Thermal analysis assisted by spectra-structure studies of BCS class II active pharmaceutical ingredients: ezetimibe and lercanidipine hydrochloride. The concept of preformulation

Chachorovska, Marina; Petrushevski, Gjorgji; Pecova, Monika Stojanovska; Ugarković, Sonja; Makreski, Petre

doi:10.1007/s10973-021-11159-6

Cited by 2 publications

(2 citation statements)

References 18 publications

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“…Thermal analyses were used to investigate the effects of thermal stress on the active substances. These analyses provided three different pieces of information about a particular phase transition: (1) the identity of the involved phase (structural information), (2) the temperature of the phase transition, and (3) the heat capacity of the system [ 46 ]. The temperature rise could cause thermal stress, which could occasionally cause the API's structural changes.…”

Section: Resultsmentioning

confidence: 99%

Impact of Methods of Preparation on Mechanical Properties, Dissolution Behavior, and Tableting Characteristics of Ibuprofen-Loaded Amorphous Solid Dispersions

Uddin,

Halder,

Deb

et al. 2024

Advances in Pharmacological and Pharmaceutical Sciences

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This study aims to improve the biopharmaceutical, mechanical, and tableting properties of a poorly soluble drug, ibuprofen (IBP), by preparing amorphous solid dispersion (ASD) followed by a sustained-release tablet formulation. A suitable polymer to develop an ASD system was chosen by utilizing the apparent solubility of IBP in various polymer solutions. ASDs containing various ratios of IBP and selected polymer were prepared by the melt fusion (MF) method. ASD containing optimized drug-polymer ratio prepared by freeze-drying (FD) method was characterized and compared physicochemically. The solubility of IBP in water increased 28-fold and 35-fold when formulated as ASD by MF and FD, respectively. Precise formulations showed amorphization of IBP and increased surface area, improving solubility. The dissolution pattern of optimized ASD-IBP in pH 6.8 phosphate buffer after 60 min in MF and FD was enhanced 3-fold. In addition, direct compression tablets comprising optimized ASD granules from MF and FD were made and assessed using compendial and noncompendial methods. ASD-IBP/MF and ASD-IBP/FD formulations showed a similar drug release profile. In addition, 12 h of sustained IBP release from the ASD-IBP-containing tablets was obtained in a phosphate buffer with a pH of 6.8. From the dissolution kinetics analysis, the Weibull model fitted well. The drug release pattern indicated minimal variations between tablets formed using ASD-IBP prepared by both procedures; however, pre- and postcompression assessment parameters differed. From these findings, the application of ASD and sustained-release polymers in matrix formation might be beneficial in improving the solubility and absorption of poorly soluble drugs such as IBP.

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Section: Resultsmentioning

confidence: 99%

Impact of Methods of Preparation on Mechanical Properties, Dissolution Behavior, and Tableting Characteristics of Ibuprofen-Loaded Amorphous Solid Dispersions

Uddin,

Halder,

Deb

et al. 2024

Advances in Pharmacological and Pharmaceutical Sciences

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“…Kinetic analysis represents an analytical method based on the data obtained from various thermal analysis techniques (thermogravimetry and differential scanning calorimetry) and it serves as an important investigational method in the pharmaceutical research [10,[25][26][27], among other scientific fields [28][29][30], leading to crucial information on stability, degradation mechanisms of the investigated compounds, and even shelf-life.…”

Section: Introductionmentioning

confidence: 99%

Thermal Stability and Kinetics of Degradation of Moxonidine as Pure Ingredient vs. Pharmaceutical Formulation

Baul,

Ledeţi,

Cîrcioban

et al. 2023

Processes

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The stability of active pharmaceutical ingredients (APIs) and the corresponding pharmaceutical formulations are nowadays of great importance in pharmaceutical research and technology. The quality of an API or of finished pharmaceutical products (FPPs) is time dependent under the influence of several parameters, such as light and air exposure, temperature, and humidity. Additionally, the stability profile of an API is influenced by the formulation composition, due to the presence of excipients or by the characteristic of the packaging materials. In this sense, the main objective of this study was to analyze the degradation kinetics of the antihypertensive drug moxonidine as a pure ingredient (MOX) and in two different solid mixtures, one corresponding to a pharmaceutical formulation (MOXTAB) and the other to an enriched pharmaceutical formulation in MOX (MOXMIX). As investigation techniques, FTIR (Fourier transform infrared) spectroscopy and TG/DTG/HF analysis were employed, while the thermoanalytical data were processed according to the ASTM E698 kinetic method and the isoconversional methods of Flynn–Wall–Ozawa (FWO) and Friedman (FR). The kinetic methods revealed that the excipients have a stabilizing effect on MOX (in terms of Ea values), but the decomposition mechanism of the samples is complex, according to the results suggested by the analysis of Ea vs. α values.

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Thermal analysis assisted by spectra-structure studies of BCS class II active pharmaceutical ingredients: ezetimibe and lercanidipine hydrochloride. The concept of preformulation

Cited by 2 publications

References 18 publications

Impact of Methods of Preparation on Mechanical Properties, Dissolution Behavior, and Tableting Characteristics of Ibuprofen-Loaded Amorphous Solid Dispersions

Impact of Methods of Preparation on Mechanical Properties, Dissolution Behavior, and Tableting Characteristics of Ibuprofen-Loaded Amorphous Solid Dispersions

Thermal Stability and Kinetics of Degradation of Moxonidine as Pure Ingredient vs. Pharmaceutical Formulation

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