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Dali, Mandar; Carstensen, J.T.

doi:10.1023/a:1016010207729

Cited by 29 publications

(9 citation statements)

References 11 publications

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“…It is well-known that the dissolution processes of drug crystals may affect bioavailability, and developing a better understanding of the dissolution processes may help to optimize the desired therapeutic effects. Crystal habit is often an important factor in influencing intrinsic dissolution rate. − Crystal habits can also affect many physical properties, such as ability to flow, compressibility, crystal face wettability, and dissolution rate anisotropy . For aspirin crystals, the dissolution rate of the (100) face was observed to be approximately 6 times faster than that of the (001) face 3 .…”

Section: Introductionmentioning

confidence: 99%

“…Crystal habit is often an important factor in influencing intrinsic dissolution rate. [1][2][3] Crystal habits can also affect many physical properties, such as ability to flow, compressibility, crystal face wettability, and dissolution rate anisotropy. 4 For aspirin crystals, the dissolution rate of the (100) face was observed to be approximately 6 times faster than that of the (001) face 3 .…”

Section: Introductionmentioning

confidence: 99%

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How Solvents Affect Acetaminophen Etching Pattern Formation: Interaction between Solvent and Acetaminophen at the Solid/Liquid Interface

Wen

Morris

et al. 2004

J. Phys. Chem. B

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The objective of this work was to further elucidate the dissolution process of acetaminophen crystals at the molecular level. The differences in the etching patterns from different solvents were used to study the interactions between solvent and acetaminophen molecules at the solid−liquid interface, such as solubilizing ability and potential solvent adsorption. The predicted etching patterns, based on the projections of attachment energies on the corresponding faces together with the solubilizing ability of the solvents, fit the observed etching patterns well. On the (001) face, the etching patterns were predominantly in the direction of the a-axis, which was also the direction of the dominant attachment energy. On the (110) face, the etching patterns were consistently in the direction of the c-axis irrespective of solvent used, and they were variable in other directions. These were well fit by the predicted etching patterns accounting for the different solubilizing ability of solvents. Both the most significant etching pattern deviations (on the (010) face) and the most significant morphology changes were observed with dichloroethane for acetaminophen. The morphology of acetaminophen crystals from different solvents showed that only the crystals from dichloroethane had significant elongation along the c-axis, which suggests the existence of stronger adsorption in the a-axis and b-axis directions than along the c-axis for dichloroethane. Overall, the current work suggests that the crystal interaction network, together with the interactions between solvent and acetaminophen, affects surface diffusion and plays an important role in the dissolution process.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

How Solvents Affect Acetaminophen Etching Pattern Formation: Interaction between Solvent and Acetaminophen at the Solid/Liquid Interface

Wen

Morris

et al. 2004

J. Phys. Chem. B

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“…Dissolution kinetics was calculated using the Noyes–Whitney dissolution model described by the following eq : where X dis is the mass of dissolved drug at time t , D eff is the diffusion coefficient, r 0 is the initial particle radius, h p is the thickness of the diffusion layer, ρ is the particle density, X tot is the total mass of undissolved and dissolved drug at time t , X ud is the mass of drug remaining to be dissolved (undissolved drug) at time t , C s is the equilibrium solubility of the drug, and V is the fluid volume. To simplify eq , 3 D eff / r 0 h p ρ is replaced by zeta ( z value), which is a dissolution parameter introduced by Takano et al Here, this dissolution model assumes that spherical and isometric drug particles dissolve with decreasing surface area of particles, and diffusion coefficient and diffusion layer thickness were regarded as constant during dissolution: …”

Section: Materials and Methodsmentioning

confidence: 99%

Utilization of Gastrointestinal Simulator, an in Vivo Predictive Dissolution Methodology, Coupled with Computational Approach To Forecast Oral Absorption of Dipyridamole

Matsui

Tsume

Takeuchi³

et al. 2017

Mol. Pharmaceutics

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Weakly basic drugs exhibit a pH-dependent dissolution profile in the gastrointestinal (GI) tract, which makes it difficult to predict their oral absorption profile. The aim of this study was to investigate the utility of the gastrointestinal simulator (GIS), a novel in vivo predictive dissolution (iPD) methodology, in predicting the in vivo behavior of the weakly basic drug dipyridamole when coupled with in silico analysis. The GIS is a multicompartmental dissolution apparatus, which represents physiological gastric emptying in the fasted state. Kinetic parameters for drug dissolution and precipitation were optimized by fitting a curve to the dissolved drug amount-time profiles in the United States Pharmacopeia apparatus II and GIS. Optimized parameters were incorporated into mathematical equations to describe the mass transport kinetics of dipyridamole in the GI tract. By using this in silico model, intraluminal drug concentration-time profile was simulated. The predicted profile of dipyridamole in the duodenal compartment adequately captured observed data. In addition, the plasma concentration-time profile was also predicted using pharmacokinetic parameters following intravenous administration. On the basis of the comparison with observed data, the in silico approach coupled with the GIS successfully predicted in vivo pharmacokinetic profiles. Although further investigations are still required to generalize, these results indicated that incorporating GIS data into mathematical equations improves the predictability of in vivo behavior of weakly basic drugs like dipyridamole.

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“…Detailed modeling of the dissolution of powders must take into account particle dimensions − (e.g., size, shape, and effective surface area), particle size distribution, contact angle between the liquid and the powder, general wettability characteristics, and physicochemical properties of the solid . The introduction of multiple chemical components complicates matters further.…”

Section: Theorymentioning

confidence: 99%

Electrochemical Determination of Dissolution Rates of Lyophilized Pharmaceutical Formulations

et al. 2001

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We present a method to measure dissolution times for rapidly dissolving lyophilized formulations. K4Fe(CN)6 was lyophilized in formulations containing sucrose, salts, and Tween 20. Dissolution of the lyophilized powders was measured by monitoring the time dependence of the oxidation of Fe(CN)6(4-) ion at the surface of a platinum rotating disk electrode. Reconstitution of lyophilized K4Fe(CN)6 formulations with aqueous solutions of 0.03% Tween 20 altered the time of dissolution for all cases. Salt and sucrose formulations without Tween 20 dissolved more slowly in a Tween 20 solution than in water alone. In contrast, formulations containing Tween 20 dissolved faster in the Tween 20 solution when compared to dissolution in water.

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Untitled

Cited by 29 publications

References 11 publications

How Solvents Affect Acetaminophen Etching Pattern Formation: Interaction between Solvent and Acetaminophen at the Solid/Liquid Interface

How Solvents Affect Acetaminophen Etching Pattern Formation: Interaction between Solvent and Acetaminophen at the Solid/Liquid Interface

Utilization of Gastrointestinal Simulator, an in Vivo Predictive Dissolution Methodology, Coupled with Computational Approach To Forecast Oral Absorption of Dipyridamole

Electrochemical Determination of Dissolution Rates of Lyophilized Pharmaceutical Formulations

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