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Haste Makes Waste: The Interplay Between Dissolution and Precipitation of Supersaturating Formulations.

ABSTRACT: Contrary to the early philosophy of supersaturating formulation design for oral solid dosage forms, current evidence shows that an exceedingly high rate of supersaturation generation could result in a suboptimal in vitro dissolution profile and subsequently could reduce the in vivo oral bioavailability of amorphous solid dispersions. In this commentary, we outline recent research efforts on the specific effects of the rate and extent of supersaturation generation on the overall kinetic solubility profiles of supersaturating formulations. Additional insights into an appropriate definition of sink versus nonsink dissolution conditions and the solubility advantage of amorphous pharmaceuticals are also highlighted. The interplay between dissolution and precipitation kinetics should be carefully considered in designing a suitable supersaturating formulation to best improve the dissolution behavior and oral bioavailability of poorly water-soluble drugs.

SUBMITTER: Sun DD

PROVIDER: S-EPMC4627464 | biostudies-literature | 2015 Nov

REPOSITORIES: biostudies-literature

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Haste Makes Waste: The Interplay Between Dissolution and Precipitation of Supersaturating Formulations.

Sun Dajun D DD Lee Ping I PI

The AAPS journal 20150903 6

Contrary to the early philosophy of supersaturating formulation design for oral solid dosage forms, current evidence shows that an exceedingly high rate of supersaturation generation could result in a suboptimal in vitro dissolution profile and subsequently could reduce the in vivo oral bioavailability of amorphous solid dispersions. In this commentary, we outline recent research efforts on the specific effects of the rate and extent of supersaturation generation on the overall kinetic solubilit ...[more]

PMID: 26338234

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Project description:Scale mineral deposition is a critical problem that hinders the daily production of oil and gas fields. Chemical removal of these scales, based on the scale type, is common. In this paper, borax and diethylene tremaine penta acetic (DTPA) acid-based formulations are used for the removal of sulfides, carbonates, and sulfate scales. In particular, the dissolution rates of sulfide (pyrite, pyrrhotite, and galena), sulfate (celestite and barite), and carbonate (calcite) scales were investigated in a rotating disc apparatus at typical well conditions. Scanning electron microscopy-energy-dispersive X-ray and X-ray diffraction analyses were performed for characterizing scale composition and type. The effect of temperature, scale type, and formulation on the dissolution rate is studied. Even though borax formulation has been developed for the sulfide scale removal, it showed a high dissolution rate for the carbonate scale (7.23 × 10-7 mol·L-1·s-1·cm-2). For the sulfide scale, the highest dissolution in borax formulation was obtained with galena (lead sulfide, PbS), followed by pyrrhotite, and the lowest dissolution was reported for pyrite (1.55 × 10-8 mol·L-1·s-1·cm-2). Borax formulation was found to be inefficient in the removal of sulfate scales with a dissolution rate lower than carbonate and sulfide scales by 3 and 2 orders of magnitude, respectively. Similarly, DTPA-based formulation has yielded the highest dissolution for the carbonate scale (7.98 × 10-6 mol·L-1·s-1·cm-2). However, for sulfate, DTPA-based formulation showed better performance than borax. The increase in temperature leads to an increase in the dissolution rate for almost all types of scales; however, DTPA-based formulation showed improved performance with temperature. Both formulations are efficient in removing sulfate- and sulfide-rich scales. The experimental results of DTPA have been validated by density functional theory calculations of binding energies between DTPA and metal ions present in the mixed scale.

Dataset Information

Haste Makes Waste: The Interplay Between Dissolution and Precipitation of Supersaturating Formulations.

Publications

Haste Makes Waste: The Interplay Between Dissolution and Precipitation of Supersaturating Formulations.

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