Dissolution Rates of High Energy Sulfathiazole‐Povidone Coprecipitates II: Characterization of Form of Drug Controlling Its Dissolution Rate via Solubility Studies

Simonelli, Anthony P.; Mehta, Surendra C.; Higuchi, William I.

doi:10.1002/jps.2600650310

Cited by 126 publications

(48 citation statements)

References 3 publications

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“…According to this analysis, the dissolution rate can be enhanced by increasing the effective surface area available for dissolution (i.e., decreasing the particle size of the solids) or by improving the kinetic solubility of the drug under physiologically relevant conditions (i.e., employing ASDs). In early studies of amorphous pharmaceuticals, pioneering researchers such as Goldberg et al (5,6), Simonelli et al (7,8), and Chiou et al (9) all conducted their dissolution experiments under sink conditions and thereby emphasized the importance of a high dissolution rate of amorphous drugs from solid dispersions (e.g., sulfathiazole-polyvinylpyrrolidone PVP, griseofulvinpolyethylene glycol PEG) or eutectic mixtures (e.g., acetaminophen-urea, griseofulvin-succinic acid) as an essential criterion for assessing the solubility improvement. Consequently, the concept of enhancing dissolution rates of amorphous pharmaceuticals by incorporating rapidly dissolving ASD carriers has been adopted and propagated to succeeding generations of formulation design for orally administered poorly water-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

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

Sun

Lee

2015

AAPS J

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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.

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Section: Introductionmentioning

confidence: 99%

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

Sun

Lee

2015

AAPS J

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“…The main reason for the increased dissolution of the drug in presence of PVP might be due to crystal growth inhibition. It has been shown that PVP may serve to inhibit precipitation of drug from the supersaturated solution (Simonelli et al, 1976;Usui et al, 1997). Another reason for the increased dissolution of drug in presence of PVP could be the increased surface area of the drug exposed to the dissolution medium as a result of the adsorption on carrier.…”

Section: Solubility and Dissolution Studiesmentioning

confidence: 99%

Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine)

Javadzadeh

Jafari-Navimipour

Nokhodchi

2007

International Journal of Pharmaceutics

173

135

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Different liquisolid formulations of carbamazepine were accomplished by dissolving the drug in the non-toxic hydrophilic liquids, and adsorbing the solution onto the surface of silica. In order to reduce the amounts of carrier and aerosil in liquisolid formulations, some additives namely polyvinylpyrrolidone (PVP), hydroxypropyle methylcellulose (HPMC) and polyethylene glycol (PEG 35000) were added to liquid medication to increase loading factor. The effects of various ratios of carrier to coating material, PVP concentration, effect of aging and type of the carrier on dissolution rate of liquisolid compacts were studied. X-ray crystallography and differential scanning calorimetery (DSC) were used for evaluation of physicochemical properties of carbamazepine in liquisolid formulations. The results showed that the drug loading factor was increased significantly in the presence of additives. Liquisolid formulations containing PVP as additive, exhibited significantly higher drug dissolution rates compared to the compacts prepared by the direct compression technique. It was shown that microcrystalline cellulose had more liquid retention potential in comparison with lactose, and the formulations containing microcrystalline cellulose as carrier, showed higher dissolution rate. By decreasing the ratio of microcrystalline cellulose to silica from 20 to 10, an improvement in dissolution rate was observed. Further decrease in the ratio of microcrystalline cellulose:silica from 10 to 5 resulted in a significant reduction in dissolution rate. Increasing of PVP concentration in liquid medication caused a dramatic increase in dissolution rate at first 30 min. The results showed that the dissolution rate of liquisolid tablets was not significantly affected by storing the tablets at 25• C/75% relative humidity for a period of 6 months. The results of DSC and X-ray crystallography did not show any changes in crystallinity of the drug and interaction between carbamazepine and exipients during the process.

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“…However, the release rates of the two forms in pH 6.8 medium were almost the same. The release rate was obtained by plotting the Higuchi equation: (2) where Q is the percentage of release of the drug, t is the release time, and K is the apparent release rate constant. In addition, the 70% release time (T 70 ) was compared to the latter half of the release.…”

Section: Resultsmentioning

confidence: 99%

Improved Dissolution of an Insoluble Drug Using a 4-Fluid Nozzle Spray-Drying Technique

Chen¹,

Tagawa²,

Hoshi

et al. 2004

CHEMICAL & PHARMACEUTICAL BULLETIN

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Dissolution Rates of High Energy Sulfathiazole‐Povidone Coprecipitates II: Characterization of Form of Drug Controlling Its Dissolution Rate via Solubility Studies

Cited by 126 publications

References 3 publications

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

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

Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine)

Improved Dissolution of an Insoluble Drug Using a 4-Fluid Nozzle Spray-Drying Technique

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