Preparation and evaluation of self-microemulsifying drug delivery system containing vinpocetine.
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.
Cui
Shu-Xia
SX
Department of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.
Nie
Shu-Fang
SF
Li
Li
L
Wang
Chang-Guang
CG
Pan
Wei-San
WS
Sun
Jian-Ping
JP
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
D004655:Emulsions; D005079:Excipients; D018697:Nootropic Agents; D009821:Oils; D013501:Surface-Active Agents; D014748:Vinca Alkaloids; C013983:vinpocetine