Formulation studies of a poorly water-soluble drug in solid dispersions to improve bioavailability

Sheen, Pai‐Chang; Khetarpal, Vinod; Cariola, Christina M.; Rowlings, Colin E.

doi:10.1016/0378-5173(94)00366-d

Cited by 72 publications

(31 citation statements)

References 6 publications

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“…But during storage nucleation and recrystallization of a crystalline drug takes place in solid dispersions [82] . Furthermore, there are many other pitfalls which also requires a profound studies and it include the inability to scale up the solid dosage formulation from a small scale melt quench or a solvent-evaporation technique, insufficient knowledge of the mechanism of dissolution of drug from the dosage form, prevention of crystallization of some drug which takes place in the gastric fluids and the poor understanding of the in vitro-in vivo correlation between these dosage forms [83,84] .…”

Section: Amorphous Contentmentioning

confidence: 99%

Enhancement of the Solubility of Poorly Water Soluble Drugs through Solid Dispersion: A Comprehensive Review

Singh¹,

Kaur²,

Gupta³

et al. 2017

pharmaceutical-sciences

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Absorption of a drug through the oral route involves its dissolution from the formulation into gastric and/ or intestinal fluids followed by its permeation through gastrointestinal cell membranes and finally into the systemic circulation. Oral solid dosage forms are one of the most commonly used formulation types having multiple benefits over other formulations/routes. However, the challenge for a pharmaceutical scientist lies in the fact that dissolution of a drug from an oral solid formulation (a key factor in drug absorption) is dependent on the aqueous solubility of the drug. Therefore, a drug with poor aqueous solubility would exhibit dissolution rate limited absorption and similarly a drug possessing poor membrane permeability undergo permeation rate limited absorption. A drug is highly soluble when highest dose of drug is soluble in ≤250 ml of water over a pH range of 1 to 7.5 and a drug is highly permeable when extent of absorption in humans is to be ≥90% of an administered dose [1] . It has been investigated that most of new chemical entities currently being discovered and intended to be used as a solid dosage form should produce an efficient and reproducible plasma concentration after oral administration. However, most of them tend to have poor water solubility, which limits the therapeutic efficacy of that drug. Moreover, poor solubility results in increased dose and frequent administration leading to higher incidences of side-effects [2][3][4][5][6] . Hence, pharmaceutical research has emphasised on elevating the oral bioavailability of poorly water-soluble drugs by improving their solubility, dissolution rate and membrane permeability. Solubility is an important determinant in drug liberation and hence drug absorption, which plays a key role in oral bioavailability of formulations. The dissolution rate of a drug directly depends upon its solubility. Most of the new drugs have poor water solubility; thereby pose a difficulty in formulating into drug delivery systems. Therefore, solubility enhancement of poorly water soluble drugs is one of the necessary preformulation steps in the pharmaceutical product development research. Solid dispersion is a unique and promising approach for enhancing the dissolution characteristics and oral bioavailability of poorly water-soluble drugs. The present review highlights portrayal of solid dispersions, its types including eutectic mixtures and solid solutions, method of preparation and also the useful carriers for the preparation of solid dispersions. Furthermore, the wide research conducted hitherto on solid dispersions for enhancing solubility of different efficacious drugs, challenges encountered in the development of solid dispersions and recent advancements to overcome its pitfalls have also been elaborated.

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Section: Amorphous Contentmentioning

confidence: 99%

Enhancement of the Solubility of Poorly Water Soluble Drugs through Solid Dispersion: A Comprehensive Review

Singh¹,

Kaur²,

Gupta³

et al. 2017

pharmaceutical-sciences

View full text Add to dashboard Cite

show abstract

“…Therefore, the favorable effect obtained can be attributed mainly to the improved drug wettability and decrease of aggregation phenomena as a consequence of a reduced interfacial tension between drug particles and dissolution media (Sheen et al 1995). In addition, the concomitant particle size reduction and consequent increase of the effective surface area exposed to the dissolution medium, as well as the intimate and fine dispersion of the drug into the hydrophilic polymer, obtained by virtue of the melting preparation method, can contribute further to the better performance of such systems.…”

Section: Resultsmentioning

confidence: 99%

Fast-Dissolving Tablets of Glyburide Based on Ternary Solid Dispersions with PEG 6000 and Surfactants

Cirri¹,

Maestrelli²,

Corti³

et al. 2007

Drug Delivery

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“…The ideal type of solid dispersion for increasing dissolution is a glassy solution, in which the drug in the amorphous form has a lower thermodynamic barrier to dissolution and a maximally reduced particle size (Goldberg et al, 1965). In addition, the incorporation of a hydrophilic excipient and/or surface-active agent can increase wetting and lead to supersaturation in the diffusion layer (Serajuddin et al, 1988;Morris et al, 1992;Sheen et al, 1995). Solid solutions and dispersions are most commonly formed either from a drug/excipient mixture via solvent casting, melt extrusion, or spray-drying techniques (Corrigan et al, 1985;Forster et al, 2001).…”

Section: Solid Dispersionmentioning

confidence: 99%

Solubility of Pharmaceutical Solids

Wiser

Gao

Jasti

et al. 2011

Oral Bioavailability

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Formulation studies of a poorly water-soluble drug in solid dispersions to improve bioavailability

Cited by 72 publications

References 6 publications

Enhancement of the Solubility of Poorly Water Soluble Drugs through Solid Dispersion: A Comprehensive Review

Enhancement of the Solubility of Poorly Water Soluble Drugs through Solid Dispersion: A Comprehensive Review

Fast-Dissolving Tablets of Glyburide Based on Ternary Solid Dispersions with PEG 6000 and Surfactants

Solubility of Pharmaceutical Solids

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