ABSTRACT
Objective: Based on the advantages of representation of herb components group clustering by characteristic spectrum integrity, to study the in vitro dissolution behavior of Daidai Flavones Dropping Pills (DFDP), and to evaluate the synchronization release situation of group clustering. Methods: Rotating basket method and HPLC characteristic spectrum were employed to evaluate the group clustering dissolution and the release characteristics of DFDP in different dissolution media (pH 1.2 hydrochloric acid solution, pH 4.5 acetic acid-sodium acetate buffer, pH 6.8 phosphate buffer, and distilled water). The single exponential, logarithmic distribution and Weibull equation model were applied to fit the dissolution curves. Results: The similarity factor (f2) of the dissolution curves of nine common peak components in characteristic spectrum of DFDP was over 50; In addition the f2 of neohesperidin and naringin was 94.86, which indicated that the group clustering of DFDP had similar dissolution curves and synchronization release characteristics. Meanwhile the dissolution mechanism of group clustering of nine common peak activity composition was following the Weibull equation model. Conclusion: The established method is simple, rapid, and stable, which provides an experimental basic for in vitro analysis and quality evaluation of DFDP.
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.