title: Surfactant-Free Solid Dispersions of Hydrophobic Drugs in an Amorphous Sugar Matrix Dried from an Organic Solvent.
abstract: 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 Cmaxand AUC0-60 minof 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 Cmaxand AUC0-60 minfor all tested model drugs, and the model drug with a lower water solubility tended to exhibit a greater extent of over-dissolution.
authors.affiliation: Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University , 3-1-1 Tsushima-naka, Kita-ku, Okayama 700-8530, Japan.
authors.forename: Koji
authors.initials: K
authors.lastname: Takeda
authors.affiliation: Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University , 3-1-1 Tsushima-naka, Kita-ku, Okayama 700-8530, Japan.
authors.forename: Yuto
authors.initials: Y
authors.lastname: Gotoda
authors.affiliation: Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University , 3-1-1 Tsushima-naka, Kita-ku, Okayama 700-8530, Japan.
authors.forename: Daichi
authors.initials: D
authors.lastname: Hirota
authors.affiliation: Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University , 3-1-1 Tsushima-naka, Kita-ku, Okayama 700-8530, Japan.
authors.forename: Fumihiro
authors.initials: F
authors.lastname: Hidaka
authors.affiliation: Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University , 3-1-1 Tsushima-naka, Kita-ku, Okayama 700-8530, Japan.
authors.forename: Tomo
authors.initials: T
authors.lastname: Sato
authors.affiliation: Mitsubishi-Kagaku Foods Co. , 1000 Kamoshida-cho, Aoba-ku, Yokohama, Kanagawa 227-8502, Japan.
authors.forename: Tsutashi
authors.initials: T
authors.lastname: Matsuura
authors.affiliation: Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University , 3-1-1 Tsushima-naka, Kita-ku, Okayama 700-8530, Japan.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Imanaka
authors.affiliation: Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University , 3-1-1 Tsushima-naka, Kita-ku, Okayama 700-8530, Japan.
authors.forename: Naoyuki
authors.initials: N
authors.lastname: Ishida
authors.affiliation: Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University , 3-1-1 Tsushima-naka, Kita-ku, Okayama 700-8530, Japan.
authors.forename: Koreyoshi
authors.identifier: 0000-0001-7912-5057
authors.initials: K
authors.lastname: Imamura
mesh_terms: D002241:Carbohydrates / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D005079:Excipients / Q000737:chemistry; D005612:Freeze Drying / Q000379:methods; D057927:Hydrophobic and Hydrophilic Interactions; D009930:Organic Chemicals / Q000737:chemistry*; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011208:Powders / Q000737:chemistry; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry*; D014867:Water / Q000737:chemistry
chemical_list: D002241:Carbohydrates; D004337:Drug Carriers; D005079:Excipients; D009930:Organic Chemicals; D004364:Pharmaceutical Preparations; D011208:Powders; D012997:Solvents; D013501:Surface-Active Agents; D014867:Water
keywords: amorphous sugar; hydrophobic drug; solid dispersion; surfactant-free; vacuum foam drying