Mechanism and Improved Dissolution of Glycyrrhetinic Acid Solid Dispersion by Alkalizers

Dong, Luning; Mai, Yaping; Liu, Qiang; Zhang, Wannian; Yang, Jianhong

doi:10.3390/pharmaceutics12010082

Cited by 48 publications

(27 citation statements)

References 69 publications

(88 reference statements)

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“…Therefore, in order to compare the effects of different molecular weight carriers on the structure of solid dispersions, a Raman spectrum analysis was performed on each sample. As presented in Figures 7(a) and 7(d), pure GA had two sharp characteristic peaks at 1620 cm -1 and 1,670 cm -1 , which is attributed to stretching vibrations of the carbonyl moiety and -COO-group [11]. Four different molecular weight PVPs also showed a significant scattering peak of carbonyls at 1670 cm -1 [42], and the peak shape is not sharp.…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 92%

“…In general, the solubility of hydrophobic drug can be improved by adding a surfactant, but a large amount of solubilizer is prone to side effects such as hemolysis. In order to overcome poor solubility of GA, in recent years, some research on new drug delivery systems of GA have been done, including GA liposomes [8], GA nanoemulsions [9], GA microparticles [10], and GA solid dispersion [11].…”

Section: Introductionmentioning

confidence: 99%

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The Effect of PVP Molecular Weight on Dissolution Behavior and Physicochemical Characterization of Glycyrrhetinic Acid Solid Dispersions

Sui

Chu

Zhang

et al. 2020

Advances in Polymer Technology

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The effect of polyvinylpyrrolidone (PVP) as glycyrrhetic acid (GA) solid dispersions carrier at different molecular weights on the dissolution behavior and physicochemical properties was investigated. PVP-GA-SDs prepared with all four molecular weight PVPs displayed good enhancement of dissolution rate and equilibrium solubility compared with pure drug and corresponding physical mixtures. The results showed that the enhancement effect of molecular weight on dissolution rate and equilibrium solubility follows PVP K 30 > PVP K 60 > PVP K 17 > PVP K 15 . In addition, the dissolution rate and solubility of the SDs with a carrier-drug ratio of 8 : 1 were better than the samples of 4 : 1. The DSC and XRD patterns showed that the crystallization of GA in SDs prepared by PVP K30 and PVP K60 was significantly inhibited, and both were transformed to amorphous. Based on FTIR and Raman detection, a hydrogen-bond between PVP and drug molecules is formed. SEM results showed that there were no significant differences in the appearance of SDs prepared with four PVPs, and no crystalline morphology of GA was seen. In conclusion, the findings of this study demonstrated that the dissolution performance of the PVP-GA-SDs prepared by the solvent method is related to the molecular weight of PVP, and the change in the molecular weight of PVP does not cause a monotonic change in dissolution of GA. The samples with PVP K30 as the carrier have the best dissolution performance.

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Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 92%

Section: Introductionmentioning

confidence: 99%

The Effect of PVP Molecular Weight on Dissolution Behavior and Physicochemical Characterization of Glycyrrhetinic Acid Solid Dispersions

Sui

Chu

Zhang

et al. 2020

Advances in Polymer Technology

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“…The angular range was 3° to 50° with a step size of 0.017° and a counting rate of 15 s/step. The analysis of the acquired data was performed using OriginPro 8 [ 31 ].…”

Section: Methodsmentioning

confidence: 99%

Combinations of Piperine with Hydroxypropyl-β-Cyclodextrin as a Multifunctional System

Stasiłowicz

Rosiak

Tykarska

et al. 2021

IJMS

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Piperine is an alkaloid that has extensive pharmacological activity and impacts other active substances bioavailability due to inhibition of CYP450 enzymes, stimulation of amino acid transporters and P-glycoprotein inhibition. Low solubility and the associated low bioavailability of piperine limit its potential. The combination of piperine with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) causes a significant increase in its solubility and, consequently, an increase in permeability through gastrointestinal tract membranes and the blood–brain barrier. X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR) were used to characterize interactions between piperine and HP-β-CD. The observed physicochemical changes should be combined with the process of piperine and CD system formation. Importantly, with an increase in solubility and permeability of piperine as a result of interaction with CD, it was proven to maintain its biological activity concerning the antioxidant potential (2,2-diphenyl-1-picryl-hydrazyl-hydrate assay), inhibition of enzymes essential for the inflammatory process and for neurodegenerative changes (hyaluronidase, acetylcholinesterase, butyrylcholinesterase).

