Evaluation of amorphous solid dispersion properties using thermal analysis techniques

Baird, Jared A.; Taylor, Lynne S.

doi:10.1016/j.addr.2011.07.009

Cited by 415 publications

(332 citation statements)

References 235 publications

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“…The miscibility between the materials used in the blends can significantly affect the processability and the qualities, such as the hardness and friability, of the finished products [24]. Therefore, predictions of the material's miscibility and likelihood of phase separation for the three sets of blend formulation were performed.…”

Section: Prediction Of Excipient-excipient and Drug-excipient Miscibimentioning

confidence: 99%

An investigation into the use of polymer blends to improve the printability of and regulate drug release from pharmaceutical solid dispersions prepared via fused deposition modeling (FDM) 3D printing

Alhijjaj

Belton

2016

European Journal of Pharmaceutics and Biopharmaceutics

232

134

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FDM 3D printing has been recently attracted increasing research efforts towards the production of personalized solid oral formulations. However, commercially available FDM printers are extremely limited with regards to the materials that can be processed to few types of thermoplastic polymers, which often may not be pharmaceutically approved materials nor ideal for optimizing dosage form performance of poor soluble compounds. This study explored the use of polymer blends as a formulation strategy to overcome this processability issue and to provide adjustable drug release rates from the printed dispersions. Solid dispersions of felodipine, the model drug, were successfully fabricated using FDM 3D printing with polymer blends of PEG, PEO and Tween 80 with either Eudragit E PO or Soluplus. As PVA is one of most widely used polymers in FDM 3D printing, a PVA based solid dispersion was used as a benchmark to compare the polymer blend systems to in terms processability. The polymer blends exhibited excellent printability and were suitable for processing using a commercially available FDM 3D printer. With 10% drug loading, all characterization data indicated that the model drug was molecularly dispersed in the matrices.During in vitro dissolution testing, it was clear that the disintegration behavior of the formulations significantly influenced the rates of drug release. Eudragit EPO based blend dispersions showed bulk disintegration; whereas the Soluplus based blends showed the 'peeling' style disintegration of strip-by-strip. The results indicated that interplay of the miscibility between excipients in the blends, the solubility of the materials in the dissolution media and the degree of fusion between the printed strips during FDM process can be used to manipulate the drug release rate of the dispersions. This brings new insight into the design principles of controlled release formulations using FDM 3D printing.

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Section: Prediction Of Excipient-excipient and Drug-excipient Miscibimentioning

confidence: 99%

An investigation into the use of polymer blends to improve the printability of and regulate drug release from pharmaceutical solid dispersions prepared via fused deposition modeling (FDM) 3D printing

Alhijjaj

Belton

2016

European Journal of Pharmaceutics and Biopharmaceutics

232

134

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“…Owing to the complex composition of the coated glass solutions, typical solid state analytical techniques such as modulated differential scanning calorimetry (mDSC) 7 or X-ray powder diffraction (XRPD) are inadequate for this specific multi-layer samples because they only provide bulk analysis (no spatial resolution). Thermal analysis by (m)DSC can detect two separate amorphous phases, provided they are larger than the critical length scale of the technique (~30nm) 8 .…”

Section: Introductionmentioning

confidence: 99%

Controlling the Release of Indomethacin from Glass Solutions Layered with a Rate Controlling Membrane Using Fluid-Bed Processing. Part 1: Surface and Cross-Sectional Chemical Analysis

et al. 2017

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den Mooter, Guy (2017) Controlling the release of indomethacin from glass solutions layered with a rate controlling membrane using fluid-bed processing. A note on versions:The version presented here may differ from the published version or from the version of record. If you wish to cite this item you are advised to consult the publisher's version. Please see the repository url above for details on accessing the published version and note that access may require a subscription. AbstractFluid bed coating has been shown to be an adequate manufacturing technique to formulate poorly soluble drugs in glass solutions. Layering inert carriers with a drug-polymer mixture enables these beads to be immediately filled into capsules, thus avoiding additional, potentially destabilizing, downstream processing. In this study fluid bed coating is proposed for the production of controlled release dosage forms of glass solutions by applying a second, rate controlling membrane on top of the glass solution. Adding a second coating layer adds to the physical and chemical complexity of the drug delivery system so a thorough understanding of the physical structure and phase behavior of the different coating layers is needed. This study aimed to investigate the surface and cross-sectional characteristics (employing SEM and ToF-SIMS) of an indomethacin-polyvinylpyrrolidone (PVP) glass solution, top-coated with a release rate controlling membrane consisting of either ethyl cellulose or Eudragit RL. The implications on the addition of a pore former (PVP) and the coating medium (ethanol or water) were also considered. In addition, polymer miscibility and the phase analysis of the underlying glass solution were investigated.Significant differences in surface and cross sectional topography of the different rate controlling membranes or the way they are applied (solution vs. dispersion) were observed. These observations can be linked to the polymer miscibility differences. The presence of PVP was observed in all rate controlling membranes, even if it is not part of the coating solution. This could be attributed to residual powder presence in the coating chamber. The distribution of PVP among the sample surfaces depends on the concentration and the rate controlling polymer used.Differences can again be linked to polymer miscibility. Finally, it was shown that the underlying glass solution layer remains amorphous after coating of the rate controlling membrane, whether formed from an ethanol solution or an aqueous dispersion.4

