The use of inorganic salts to improve the dissolution characteristics of tablets containing Soluplus®-based solid dispersions

Hughey, Justin R.; Keen, Justin M.; Miller, Dave A.; Kolter, Karl; Langley, Nigel; McGinity, James W.

doi:10.1016/j.ejps.2013.01.004

Cited by 84 publications

(63 citation statements)

References 33 publications

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“…It was chosen for comparison in the release of nifedipine from co-precipitate for its ability to form a gel at about 37°C, similarly to soluplus [38] . Due to this property this sucrester does not drive the notable improvement of nifedipine release, differently to what reported [39][40][41] . No micro-precipitate was observed, since the different molecular structures for soluplus and sucrester prevent interactions with nifedipine, responsible of decreasing hydrophilicity of the system and of the precipitate formation: the gelling properties of the carrier alone account for the reduction of the release extent, but not for the formation of micro-particulate.…”

Section: Discussioncontrasting

confidence: 79%

Release Problems for Nifedipine in the Presence of Soluplus

Fini¹,

Cavallari²,

Ternullo³

et al. 2016

JPP

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Nifedipine/soluplus co-precipitates were prepared at 1:9 and 1:1 weight ratios, using the solvent method, with the aim to obtain an improvement of the drug release. The release, though accelerated with respect to physical mixtures and pure drug, resulted slow with respect to similar systems containing soluplus and are characterized by the appearance in suspension of micro-particulates that, at the optical microscope, revealed a large variety of shapes typical of flower-like aggregates, not previously reported. For comparison systems were also prepared with PVP K30 and sucrester P1670 and two mixtures, without any evidence of this last phenomenon. The systems were studied by thermal (differential scanning calorimetry -DSC, thermomicroscopy -HSM) and spectroscopic (SEM, FT-IR, micro-Raman) analysis. Slow release of nifedipine and formation of colloidal micro-particulates were hypothesized due to the gelling tendency of soluplus associated to drug/polymer multi-site-interactions: when one of these parameters is absent in the system the two phenomena could not be observed together, such as in the case of PVP K30 or sucrester P1670, when used as carriers for nifedipine release.

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Section: Discussioncontrasting

confidence: 79%

Release Problems for Nifedipine in the Presence of Soluplus

Fini¹,

Cavallari²,

Ternullo³

et al. 2016

JPP

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“…The maximum release of 28% was achieved after 6 hours in vitro dissolution. Although Soluplus has been reported to be a water-soluble polymer, the addition of the inorganic salts in the dissolution medium can depress the cloud point of the polymer and reduce the solubility of the polymer in the media [35]. Figure 10 captures the start of the disintegration process of CMS discs between 60 to 90 minutes into the dissolution test.…”

Section: In Vitro Disintegration and Drug Release Study Of Fdm Printementioning

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

230

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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“…After 45 min, a substantial amount of these tablets remained and when broken, were observed to have a dry core. The different behaviors observed between polymer types may be attributed to the differences in hygroscopicity and polymer solubility in the dissolution media (Hughey et al 2013). Hydrophilic polymers, such as PVP, HPMC, and PVP-PVA, often produce a slowly eroding tablet that quickly forms a thick gel layer near the outer edge of the tablet upon dispersing in aqueous based media (DiNunzio et al 2012).…”

Section: Impact Of Spray Dried Particle Physical Properties On Oral Smentioning

confidence: 98%

“…The particle size, shape, density and surface charge can have a substantial impact on powder flow, both as neat spray dried powder as well as diluted within a formulation (Prescott and Barnum 2000). In addition, the polymer molecular structure and hygroscopicity play a major role in the tablet disintegration properties (Hughey et al 2013). …”

Section: Impact Of Spray Dried Particle Physical Properties On Oral Smentioning

confidence: 99%

Practical Considerations for Spray Dried Formulation and Process Development

Lowinger

Baumann

Vodak

et al. 2014

Discovering and Developing Molecules With Optimal Drug-Like Properties

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Spray drying is a broadly applicable process for the manufacture of many products in the food, chemical, and pharmaceutical areas. Powders are produced in a continuous process during the drying of liquid feed stocks through an atomization and drying process. The ability to control the final product attributes to maintain the desired physical state, performance, and bulk powder attributes for downstream processing has made spray drying an important unit operation for the manufacture of amorphous solid dispersions. It can enable progression of compounds with poor aqueous solubility throughout the drug development lifecycle from discovery through commercial production.Efficient development of the process for spray dried amorphous solid dispersions has been demonstrated to ensure the critical quality attributes are maintained during development and scale-up, for example with Vertex Pharmaceuticals' Incivek. To successfully achieve these goals, it is necessary to have a deep understanding of the process and the key formulation attributes along with their potential interaction. By developing this understanding, it is possible to achieve a robust process and formulation that have both been designed to maximize the success during drug development and to achieve the target performance and stability goals.

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The use of inorganic salts to improve the dissolution characteristics of tablets containing Soluplus®-based solid dispersions

Cited by 84 publications

References 33 publications

Release Problems for Nifedipine in the Presence of Soluplus

Release Problems for Nifedipine in the Presence of Soluplus

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

Practical Considerations for Spray Dried Formulation and Process Development

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