Bioavailability of self-microemulsifying pellets of daidai flavones in rats / 中国药学杂志

ABSTRACT

OBJECTIVE: To develop an HPLC method for simultaneously determining the contents of naringin and neohespiridin in rat plasma, and to investigate the pharmacokinetics and relative bioavailability of self-microemulsifying pellets of daidai flavones in rats. METHODS: The rats were divided into two groups randomly. They were administered orally suspension of daidai flavones effective parts and its self-microemulsifying pellets, which both contained 120 mg · kg-1 of flavonoids. Blood samples were collected at 0.083, 0.167, 0.333, 0.5, 0.667, 1, 2, 4, 6, 8, 10, 12 and 24 h and the concentrations of naringin and neohesperidin in rat plasma were simultaneously determined by HPLC. The pharmacokinetic parameters were calculated by DAS 3.0 pharmacokinetic program. RESULTS: The pharmacokintic parameters of naringin in the self-microemulsifying pellets of daidai flavones and the suspension were as follows AUC0-24 (17.710 ± 6.588) and( 9.139 ± 1.982) mg · h · L-1, ρmax (4.816 ± 1.329) and (1.572 ± 0.324) mg · L-1, tmax (0.611 ± 0.086) and (1.575 ± 0.324)h, and t1/2 (13.078 ± 6.382) and (11.678 ± 6.919)h, respectively. And the pharmacokintic parameters of neohesperidin were as follow AUC0-24 (18.094 ± 4.892) and (10.961 ± 2.276)mg · h · L-1, ρmax (5.657 ± 1.391) and (2.096 ± 0.512) mg · L-1, tmax(0.583 ± 0.091) and (0.806 ± 0.222) h, and t1/2 (14.606 ± 7.562) and (10.985 ± 6.963)h, respectively. The relative bioavailabilities of naringin and neohesperidin in the self-microemulsifying pellets of daidai flavones were 193.78% and 165.08%, respectively. CONCLUSION: The bioavailability of daidai flavones is increased by making them into self-microemulsifying pellets, and the biopharmaceutical property of the flavones is improved.