Solid‐State Characterization of Amorphous Dispersions

Vogt, Frederick G.

doi:10.1002/9780470571224.pse525

Cited by 7 publications

(4 citation statements)

References 155 publications

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“…The changes in frequency of the carbonyl bond (H-bond acceptor) in the dispersion can also be related to intermolecular interactions. 43 The obtained FTIR spectra showed the characteristic peak at 1011 cm −1 confirming the polymorphic form I of the RXB. 44 The crystalline RXB shows the secondary amide N−H stretching vibration band at 3354 cm −1 , and the bending mode (scissoring) appears as medium intensity bands at 1547 and 1518 cm −1 .…”

Section: ■ Results and Discussionmentioning

confidence: 72%

“…In particular, the stretching frequencies of N–H and O–H groups act as hydrogen bond (H-bond) donors; thus, their bands tend to broaden, decrease, or disappear depending on the H-bond donor–acceptor distances. The changes in frequency of the carbonyl bond (H-bond acceptor) in the dispersion can also be related to intermolecular interactions …”

Section: Results and Discussionmentioning

confidence: 99%

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Enhanced Biopharmaceutical Performance of Rivaroxaban through Polymeric Amorphous Solid Dispersion

et al. 2018

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Rivaroxaban (RXB) is an orally active direct inhibitor of the activated serine protease Factor Xa, given as monotherapy in the treatment of venous thromboembolism (VTE). It has been characterized in vitro as a substrate for the active, nonsaturable efflux via P-gp transporter, limiting its high permeability. Therefore, the role of P-gp inhibiting polymers in enhancing the biopharmaceutical performance of RXB by preparing polymeric amorphous solid dispersion and subsequent improvement in solubility and permeability was investigated. Initially, solubility parameter and Flory-Huggins interaction parameter were determined for miscibility studies between drug and polymers. Binary dispersions were prepared by dissolving drug with polymers eudragit S100, eudragit L100, and soluplus in common solvent (5% v/v water in tetrahydrofuran) using spray dryer. Prepared binary dispersions were analyzed by differential scanning calorimetry (DSC), microscopy, powder X-ray diffractometry (PXRD), Fourier transform infrared spectroscopy (FTIR), dynamic vapor sorption (DVS), and solution nuclear magnetic resonance (NMR) spectroscopy. Superior performance of binary dispersions was observed upon dissolution and solubility studies over micronized active pharmaceutical ingredient. Amorphous solid dispersion (ASD) prepared with soluplus showed 10-fold increase in apparent solubility and maintenance of supersaturation for 24 h compared to the crystalline RXB. Further, pharmacokinetic study performed in animals was in good correlation with the solubility data. Increases of 5.7- and 6.7-fold were observed in AUC and C, respectively, for ASDs prepared with soluplus compared to those with crystalline RXB. FTIR and NMR spectroscopy unveiled the involvement of N-H group of RXB with C═O group of polymers in intermolecular interactions. The decreased drug efflux ratio was observed for ASDs prepared with eudragit S100 and soluplus in Caco-2 transport study suggesting improvement in the absorption of RXB. Hence, the present study demonstrates ASD using soluplus as a promising formulation strategy for enhancing the biopharmaceutical performance of RXB by increasing the solubility and circumventing the P-gp activity.

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Section: ■ Results and Discussionmentioning

confidence: 72%

Section: Results and Discussionmentioning

confidence: 99%

Enhanced Biopharmaceutical Performance of Rivaroxaban through Polymeric Amorphous Solid Dispersion

et al. 2018

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“…Recent studies on DNP SS‐NMR of amorphous indomethacin and of diflunisal–PVP ASD verify the utility of this technique. On the basis of the estimated extent of room temperature signal enhancement in 13 C CPMAS DNP SS‐NMR spectra, the acquisition time can be reduced by more than 2000‐fold when compared to the conventional measurement.…”

Section: Current Hurdles and Future Directionsmentioning

confidence: 88%

Structural and Dynamic Properties of Amorphous Solid Dispersions: The Role of Solid-State Nuclear Magnetic Resonance Spectroscopy and Relaxometry

Paudel

Geppi

Mooter

2014

Journal of Pharmaceutical Sciences

116

103

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“…Measuring the small phase angle during polarization is however challenging. Spectroscopic methods such as Raman, IR, and NMR may be used for the characterization and evaluating drugcarrier compatibilities of SEDDS (30)(31)(32). Phase separation evaluation is used to decipher the stability of prepared SEDDS.…”

Section: Size Surface Morphology and Phase Separationmentioning

confidence: 99%

Self-Emulsifying Oral Lipid Drug Delivery Systems: Advances and Challenges

et al. 2019

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The attempts to oral delivery of lipids can be challenging. Self-emulsifying drug delivery system (SEDDS) plays a vital role to tackle this problem. SEDDS is composed of an oil phase, surfactants, co-surfactants, emulsifying agents, and co-solvents. SEDDS can be categorized into self-nano-emulsifying agents (SNEDDS) and self-micro-emulsifying agents (SMEDDS). The characterization of SEDDS includes size, zeta potential analysis, and surface morphology via electron microscopy and phase separation methods. SEDDS can be well characterized through different techniques for size and morphology. Supersaturation is the phenomenon applied in case of SEDDS, in which polymers and copolymers are used for SEDDS preparation. A supersaturated SEDDS formulation kinetically and thermodynamically inhibits the precipitation of drug molecules by retarding nucleation and crystal growth in the aqueous medium. Self-emulsification approach has been successful in the delivery of anti-cancer agents, anti-viral drugs, anti-bacterial, immunosuppressant, and natural products such as antioxidants as well as alkaloids. At present, more than four SEDDS drug products are available in the market. SEDDS have tremendous capabilities which are yet to be explored which would be beneficial in oral lipid delivery.

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Solid‐State Characterization of Amorphous Dispersions

Cited by 7 publications

References 155 publications

Enhanced Biopharmaceutical Performance of Rivaroxaban through Polymeric Amorphous Solid Dispersion

Enhanced Biopharmaceutical Performance of Rivaroxaban through Polymeric Amorphous Solid Dispersion

Structural and Dynamic Properties of Amorphous Solid Dispersions: The Role of Solid-State Nuclear Magnetic Resonance Spectroscopy and Relaxometry

Self-Emulsifying Oral Lipid Drug Delivery Systems: Advances and Challenges

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