Compatibility study between antiparkinsonian drug Levodopa and excipients by FTIR spectroscopy, X-ray diffraction and thermal analysis

Ledeți, Ionuț; Bolintineanu, Sorin; Vlase, Gabriela; Circioban, Denisa; Ledeţi, Adriana; Vlase, Titus; Suta, Lenuta-Maria; Caunii, Angelica; Murariu, Marius

doi:10.1007/s10973-017-6393-2

Cited by 30 publications

(16 citation statements)

References 17 publications

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“…Since these techniques present different work fundamentals and vary the analysis time, amount of sample, and mechanical and/or thermal stress employed, the results obtained are complementary and provide different conclusions. However, in the absence of evidence of interaction, compatibility should be confirmed by FTIR [ 43 , 48 ].…”

Section: Resultsmentioning

confidence: 99%

Tablet of Ximenia Americana L. Developed from Mucoadhesive Polymers for Future Use in Oral Treatment of Fungal Infections

et al. 2019

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The use of biocompatible polymers such as Hydroxypropylmethylcellulose (HPMC), Hydroxyethylcellulose (HEC), Carboxymethylcellulose (CMC), and Carbopol in solid formulations results in mucoadhesive systems capable of promoting the prolonged and localized release of Active Pharmaceutical Ingredients (APIs). This strategy represents a technological innovation that can be applied to improving the treatment of oral infections, such as oral candidiasis. Therefore, the aim of this study was to develop a tablet of Ximenia americana L. from mucoadhesive polymers for use in the treatment of oral candidiasis. An X. americana extract (MIC of 125 μg·mL−1) was obtained by turbolysis at 50% of ethanol, a level that demonstrated activity against Candida albicans. Differential Thermal Analysis and Fourier Transform Infrared Spectroscopy techniques allowed the choice of HPMC as a mucoadhesive agent, besides polyvinylpyrrolidone, magnesium stearate, and mannitol to integrate the formulation of X. americana. These excipients were granulated with an ethanolic solution 70% v/v at PVP 5%, and a mucoadhesive tablet was obtained by compression. Finally, mucoadhesive strength was evaluated, and the results demonstrated good mucoadhesive forces in mucin disk and pig buccal mucosa. Therefore, the study allowed a new alternative to be developed for the treatment of buccal candidiasis, one which overcomes the inconveniences of common treatments, costs little, and facilitates patients’ adhesion.

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Section: Resultsmentioning

confidence: 99%

Tablet of Ximenia Americana L. Developed from Mucoadhesive Polymers for Future Use in Oral Treatment of Fungal Infections

et al. 2019

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“…However, in both cases, the decomposition of the API due to chemical processes or even physical transitions (phase transitions such as polymorphism and crystallization) in the presence of excipients dictates the shelf-life of the formulation [27,28]. Additionally, an adequate selection of excipients can lead to formulations with longer shelf-lives, as the presence of the excipients may have a stabilizing effect on the decomposition of APIs in formulation, relative to the same API as pure compound [29][30][31][32][33][34]. The literature is rather poor in presenting the physico-chemical characterization of candesartan and the prodrug CC.…”

Section: Introductionmentioning

confidence: 99%

Solid State Stability and Kinetics of Degradation for Candesartan—Pure Compound and Pharmaceutical Formulation

et al. 2020

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The aim of this work was to assess the impact of an excipient in a pharmaceutical formulation containing candesartan cilexetil over the decomposition of the active pharmaceutical ingredient and to comparatively investigate the kinetics of degradation during thermolysis in an oxidative atmosphere under controlled thermal stress. To achieve this, the samples were chosen as follows: pure candesartan cilexetil and a commercial tablet of 32 mg strength. As a first investigational tool, Universal attenuated total reflection Fourier transform infrared (UATR-FTIR) spectroscopy was chosen in order to confirm the purity and identity of the samples, as well as to check if any interactions took place in the tablet between candesartan cilexetil and excipients under ambient conditions. Later on, samples were investigated by thermal analysis, and the elucidation of the decomposition mechanism was achieved solely after performing an in-depth kinetic study, namely the use of the modified non-parametric kinetics (NPK) method, since other kinetic methods (American Society for Testing and Materials—ASTM E698, Friedman and Flynn–Wall–Ozawa) led to inadvertencies. The NPK method suggested that candesartan cilexetil and the tablet were degraded by the contribution of two steps, the main being represented by chemical degradation and the secondary being a physical transformation. The excipients chosen in the formulation seemed to have a stabilizing effect on the decomposition of the candesartan cilexetil that was incorporated into the tablet, relative to pure active pharmaceutical ingredient (API), since the apparent activation energy for the decomposition of the tablet was 192.5 kJ/mol, in comparison to 154.5 kJ/mol for the pure API.

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“…The summarization of thermoanalytical data is presented in Table 3. In previous papers, we also carried out diffractometric (XRPD) studies on binary mixtures kept under ambient conditions, when the corroboration of thermoanalytical data with the ones suggested by the FTIR spectroscopy were not concluding [23,25,26,35,39]. However, in the case of LTSS mixtures with selected excipients, no discrepancies were noticed between the selected instrumental techniques, as the incompatibilities suggested by the FTIR study were confirmed by the thermal analysis.…”

Section: Thermal Stability Investigationsmentioning

confidence: 99%

“…It is well known that magnesium stearate (MgSt) is an excipient that commonly shows interactions to various APIs [25,39]. Surprisingly, in the case of the LTSS+MgSt mixture, interaction is not observed.…”

Section: Thermal Stability Investigationsmentioning

confidence: 99%

Stability and Compatibility Studies of Levothyroxine Sodium in Solid Binary Systems—Instrumental Screening

et al. 2020

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The influence of excipients on the stability of sodium levothyroxine pentahydrate (LTSS) under ambient conditions and thermal stress was evaluated. Since LTSS is a synthetic hormone with a narrow therapeutic index, the interactions of LTSS with excipients can lead to a drastic diminution of therapeutic activity. Ten commonly used pharmaceutical excipients with different roles in solid formulations were chosen as components for binary mixtures containing LTSS, namely, starch, anhydrous lactose, D-mannitol, D-sorbitol, gelatin, calcium lactate pentahydrate, magnesium stearate, methyl 2-hydroxyethyl cellulose (Tylose), colloidal SiO2 (Aerosil) and talc. As investigational tools, universal attenuated total reflectance- Fourier transform infrared spectroscopy UATR-FTIR spectroscopy and thermal analysis were chosen and used as follows: UATR-FTIR spectra were drawn up for samples kept under ambient conditions, while thermoanalytical tools (TG/DTG/HF data) were chosen to evaluate the inducing of interactions during thermal stress. The corroboration of instrumental results led to the conclusion that LTSS is incompatible with lactose, mannitol and sorbitol, and these excipients should not be considered in the development of new generic solid formulations.

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Compatibility study between antiparkinsonian drug Levodopa and excipients by FTIR spectroscopy, X-ray diffraction and thermal analysis

Cited by 30 publications

References 17 publications

Tablet of Ximenia Americana L. Developed from Mucoadhesive Polymers for Future Use in Oral Treatment of Fungal Infections

Tablet of Ximenia Americana L. Developed from Mucoadhesive Polymers for Future Use in Oral Treatment of Fungal Infections

Solid State Stability and Kinetics of Degradation for Candesartan—Pure Compound and Pharmaceutical Formulation

Stability and Compatibility Studies of Levothyroxine Sodium in Solid Binary Systems—Instrumental Screening

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