Synchronized and sustained release of multiple components in silymarin from erodible glyceryl monostearate matrix system.
Development of sustained delivery systems for herbal medicines was very difficult because of their complexity in composition. The concept of synchronized release from sustained release systems, which is characterized by release of multiple components in their original ratio that defines a herbal medicine, served as the basis for keeping the original pharmacological activity. In this study, erodible matrix systems based on glyceryl monostearate and polyethylene glycol 6000 or poloxamer 188 were prepared to perform strict control on synchronized release of the five active components of silymarin, i.e. taxifolin, silychrystin, silydianin, isosilybin and silybin. The matrix system was prepared by a melt fusion method. Synchronized release was achieved with high similarity factor f(2) values between each two of the five components. Erosion profiles of the matrix were in good correlation with release profiles of the five components, showing erosion-controlled release mechanisms. Through tuning some of the formulation variables, the system can be adjusted for synchronized and sustained release of silymarin for oral administration. In vitro hemolysis study indicated that the synchronized release samples showed a much better stabilizing effect on erythrocyte membrane.
Lu
Cheng
C
School of Pharmacy, Fudan University, Shanghai, PR China.
Lu
Yi
Y
Chen
Jian
J
Zhang
Wentong
W
Wu
Wei
W
D000818:Animals; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D044948:Flavonols / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry*; D006461:Hemolysis / Q000187:drug effects; D066298:In Vitro Techniques; D015394:Molecular Structure; D020442:Poloxamer / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D020011:Protective Agents / Q000737:chemistry* / Q000494:pharmacology; D011794:Quercetin / Q000031:analogs & derivatives / Q000737:chemistry; D011817:Rabbits; D000077385:Silybin; D012838:Silymarin / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D044948:Flavonols; D005989:Glycerides; D020011:Protective Agents; D012838:Silymarin; D020442:Poloxamer; C048159:glyceryl monostearate; D011092:Polyethylene Glycols; D000077385:Silybin; C075820:isosilybin; C015505:silidianin; D011794:Quercetin; C003377:taxifolin; C015504:silychristin