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“…The angular range was 3° to 50° with a step size of 0.017° and counting rate of 15 s/step. OriginPro 8 was used to analyze the acquired data [ 14 , 15 ].…”

Section: Methodsmentioning

confidence: 99%

Structural Polymorphism of Sorafenib Tosylate as a Key Factor in Its Solubility Differentiation

et al. 2021

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The presence of active pharmaceutical ingredients (APIs) in the forms of different polymorphic states can induce differences in their physicochemical properties. In the case of poorly soluble APIs, like the oncological drug sorafenib tosylate, small variations in solubility may result in large bioavailability differences. The control of its therapeutic dose is crucial from the effective pharmacotherapy point of view and the reduction of side effects. Therefore, this study aimed to assess the influence of sorafenib tosylate polymorphic forms on its solubility and, consequently, permeability, based on passive diffusion through membranes simulating the gastrointestinal tract (GIT) conditions. In the first part of the work, two crystalline forms of sorafenib tosylate were identified using the X-ray powder diffraction, FT-IR, and Raman spectroscopy. Subsequently, solubility studies were carried out. Both forms of sorafenib tosylate were insoluble in 0.1 N hydrochloric acid (HCl), in acetate buffer (pH 4.5), and in phosphate buffer (pH 6.8). Solubility (mg/mL) of form I and III of sorafenib tosylate in 0.1 N HCl + 1.0% SDS was 0.314 ± 0.006 and 1.103 ± 0.014, respectively, in acetate buffer pH 4.5 + 1.0% SDS it was 2.404 ± 0.012 and 2.355 ± 0.009, respectively, and in phosphate buffer pH 6.8 + 1.0% SDS it was 0.051 ± 0.005 and 1.805 ± 0.023, respectively. The permeability study was assessed using the parallel artificial membrane permeability assay (PAMPA) model. The apparent permeability coefficient (Papp—cm s−1) of form I and III in pH 1.2 was 3.01 × 10−5 ± 4.14 × 10−7 and 3.15 × 10−5 ± 1.89 × 10−6, respectively, while in pH 6.8 it was 2.72 × 10−5 ± 1.56 × 10−6 and 2.81 × 10−5 ± 9.0 × 10−7, respectively. Changes in sorafenib tosylate concentrations were determined by chromatography using the high-performance liquid chromatography (HPLC)–DAD technique. As a result of the research on the structural polymorphism of sorafenib tosylate, its full spectral characteristics and the possibility of using FT-IR and Raman spectroscopy for the study of polymorphic varieties were determined for the first time, and the HPLC method was developed, which is appropriate for the assessment of sorafenib solubility in various media. The consequences of various physicochemical properties resulting from differences in the solubility of sorafenib tosylate polymorphs are important for pre-formulation and formulation studies conducted with its participation and for the safety of oncological sorafenib therapy.

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Mechanism and Improved Dissolution of Glycyrrhetinic Acid Solid Dispersion by Alkalizers

Cited by 48 publications

References 69 publications

The Effect of PVP Molecular Weight on Dissolution Behavior and Physicochemical Characterization of Glycyrrhetinic Acid Solid Dispersions

The Effect of PVP Molecular Weight on Dissolution Behavior and Physicochemical Characterization of Glycyrrhetinic Acid Solid Dispersions

Combinations of Piperine with Hydroxypropyl-β-Cyclodextrin as a Multifunctional System

Structural Polymorphism of Sorafenib Tosylate as a Key Factor in Its Solubility Differentiation

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