Comprehensive studies on physical and chemical stability in liquid and glassy states of telmisartan (TEL): solubility advantages given by cryomilled and quenched material

Adrjanowicz, Karolina; Grzybowska, K.; Kamiński, Kamil; Hawełek, ᴌ.; Paluch, Marian; Żakowiecki, Daniel

doi:10.1080/14786435.2010.534742

Cited by 29 publications

(38 citation statements)

References 54 publications

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“…It should be mentioned that this method requires the assumption that the shape of the structural relaxation peak does not change from the region above the glass transition temperature T g to the region below it. As we found previously, this procedure is able to predict quite well the time scale of molecular motion in the vicinity of the glass transition (T < T g ) [44].…”

Section: Prediction Of the Structural Relaxation Times In The Glassupporting

confidence: 76%

Molecular dynamics and crystallization phenomenon of supercooled and glassy DNA and RNA nucleosides:β-adenosine,β-thymidine, andβ-uridine

et al. 2011

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Nucleosides are chemical compounds that have an extremely important biological role; they can be found in all types of living organisms. They are crucial components from which DNA and RNA acids are built. In addition, nucleosides are key regulators of many physiological processes. In this paper, the molecular dynamics in the liquid and glassy state of three selected nucleosides, β-adenosine, β-thymidine, and β-uridine, was investigated by means of dielectric spectroscopy. Our results revealed multiple relaxation processes associated with different types of molecular motions. Besides the primary α relaxation, two secondary modes in the glassy states of examined compounds were identified. Crystallization progress monitored by dielectric spectroscopy and x-ray diffraction technique at isostructural relaxation conditions revealed that the examined nucleosides possess completely different tendencies to recrystallize from the liquid as well as the glassy state. We have also made an attempt to predict the time scale of molecular motion below the glass transition temperatures of the respective nucleosides to discuss their potential stability at room temperature over prolonged storage time. Finally, combination of molecular mobility studies with evaluation of thermodynamic parameters from calorimetric measurements allowed us to discuss the fundamental roles of both kinetic and thermodynamic factors in governing the physical stability of the glassy state.

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Section: Prediction Of the Structural Relaxation Times In The Glassupporting

confidence: 76%

Molecular dynamics and crystallization phenomenon of supercooled and glassy DNA and RNA nucleosides:β-adenosine,β-thymidine, andβ-uridine

et al. 2011

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“…The sample was decomposed in a single weight loss. This was supported by the derivative curve which exhibits only a single peak [35,36]. …”

Section: Thermogravimetric Analysismentioning

confidence: 99%

“…Adrjanowicz et al [35] determined the water content by the Karl Fischer method. For cryomilled Telmisartan sample, they have found 4% of water.…”

Section: Coulometrymentioning

confidence: 99%

Telmisartan

Bakheit

Abdelgalil

Mustafa

et al. 2015

Profiles of Drug Substances, Excipients and Related Methodology

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“…Moreover, it has been found that the amorphous form of API remained stable even after 1 year of storage under room conditions (22). In this context, application of acetylated saccharides in the formulation seems to be a promising option (11,17,18).…”

Section: Introductionmentioning

confidence: 99%

“…Amorphous substances show altered physico-chemical properties in comparison to their crystalline counterparts (9). Consequently, they often exhibit improved solubility, enhanced dissolution rate, and improved bioavailability (11)(12)(13)(14)(15)(16). Amorphization can be achieved by various routes, i.e., (i) solvent evaporation, (ii) milling, (iii) freeze-or spray drying, and (iv) quench cooling.…”

Section: Introductionmentioning

confidence: 99%

Melts of Octaacetyl Sucrose as Oral-Modified Release Dosage Forms for Delivery of Poorly Soluble Compound in Stable Amorphous Form

Haznar-Garbacz

Kamińska

Żakowiecki³

et al. 2017

AAPS PharmSciTech

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Abstract. The presented work describes the formulation and characterization of modified release glassy solid dosage forms (GSDFs) containing an amorphous nifedipine, as a model BCS (Biopharmaceutical Classification System) class II drug. The GSDFs were prepared by melting nifedipine together with octaacetyl sucrose. Dissolution profiles, measured under standard and biorelevant conditions, were compared to those obtained from commercially available formulations containing nifedipine such as modified release (MR) tablets and osmotic release oral system (OROS). The results indicate that the dissolution profiles of the GSDFs with nifedipine are neither affected by the pH of the dissolution media, type and concentration of surfactants, nor by simulated mechanical stress of biorelevant intensity. Furthermore, it was found that the dissolution profiles of the novel dosage forms were similar to the profiles obtained from the nifedipine OROS. The formulation of GSDFs is relatively simple, and the dosage forms were found to have favorable dissolution characteristics.

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Comprehensive studies on physical and chemical stability in liquid and glassy states of telmisartan (TEL): solubility advantages given by cryomilled and quenched material

Cited by 29 publications

References 54 publications

Molecular dynamics and crystallization phenomenon of supercooled and glassy DNA and RNA nucleosides:β-adenosine,β-thymidine, andβ-uridine

Molecular dynamics and crystallization phenomenon of supercooled and glassy DNA and RNA nucleosides:β-adenosine,β-thymidine, andβ-uridine

Telmisartan

Melts of Octaacetyl Sucrose as Oral-Modified Release Dosage Forms for Delivery of Poorly Soluble Compound in Stable Amorphous Form

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