Determination of Solubility and Nucleation Kinetics of Valnemulin Hydrochloride Solvate

Ouyang, Jinbo; Na, Bing; Liu, Zhongfan; Zhou, Limin; Hao, Hongxun

doi:10.1007/s10953-019-00861-7

Cited by 11 publications

(3 citation statements)

References 27 publications

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“…The dissolution enthalpy and entropy of icariin can be calculated from the slope and intersect of these plots in Table 4. The Gibbs energy of the solution can be calculated by the following equation 19,20 : Table 4 shows that the process of icariin solution in the 4 solvents over the experimental temperature range is endothermic (ΔH d > 0), which explains the enhanced solubility of icariin in the 4 organic solvents with the rise of temperature. The heat of solution of icariin in acetone is larger than that found in the other 3 solvents.…”

Section: Resultsmentioning

confidence: 99%

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Determination of the Solubility, Dissolution Enthalpy, and Entropy of Icariin in Acetone, Acetoacetate, Chloroform, and Light Petroleum

Xie

Zhang

Wang

et al. 2020

Natural Product Communications

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The solubility of icariin in acetone, acetoacetate, chloroform, and light petroleum in the 283.2‐318.2 K range was measured by ultraviolet-visible spectrophotometry. As the temperature increased, the solubility of icariin in the 4 solvents gradually increased. The solubility data correlated with the modified Apelblat equation. The dissolution enthalpy and entropy of icariin were determined using van’t Hoff plots. The dissolution enthalpy and entropy of icariin in the 4 solvents increases as acetone >acetoacetate >chloroform >light petroleum, which can be explained by the difference of the polarity indices between them. The polarity indices of the solvents affect the solubility behavior.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Determination of the Solubility, Dissolution Enthalpy, and Entropy of Icariin in Acetone, Acetoacetate, Chloroform, and Light Petroleum

Xie

Zhang

Wang

et al. 2020

Natural Product Communications

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show abstract

“…Cations mainly refer to the cationic amino acids [11]. In recent years, pharmaceutical cocrystals also open a new door for solid forms that can enable substantial modification of physicochemical properties of API [12][13][14]. Pharmaceutical cocrystals are multi-component crystalline forms made of neutral molecular components, usually involving an API and one cocrystal former, also exhibiting a definite stoichiometry ratio, often leading to a hydrogen-bonded molecular complex [15,16].…”

Section: Introductionmentioning

confidence: 99%

Effect of Solid Forms on Physicochemical Properties of Valnemulin

et al. 2019

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To improve the physicochemical properties of valnemulin (VLM), different solid forms formed by VLM and organic acids, including tartaric acid (TAR), fumaric acid (FUM), and oxalic acid (OXA), were successfully prepared and characterized by using differential scanning calorimetry (DSC), scanning electron microscope (SEM), X-ray powder diffraction (XRPD), and Fourier-transform infrared spectroscopy (FT-IR). The excess enthalpy Hex between VLM and other organic acids was calculated by COSMOthermX software and was used to evaluate the probability of forming multi-component solids between VLM and organic acids. By thermal analysis, it was confirmed that multi-component solid forms of VLM were thermodynamically more stable than VLM itself. Through dynamic vapor sorption (DVS) experiments, it was found that three multi-component solid forms of VLM had lower hygroscopicity than VLM itself. Furthermore, the intrinsic dissolution rate of VLM and its multi-component forms was determined in one kind of acidic aqueous medium by using UV-vis spectrometry. It was found that the three multi-component solid forms of VLM dissolved faster than VLM itself.

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Effect of Sodium Sulfate on Nucleation Behavior and the Crystal Morphology of Taurine

Zhang

Luo

et al. 2020

Crystal Research and Technology

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Two theoretical methods, self‐consistent Nývlt‐like approach and Sangwal's classical 3D nucleation theory‐based method, are employed to analyze the effects of additives (sodium sulfate) on the nucleation behavior of taurine. By correlating the measured metastable zone width of taurine containing different sodium sulfate concentrations, with saturation temperature and cooling rate, nucleation kinetic parameters in both two methods are determined. Fitting results demonstrate that higher sodium sulfate concentration results in the increase of solid–liquid interfacial energy γ, contrarily higher saturation temperature has the opposite effect thus changing of nucleation rate. The molecular modeling techniques are then applied to investigate the changes in the morphology of taurine which caused by the presence of sodium sulfate. Through molecular dynamic simulations, the interaction energy of sodium sulfate with taurine crystal faces are obviously larger than those of taurine and these differences on the (011) and (11‐1) are more significant than those on (021) and (111) faces. As a result, the growth of (011) and (11‐1) faces is inhibited and the morphology of taurine crystal is modified from needle to columnar. The influence of sodium sulfate on taurine studied in this work provides theoretical guidance for industrial production.

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Determination of Solubility and Nucleation Kinetics of Valnemulin Hydrochloride Solvate

Cited by 11 publications

References 27 publications

Determination of the Solubility, Dissolution Enthalpy, and Entropy of Icariin in Acetone, Acetoacetate, Chloroform, and Light Petroleum

Determination of the Solubility, Dissolution Enthalpy, and Entropy of Icariin in Acetone, Acetoacetate, Chloroform, and Light Petroleum

Effect of Solid Forms on Physicochemical Properties of Valnemulin

Effect of Sodium Sulfate on Nucleation Behavior and the Crystal Morphology of Taurine

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