Development of clinical dosage forms for a poorly water soluble drug I: Application of polyethylene glycol–polysorbate 80 solid dispersion carrier system

Dannenfelser, Rose‐Marie; He, Handan; Joshi, Yatindra M.; Bateman, Simon; Serajuddin, Abu T.M.

doi:10.1002/jps.20044

Cited by 114 publications

(61 citation statements)

References 23 publications

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“…Therefore, surfactants can be added to the PEG matrix to solubilize the dispersed drug. [25][26][27][28] Goldberg et al reported on the potential drawbacks of the melting methods, such as thermal degradation, sublimation and polymorphic modifications. [29] Also, miscibility gaps in the liquid state influence the degree of dispersion in the solid state.…”

Section: Preparation and Classification Of Solid Dispersionsmentioning

confidence: 99%

Review: physical chemistry of solid dispersions

2009

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Objectives With poorly soluble drug candidates emerging in the drug discovery pipeline, the importance of the solid dispersion formulation approach is increasing. This strategy includes complete removal of drug crystallinity, and molecular dispersion of the poorly soluble compound in a hydrophilic polymeric carrier. The potential of this technique to increase oral absorption and hence bioavailability is enormous. Nevertheless, some issues have to be considered regarding thermodynamic instability, as well in supersaturated solutions that are formed upon dissolution as in the solid state. Key findings After a brief discussion on the historical background of solid dispersions and their current role in formulation, an overview will be given on the physical chemistry and stability of glass solutions as they form supersaturated solutions, and during their shelf life. Conclusions Thorough understanding of these aspects will elicit conscious evaluation of carrier properties and eventually facilitate rational excipient selection. Thus, full exploitation of the solid dispersion strategy may provide an appropriate answer to drug attrition due to low aqueous solubility in later stages of development.

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Section: Preparation and Classification Of Solid Dispersionsmentioning

confidence: 99%

Review: physical chemistry of solid dispersions

2009

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“…Dannenfelser et al 17 found that a combined carrier consisting of PEG and Polysorbate 80 could improve the dissolution and enhance the bioavailability of LAB687, a poorly water-soluble drug with an aqueous solubility of 0.17 μg/mL at room temperature.…”

Section: Introductionmentioning

confidence: 99%

Improved dissolution of oleanolic acid with ternary solid dispersions

Liu

Wang

2007

AAPS PharmSciTech

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The purpose of this study was to enhance the dissolution of oleanolic acid by solid dispersions consisting of the drug, a polymeric carrier, and a surfactant. Binary solid dispersions consisting of oleanolic acid and polyvinylpyrrolidone were prepared for comparison. Polysorbate 80, a nonionic surfactant, was incorporated into binary solid dispersions as the third component to prepare ternary solid dispersions. Solid dispersions were characterized by differential scanning calorimetry, Fourier transform infrared spectroscopy, and dissolution tests. The crystallinization of OA was prohibited in solid dispersions. Both the binary and ternary solid dispersions enhanced the dissolution of OA. Moreover, the dissolution of ternary solid dispersion was faster compared with that of binary solid dispersion. Polysorbate 80 played an important positive role in dissolution of the solid dispersion.

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“…The resulting product is then collected after cooling at room temperature and milled 46,47 . A reduction in processing temperature can be achieved by the association of hot-stage extrusion with the use of carbon dioxide as a plasticizer 48,49 which broadens the application of hot-stage extrusion to thermally labile compounds 48 .…”

Section: Fig 4: Manufacturing Processes Used To Produce Solid Dispermentioning

confidence: 99%

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2010

IJPSR

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The solubility behavior of drugs remains one of the most challenging aspects in the formulation development. Although there was a great interest in solid dispersion systems during the past four decades to increase solubility by improving dissolution rate and bioavailability of poorly soluble drugs; there commercial use has been very limited, primarily because of manufacturing difficulties and various stability problems. It can be carried out by reducing drug particle size to the absolute minimum, and hence improving drug wet-ability, bioavailability may be significantly improved. Solid dispersion of drugs was generally produced by melt or solvent evaporation methods. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the eminent approach to improve the solubility or the dissolution rate and recent revival has been discussed.

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Development of clinical dosage forms for a poorly water soluble drug I: Application of polyethylene glycol–polysorbate 80 solid dispersion carrier system

Cited by 114 publications

References 23 publications

Review: physical chemistry of solid dispersions

Review: physical chemistry of solid dispersions

Improved dissolution of oleanolic acid with ternary solid dispersions

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