Amorphous Stabilization and Dissolution Enhancement of Amorphous Ternary Solid Dispersions: Combination of Polymers Showing Drug–Polymer Interaction for Synergistic Effects

The aim of this study was to manufacture the ternary solid dispersions composed of nifedipine, Eudragit® E and adsorbent. Dissolution enhancement of nifedipine was also investigated. The inert solid carriers were added in the mixtures of nifedipine and Eudragit® E at varying ratios. The physicochemical properties of ternary systems, compared to physical mixtures, were analyzed using powder x-ray diffraction (PXRD) and differential scanning calorimetry (DSC). The dissolution of nifedipine from ternary systems was compared to the drug alone. The influence of drug:polymer: adsorbent ratio and type of adsorbent on the dissolution rate of the drug was also evaluated. The PXRD and DSC results of the systems with high amount of polymer showed that the drug was present in an amorphous form. On the other hand, the diffraction patterns and DSC thermograms of the physical mixtures revealed that to some extent the drug was present in a crystalline form. The results from this study demonstrated that an improvement in dissolution rate of nifedipine with Eudragit® E and adsorbents was obtained.

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Investigation of drug–polymer interaction in solid dispersions by vapour sorption methods

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2014.04.048 ◽

2014 ◽

Vol 469 (1) ◽

pp. 159-167 ◽

Cited By ~ 37

Author(s):

Kateřina Punčochová ◽

Jerry Y.Y. Heng ◽

Josef Beránek ◽

František Štěpánek

Keyword(s):

Solid Dispersions ◽

Vapour Sorption ◽

Drug Polymer Interaction ◽

Polymer Interaction

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Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer based controlled release tablets of aceclofenac to simultaneously enhance the solubility and bioavailability

Main Group Chemistry ◽

10.3233/mgc-210057 ◽

2021 ◽

pp. 1-13

Author(s):

Barkat Ali Khan ◽

Muhammad Kamran Khan ◽

Naeem Haider ◽

Farid Menaa ◽

Muhammad Khalid Khan

Keyword(s):

Polyethylene Glycol ◽

Controlled Release ◽

Polyvinyl Acetate ◽

Solid Dispersions ◽

Compression Method ◽

Zero Order Kinetics ◽

Drug Polymer Interaction ◽

Tablet Dosage ◽

Controlled Release Tablets ◽

Polymer Interaction

The aim of this study was to enhance the solubility of Aceclofenac with a new polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer (Soloplus ®) and formulate it in controlled release (CR) tablet dosage form by direct compression method with HPMC K-15. Solid dispersions were prepared in different ratio of Aceclofenac and Soloplus ® as F1, F2 and F3 with different polymer ratios i.e. 30%, 50%, and 70% respectively. All the quality control tests were performed for the prepared controlled release tablets. Drug polymer interaction studies of Aceclofenac and Soloplus ® were carried using FTIR and XRD. Dissolution study was carried out against Alkaris ® as a standard reference. The formulation F3 showed optimum results and followed zero order kinetics. The Soloplus ® improved the solubility of the drug and the CR formulation enhanced the delivery in a sustained manner. Hence, the CR formulation enhanced the delivery of aceclofenac in a sustained manner, thereby an efficient drug delivery may lead to an effective anti-inflammatory activity.

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Ternary Solid Dispersions of Celecoxib: from Physical Characterization to Dissolution Enhancement

Journal of Pharmaceutical Research ◽

10.18579/jpcrkc/2013/12/2/79154 ◽

2013 ◽

Vol 12 (2) ◽

pp. 80

Author(s):

M. V. Nagabhushanam ◽

Ch. V . Prasada Rao ◽

M. Beena Devi ◽

J. Suresh Kumar

Keyword(s):

Solid Dispersions ◽

Physical Characterization ◽

Dissolution Enhancement ◽

Ternary Solid Dispersions

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Molecular Interactions for the Curcumin-Polymer Complex with Enhanced Anti-Inflammatory Effects

Pharmaceutics ◽

10.3390/pharmaceutics11090442 ◽

2019 ◽

Vol 11 (9) ◽

pp. 442 ◽

Cited By ~ 6

Author(s):

Yan He ◽

Hongfei Liu ◽

Wangqing Bian ◽

Yue Liu ◽

Xinyang Liu ◽

...

Keyword(s):

Molecular Interactions ◽

Solid Dispersions ◽

Amorphous Solid ◽

Dynamics Simulation ◽

Amorphous Solid Dispersion ◽

Polymer Complex ◽

Formulation Development ◽

Anti Inflammatory ◽

Drug Polymer Interaction ◽

Polymer Interaction

The molecular interactions between compound and polymeric carriers are expected to highly contribute to high drug load and good physical stability of solid dispersions. In this study, a series of amorphous solid dispersions (ASD) of Curcumin (Cur) were prepared with different polymers by the solvent evaporation method. With the carrier polyvinylpyrrolidone (PVP), the amorphous solid dispersion system exhibits a better solubility and stability than that with poloxamers and HP-β-CD due to the strong drug-polymer interaction. The drug/polymer interaction and their binding sites were investigated by combined experimental (XRD, DSC, FTIR, SEM, Raman, and 1H-NMR) and molecular dynamics simulation techniques. The Curcumin ASD demonstrated enhanced bioavailability by 11-fold and improved anti-inflammatory activities by the decrease in cytokine production (MMP-9, IL-1β, IL-6, VEGF, MIP-2, and TNF-α) compared to the raw Curcumin. The integration of experimental and modeling techniques is a powerful tool for the rational design of formulation development.

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