ABSTRACT
The active ingredient of Ge Tong Tong Luo Capsule is the total flavonoids of Pueraria lobata, which mainly consists of puerarin, daidzein, daidzein-4V and other components. In the treatment of cerebral infarction, Ge Tong Tong Luo Capsule and its main pharmacological components have shown to inhibit the progression of atherosclerotic plaque, scavenge oxygen free radicals, anti-platelet aggregation, and inhibit neuronal apoptosis. In terms of adverse events, most of the studies were obvious adverse reactions caused by drugs. In rare studies, although there were adverse events such as palpitation and dry throat, they were relieved without treatment. This article introduces the pharmacological effects, clinical efficacy and adverse reactions of Ge Tong Tong Luo Capsule and its main pharmacological components, and provides a reference for clinical safe and rational drug use.
ABSTRACT
To study the bioavailability of pueraria flavonoids bio-adhesive and floating pellets, the absorption of puerarin was studied using Caco-2 cell monolayer by liquid chromatography (HPLC) method, comparing the Papp of pueraria flavonoids bio-adhesive and floating pellets with different bio-adhesive materials. Drugs were administered at a dose of 100 mg·kg-1 via ig. The plasma concentration of puerarin was determined by HPLC, the pharmacokinetics were calculated with the WinNonlin 6.0 software. The results showed that the Papp of bio-adhesive and floating pellets with hydroxypropyl methylcellulose (HPMC)-cabomer was largest, which had a significant difference (P0-t of pueraria flavonoids bio-adhesive and floating pellets was 1.79 times of pueraria flavonoids, the Cmax of pueraria flavonoids bio-adhesive and floating pellets and pueraria flavonoids had a significant difference (P<0.05). What's more the MRT had prolonged. In conclusion, pueraria flavonoids bio-adhesive and floating pellets with HPMC-cabomer could significantly facilitate the transport of puerarin on Caco-2 cellular monolayers. The bioavailability of pueraria flavonoids bio-adhesive and floating pellets with HPMC-cabomer was increased more than pueraria flavonoids with a sustained release effect.
ABSTRACT
Objective: To prepare the lyophilized powder of Pueraria flavonoids loaded solid lipid nanoparticles (PF-SLN) and determine the dissolution rate of its four effective components: 3'-hydroxypuerarin, puerarin, daidzin, and daidzein. Methods: PF-SLN was prepared by the high pressure homogenization (HPH) technology. The lyophilized formula contained mannitol as cryoprotectant. The release rates of the four effective components from the PF-SLN lyophilized powder as well as the physical mixture were determined, with artificial gastric juice (pH 1.2) as dissolvent. Results: The technical parameters of PF-SLN preparation optimized by orthogonal test were as follows: The ratio and the dosage of lipid-surfactant were 2:1 and 2.0%, PF dosage was 2.5%, and 150 MPa homogeneity was 15 cycles. The optimal PF-SLN lyophilized powder was loosen with the particle size of (517.1 ± 10.3) nm, polydisperse index of 0.484 ± 0.210, and Zeta potential of (-21.91 ± 2.03) mV, respectively. The in vitro accumulated dissolution rates of PF-SLN lyophilized powder were slower than those of the physical mixture. Conclusion: The method employed to prepare PF-SLN lyophilized powder is feasible. PF-SLN lyophilized powder could delay the in vitro dissolution rate notablely. It might be a novel vehicle potentially for nano-drug delivery system of Pueraria flavonoids.
ABSTRACT
Objective: To prepare the lyophilized powder of Pueraria flavonoids nanosuspension (PF-NS) and to determine the dissolution rates of its four effective components (3'-hydroxypuerarin, puerarin, daidzin, and daidzein). Methods: PF-NS was prepared by the high pressure homogenization (HPH) technology. The lyophilized formula contained mannitol as lyoprotectant. The dissolution rates of the four effective components from lyophilized powder of PF-NS as well as the physical mixture were determined, with artificial gastric juice (pH 1.2) as dissolvent. Results: The optimal lyophilized powder of PF-NS was loosed with the particle size of (479.7 ± 14.7) nm, polydisperse index of 0.524 ± 0.220, and Zeta potential of (29.68 ± 3.97) mV, respectively. The in vitro accumulated dissolution rate of lyophilized powder of PF-NS was higher than that of the physical mixture. Conclusion: The method employed to prepare the lyophilized powder in PF-NS is simple and feasible. The lyophilized powder of PF-NS could improve the in vitro dissolution rate notablely. It might be a novel vehicle potentially for nano-drug delivery system of PF.