title: Preparation and evaluation of self-microemulsifying drug delivery system containing vinpocetine.
abstract: The main purpose of current investigation is to prepare a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of vinpocetine, a poorly water-soluble drug. Suitable vehicles were screened by determining the solubility of vinpocetine in them. Certain surfactants were selected according to their emulsifying ability with different oils. Ternary phase diagrams were used to identify the efficient self-microemulsifying region and to screen the effect of surfactant/cosurfactant ratio (K(m)). The optimized formulation for in vitro dissolution and bioavailability assessment was oil (ethyl oleate, 15%), surfactant (Solutol HS 15, 50%), and cosurfactant (Transcutol P, 35%). The release rate of vinpocetine from SMEDDS was significantly higher than that of the commercial tablet. Pharmacokinetics and bioavailability of SMEDDS were evaluated. It was found that the oral bioavailability of vinpocetine of SMEDDS was 1.72-fold higher as compared with that of the commercial tablet. These results obtained demonstrated that vinpocetine absorption was enhanced significantly by employing SMEDDS. Therefore, SMEDDS might provide an efficient way of improving oral bioavailability of poorly water-soluble drugs.
authors.affiliation: Department of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.
authors.forename: Shu-Xia
authors.initials: SX
authors.lastname: Cui
authors.forename: Shu-Fang
authors.initials: SF
authors.lastname: Nie
authors.forename: Li
authors.initials: L
authors.lastname: Li
authors.forename: Chang-Guang
authors.initials: CG
authors.lastname: Wang
authors.forename: Wei-San
authors.initials: WS
authors.lastname: Pan
authors.forename: Jian-Ping
authors.initials: JP
authors.lastname: Sun
mesh_terms: D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004285:Dogs; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004655:Emulsions; D005079:Excipients; D018697:Nootropic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D012995:Solubility; D013501:Surface-Active Agents; D014748:Vinca Alkaloids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D004655:Emulsions; D005079:Excipients; D018697:Nootropic Agents; D009821:Oils; D013501:Surface-Active Agents; D014748:Vinca Alkaloids; C013983:vinpocetine