for the successful design and development of amorphous solid dispersion formulation. The purpose of the present work is to provide an example of the theoretical estimation of drug–polymer miscibility and solubility on the basis of Flory–Huggins (F–H) theory and experimental validation of the phase diagram. The F–H interaction parameter, χ _d-p, of model system, aceclofenac and Soluplus, was estimated by two methods: by melting point depression of drug in presence of different polymer fractions and by Hildebrand and Scott solubility parameter calculations. The simplified relationship between the F–H interaction parameter and temperature was established. This enabled us to generate free energy of mixing (ΔG _mix) curves for varying drug–polymer compositions at different temperatures and finally the spinodal curve. The predicted behavior of the binary system was evaluated through X-ray diffraction, differential scanning calorimetry, and in vitro dissolution studies. The results suggest possibility of employing interaction parameter as preliminary tool for the estimation of drug–polymer miscibility.