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Physicochemical characteristics and bioavailability of a novel intestinal metabolite of ginseng saponin (IH901) complexed with beta-cyclodextrin.
Int J Pharm. 2006 Jun 19; 316(1-2):29-36.IJ

Abstract

In an effort to improve the bioavailability (BA) of the insoluble compound 20-O-(beta-d-glucopyranosyl)-20(S)-protopanaxadiol (IH901), we prepared beta-cyclodextrin (betaCD) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) inclusion complexes containing IH901. IH901 is a major metabolite formed by intestinal bacteria from protopanaxadiol ginseng saponins. We developed and validated an HPLC-based method to measure IH901 levels from samples prepared in vitro. The phase solubility profiles with both cyclodextrins (CDs) were classified as AL-type, indicating the formation of a 1:1 stoichiometric inclusion complex. Stability constants (Ks) calculated from the phase solubility diagrams showed that the betaCD complex was more stable than the HPbetaCD complex. Consequently, complexes of IH901 and betaCD were prepared by a freeze-drying method and were analyzed by fourier transformation-infrared spectroscopy (FT-IR), X-ray diffraction, differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). From these physicochemical characterizations, we confirmed the presence of a new solid phase in the freeze-dried samples. The IH901 released from the complex in a pH 1.2 solution, the pH range of gastric fluids, was considerably lower than the amount released in the other solutions. The IH901 released from the complex in pH 6.8 solution, the range of intestinal fluids, was 9.0-fold greater than pure IH901 powder. However, the amount of IH901 released from the complex in pH 4.0-8.0 was less than 20%. After oral administration of the IH901-betaCD inclusion complex (30 mg/kg IH901) into rats, plasma concentrations were determined by LC/MS/MS. The peak concentration (Cmax) for the inclusion complex was 2.8-fold higher than that for pure IH901 powder. The BA, calculated from the ratio of the AUCoral to the AUCi.v., for the pure IH901 powder, the IH901-betaCD physical mixture, and the inclusion complex was 3.52, 4.34, and 6.57%, respectively. These results indicate that the BA for the inclusion complex was 1.9-fold higher than that for the pure IH901 powder.

Authors+Show Affiliations

National Research Laboratory (NRL) of PK/PD, Biotechnology Research Institute, College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, South Korea.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

16574357

Citation

Lee, Pung Sok, et al. "Physicochemical Characteristics and Bioavailability of a Novel Intestinal Metabolite of Ginseng Saponin (IH901) Complexed With Beta-cyclodextrin." International Journal of Pharmaceutics, vol. 316, no. 1-2, 2006, pp. 29-36.
Lee PS, Han JY, Song TW, et al. Physicochemical characteristics and bioavailability of a novel intestinal metabolite of ginseng saponin (IH901) complexed with beta-cyclodextrin. Int J Pharm. 2006;316(1-2):29-36.
Lee, P. S., Han, J. Y., Song, T. W., Sung, J. H., Kwon, O. S., Song, S., & Chung, Y. B. (2006). Physicochemical characteristics and bioavailability of a novel intestinal metabolite of ginseng saponin (IH901) complexed with beta-cyclodextrin. International Journal of Pharmaceutics, 316(1-2), 29-36.
Lee PS, et al. Physicochemical Characteristics and Bioavailability of a Novel Intestinal Metabolite of Ginseng Saponin (IH901) Complexed With Beta-cyclodextrin. Int J Pharm. 2006 Jun 19;316(1-2):29-36. PubMed PMID: 16574357.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physicochemical characteristics and bioavailability of a novel intestinal metabolite of ginseng saponin (IH901) complexed with beta-cyclodextrin. AU - Lee,Pung Sok, AU - Han,Jin-Yi, AU - Song,Tae Won, AU - Sung,Jong Hwan, AU - Kwon,Oh-Seung, AU - Song,Sukgil, AU - Chung,Youn Bok, Y1 - 2006/03/29/ PY - 2005/08/15/received PY - 2006/01/23/revised PY - 2006/02/15/accepted PY - 2006/4/1/pubmed PY - 2006/11/7/medline PY - 2006/4/1/entrez SP - 29 EP - 36 JF - International journal of pharmaceutics JO - Int J Pharm VL - 316 IS - 1-2 N2 - In an effort to improve the bioavailability (BA) of the insoluble compound 20-O-(beta-d-glucopyranosyl)-20(S)-protopanaxadiol (IH901), we prepared beta-cyclodextrin (betaCD) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) inclusion complexes containing IH901. IH901 is a major metabolite formed by intestinal bacteria from protopanaxadiol ginseng saponins. We developed and validated an HPLC-based method to measure IH901 levels from samples prepared in vitro. The phase solubility profiles with both cyclodextrins (CDs) were classified as AL-type, indicating the formation of a 1:1 stoichiometric inclusion complex. Stability constants (Ks) calculated from the phase solubility diagrams showed that the betaCD complex was more stable than the HPbetaCD complex. Consequently, complexes of IH901 and betaCD were prepared by a freeze-drying method and were analyzed by fourier transformation-infrared spectroscopy (FT-IR), X-ray diffraction, differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). From these physicochemical characterizations, we confirmed the presence of a new solid phase in the freeze-dried samples. The IH901 released from the complex in a pH 1.2 solution, the pH range of gastric fluids, was considerably lower than the amount released in the other solutions. The IH901 released from the complex in pH 6.8 solution, the range of intestinal fluids, was 9.0-fold greater than pure IH901 powder. However, the amount of IH901 released from the complex in pH 4.0-8.0 was less than 20%. After oral administration of the IH901-betaCD inclusion complex (30 mg/kg IH901) into rats, plasma concentrations were determined by LC/MS/MS. The peak concentration (Cmax) for the inclusion complex was 2.8-fold higher than that for pure IH901 powder. The BA, calculated from the ratio of the AUCoral to the AUCi.v., for the pure IH901 powder, the IH901-betaCD physical mixture, and the inclusion complex was 3.52, 4.34, and 6.57%, respectively. These results indicate that the BA for the inclusion complex was 1.9-fold higher than that for the pure IH901 powder. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/16574357/Physicochemical_characteristics_and_bioavailability_of_a_novel_intestinal_metabolite_of_ginseng_saponin__IH901__complexed_with_beta_cyclodextrin_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(06)00178-5 DB - PRIME DP - Unbound Medicine ER -