Effects of Berberine and Hwangryunhaedok-Tang on Oral Bioavailability and Pharmacokinetics of Ciprofloxacin in Rats

Abstract

Hwangryunhaedok-Tang (HR) and berberine-containing single herbs are used to treat bacterial infection and inflammatory diseases in eastern Asia. The combination of berberine-containing herbal medicines and ciprofloxacin can be an excellent antibacterial chemotherapy against multidrug resistance bacteria. To evaluate the pretreatment effect of berberine and HR, vehicle, berberine (25 and 50 mg/kg/day), and HR (1.4 g/kg/day) were daily administered to rats for five consecutive days. On day 6, ciprofloxacin was administered (10 mg/kg, i.v. and 20 mg/kg, p.o.) to rats. To assess cotreatment effect of berberine and ciprofloxacin, berberine (50 mg/kg) and ciprofloxacin (20 mg/kg) were coadministered by single oral gavage. Pharmacokinetic data were estimated by noncompartmental model. Compared with ciprofloxacin alone (control group), coadministration of berberine (50 mg/kg) and ciprofloxacin significantly decreased C max of ciprofloxacin (P < 0.05). In addition, the pretreatment of berberine (50 mg/kg/day) and HR (1.4 g/kg/day) significantly decreased C max and AUC0→∞, compared with control group (P < 0.05). The oral bioavailability of ciprofloxacin was reduced by cotreatment of berberine and pretreatment of berberine and HR. Our results suggest that the expression of P-glycoprotein and organic anion and/or organic cation transporters (OAT/OCT) could take a role in reduced oral bioavailability of ciprofloxacin by berberine and HR.

Development and Evaluation of EDTA-Treated Rabbits for Bioavailability Study of Chelating Drugs Using Levofloxacin, Ciprofloxacin, Hemiacetal Ester Prodrugs, and Tetracycline

“…In rats, the reported absolute oral bioavailability of CFX was 69.9% at a dose of 20 mg/kg [ 85 ]. In contrast, another group reported that the oral bioavailability of CFX was 19.87% when administered at a dose of 20 mg/kg in rats [ 88 ]. This reported value (19.87% in rats) is the same as the present results obtained in EDTA-treated rabbits (19.37 ± 2.28%) as shown in Table 9 .…”

Effects of Thylakoid-Rich Spinach Extract on the Pharmacokinetics of Drugs in Rats

“…Generally, it is well-known that spinach is rich in minerals, such as Ca, Mg, Fe and Al. 32) For preparation of thylakoid-rich spinach extract, Appethyl ® , reagents containing these metals are not used. 12) Thus, we speculate that these metals in the thylakoid-rich spinach extract are derived from spinach itself.…”

Comparison of the Ingredient Quantities, and Antioxidant and Anti-inflammatory Activities of &lt;i&gt;Hwangryunhaedok&lt;/i&gt; Decoction Pharmacopuncture by Preparation Type

“…As a result, mixed extraction with decoction and distillation of HRHD-D was shown to demonstrate higher anti-inflammatory activity then distillation only. A major ingredient of Copris japonica, berberine, and a main ingredient of Phellodendron amurense, palmatine, are alkaloids whose anti-inflammatory properties of cortex phellodendri amurensis in vitro and in vivo may explain its utility for attenuating inflammationrelated diseases and effectively inhibiting bacteria, fungi and viruses 18,19) . Additionally, it was reported by Peng et al 20) that Gardenia jasminoides(Schisandra chinensis) showed strong inhibitory effects on NO production when evaluated for its effect using macrophages.…”