Surfactant-free solid dispersion of fat-soluble flavour in an amorphous sugar matrix

Satoh, Tomo; Hidaka, Fumihiro; Miyake, K.; Yoshiyama, Natsuki; Takeda, Koji; Matsuura, Tsutashi; Imanaka, Hiroyuki; Ishida, Naoyuki; Imamura, Koreyoshi

doi:10.1016/j.foodchem.2015.11.097

Cited by 17 publications

(18 citation statements)

References 32 publications

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“…An alternate methodology for improving the water solubility of a hydrophobic drug is based on the amorphization of the drug . Namely, the amorphous state can be regarded as a frozen solid of the constituents in the amorphous material, and when the constituent molecules are dispersed in a solvent in which the constituents are poorly soluble, it follows that they would temporarily behave as dissolved materials, a phenomenon that is referred to as “super-saturation” − or “over-dissolution.” It has actually been demonstrated that the water solubility of a water-insoluble drug can be approximately doubled as the result of amorphization. ,− Since amorphous hydrophobic drugs are usually unstable and have a tendency to crystallize, they are often amorphized in the presence of carrier matrix forming agents. − This strategy is categorized as a solid dispersion. − In the solid dispersion of water-insoluble drugs, an amphiphilic polymer such as polyvinylpyrrolidone is frequently used as the carrier matrix, , and a combination of a surfactant with an amorphous carbohydrate matrix has also been reported to be effective for the stable dispersion of drugs. , …”

Section: Introductionmentioning

confidence: 99%

Surfactant-Free Solid Dispersions of Hydrophobic Drugs in an Amorphous Sugar Matrix Dried from an Organic Solvent

et al. 2017

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The technique for homogeneously dispersing hydrophobic drugs in a water-soluble solid matrix (solid dispersion) is a subject that has been extensively investigated in the pharmaceutical industry. Herein, a novel technique for dispersing a solid, without the need to use a surfactant, is reported. A freeze-dried amorphous sugar sample was dissolved in an organic solvent, which contained a soluble model hydrophobic component. The suspension of the sugar and the model hydrophobic component was vacuum foam dried to give a solid powder. Four types of sugars and methanol were used as representative sugars and the organic medium. Four model drugs (indomethacin, ibuprofen, gliclazide, and nifedipine) were employed. Differential scanning calorimetry analyses indicated that the sugar and model drug (100:1) did not undergo segregation during the drying process. The dissolution of the hydrophobic drugs in water from the solid dispersion was then evaluated, and the results indicated that the C and AUC of the hydrophobic drug in water were increased when the surfactant-free solid dispersion was used. Palatinose and/or α-maltose were superior to the other tested carbohydrates in increasing C and AUC for all tested model drugs, and the model drug with a lower water solubility tended to exhibit a greater extent of over-dissolution.

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Section: Introductionmentioning

confidence: 99%

Surfactant-Free Solid Dispersions of Hydrophobic Drugs in an Amorphous Sugar Matrix Dried from an Organic Solvent

et al. 2017

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“…The single T g indicates SAC and VAL in the co-amorphous state were completely dissolved in each other as a homogeneous phase [40]. The co-amorphous LM SDs showed T g values that were lower than the corresponding values of co-amorphous and co-amorphous MCC SDs (Figure 3c).…”

Section: Discussionmentioning

confidence: 91%

Combining Co-Amorphous-Based Spray Drying with Inert Carriers to Achieve Improved Bioavailability and Excellent Downstream Manufacturability

Zhang

Gao

et al. 2020

Pharmaceutics

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It is crucial to improve poorly water-soluble orally administered drugs through both preclinical and therapeutic drug discovery. A co-amorphous formulation consisting of two low molecular weight (MW) molecules offers a solubility/dissolubility advantage over its crystalline form by maintaining their amorphous status. Here, we report on a co-amorphous solid dispersion (SD) system that includes inert carriers (lactose monohydrate or microcrystalline cellulose) and co-amorphous sacubitril (SAC)-valsartan (VAL) using the spray drying process. The strong molecular interactions between drugs were the driving force for forming robust co-amorphous SDs. Our system provided the highest solubility with more than ~11.5- and 3.12-times solubility increases when compared with the physical mixtures. Co-amorphous lactose monohydrate (LM) SDs showed better bioavailability of APIs (~356.27.8% and 154.01% for the relative bioavailability of LBQ 657 and valsartan, respectively). Co-amorphous inert carrier SDs possessed an excellent compressibility for the production of a direct compression pharmaceutical product. In conclusion, these brand-new co-amorphous SDs could reduce the number of unit processes to produce a final pharmaceutical product for downstream manufacturability.

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“…Specific Molar Volume Analysis A ten mL of methanol or water was put in a 20 mL graduated cylinder, and 0.1~2 g (0.3~6 mmol) of amorphous sugar cake that had been freeze-dried from water and then thoroughly dehydrated over P2O5 [12] was then added to the methanol. α-Maltose was used as a sugar since it can be highly dissolved in methanol from amorphous state compared to the other sugars [10]. The freeze-dried amorphous α-maltose was absolutely dissolved by gently inverting the graduated cylinder several times.…”

Section: Vacuum Foam Drying and Heat Treatmentmentioning

confidence: 99%

“…In the solid dispersion of hydrophobic drugs, an amphiphilic polymer such as polyvinylpyrrolidone and hydroxypropyl methylcellulose is frequently used as the carrier matrix [6,7], and a combination of a surfactant with an amorphous carbohydrate matrix has also been reported to be effective for the stable dispersion of drugs [8,9]. On the other hand, we recently developed a new ASD technique that does not involve the use of a surface active agent [10]. In this method, (i) sugar is amorphized and (ii) added to an organic solvent containing a hydrophobic substance, followed by homogenization.…”

Section: Introductionmentioning

confidence: 99%

Thermal stability of amorphous sugar matrix, dried from methanol, as an amorphous solid dispersion carrier

Imamura

Takeda

Yamamoto

et al. 2018

Proceedings of 21th International Drying Symposium

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Developing a technique to disperse hydrophobic ingredients homogeneously in a water-soluble solid matrix (solid dispersion) is one of the topics that have been extensively investigated in the pharmaceutical and food industries. Recently, we have devised a novel solid dispersion technique (surfactant-free solid dispersion), in which a preliminarily amorphized sugar was dissolved in an organic media containing hydrophobic component, without using any surface active substances, and then vacuum dried into the amorphous solid mixture [Food Chem., 197 (2016) 1136 Mol. Pharm., 14 (2017) 791]. In this study, the physicochemical properties, especially thermal stability of the surfactant-free amorphous solid dispersion, were investigated. 997 Thermal stability of amorphous sugar matrix, dried from methanol, as an amorphous solid dispersion carrier 21 ST INTERNATIONAL DRYING SYMPOSIUM EDITORIAL UNIVERSITAT POLITÈCNICA DE VALÈNCIA

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Surfactant-free solid dispersion of fat-soluble flavour in an amorphous sugar matrix

Cited by 17 publications

References 32 publications

Surfactant-Free Solid Dispersions of Hydrophobic Drugs in an Amorphous Sugar Matrix Dried from an Organic Solvent

Surfactant-Free Solid Dispersions of Hydrophobic Drugs in an Amorphous Sugar Matrix Dried from an Organic Solvent

Combining Co-Amorphous-Based Spray Drying with Inert Carriers to Achieve Improved Bioavailability and Excellent Downstream Manufacturability

Thermal stability of amorphous sugar matrix, dried from methanol, as an amorphous solid dispersion carrier

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