Comparison of Dissolution Rates of Different Crystalline Phases of Fluprednisolone by In Vitro and In Vivo Methods

Haleblian, John K.; Koda, Robert T.; Biles, John A.

doi:10.1002/jps.2600601009

Cited by 15 publications

(4 citation statements)

References 8 publications

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“…The in vivo DRs were determined by the pellet implantation technique described by Haleblian et al 18 . Accordingly, thin, cylindrical pellets of DEF-ea and DEF-t-bw (7mm in diameter), having a mean weight of $50 mg, were compressed (Hidraulicos Delfabro press, Argentina) at 600 kg for 15 s. Six adult male Wistar rats (mean weight of 185 g) were used to test each solid phase.…”

Section: In Vivo Dr Studiesmentioning

confidence: 99%

“…where DW is the weight change of the disks; Dt is equal to 72 h (the animal time exposition to the implanted pellets) and DA is the pellet area variation 18 . The animal weight loss was also determined to complement the DR IV results.…”

Section: In Vivo Dr Studiesmentioning

confidence: 99%

“…The intrinsic dissolution rates (DRs) of the samples that represented the different physical phases were analyzed based on the rotating disk method. In vivo studies were also performed using the implantation technique in rats described by Haleblian et al 18 .…”

Section: Introductionmentioning

confidence: 99%

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Preparation and characterization of polymorphs of the glucocorticoid deflazacort

Kassuha¹,

Aiassa²,

Bruno³

et al. 2014

Pharmaceutical Development and Technology

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The polymorphism of new and old active pharmaceutical ingredients (APIs) is of great importance due to performance, stability and processability aspects. The objective of this study was to investigate the polymorphism of deflazacort (DEF), a glucocorticoid discovered >40 years ago, since this phenomenon has not been previously investigated for this API. Using different methods for solid form screening, it was determined for the first time that DEF is able to exist as three forms: a crystalline (DEF-1); a hydrated X-ray amorphous (DEF-t-bw) and an anhydrous amorphous phase (DEF-g) obtained from manually grinding DEF-1. The in vitro and in vivo dissolution rates (DRs) of DEF-1 and DEF-t-bw, which were measured using the rotating disk method in water at 37 °C and the pellet implantation technique in rats, respectively, indicated that DEF-t-bw exhibited slightly faster in vitro and in vivo DRs than those of the crystalline form, but the values were not significantly different. In addition, it was determined that DEF-t-bw devitrifies to DEF-1 by the effect of pressure, humidity and heat. It was concluded that DEF is glucorticoid with low tendency to exhibit different crystalline forms and that DEF-t-bw has no advantages over DEF-1 in terms of solubility, DRs and solid-state stability.

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Section: In Vivo Dr Studiesmentioning

confidence: 99%

Section: In Vivo Dr Studiesmentioning

confidence: 99%

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Preparation and characterization of polymorphs of the glucocorticoid deflazacort

Kassuha¹,

Aiassa²,

Bruno³

et al. 2014

Pharmaceutical Development and Technology

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show abstract

“…Different polymorphs of a drug may exhibit significantly different biological activities due to their different solubility and dissolution rate [3]. The rate of dissolution depends on the enthalpy of dissolution, which in fact is the sum of three terms in accordance with the first law of thermodynamics:…”

Section: Thermodynamic Approachmentioning

confidence: 99%

Polymorphism and solvates. Application to pharmaceutical compounds

Légendre

2001

J. Phys. IV France

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Abstract. This article is the text of the lecture presented for the XXVlI JEEP in Montpellier.Polymorphism is well known in inorganic chemistry, it is relative to the variation of temperature and pressure. In organic chemistry the subject is more delicate because it does not depend only on these two functions, but also the way of preparation of the substance, the nature of the solvent of crystallisation, its rate of evaporation, and for melted compounds, the rate of cooling is also an important factor. In these conditions the study of polymorphism cannot be dissociated of the study of solvates. General knowledge will be presented in this paper, but also some particular cases in which equilibrium is difficult to reach.

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Pharmaceutical Sciences—1971: Literature Review of Pharmaceutics

Hamlin¹,

Shah²

1972

Journal of Pharmaceutical Sciences

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Comparison of Dissolution Rates of Different Crystalline Phases of Fluprednisolone by In Vitro and In Vivo Methods

Cited by 15 publications

References 8 publications

Preparation and characterization of polymorphs of the glucocorticoid deflazacort

Preparation and characterization of polymorphs of the glucocorticoid deflazacort

Polymorphism and solvates. Application to pharmaceutical compounds

Pharmaceutical Sciences—1971: Literature Review of Pharmaceutics

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