Interactions Between Paracetamol and Hypromellose in the Solid State

Leyk, Edyta; Wesołowski, Marek

doi:10.3389/fphar.2019.00014

Cited by 26 publications

(12 citation statements)

References 41 publications

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“…In order to develop the solubility curve, the quantity of crystalline substance that can be dissolved in a polymer at a given temperature was determined. The melting point, the heat of fusion and the Hansen solubility parameters were used for the calculations, according to the approach presented elsewhere [15,26,27]. Literature data on the solubility parameters indicating intermolecular interactions were also used in the calculations [28][29][30].…”

Section: Calculations For Phase Diagramsmentioning

confidence: 99%

Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose

Leyk

Wesołowski

2021

Pharmaceutics

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As amorphization may improve the solubility and bioavailability of a drug substance, the aim of this work was to assess to what extent the crystallinity of caffeine (CAF) and theophylline (TF) can be reduced by homogenization with a polymeric excipient. To realize this purpose, the physical mixtures of both methylxanthines with hydroxypropyl methylcellulose (HPMC) were examined using differential scanning calorimetry (DSC), hot-stage microscopy (HSM), Fourier-transform infrared (FTIR) and Raman spectroscopy. Moreover, phase diagrams for the physical mixtures were calculated using theoretical data. Results of DSC experiments suggested that both CAF and TF underwent amorphization, which indicated proportional loss of crystallinity for methylxanthines in the mixtures with HPMC. Additionally, HSM revealed that no other crystalline or amorphous phases were created other than those observed for CAF and TF. FTIR and Raman spectra displayed all the bands characteristic for methylxanthines in mixtures with HPMC, thereby excluding changes in their chemical structures. However, changes to the intensity of the bands created by hydrogen bonds imply the formation of hydrogen bonding in the carbonyl group of methylxanthines and the methyl polymer group. This is consistent with data obtained using principal component analysis. The findings of these studies revealed the quantities of methylxanthines which may be dissolved in the polymer at a given temperature and the composition at which methylxanthines and polymer are sufficiently miscible to form a solid solution.

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Section: Calculations For Phase Diagramsmentioning

confidence: 99%

Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose

Leyk

Wesołowski

2021

Pharmaceutics

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“…Usually, TG and DSC are used for the characterization of powder and binary mixtures [15]. This method offers an evaluation of the thermal characteristics, dehydration and could be a tool for describing possible interactions between the API and excipients [6,23]. It can be used also in the evaluation of the absorption or desorption of water [15].…”

Section: Introductionmentioning

confidence: 99%

Structural and Thermal Analysis of Cannabidiol Orodispersible Formulations

Vlad¹

2021

FARMACIA

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Cannabidiol (CBD) is an alkaloid that can be found in the Cannabis species, currently used in United States of America under the name of Epidiolex ® , which was approved by Food and Drug Administration (FDA) for seizures treatment. The purpose of this study was to investigate the structural characteristics of the raw materials and to compare 2 film formulations with different analytical methods. In order to differentiate the structural properties, the following methods were used: X-ray powder diffraction (XRPD) and Fourier transform-infrared (FTIR) spectroscopy. The thermal properties of the raw materials and films was also obtained using differential scanning calorimetry (DSC) and thermogravimetry analysis (TGA). As in the case of structural properties for the thermal decomposition, two films formulations that presented the highest differences were selected. Thermal analysis, FTIR and XRPD were utilized to present the characteristics of the raw materials and the selected orodispersible films. RezumatCanabidiolul (CBD) este unul din alcaloizii ce se regăsește în speciile de Cannabis. Ca produs medicamentos este prezent în Statele Unite ale Americii sub denumirea comercială de Epidiolex ® (medicament aprobat de Food and Drug Administration -FDA) pentru tratamentul epilepsiei. Scopul acestui studiu constă în prezentarea caracteristicilor structurale ale excipienților, substanței active, respectiv compararea a două formulări de filme orodispersabile prin metode analitice diferite. Pentru a pune în evidență proprietățile structurale ale formularilor s-au folosit următoarele metode: difracția de raze X și spectrometria în infraroșu cu transformată Fourier. Proprietățile termice ale excipienților, substanței active precum și cele ale filmelor au fost analizate utilizând calorimetria cu scanare diferențială și analiza termogravimetrică. La fel ca în cazul analizei proprietăților structurale, și în cazul analizei termice au fost selectate două formulări de filme ce au prezentat proprietăți distincte. FTIR și XRPD au fost utilizate pentru a evidenția proprietățile structurale, cele termice fiind evaluate utilizând DSC și ATG.

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“…For this reason, at a content of 2.16% of paracetamol in the mixtures with Estram H15 and of 6.89% in those with Witepsol S58, drug fusion could not be detected. Potential interaction between paracetamol and excipients resulting in reduced drug crystallinity and lowered enthalpy of fusion can be found in the literature (33). These interactions are due to mutual miscibility and solubility of ingredients in the solid-state.…”

Section: Calibration Techniquesmentioning

confidence: 99%

Determination of Paracetamol in Commercial Suppositories Using Differential Scanning Calorimetry

Leyk¹,

Komar²,

Wesołowski³

2019

Acta Poloniae Pharmaceutica - Drug Research

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Paracetamol, also known as acetaminophen, has been commonly used as a major active pharmaceutical ingredient in numerous analgesics for over 30 years. This means that specific and reliable methods are crucial for quality control of its formulations. The purpose of this work was to show to what extent differential scanning calorimetry (DSC) can be useful for the determination of paracetamol in formulations intended for rectal use. Suppositories commonly available in Polish pharmacies were chosen for the study. In order to assess the impact of various suppository bases on active ingredient determination in the formulations analyzed, the selection was made from various producers and with varying doses of paracetamol. DSC scans were taken on a heat-flux instrument with a liquid nitrogen cooling system. To achieve the aim of this study, a well-defined endothermic DSC peak was used, assigned to the melting-point of paracetamol at 168.64 O C with the heat of transition of 183.99 J/g. A multiple standard addition method was chosen for the calibration. Except for one formulation containing 50 mg of paracetamol, the relative standard deviation for all the DSC determinations varied over the range of 0.27 to 2.64%, while the relative error varied between 0.24 and 12.50%. The study demonstrated that DSC could successfully be employed as a simple, specific and reliable method for the determination of paracetamol in rectal preparations based on the measurement of its heat of fusion. The results are consistent with the data obtained using UV spectrophotometry (pharmacopoeial method) as reference.

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Interactions Between Paracetamol and Hypromellose in the Solid State

Cited by 26 publications

References 41 publications

Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose

Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose

Structural and Thermal Analysis of Cannabidiol Orodispersible Formulations

Determination of Paracetamol in Commercial Suppositories Using Differential Scanning Calorimetry

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