Increasing Dissolution Rates and Gastrointestinal Absorption of Drugs Via Solid Solutions and Eutectic Mixtures I

Goldberg, Arthur H.; Gibaldi, Milo; Kanig, Joseph L.

doi:10.1002/jps.2600540810

Cited by 167 publications

(56 citation statements)

References 8 publications

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“…[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. [30] The advantage of the fusion method is that no organic solvents are involved, which reduces production costs.…”

Section: Preparation and Classification Of Solid Dispersionsmentioning

confidence: 99%

“…This was referred to as discontinuous solid solutions. Indeed, the phase diagram of the eutectic sulfathiazole-urea system introduced by Sekiguchi and Obi [14] was later interpreted by Goldberg et al [29] as a system with limited solid solubility, with the maximum solid solubility of sulfathiazole in urea being ca. 10% w/w and the maximum solid solubility of urea into sulfathiazole ca.…”

Section: Solid Solutionsmentioning

confidence: 99%

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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%

Section: Solid Solutionsmentioning

confidence: 99%

Review: physical chemistry of solid dispersions

2009

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“…By definition, solid dispersions and solid solutions can be differentiated based on the molecular state of the drug in the carrier matrix. If the drug is converted to amorphous form and forms one phase system with polymer, it can be classified as a solid solution, whereas if the drug exists as microcrystalline dispersion, i.e., forms two-phase system, it is generally referred to as a solid dispersion (Goldberg, Gibaldi, and Kanig 1965;Sekiguchi and Obi 1961).…”

mentioning

confidence: 99%

Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

et al. 2007

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“…The solubility issues complicate the delivery of these new drugs and many existing drugs (1). Poorly water-soluble drugs show unpredictable absorption and high intrasubject and intersubject variability (2)(3)(4). Therefore, constant surveillance of marketed, poorly water-soluble drugs by the government, manufacturers, and independent research groups is essential to ensure availability of quality medicines.…”

mentioning

confidence: 99%

Evaluation of In Vitro Equivalence for Tablets Containing the Poorly WaterSoluble Compound Atorvastatin

Popy¹,

Dewan²,

Parvin³

et al. 2012

Dissolution Technol.

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This paper describes the evaluation of the in vitro equivalence of tablets containing a poorly water-soluble compound, atorvastatin, marketed in Bangladesh under biowaiver conditions. Drug release was compared with that of a reference product. The in vitro equivalence test was carried out in three different media (pH 1.2, pH 4.5, and pH 6.8). Test results were subjected to statistical analysis to compare the dissolution profiles. Model-independent approaches of difference factor (f 1 ), similarity factor (f 2 ), and dissolution efficiency (%DE) were employed. Dissolution profiles of test and reference (innovator) atorvastatin are equivalent at pH 6.8 without statistical treatment. The test products are equivalent at pH 4.5 (f 1 < 15 and f 2 > 50) and not equivalent at pH 1.2 (f 1 > 15 and f 2 < 50). Other general quality parameters of these tablets (e.g., weight variation, crushing strength, friability, and disintegration time) were also determined according to established protocols, and test results were within limit.

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Increasing Dissolution Rates and Gastrointestinal Absorption of Drugs Via Solid Solutions and Eutectic Mixtures I

Cited by 167 publications

References 8 publications

Review: physical chemistry of solid dispersions

Review: physical chemistry of solid dispersions

Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

Evaluation of In Vitro Equivalence for Tablets Containing the Poorly WaterSoluble Compound Atorvastatin

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