title: Oral sustained-release suspension based on a lauryl sulfate salt/complex.
abstract: The objective of this study was to evaluate the feasibility of lauryl sulfate (LS) salt/complex as a novel carrier in oral sustained-release suspensions. Mirabegron, which has a pH-dependent solubility, was selected as the model drug. Sodium lauryl sulfate (SLS) was bound to mirabegron in a stoichiometric manner to form an LS salt/complex. LS salt/complex formulation significantly reduced the solubility of mirabegron and helped mirabegron achieve sustained-release over a wide range of pH conditions. Microparticles containing the LS salt/complex were prepared by spray drying with the aqueous dispersion of ethylcellulose (Aquacoat®ECD). The diameter of the microparticles was less than 200μm, which will help avoid a gritty taste. In vitro results indicated the microparticles had slower dissolution profiles than the LS salt/complex. The dissolution rate could be controlled flexibly by changing the amount of Aquacoat®ECD. The microparticle suspension retained the desired sustained-release property and dissolution profile after being stored for 30days at 40°C. In addition, the suspension displayed sustained-release behavior in dogs without a pronounced Cmaxpeak, which will help prevent side effects. These results suggest that microparticles containing LS salt/complex may be useful as a novel sustained-release suspension for oral delivery.
authors.affiliation: Pharmaceutical and Technology Labs, Astellas Pharma Inc., 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan; Department of Pharmacy Practice and Science, School of Pharmaceutical Sciences University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
authors.forename: Yuuki
authors.initials: Y
authors.lastname: Kasashima
authors.affiliation: Department of Pharmacy Practice and Science, School of Pharmaceutical Sciences University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan. Electronic address: uchidas@u-shizuoka-ken.ac.jp.
authors.forename: Shinya
authors.initials: S
authors.lastname: Uchida
authors.affiliation: Pharmaceutical and Technology Labs, Astellas Pharma Inc., 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan.
authors.forename: Keiichi
authors.initials: K
authors.lastname: Yoshihara
authors.affiliation: Pharmaceutical and Technology Labs, Astellas Pharma Inc., 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan.
authors.forename: Takehiko
authors.initials: T
authors.lastname: Yasuji
authors.affiliation: Pharmaceutical and Technology Labs, Astellas Pharma Inc., 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan.
authors.forename: Kazuhiro
authors.initials: K
authors.lastname: Sako
authors.affiliation: Department of Pharmacy Practice and Science, School of Pharmaceutical Sciences University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan. Electronic address: namiki@u-shizuoka-ken.ac.jp.
authors.forename: Noriyuki
authors.initials: N
authors.lastname: Namiki
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations / Q000737:chemistry* / Q000493:pharmacokinetics; D004285:Dogs; D006863:Hydrogen-Ion Concentration; D010316:Particle Size; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry*; D012995:Solubility; D013535:Suspensions / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D003692:Delayed-Action Preparations; D013535:Suspensions; D012967:Sodium Dodecyl Sulfate; C013517:ethyl cellulose; D002482:Cellulose
keywords: Complex; Lauryl sulfate; Salt; Spray drying; Suspension; Sustained-release