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“…The dissolution medium was at pH 1.2 (900 mL) equilibrated to 37 °C ± 0.5 °C with the baskets rotated at 50 rpm. Samples were withdrawn at selected time intervals (5,10,15,20,25,30,40,50,60,75, 90, 105 and 120 min) using a peristaltic pump. The concentrations of PXM in the samples were determined by UV spectrophotometer at 333 nm.…”

Section: Dissolution Studiesmentioning

confidence: 99%

“…BCS class II drugs are characterized by high membrane permeability but low aqueous solubility therefore; there is a low drug concentration gradient between the gut and the blood vessels limiting drug transport and oral bioavailability. The poor solubility of drugs has always been a major problem in pharmaceutical development and this problem is now more prevalent with more than 40 % of the new chemical entities being practically insoluble in water or lipophilic in nature [3][4][5][6][7]. As dissolution rates are typically the rate-limiting step for bioavailability, especially for poorly soluble drugs, enhancement of solubility is vital to attaining suitable systemic concentrations for therapeutic effect [8].…”

Section: Introductionmentioning

confidence: 99%

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Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

Adebisi

Kaialy

Hussain

et al. 2016

Colloids and Surfaces B: Biointerfaces

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Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions, Colloids and Surfaces B: Biointerfaces http://dx.doi.org/10. 1016/j.colsurfb.2016.07.032 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. 4. GLU improved the handling of PXM as it significantly reduced its charge in all the spray dried formulations. Technique could be used to determine appropriate formulations that improve handling AbstractThis work explores the use of both spray drying and D-glucosamine HCl (GLU) as a hydrophilic carrier to improve the dissolution rate of piroxicam (PXM) whilst investigating the electrostatic charges associated with the spray drying process. Spray dried PXM:GLU solid dispersions were prepared and characterised (XRPD, DSC, SEM). Dissolution and triboelectric charging was also conducted. The results showed that the spray dried PXM alone, without GLU produced some PXM form II (DSC results) with no enhancement in solubility relative to that of the parent PXM.XRPD results also showed the spray drying process to decrease the crystallinity of GLU and solid dispersions produced. The presence of GLU improved the dissolution rate of PXM. Spray dried PXM: GLU at a ratio of 2:1 had the most improved dissolution. The spray drying process generally yielded PXM-GLU spherical particles of around 2.5 µm which may have contributed to the improved dissolution. PXM showed a higher tendency for charging in comparison to the carrier GLU (-3.8 versus 0.5 nC/g for untreated material and -7.5 versus 3.1 nC/g for spray dried materials). Spray dried PXM and spray dried GLU demonstrated higher charge densities than untreated PXM and untreated GLU, respectively. Regardless of PXM:GLU ratio, all spray dried PXM:GLU solid dispersions showed a negligible charge density (net-CMR: 0.1 -0.3 3 nC/g). Spray drying of PXM:GLU solid dispersions can be used to produce formulation powders with practically no charge and thereby improving handling as well as dissolution behaviour of PXM.

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Evaluation of amorphous solid dispersion properties using thermal analysis techniques

Cited by 415 publications

References 235 publications

An investigation into the use of polymer blends to improve the printability of and regulate drug release from pharmaceutical solid dispersions prepared via fused deposition modeling (FDM) 3D printing

An investigation into the use of polymer blends to improve the printability of and regulate drug release from pharmaceutical solid dispersions prepared via fused deposition modeling (FDM) 3D printing

Controlling the Release of Indomethacin from Glass Solutions Layered with a Rate Controlling Membrane Using Fluid-Bed Processing. Part 1: Surface and Cross-Sectional Chemical Analysis

Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

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