Enhancing solubility and bioavailability of coenzyme Q10: formulation of solid dispersions using Soluplus® as a carrier

Lamichhane, Shrawani; Seo, Jeong-Sun; Keum, Taekwang; Noh, Gyubin; Bashyal, Santosh; Cho, Seong-Wan; Lee, Eun-Hee; Lee, Sang Kil

doi:10.1007/s12272-022-01368-4

Cited by 6 publications

(10 citation statements)

References 26 publications

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“…In DSC analysis, a pure crystalline drug typically exhibits a very intense and sharp endothermic peak, and when polymers are used as carriers for SD formulation, generally reduced and unclear peak is observed 21,22 . In the DSC results, a clear and sharp endothermic peak was observed from TPZ, while the typical endothermic peaks of TPZ were disappeared in F1–F4 SDs.…”

Section: Resultsmentioning

confidence: 97%

“…An important change expected from the development of SD formulations is the conversion of crystalline state into water‐soluble amorphous forms 21 . SEM image observation revealed that TPZ existed as a fine powder composed of very small particles.…”

Section: Resultsmentioning

confidence: 99%

“…Here,

Δ {G^{°}}_{T}^{Am orphous, Crystalline}

is the energy difference between the crystalline and amorphous structures, R is the gas constant, T is the absolute temperature of concern and

[\frac{σ_{T}^{Am orphous}}{σ_{T}^{Crystalline}}]

is the solubility ratio of each form 21 …”

Section: Resultsmentioning

confidence: 99%

“…An important change expected from the development of SD formulations is the conversion of crystalline state into water-soluble amorphous forms. 21 SEM image observation revealed that TPZ existed as a fine powder composed of very small particles. SD formulations F1-F4 showed no specific crystalline morphology, exhibiting glass-like lumps or a broken-piece-like appearance.…”

Section: Physicochemical Characteristicsmentioning

confidence: 99%

“…is the solubility ratio of each form. 21 Equation ( 1) states that amorphous form has a higher theoretical solubility than the crystalline form because of its thermodynamic properties. In other words, drug molecules easily interact and dissolve with solvent molecules through intermolecular interactions; no additional energy is required to destroy the crystal lattice structure once the crystallinity of TPZ is lost after the SD process.…”

Section: Amorphouscrystallinementioning

confidence: 99%

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Polymeric solid dispersion enhances the equilibrium solubility and oral bioavailability of tegoprazan

Won

Yang²,

Hong

et al. 2023

Bulletin Korean Chem Soc

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The recently developed water‐insoluble tegoprazan (TPZ) belongs to the biopharmaceutical classification system (BCS) class II group was formulated through solid dispersion (SD) technology. SD formulations of TPZ were prepared using hydroxymethylcellulose (HPMC) and polyvinylpyrrolidone (PVP) polymers via the solvent evaporation method. SDs were characterized by scanning electron microscopy (SEM), powder x‐ray diffraction (PXRD), and differential scanning calorimetry (DSC). In addition, the equilibrium solubility of SDs, in vitro dissolution, and in vivo bioavailability (BA) study in rats were performed. PXRD and DSC revealed that TPZ was successfully transformed to amorphous forms in SDs. The equilibrium solubility was enhanced by 15–18‐fold, and in vitro dissolution was improved by approximately 2.2‐fold. Consequently, the BA of TPZ was increased up to 2.1‐fold. In conclusion, the use of SDs of TPZ using HPMC and PVP are considered a potential strategy to improve the therapeutic effect of TPZ via enhanced dissolution and BA.

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Section: Resultsmentioning

confidence: 97%

Section: Resultsmentioning

confidence: 99%

“…Here,