Rethinking the Use of Water as a Dissolution Medium

Noory, Carol; Tran, Nhan L.; Ouderkirk, Larry; Brown, Sara J.; Perry, Jesse; Colon, Miquel; Faberlle, Marisol; Henry, Kermit; Rorberg, Julie; Ali, S.N.; Shah, V. M.

doi:10.14227/dt060499p6

Cited by 12 publications

(6 citation statements)

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“…Also, water lacks buffering capacity and thus, in some instances, the pH of the medium may change as the drug dissolves (as for salts). In addition, because water is not representative of the gastrointestinal environment, it is not considered a physiologically relevant medium (6).…”

Section: Water As a Dissolution Mediummentioning

confidence: 99%

Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Kuppusamy¹

2010

Dissolution Technol.

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The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to both the pharmaceutical industry and the agencies that regulate them. These challenges include developing and validating the test methods, ensuring that methods are appropriately discriminatory, and addressing the potential for an in vivo-in vitro correlation (IVIVC). Dissolution test media selection should be justified for pH (recommended pH range is 1.2-7.5) as well as surfactant type (ionic versus non-ionic) and amount. If the drug is not soluble in the in vivo pH range, with or without surfactants, then the use of nonaqueous media can be preferred with proper justifications. Physical modifications of the drug, such as particle size reduction, use of metastable polymorphs, eutectic mixtures, solid dispersions, or complexation, are being widely used in the industry to enhance the drug dissolution characteristics. In recent years, newer physical modifications (e.g., microemulsions and nanocrystals) are giving promising results in enhancement of drug dissolution and bioavailability of poorly soluble drugs. Whatever method is used by the dissolution scientists, it must aim towards the cheaper but most effective approach to enhance the dissolution behavior of poorly soluble drugs.

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Section: Water As a Dissolution Mediummentioning

confidence: 99%

Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Kuppusamy¹

2010

Dissolution Technol.

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“…It has been suggested that including surface-active agents in dissolution media is important for poorly soluble compounds, because the lack of a surface tension lowering agent would result in poorer wetting and in vitro dissolution rates that are not representative of in vivo rates (28). The FDA has permitted the use of surfactants in media for conducting dissolution studies of poorly soluble compounds (29).…”

Section: Wettability and Dissolution Studiesmentioning

confidence: 99%

Physicochemical Characterization and Dissolution Study of Solid Dispersions of Furosemide with Polyethylene Glycol 6000 and Polyvinylpyrrolidone K30

Patel¹,

Patel²,

Bhimani³

et al. 2008

Dissolution Technol.

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Solid dispersions traditionally have been used as effective methods to improve the dissolution properties and bioavailability of poorly water-soluble drugs. The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug, furosemide, by a solid dispersion technique. Solid dispersions were prepared using polyethylene glycol 6000 (PEG 6000) and polyvinylpyrrolidone K30 (PVP K30) in different drug-to-carrier ratios. Dispersions with PEG 6000 were prepared by fusion-cooling and solvent evaporation, while dispersions containing PVP K30 were prepared by solvent evaporation technique. These new formulations were characterized in the liquid state by phase solubility studies and in the solid state by differential scanning calorimetry, powder X-ray diffraction, and FTIR spectroscopy. The aqueous solubility of furosemide was favored by the presence of both polymers. Solid state characterizations indicated that furosemide was present as an amorphous material and entrapped in polymer matrix. In contrast to the very slow dissolution rate of pure furosemide, the dispersion of the drug in the polymers considerably enhanced the dissolution rate. Solid dispersion prepared with PEG showed the most improvement in wettability and dissolution rate of furosemide. Even physical mixtures of furosemide prepared with both polymers also showed better dissolution profiles as compared with that of pure furosemide. Tablets prepared using solid dispersions showed significant improvement in the release profile of furosemide as compared with conventional tablets prepared using furosemide without PEG or PVP.

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“…The active compound dissolution rate was determined according to the US Pharmacopeia (USP, 2003) and European Pharmacopeia (2001) methods using a flow-through cell (12 mm) and approximately 1 g of pellets from each formulation. The use of surfactants in the media for conducting dissolution studies of poorly soluble compounds under sink conditions have been described elsewhere (Noory et al, 1999;Pharmeuropa, 2001). An aqueous solution of SDS has been suggested as being physiologically representative of human intestinal fluid (Dressman et al, 1998;Dressman and Reppas, 2000).…”

Section: Characterization Of Pelletsmentioning

confidence: 99%

Use of rotary fluidized-bed technology for development of sustained-release plant extracts pellets: Potential application for feed additive delivery1

Meunier

Cardot

Gauthier

et al. 2006

Journal of Animal Science

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The aim of this study was to develop sustained release plant extracts as a potential alternative to antibiotic growth promoters for growing pigs. Pellets with a core based on microcrystalline cellulose and 3 active compounds (eugenol, carvacrol, and thymol) were prepared using rotary fluidized-bed technology. Two particle sizes were produced that had a mean size of approximately 250 and 500 mum. Results show the process was able to produce pellets with a spherical and homogenous form when 10% of the active compounds were incorporated into the core. When active compounds were increased to 20%, the pellet became stickier, and the yield decreased from 90 to 65%. Different amounts of coating in the form of an aqueous-based ethylcellulose (EC) dispersion (Surelease) were applied to the core to modify the release of active compounds. The efficacy of the coating was evaluated in vitro using a flow-through cell apparatus. The time to achieve 50 and 90% dissolution increased with the increase in particle size (P < 0.05) and the increase in EC-coating level from 10 to 20% (wt/wt; P < 0.05), indicating the ability of the process to slow release depending on particle size and the amount of polymer applied. Differences in the release of the active compounds were observed in the same formulation of pellets, except for the formulation with small 10%-EC-coated particles, in which the active compounds were rapidly dissolved (more than 85% in 15 min or less). For all other formulations, the dissolution time for eugenol was always faster than for thymol or carvacrol. The close monitoring of plant extract behavior in the gastrointestinal tract could become a key factor in the continued use of phyto-molecules as alternatives to antibiotic growth promoters and in optimizing the balance between cost and efficacy. Different microencapsulation technologies can be used, of which the rotary fluidized bed warrants consideration because of the quality of the products obtained.

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Rethinking the Use of Water as a Dissolution Medium

Cited by 12 publications

References 0 publications

Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Physicochemical Characterization and Dissolution Study of Solid Dispersions of Furosemide with Polyethylene Glycol 6000 and Polyvinylpyrrolidone K30

Use of rotary fluidized-bed technology for development of sustained-release plant extracts pellets: Potential application for feed additive delivery1

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