Physicochemical Characterization of Rutaecarpine-Loaded Microemulsion System

• Published in: Drug development and industrial pharmacy 2005-01, Vol.31 (7), p.639-643
• Main Authors: Choi, Han-Gon, Park, Byung-Joo, Kim, Jong Oh, Park, Young-Joon, Kim, Jin-Ki, Yoo, Bong-Kyu, Rhee, Jong-Dal, Jahng, Yurngdong, Yong, Chul Soon
• Format: Article
• Language: English
• Subjects: Alkaloids - chemistry; Biological and medical sciences; Emulsions; Ethanol - chemistry; General pharmacology; Indole Alkaloids; Medical sciences; Microemulsion; Oils - chemistry; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Platelet Aggregation Inhibitors - chemistry; Polyethylene Glycols - chemistry; Polysorbates - chemistry; Quinazolines; Rutaecarpine; Solubility; Stability; Surface-Active Agents - chemistry; Vasodilator Agents - chemistry; Water - chemistry
• ISSN: 0363-9045; 1520-5762
• DOI: 10.1080/03639040500216303

To develop an o/w microemulsion system containing poorly water-soluble rutaecarpine, the solubility of rutaecarpine in water, ethanol, various oils, and surfactants were investigated. Among the surfactants and oils tested, Tween 20/PEG 400 and castor oil were chosen as the surfactant system and oil phase of the microemulsion, as rutaecarpine was most soluble in them, respectively. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, and cosurfactant for microemulsion formation, and the stability test of rutaecarpine delivered by microemulsion formation was then evaluated. Pseudoternary phase diagrams show that the areas of microemulsion appeared at those with 0-20% Smix (PEG 400/Tween80 = 60/40), 64-81% water, and 10-20% oil. The rutaecarpine (300 µg/g)-loaded microemulsion composed of 10.8% PEG 400, 7.2% Tween 80, 20% caster oil, and 72% water was physically and chemically stable for at least 6 months. Thus, the microemulsion system composed of castor oil, PEG 400, Tween 80, and water could be a stable dosage form for rutaecarpine.