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      In vivo pharmacokinetic comparisons of ferulic acid and puerarin after oral administration of monomer, medicinal substance aqueous extract and Nao-De-Sheng to rats

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          Abstract

          Background:

          Nao-De-Sheng decoction (NDS), a traditional Chinese medicine (TCM) prescription containing Radix puerariae lobatae, Floscarthami, Radix et Rhizoma Notoginseng, Rhizoma chuanxiong and Fructus crataegi, is effective in the treatment of cerebral arteriosclerosis, ischemic cerebral stroke and apoplexy linger effect. Ferulic acid and puerarin are the main absorbed effective ingredients of NDS.

          Objective:

          To assess the affection of other components in medical material and compound recipe compatibility on the pharmacokinetics of ferulaic acid and puerarin, of ferulic acid from the monomer Rhizoma chuanxiong aqueous extract and NDS were studied. And pharmacokinetics comparisons of puerarin from the monomer Radix puerariae extract and NDS decoction were investigated simultaneously.

          Materials and Methods:

          At respective different time points after oral administration of the monomer, medicinal substance aqueous extract and NDS at the same dose in rats, plasma concentrations of ferulic acid and puerarin in rats were determined by RP-HPLC, and the main pharmacokinetic parameters were estimated with 3P97 software.

          Results:

          The plasma concentration-time curves of ferulaic acid and puerarin were both best fitted with a two-compartment model. AUC 0− t , AUC 0→ ∞, T max, and C max of ferulic acid in the monomer and NDS decoction were increased significantly ( P < 0.05) compared with that in Rhizoma chuanxiong aqueous extract. And statistically significant increase ( P < 0.05) in pharmacokinetic parameters of puerarin including AUC 0− t , AUC 0→ ∞, CL, T max and C max were obtained after oral administration of puerarin monomer compared with Radix puerariae extract. Although the changes of AUC 0− t , AUC 0→ ∞ and CL had no statistically significant, C max of puerarin in NDS was increased remarkably ( P < 0.05) compared with that in single puerarin.

          Conclusions:

          Some ingredients of Rhizoma chuanxiong and Radix puerariae may be suggested to remarkably influence plasma concentrations of ferulaic acid and puerarin. Some ingredients in NDS may increase dissolution and absorption of ferulaic acid and puerarin, delay elimination, and subsequently enhance bioavailability of ferulaic acid and puerarin in rats after compatibility.

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          Antihyperglycemic effect of puerarin in streptozotocin-induced diabetic rats.

          Juei-Tang Cheng, Chiu-Huang Kuo, Po-Chuan Chen … (2003)
          The antihyperglycemic action of puerarin, purified from the roots of Pueraria lobata, was investigated in streptozotocin-induced diabetic rats (STZ-diabetic rats). Bolus intravenous injection of puerarin decreased the plasma glucose concentrations in a dose-dependent manner in STZ-diabetic rats. Similar treatment with puerarin also decreased the plasma glucose in normal rats, although the effect was not as great as that in STZ-diabetic rats. Puerarin at the effective dose (15.0 mg/kg) significantly attenuated the increase of plasma glucose induced by an intravenous glucose challenge test in normal rats. In the isolated soleus muscle of STZ-diabetic rats, puerarin enhanced the uptake of radioactive glucose in a concentration-dependent manner. Moreover, the mRNA and protein levels of the subtype 4 form of glucose transporter (GLUT4) in soleus muscle were increased after repeated intravenous administration of puerarin in STZ-diabetic rats for 3 days. These results suggest that puerarin can increase the glucose utilization to lower plasma glucose in diabetic rats lacking insulin.
          Article 0 comments Cited 36 times – based on 0 reviews     Review now
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            Pharmacokinetics and bioavailability of herbal medicinal products.

