Tranilast-matrine co-amorphous system: Strong intermolecular interactions, improved solubility, and physiochemical stability

Hu, Dandan; Chen, Xin; Li, Duanxiu; Zhang, Hailu; Duan, Yanwen; Huang, Yong

doi:10.1016/j.ijpharm.2023.122707

Cited by 16 publications

(3 citation statements)

References 61 publications

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“…Approximately 2 mg of each dried sample was uniformly mixed with 200 mg of KBr by grinding in an agate mortar under infrared light and compressed into tablets before measurement. Spectral data were collected by performing 32 scans in transmission mode, covering the wavenumber range from 4000 to 400 cm −1 with a resolution of 4 cm −1 [16]. The FTIR spectrum of pure KBr served as the background of all samples.…”

Section: Fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

“…Samipillai et al found that the dissolution rates of dasatinib-saccharin and olanzapine-saccharin were enhanced in phosphate-buffered saline (PBS, pH 7.2) at 37 • C, with enhancements of 20-30 times compared to the pure drugs [15]. Hu et al reported that the solubility of tranilast-matrine in both water and PBS (pH 6.8) was over 100 times higher than that of crystalline tranilast, with significantly increased release rates [16]. However, at present, the co-amorphous system is mainly used in the pharmaceutical field, with limited utilization in the health products sector.…”

Section: Introductionmentioning

confidence: 99%

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Preparation and Characterization of Lutein Co-Amorphous Formulation with Enhanced Solubility and Dissolution

Song,

Luo,

Zhao

et al. 2024

Foods

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Lutein is an oxygenated fat-soluble carotenoid and a functional compound with proven health benefits for the human body. Nevertheless, the poor water solubility and low oral bioavailability of lutein greatly limit its application. To address this, we developed an effective approach to enhance the water solubility of lutein through co-amorphous formulation. Specifically, the lutein-sucralose co-amorphous mixture was prepared at a molar ratio of 1:1 using ethanol and water as solvents by employing the solvent evaporation method, followed by solid-state characterization and dissolution testing conducted to assess the properties of the formulation. The X-ray diffraction pattern with an amorphous halo and the differential scanning calorimetry thermogram with no sharp melting peaks confirmed the formation of a binary co-amorphous system. Changes in peak shape, position, and intensity observed in the Fourier transform infrared spectroscopy spectrum revealed intermolecular interactions between lutein and sucralose molecules, while molecular dynamics simulations identified interaction sites between their hydroxyl groups. Additionally, dissolution testing demonstrated better dissolution performance of lutein in the co-amorphous form compared to pure lutein and physical mixture counterparts. Our findings present a novel strategy for improving the water solubility of lutein to make better use of it.

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Section: Fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Lutein Co-Amorphous Formulation with Enhanced Solubility and Dissolution

Song,

Luo,

Zhao

et al. 2024

Foods

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show abstract

“…Table 5 summarizes the solvatochromic parameters,α, β, and π, as well as the Hansen solubility parameters of 15 solvents studied in this research taken from the literature. (28)(29)(30)(31)(32) Table 5. Solvatochromic parameters and total Hansen solubility parameter of some solvent studied.…”

Section: Solvent Effects: Kat-lser Modelmentioning

confidence: 99%

Solubility data and solubility parameters of barnidipine in different pure solvents

Peña-Fernández,

Spanò,

Torres Pabón

et al. 2023

Ars Pharm

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Introduction: Solubility studies and obtaining physicochemical data on drugs in pure solvents belonging to different chemical classes are key to developing new drug formulations. In this work, Hansen partial solubility parameters (HSP) were calculated to assess the miscibility and intermolecular interactions of barnidipine in seventeen pure solvents. The comparison of the results obtained with the theoretical values calculated according to the structure of barnidipine, were valuable to analyse the influence of the solute-solute, solute-solvent relationships of the additive contribution groups, on the chemical and physical properties of this molecule with the solvents of different polarity tested, to provide relevant information highly useful in the pharmaceutical industry. Method: Equilibrium barnidipine solubilities in mono-solvents was determined using the classical shake-flask method, followed by UV-spectrophotometric analysis at 298.15 K. The partial solubility parameters were calculated by applying theoretical group contribution methods, proposed by Hoftyzer-Van Krevelen and Fedors. The KAT-LSER model was used to investigate the effect of solvent based on the concept of linear solvation energy relationships. The mole fraction was obtained from the densities of the solutions. Solid-phase analyses were made by calorimetry differential scanning. Results: The modification introduced in the extended Hansen method, that is, the use of lnX2 as the dependent variable, provided excellent results. The highest solubility values have been found in polar solvents. It is observed that solvent-solvent and solute-solvent intermolecular interactions through hydrogen bonds and van der Waals forces, significantly influence drug solubility. Conclusions: The affinity between barnidipine and each one of the selected solvent was evaluated by using HSP. Results showed that HSP could be well used to analyse drug solubility in particular solvents. Barnidipine is easier to dissolve in solvents with shorter carbon chains and higher polarity.

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Tranilast alleviates skin inflammation and fibrosis in rosacea-like mice induced by long-term exposure to LL-37

Jin,

Wu,

Zhang

et al. 2024

Biochemical and Biophysical Research Communications

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Tranilast-matrine co-amorphous system: Strong intermolecular interactions, improved solubility, and physiochemical stability

Cited by 16 publications

References 61 publications

Preparation and Characterization of Lutein Co-Amorphous Formulation with Enhanced Solubility and Dissolution

Preparation and Characterization of Lutein Co-Amorphous Formulation with Enhanced Solubility and Dissolution

Solubility data and solubility parameters of barnidipine in different pure solvents

Tranilast alleviates skin inflammation and fibrosis in rosacea-like mice induced by long-term exposure to LL-37

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