Preparation and In Vitro Evaluation of Self-Microemulsifying Drug Delivery Systems Containing Idebenone

A new self-microemulsifying drug delivery system (SMEDDS) was developed to increase the dissolution rate, solubility, and, ultimately, bioavailability of a poorly water soluble drug, idebenone. Pseudoternary phase diagrams were used to evaluate the self-microemulsification existence area, and the re...

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Bibliographic Details
Published in:Drug development and industrial pharmacy 2000-01, Vol.26 (5), p.523-529
Main Authors: Kim, Ho-Jin, Yoon, Kyung Ae, Hahn, Mikyoung, Park, Eun-Seok, Chi, Sang-Cheol
Format: Article
Language:English
Subjects:
Antioxidants - administration & dosage
Antioxidants - pharmacokinetics
Benzoquinones - administration & dosage
Benzoquinones - pharmacokinetics
Biological and medical sciences
Biological Availability
Chemistry, Pharmaceutical
Dissolution
Drug Delivery Systems
Emulsions
General pharmacology
Idebenone
Medical sciences
Neuropharmacology
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
SMEDDS
Solubility
Surface-Active Agents
Ubiquinone - analogs & derivatives
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Summary:A new self-microemulsifying drug delivery system (SMEDDS) was developed to increase the dissolution rate, solubility, and, ultimately, bioavailability of a poorly water soluble drug, idebenone. Pseudoternary phase diagrams were used to evaluate the self-microemulsification existence area, and the release rate of idebenone was investigated. The mixtures consisting of Labrafac hydro or Labrafil 2609 (HLB values > 4) with the surfactant (Labrasol containing 80% Transcutol) and cosurfactant (Plurol oleique WL 1173) were found to be optimum formulations. Using the SMEDDS formulations of 5% to 20% of Labrafac hydro or Labrafil 2609 in combination with the surfactant cosurfactant mixing ratio of 3, the microemulsion existence field was wider compared to the other SMEDDS formulations due to high affinity for the continuous phase. The in vitro dissolution rate of idebenone from SMEDDS was more than twofold faster compared with that of tablets. The developed SMEDDS formulation can be used as a possible alternative to traditional oral formulations of idebenone to improve its bioavailability.
ISSN:0363-9045
1520-5762
DOI:10.1081/DDC-100101263