            M Veit, Hartmut Derendorf, Claudia Kohlert … (2001)
            The use of herbs for treating various ailments dates back several centuries. Usually, herbal medicine has relied on tradition that may or may not be supported by empirical data. The belief that natural medicines are much safer than synthetic drugs has gained popularity in recent years and led to tremendous growth of phytopharmaceutical usage. Market driven information on natural products is widespread and has further fostered their use in daily life. In most countries there is no universal regulatory system that insures the safety and activity of phytopharmaceuticals. Evidence-based verification of the efficacy of HMPs (herbal medicinal products, botanicals) is still frequently lacking. However, in recent years, data on evaluation of the therapeutic and toxic activity of herbal medicinal products became available. The advances in analytical technology have led to discovery of many new active constituents and an ever-increasing list of putatively active constituents. Establishing the pharmacological basis for efficacy of HMPs is a constant challenge. Of particular interest is the question of bioavailability to assess to what degree and how fast compounds are absorbed after administration of HMPs. Of further interest is the elucidation of metabolic pathways (yielding potentially new active compounds), and the assessment of elimination routes and their kinetics. These data become an important issue to link data from pharmacological assays and clinical effects. Of interest are currently also interactions of herbal medicinal products with synthetically derived drug products. A better understanding of the pharmacokinetics and bioavailability of phytopharmaceuticals can also help in designing rational dosage regimens. In this review, pharmacokinetic and bioavailability studies that have been conducted for some of the more important or widely used phytopharmaceuticals are critically evaluated. Furthermore, various drug interactions are discussed which show that caution should be exercised when combining phytopharmaceuticals with chemically derived active pharmaceutical ingredients.
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              LC-MS determination and pharmacokinetic studies of ursolic acid in rat plasma after administration of the traditional chinese medicinal preparation Lu-Ying extract.

              Kaishun Bi, Qiutao Gao, Ying-Jia Tong … (2005)
              Sambucus chinensis L. is a native perennial herb distributed throughout China. In traditional Chinese medicine (TCM), this herb is known as Lu-Ying. Ursolic acid is the major effective constituent of Lu-Ying. A rapid, sensitive, and accurate liquid chromatography-mass spectrometry (LC-MS) method for the determination of ursolic acid in rat plasma was developed and validated. Plasma samples taken from rats that had received Lu-Ying extract orally were acidified with acetic acid and then extracted with a mixture of hexane-dichloromethane-2-propanol (20:10:1, v/v/v). Separation of ursolic acid was accomplished on a C(18) column interfaced with a single quadrupole mass spectrometer. The mobile phase consisting of methanol and water (95:5, v/v) was delivered at a flow rate of 1.0 ml/min. Atmospheric pressure chemical ionization was operated in negative-ion mode. Using selected ion-monitoring mode, the deprotonated molecules [M-H](-) at m/z 455 and 469 were used to quantify ursolic acid and glycyrrhetic acid (internal standard), respectively. The assay was shown to be linear over the range of 10-1000 ng/ml (r> or =0.9960) with a lower limit of quantification of 10 ng/ml. The method was shown to be reproducible and reliable with intraday precision below 7.8%, interday precision below 8.1%, accuracy within +/-4.3%, and mean extraction recovery excess of 83.6%, which were all calculated from the blank plasma sample spiked with ursolic acid at three concentrations of 20, 200, and 800 ng/ml. The LC-MS method has been successfully applied to pharmacokinetic studies of ursolic acid after oral administration of Lu-Ying ethanolic extract (at a dose containing 80.32 mg/kg ursolic acid) to rats. The main pharmacokinetic parameters were: t(1/2), 4.3 h; K(e), 0.16 1/h; t(max), 1.0 h; C(max), 294.8 ng/ml; AUC(0-t) and AUC(0-infinity), 1007.1 ng.h/ml and 1175.3 ng.h/ml, respectively.
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                Author and article information

                Journal
                Journal ID (nlm-ta): Pharmacogn Mag
                Journal ID (iso-abbrev): Pharmacogn Mag
                Journal ID (publisher-id): PM
                Title: Pharmacognosy Magazine
                Publisher: Medknow Publications & Media Pvt Ltd (India )
                ISSN (Print): 0973-1296
                ISSN (Electronic): 0976-4062
                Publication date (Print): Oct-Dec 2012
                Volume: 8
                Issue: 32
                Pages: 256-262
                Affiliations
                [1] School of Pharmacy, Pharmacognosy Jiangsu University, Zhenjiang, 212013, PR China
                Author notes
                Address for correspondence: Prof. Zhen Ouyang, School of Pharmacy, Jiangsu University, Zhenjiang 212013, PR China. E-mail: zhenouyang@ 123456ujs.edu.cn
                Article
                Publisher ID: PM-8-256
                DOI: 10.4103/0973-1296.103648
                PMC ID: 3785161
                PubMed ID: 24082627
                SO-VID: c96c4ed8-9c95-4263-be06-4b42fc9c3e62
                Copyright © Copyright: © Pharmacognosy Magazine
                License:

                This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                Date received : 17 December 2011
                Date revision received : 26 June 2012
                Date accepted : 22 November 2012
                Categories
                Subject: Original Article

                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine
                Keywords: medicinal substance aqueous extract,nao-de-sheng,puerarin,pharmacokinetics comparisons,ferulic acid
                Data availability:
                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine
                Keywords: medicinal substance aqueous extract, nao-de-sheng, puerarin, pharmacokinetics comparisons, ferulic acid

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