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Improvement of intestinal absorption of forsythoside A and chlorogenic acid by different carboxymethyl chitosan and chito-oligosaccharide, application to Flos Lonicerae-Fructus Forsythiae herb couple preparations.
PLoS One. 2013; 8(5):e63348.Plos

Abstract

The current study aims to investigate the effect of chitosan derivatives on the intestinal absorption and bioavailabilities of forsythoside A (FTA) and Chlorogenic acid (CHA), the major active components in Flos Lonicerae-Fructus Forsythiae herb couple. Biopharmaceutics and pharmacokinetics properties of the two compounds have been characterized in vitro, in situ as well as in rats. Based on the identified biopharmaceutics characteristics of the two compounds, the effect of chitosan derivatives as an absorption enhancer on the intestinal absorption and pharmacokinetics of FTA and CHA in pure compound form as well as extract form were investigated in vitro, in situ and in vivo. Both FTA and CHA demonstrated very limited intestinal permeabilities, leading to oral bioavailabilities being only 0.50% and 0.13% in rats, respectively. Results from both in vitro, in situ as well as in vivo studies consistently indicated that Chito-oligosaccharide (COS) at dosage of 25 mg/kg could enhance intestinal permeabilities significantly as well as the in vivo bioavailabilities of both FTA and CHA than CMCs in Flos Lonicerae-Fructus Forsythiae herb couple preparations, and was safe for gastrointestine from morphological observation. Besides, treatment with Flos Lonicerae-Fructus Forsythiae herb couple preparations with COS at the dosage of 25 mg/kg prevented MDCK damage after influenza virus propagation, which was significantly better than control. The current findings not only identified the usefulness of COS for the improved delivery of Flos Lonicerae-Fructus Forsythiae preparations but also demonstrated the importance of biopharmaceutical characterization in the dosage form development of traditional Chinese medicine.

Authors+Show Affiliations

College of Pharmacy, Nan'jing University of Chinese Medicine, Nan'jing, People's Republic of China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23675483

Citation

Zhou, Wei, et al. "Improvement of Intestinal Absorption of Forsythoside a and Chlorogenic Acid By Different Carboxymethyl Chitosan and Chito-oligosaccharide, Application to Flos Lonicerae-Fructus Forsythiae Herb Couple Preparations." PloS One, vol. 8, no. 5, 2013, pp. e63348.
Zhou W, Wang H, Zhu X, et al. Improvement of intestinal absorption of forsythoside A and chlorogenic acid by different carboxymethyl chitosan and chito-oligosaccharide, application to Flos Lonicerae-Fructus Forsythiae herb couple preparations. PLoS ONE. 2013;8(5):e63348.
Zhou, W., Wang, H., Zhu, X., Shan, J., Yin, A., Cai, B., & Di, L. (2013). Improvement of intestinal absorption of forsythoside A and chlorogenic acid by different carboxymethyl chitosan and chito-oligosaccharide, application to Flos Lonicerae-Fructus Forsythiae herb couple preparations. PloS One, 8(5), e63348. https://doi.org/10.1371/journal.pone.0063348
Zhou W, et al. Improvement of Intestinal Absorption of Forsythoside a and Chlorogenic Acid By Different Carboxymethyl Chitosan and Chito-oligosaccharide, Application to Flos Lonicerae-Fructus Forsythiae Herb Couple Preparations. PLoS ONE. 2013;8(5):e63348. PubMed PMID: 23675483.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improvement of intestinal absorption of forsythoside A and chlorogenic acid by different carboxymethyl chitosan and chito-oligosaccharide, application to Flos Lonicerae-Fructus Forsythiae herb couple preparations. AU - Zhou,Wei, AU - Wang,Haidan, AU - Zhu,Xuanxuan, AU - Shan,Jinjun, AU - Yin,Ailing, AU - Cai,Baochang, AU - Di,Liuqing, Y1 - 2013/05/13/ PY - 2013/01/16/received PY - 2013/03/31/accepted PY - 2013/5/16/entrez PY - 2013/5/16/pubmed PY - 2013/12/16/medline SP - e63348 EP - e63348 JF - PloS one JO - PLoS ONE VL - 8 IS - 5 N2 - The current study aims to investigate the effect of chitosan derivatives on the intestinal absorption and bioavailabilities of forsythoside A (FTA) and Chlorogenic acid (CHA), the major active components in Flos Lonicerae-Fructus Forsythiae herb couple. Biopharmaceutics and pharmacokinetics properties of the two compounds have been characterized in vitro, in situ as well as in rats. Based on the identified biopharmaceutics characteristics of the two compounds, the effect of chitosan derivatives as an absorption enhancer on the intestinal absorption and pharmacokinetics of FTA and CHA in pure compound form as well as extract form were investigated in vitro, in situ and in vivo. Both FTA and CHA demonstrated very limited intestinal permeabilities, leading to oral bioavailabilities being only 0.50% and 0.13% in rats, respectively. Results from both in vitro, in situ as well as in vivo studies consistently indicated that Chito-oligosaccharide (COS) at dosage of 25 mg/kg could enhance intestinal permeabilities significantly as well as the in vivo bioavailabilities of both FTA and CHA than CMCs in Flos Lonicerae-Fructus Forsythiae herb couple preparations, and was safe for gastrointestine from morphological observation. Besides, treatment with Flos Lonicerae-Fructus Forsythiae herb couple preparations with COS at the dosage of 25 mg/kg prevented MDCK damage after influenza virus propagation, which was significantly better than control. The current findings not only identified the usefulness of COS for the improved delivery of Flos Lonicerae-Fructus Forsythiae preparations but also demonstrated the importance of biopharmaceutical characterization in the dosage form development of traditional Chinese medicine. SN - 1932-6203 UR - https://www.unboundmedicine.com/medline/citation/23675483/Improvement_of_intestinal_absorption_of_forsythoside_A_and_chlorogenic_acid_by_different_carboxymethyl_chitosan_and_chito_oligosaccharide_application_to_Flos_Lonicerae_Fructus_Forsythiae_herb_couple_preparations_ L2 - http://dx.plos.org/10.1371/journal.pone.0063348 DB - PRIME DP - Unbound Medicine ER -