The present study aimed to determine the pharmacokinetic parameters and bioavailability of silymarin 140 mg SMEDDS formulation. An open-label, single-dose pharmacokinetic study was conducted. Twelve healthy volunteers were included in the study. After the volunteers had fasted overnight for 10 h, a single-dose generic silymarin 140 mg SMEDDS soft capsule was administered. Then 10 ml blood samples were taken at 0.0, 0.25, 0.50, 0.75, 1.0, 1.33, 1.67, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, 10.0, and 12.0 h. The plasma silybin concentrations were analyzed using validated LC-MS/MS. The pharmacokinetic parameters were analyzed and calculated. The pharmacokinetic parameters were calculated after silymarin had been administered as a single capsule. The mean (range) Cmax was 812.43 (259.47–1505.47) ng/ml at 0.80 (0.25–1.67) h (tmax). The mean (range) AUC0-t and AUC0-inf were 658.80 (268.29–1045.01) ng.h/ml and 676.98 (274.10–1050.96) ng.h/ml, respectively. The mean ke and t1/2 were 0.5386 h−1 and 1.91 h, respectively. The silymarin SMEDDS formulation soft capsule showed rapid absorption and high oral bioavailability.
Echinacea purpurea contains many beneficial constituents for protection of skin from oxidative stress and for improving hydration of skin. This study aimed to investigate the stability and dermatological efficacy of E. purpurea cream and gel. Echinacea purpurea extract was incorporated into suitable cream and gel bases. Stability of the extract in the formulations was investigated by determining its residual total phenolic content and antioxidant activity after storage at 4°C, 30°C and 40°C for 6 months. The effect of those formulations on skin irritation, hydration level and wrinkle reduction was evaluated in 10 healthy volunteers, aged 25-40 years. The shelf lives of E. purpurea cream and gel in terms of total phenolic content and antioxidant activity were only 2 and 4 months respectively at 4°C and could be extended up to 7 months by incorporation of α-tocopherol or disodium editate. The corneometer hydration indices increased up to 10.6 AU and 11.4 AU, and the wrinkles decreased 9.47% and 14.92% because of the application of E. purpurea cream and gel for 1 month. Both formulations showed no irritation to skin. Echinacea purpurea cream and gel developed in this study were effective in improving skin hydration and reducing wrinkle, but showed low storage stability.
The effects of variety and modification of rice on its antioxidant and anti-inflammatory activities were investigated. White rice varieties; Jasmine (JM) and Saohai (SH), and pigmented rice varieties; Doisket (DS) and Homnil (HN) were used. The modified rice samples were obtained from chemical modification using etherification reaction. The activities of the modified rice samples were compared with the ethanol extracts of the raw rice at the same rice concentration. Antioxidant activity was measured by the free radical scavenging activity tests and ferric reducing power assay. Results indicated that the ethanol extracts of raw rice had higher antioxidant activity than the modified rice. Among the raw rice tested, the pigmented rice showed higher antioxidant activity than white rice. Trolox equivalent antioxidant capacity values from free radical scavenging activity test were revealed that 50% ethanol extracts of HN and DS possessed the highest antioxidant activity. Ferric reducing power assay showed that 50% ethanol extracts of DS had the highest antioxidant activity. The anti-inflammatory activity was evaluated in vitro using a lipopolysaccharide-stimulated RAW264.7 macrophage cell model with enzyme-linked immunosorbent assay. Absolute ethanol extracts of HN reduced interleukin-6 secretion whereas that of DS suppressed interleukin-6 and tumor necrosis factor -α secretion. These results indicate that variety of rice, chemical modification, and extracting solvent were the factors that play an important role on antioxidant and anti-inflammatory activity. This study supports the potential use of the pigmented rice, especially DS, as a promising choice of a natural source because of its antioxidant and anti-inflammatory activities.
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