ABSTRACT
Shuxiong prescription (Notoginseng Radix et Rhizoma, Chuanxiong Rhizome and Carthami Flos) has the function of activating blood circulation to dissipate blood stasis, activating meridians to stop pain. This paper was mainly aimed to discuss the transport characteristics of Shuxiong prescription across Caco-2 cell monolayer. Safe concentration range of Shuxiong prescription against Caco-2 cell monolayer model was determined by MTT assay. The mechanism of Shuxiong prescription bidirectional transport was investigated by Caco-2 cell monolayer model. The apparent permeability coefficient Papp of digoxin was determined by high performance liquid chromatography (HPLC). The test results showed that the Papp of extract from Notoginseng Radix et Rhizoma, Chuanxiong Rhizome, Carthami Flos, Chuanxiong Rhizome+Carthami Flos and Shuxiong prescription transport from apical (AP) side to basolateral (BL) side was (3.12±0.73)×10⁻⁶, (2.58±0.41)×10⁻⁶, (4.97±0.64)×10⁻⁶, (4.63±0.57)×10⁻⁶, (5.79±0.68)×10⁻⁶ cm·s⁻¹, respectively, indicating that the transport of digoxin across Caco-2 cell monolayer model was active absorption, and the P-gp protein took part in the process. Chuanxiong Rhizome could significantly decrease the transport of digoxin from BL→AP(<0.01) and increase its transport from AP→BL(<0.05) significantiy. After the addition of Shuxiong prescription, the transport of digoxin from BL→AP was significantly inhibited(<0.01). The results suggested that the extract of safflower had no effect on P-gp transport, nor on the independence diffusion of digoxin. The transport of digoxin could be degraded by the extract of Chuanxiong Rhizome and the extract of Shuxiong prescription from BL→AP(<0.01), significantly; pseudo-ginseng had no effect on the independence diffusion of digoxin; the extract of safflower+Chuanxiong Rhizome had the same experimental result as Chuanxiong Rhizome extract.
Subject(s)
Humans , Biological Transport , Caco-2 Cells , Chromatography, High Pressure Liquid , Digoxin , Pharmacokinetics , Drugs, Chinese Herbal , PharmacokineticsABSTRACT
Objective: To study the in vivo pharmacokinetic law and difference of active compounds from Chuanxiong Rhizoma and Corydalis Rhizoma between control and model rats. Methods: Sixteen Sprague-Dawley rats were randomly divided into two groups: control and model rats with endometriosis, eight rats in each group. All the rats were ig administrated of tetramethylpyrazine (50 mg/kg), ferulic acid (30 mg/kg), and tetrahydropalmatine (20 mg/kg). All the concentration of tetramethylpyrazine, ferulic acid, and tetrahydropalmatine in plasma was analyzed by RP-HPLC and the data were treated by DAS 2.0 program. Results: The main pharmacokinetic parameters of tetramethylpyrazine in the model group, such as AUC0~t, Cmax, tmax, t1/2, and MRT0~t, were no significant difference compared with the control group (P > 0.05), and AUC0~t, Cmax, and tmax of ferulic acid in model group were less than those in the control group with no significant difference (P > 0.05); t1/2 and MRT0~t of ferulic acid in the model group were obviously less than those in control group (P0~t, Cmax, tmax, and MRT0~t of tetrahydropalmatine in the model group were bigger than those in the control group with significant difference (P < 0.05). Conclusion: There is difference of pharmacokinetics of the main active compounds from Chuanxiong Rhizoma and Corydalis Rhizoma between model and control rats. Ferulic acid is removed more quickly in model rats, tetrahydropalmatine is absorbed highly but removed slower, tetramethylpyrazine is no significant difference comparee with the control group.
ABSTRACT
Objective: To establish a RP-HPLC method for the determination of ligustrazine hydrochloride, ferulic acid, hydrosafflower yellow A, ginsenoside Rg1, ginsenoside Rb1, ginsenoside Re, and notoginsenoside R1 in Shuxiong prescription. Methods: The Inertsil ODS-SP (250 mm × 4.6 mm, 5 μm) was used. The mobile phase, consisting of acetonitrile-0.05% phosphoric acid solution, was programmed for a gradient elution. The flow rate was 1.0 mL/min, the detection wavelength was 203 nm, and the column temperature was 30℃. Results: The excellent linearity with correlation coefficients (r) of 0.999 3-0.999 9 was obtained. The average recoveries of the seven compounds were 97.25%-103.52% and all RSD values were less than 3%. Conclusion: The method appears to be simple, accurate, and well reproducible, which could be used for the simultaneous determination of the above-mentioned seven compounds in Shuxiong prescription.
ABSTRACT
Objective: To investigate the effects of tetramethylpyrazine (TMP) and ferulic acid (FA) on pharmacokinetics of tetrahydropalmatine (THP) in rats. Methods: Thirty-two Sprague-Dawley rats were randomly divided into four groups such as THP 20 mg∙kg-1, THP 20 mg∙kg-1 + FA 50 mg∙kg-1, THP 20 mg∙kg-1 + TMP 30 mg∙kg-1, and THP 20 mg∙kg-1 + FA50 mg∙kg-1 + TMP 30 mg∙kg-1 groups. All the rats were ig administered and then blood samples were obtained from fossa orbitalis at several time points. All the plasma concentration was analyzed by RP-HPLC method and the data were treated by DAS 2.0 program. Results: Compared with THP alone, THP combined with TMP or FA could increase the AUC0~t, tmax, and Cmax, and prolong the t1/2 and MRT0~t (P < 0.05). Compared with THP alone, THP combined with TMP and FA could increase the AUC0~t, MRT0~t, t1/2, and tmax, but had no influence on the Cmax. Conclusion: FA and TMP can prolong the action time of THP in rats, and increase of THP absorption in rats in vivo.