title: Self nano-emulsifying simvastatin based tablets: design and in vitro/in vivo evaluation.
abstract: The aim of this work is to improve the oral bioavailability of poorly water soluble drug, simvastatin (SV) through combining the advantages of self-nanoemulsifying systems (SNEs) and tablets. Ternary phase diagram was constructed using Labrafil, Tween 80 and Transcutol, in order to evaluate self-nanoemulsification domain. The particle size distribution and zeta potential of the prepared systems were evaluated using Malvern Zetasizer. Liquisolid powders were prepared using Aeroperl(®) as a coating material and Avicel(®) or Starch 1500 as carrier materials, the powder flow properties were then evaluated. Compressed SV SNE based tablets were evaluated regarding their physical characteristics, in-vitro release properties as well as in-vivo pharmacokinetic evaluation in six healthy human volunteers using a validated LC/MS/MS method. The in-vitro release results revealed that the developed SNE based tablets improved the release of SV significantly, compared to commercially available SV tablets (Zocor(®)). The optimal SV SNE tablet formulation was S3St10 (10% Labrafil, 60% Tween 80, and 30% Transcutol). The in-vivo evaluation of S3St10 revealed that rapid and enhanced absorption of SV could be obtained from the SNE based tablet, with a 1.5 fold increase in bioavailability than that obtained after administration of Zocor(®). Hence such an approach could be promising in improving the bioavailability of SV.
authors.affiliation: Department Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt. gabdelbary@gmail.com
authors.forename: Ghada
authors.initials: G
authors.lastname: Abdelbary
authors.forename: Maha
authors.initials: M
authors.lastname: Amin
authors.forename: Salwa
authors.initials: S
authors.lastname: Salah
mesh_terms: D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D018592:Cross-Over Studies; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D016503:Drug Delivery Systems / Q000379:methods; D045703:Emulsifying Agents / Q000737:chemistry* / Q000493:pharmacokinetics; D004655:Emulsions / Q000737:chemistry* / Q000493:pharmacokinetics; D005026:Ethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics; D005079:Excipients / Q000138:chemical synthesis / Q000493:pharmacokinetics; D006801:Humans; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry / Q000493:pharmacokinetics; D011208:Powders / Q000737:chemistry / Q000493:pharmacokinetics; D019821:Simvastatin / Q000737:chemistry* / Q000493:pharmacokinetics; D012995:Solubility; D013607:Tablets / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D004337:Drug Carriers; D045703:Emulsifying Agents; D004655:Emulsions; D005026:Ethylene Glycols; D005079:Excipients; D011136:Polysorbates; D011208:Powders; D013607:Tablets; C010111:carbitol; D019821:Simvastatin