Amorphous solid dispersions of piroxicam and Soluplus®: Qualitative and quantitative analysis of piroxicam recrystallization during storage

Lust, Andres; Strachan, Clare J.; Veski, Peep; Aaltonen, Jaakko; Heinämäki, Jyrki; Yliruusi, Jouko; Kogermann, Karin

doi:10.1016/j.ijpharm.2015.03.079

Cited by 58 publications

(20 citation statements)

References 40 publications

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“…All formulations exhibited increased dissolution compared with the bulk drug. The Soluplus-based formulation exhibited a higher dissolution than the PEO one, but the amount dissolved was only 32.7% at 1 h. This drug carrier did not markedly increase the dissolution as reported in the literature [13], and this might be because of the limited interaction between Soluplus and nisoldipine. However, the Kollidon VA64-based formulation exhibited complete drug dissolution within 30 min and, so, Kollidon VA64 was chosen as the stabilizer in this study.…”

Section: Formulation Of Nisoldipine Asdsupporting

confidence: 53%

A physically stabilized amorphous solid dispersion of nisoldipine obtained by hot melt extrusion

Fang

Hou

et al. 2016

Powder Technology

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Section: Formulation Of Nisoldipine Asdsupporting

confidence: 53%

A physically stabilized amorphous solid dispersion of nisoldipine obtained by hot melt extrusion

Fang

Hou

et al. 2016

Powder Technology

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“…More sensitive methods to detect the beginning of drug recrystallisation and to monitor the growth of drug crystals in their ASDs are thus highly desired [265]. A series of new protocols has been investigated to this end [266][267][268][269][270]. The Nagy group recently investigated the applications of some of these methods to monitor drug recrystallisation in electrospun ASDs and to determine their long-term stability.…”

Section: Stabilitymentioning

confidence: 99%

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Williams

et al. 2018

Journal of Controlled Release

232

156

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The development of oral dosage forms for poorly water-soluble active pharmaceutical ingredients (APIs) is a persistent challenge. A range of methods has been explored to address this issue, and amorphous solid dispersions (ASDs) have received increasing attention. ASDs are typically prepared by starting with a liquid precursor (a solution or melt) and applying energy for solidification. Many techniques can be used, with the emergence of electrospinning as a potent option in recent years. This method uses electrical energy to induce changes from liquid to solid. Through the direct applications of electrical energy, electrospinning can generate nanofiber-based ASDs from drug-loaded solutions, melts and melt-solutions. The technique can also be combined with other approaches using the application of mechanical, thermal or other energy sources. Electrospinning has numerous advantages over other approaches to produce ASDs. These advantages include extremely rapid drying speeds, ease of implentation, compatibility with a wide range of active ingredients (including those which are thermally labile), and the generation of products with large surface areas and high porosity. Furthermore, this technique exhibits the potential to create so-called 'fifth-generation' ASDs with nanostructured architectures, such as core/shell or Janus systems and their combinations. These advanced systems can improve dissolution behaviour and provide programmable drug release profiles. Additionally, the fiber components and their spatial distributions can be precisely controlled. Electrospun fiber-based ASDs can maintain an incorporated active ingredient in the amorphous physical form for prolonged periods of time because of their homogeneous drug distribution within the polymer matrix (typically they comprise solid solutions), and ability to inhibit molecular motion. These ASDs can be utilised to generate oral dosage forms for poorly water-soluble drugs, resulting in linear or multiple-phase release of one or more APIs. Electrospun ASDs can also be exploited as templates for manipulating molecular self-assembly, offering a bridge between ASDs and other types of dosage forms. This review addresses the development, advantages and pharmaceutical applications of electrospinning for producing polymeric ASDs. Material preparation and analysis procedures are considered. The mechanisms through which performance has been improved are also discussed.

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“…The temperatures ranged from 2°C to 60°C and the relative humidity varied between 0% and 100%. The duration also varied significantly, with stability studies lasting from 24 h to two years (73,74,81,82,84,86,88,92,93,104,105,109,110,113,115,116,118,120,123,124,126,127,129,130,132,134,135,139,143,146,149,153,158,166,169,172,175,176). While most of the studies did not mention the container used for the physical stability test, a few specified, for example, whether a closed or open container was used (88,92,113,123,132,146).…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

“…deionized, degassed, distilled, purified), HCl, and phosphate/acetate buffers at pHs ranging from 1.2 to 7.4 (71–74,77–79,81–88,90–92,95,100–107,109–111,113–119,121,126,127,129–133,135–139,149,150,153,154,156,160,161,166,168–177). Among the 88 studies that reported a dissolution assay, only sixteen (~18%) used a biorelevant dissolution medium (BDM) such as simulated gastrointestinal fluids and simulated saliva (77,79,82,97,121,123,130,135,136,145,152,154,160,169,170,176). These disparities in medium used affect the conclusions, which (as with the stability studies) make head-to-head comparison difficult.…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.

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Amorphous solid dispersions of piroxicam and Soluplus®: Qualitative and quantitative analysis of piroxicam recrystallization during storage

Cited by 58 publications

References 40 publications

A physically stabilized amorphous solid dispersion of nisoldipine obtained by hot melt extrusion

A physically stabilized amorphous solid dispersion of nisoldipine obtained by hot melt extrusion

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

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