Solution-mediated phase transformation of different roxithromycin solid-state forms: Implications on dissolution and solubility

Aucamp, Marique; Stieger, Nicóle; Barnard, Neil B.; Liebenberg, Wilna

doi:10.1016/j.ijpharm.2013.03.048

Cited by 15 publications

(15 citation statements)

References 10 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…An active pharmaceutical ingredient (API) may crystallize into various solid forms which frequently possess different physicochemical and mechanical properties . Some pharmaceutical properties including solubility and stability are always affected by the solid performance of an API .…”

Section: Introductionmentioning

confidence: 99%

Crystal characterization and transformation of the forms I and II of anticoagulant drug rivaroxaban

Liu

et al. 2017

Crystal Research and Technology

View full text Add to dashboard Cite

The crystal forms I and II of rivaroxaban were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy. Powder dissolution testing was carried out at 310.15 K in the dissolution media at pH = 1.0 and pH = 6.8, respectively. The solution-mediated phase transformation from form II to form I was investigated under different temperature, slurry density and stirring speed, respectively, by use of the FTIR spectroscopy. The results showed that, the two forms were monotropically-related, and in the both dissolution media the concentration of form II was obviously higher than that of form I at the same time which demonstrated that form II was the metastable form. Among the evaluated solid-state kinetic models the Prout-Tompkins and Avrami-Erofeev (n = 3) equations gave a satisfactory correlation of the phase transformation process from form II to form I. The activation energy of phase transformation was calculated as 19.151 kJ·mol −1 by means of Arrhenius analysis. In addition, the phase transformation rate increased with increasing temperature, slurry density and stirring speed.

show abstract

Section: Introductionmentioning

confidence: 99%

Crystal characterization and transformation of the forms I and II of anticoagulant drug rivaroxaban

Liu

et al. 2017

Crystal Research and Technology

View full text Add to dashboard Cite

show abstract

“…Solution-mediated phase transformation can occur from a supersaturated solution or on the surface of a dissolving solid during dissolution, and in the course of manufacture and storage of liquid dosage forms as aqueous suspensions [77]. Phase transformation can lead to the precipitation of a less soluble and stable solid form from a metastable form [78]. Exposure to high humidity over the shelf life of the therapeutic product may also lead to the transformation of APIs and excipients to hydrated phases [20].…”

Section: Phase Transformation Of Hydrates and Solvatesmentioning

confidence: 99%

Pharmaceutical solvates, hydrates and amorphous forms: A special emphasis on cocrystals

Healy

Worku

Kumar

et al. 2017

Advanced Drug Delivery Reviews

257

189

View full text Add to dashboard Cite

a b s t r a c t a r t i c l e i n f oActive pharmaceutical ingredients (APIs) may exist in various solid forms, which can lead to differences in the intermolecular interactions, affecting the internal energy and enthalpy, and the degree of disorder, affecting the entropy. Differences in solid forms often lead to differences in thermodynamic parameters and physicochemical properties for example solubility, dissolution rate, stability and mechanical properties of APIs and excipients. Hence, solid forms of APIs play a vital role in drug discovery and development in the context of optimization of bioavailability, filing intellectual property rights and developing suitable manufacturing methods. In this review, the fundamental characteristics and trends observed for pharmaceutical hydrates, solvates and amorphous forms are presented, with special emphasis, due to their relative abundance, on pharmaceutical hydrates with single and two-component (i.e. cocrystal) host molecules.

show abstract

“…Solution-mediated transformation of roxithromycin metastable forms to the thermodynamically favoured form was identified during dissolution studies. Powder dissolution studies were done using three solid-state forms of roxithromycin [16]. During the dissolution studies of the roxithromycin solid-state forms, the solid-state transformation of the metastable forms to the stable monohydrate was demonstrated.…”

Section: Implications Of Solvent-interactive Transformationsmentioning

confidence: 99%

Solvent-Interactive Transformations of Pharmaceutical Compounds

Aucamp¹,

Liebenberg²,

Stieger³

2015

Advanced Topics in Crystallization

Self Cite

View full text Add to dashboard Cite

Solution-mediated phase transformation of different roxithromycin solid-state forms: Implications on dissolution and solubility

Cited by 15 publications

References 10 publications

Crystal characterization and transformation of the forms I and II of anticoagulant drug rivaroxaban

Crystal characterization and transformation of the forms I and II of anticoagulant drug rivaroxaban

Pharmaceutical solvates, hydrates and amorphous forms: A special emphasis on cocrystals

Solvent-Interactive Transformations of Pharmaceutical Compounds

Contact Info

Product

Resources

About