Skip to main content
Log in

Preparation and In Vitro Evaluation of Solid Dispersions of Total Flavones of Hippophae rhamnoides L.

  • Research Article
  • Published:
AAPS PharmSciTech Aims and scope Submit manuscript

Abstract

The purpose of this study was to enhance the dissolution of total flavones of Hippophae rhamnoides L. (TFH) by solid dispersions consisting of the drug and a polymeric carrier, poloxamer 188 (PXM). The solvent evaporation method was used to prepare solid dispersions. A 32 full-factorial design approach was used for optimization wherein the amount of solvent (X 1) and the drug-to-polymer ratio (X 2) were selected as independent variables and the percentage of TFH dissolved in 10 min (Q 10) was selected as the dependent variable. Multiple linear regression analysis revealed that a suitable level of X 1 and X 2 was required for obtaining higher dissolution of TFH from PXM solid dispersions. Solid dispersions were characterized by differential scanning calorimetry, X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy, and dissolution tests. Characterization studies revealed that solid dispersion of TFH–PXM showed enhancement of TFH dissolution due to the conversion of TFH into a less crystalline and/or amorphous form. In conclusion, dissolution enhancement of TFH was obtained by preparing its solid dispersions in PXM using solvent method.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5

Similar content being viewed by others

References

  1. Lachman J, Pivec V, Hubacek J, Rehakova V. Flavonoid substances in the fruit s of sea buckthorn (Hippophae rhamnoides). Sci Agric Bohem 1985;3:169–82.

    Google Scholar 

  2. Chen C, Zhang H, Xiao W, Yong ZP, Bai N. High-performance liquid chromatographic fingerprint analysis for different origins of sea buckthorn berries. J Chromatogr A 2007;1154:250–9.

    Article  PubMed  CAS  Google Scholar 

  3. Zhang Q, Cui H. Simultaneous determination of quercetin, kaempferol, and isorhamnetin in phytopharmaceuticals of Hippophae rhamnoides L. by high-performance liquid chromatography with chemiluminescence detection. J Sep Sci 2005;28:1171–8.

    Article  PubMed  CAS  Google Scholar 

  4. Zu Y, Li C, Fu Y, Zhao C. Simultaneous determination of catechin, rutin, quercetin kaempferol and isorhamnetin in the extract of sea buckthorn(Hippophae rhamnoides L.) leaves by RP-HPLC with DAD. J Pharm Biomed Anal 2006;41:714–9.

    Article  PubMed  CAS  Google Scholar 

  5. Suomela JP, Ahotupa M, Yang B, Vasankari T, Kallio H. Absorption of flavonols derived from sea buckthorn (Hippophae rhamnoides L.) and their effect on emerging risk factors for cardiovascular disease in humans. J Agric Food Chem. 2006;54:7364–9.

    Article  PubMed  CAS  Google Scholar 

  6. Pang X, Zhao J, Zhang W, Zhuang X, Wang J, Xu R, et al. Antihypertensive effect of total flavones extracted from seed residues of Hippophae rhamnoides L. in sucrose-fed rats. J Ethnopharmacol. 2008;117:325–31.

    Article  PubMed  CAS  Google Scholar 

  7. Cheng J, Kondo K, Suzuki Y, Ikeda Y, Meng X, Umemura K. Inhibitory effects of total flavones of Hippophae rhamnoides L. on thrombosis in mouse femoral artery and in vitro platelet aggregation. Life Sci. 2003;72:2263–71.

    Article  PubMed  CAS  Google Scholar 

  8. Damian F, Blaton N, Naesens L, et al. Physicochemical characterization of solid dispersions of the antiviral agent UC-781 with polyethylene glycol 6000 and Gelucire 44/14. Eur J Pharm Sci. 2000;10:311–22.

    Article  PubMed  CAS  Google Scholar 

  9. Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci. 1971;60:1281–302.

    Article  PubMed  CAS  Google Scholar 

  10. Ford JL. The current status of solid dispersions. Pharm Acta Helv. 1986;61:69–88.

    PubMed  CAS  Google Scholar 

  11. Sethia S, Squillante E. Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods. Int J Pharm. 2004;272:1–10.

    Article  PubMed  CAS  Google Scholar 

  12. Liu L, Wang X. Improved dissolution of oleanolic acid with ternary solid dispersions. AAPS PharmSci Tech. 2007;8(4):E1–5.

    Article  Google Scholar 

  13. Cirri M, Maestrelli F, Corti G, Mura P. Fast-dissolving tablets of glyburide based on ternary solid dispersions with PEG 6000 and surfactants. Drug Deliv. 2007;14:247–55.

    Article  PubMed  CAS  Google Scholar 

  14. Kwon SH, Kim SY, Ha KW, Kang MJ, et al. Pharmaceutical evaluation of genistein-loaded pluronic micelles for oral delivery. Arch Pharm Res. 2007;30:1138–43.

    Article  PubMed  CAS  Google Scholar 

  15. Abdul-Fattah AM, Bhargava HN. Preparation and in vitro evaluation of solid dispersions of halofantrine. Int J Pharm. 2002;235:17–33.

    Article  PubMed  CAS  Google Scholar 

  16. Zheng X, Yang R, Tang X, Zheng L. Part I: characterization of solid dispersions of nimodipine prepared by hot-melt extrusion. Drug Dev Ind Pharm. 2007;33:791–802.

    Article  PubMed  CAS  Google Scholar 

  17. Chen Y, Zhang GGZ, Neilly J, Marsh K, Mawhinney D, Sanzgiri YD. Enhancing the bioavailability of ABT-963 using solid dispersion containing Pluronic F-68. Int J Pharm. 2004;286:69–80.

    Article  PubMed  CAS  Google Scholar 

  18. Passerini N, Albertini B, Gonzalez-Rodriguez ML, Cavallari C, Rodriguez L. Preparation and characterization of ibuprofen–poloxamer 188 granules obtained by melt granulation. Eur J Pharm Sci. 2002;15:71–8.

    Article  PubMed  CAS  Google Scholar 

  19. Kwon GS. Polymeric micelles for delivery of poorly water-soluble compounds. Crit Rev Ther Drug Carrier Syst. 2003;20:357–403.

    Article  PubMed  CAS  Google Scholar 

  20. Yong CS, Yang CH, Rhee JD, et al. Enhanced rectal bioavailability of ibuprofen in rats by poloxamer 188 and menthol. Int J Pharm. 2004;269:169–76.

    Article  PubMed  CAS  Google Scholar 

  21. Hamed E, Sakr A. Application of multiple response optimization technique to extended release formulations design. J Control Rel. 2001;73:329–38.

    Article  CAS  Google Scholar 

  22. Rhee Y-S, Chang S-Y, Park C-W, et al. Optimization of ibuprofen gel formulations using experimental design technique for enhanced transdermal penetration. Int J Pharm. 2008;364:14–20.

    Article  PubMed  CAS  Google Scholar 

  23. Patel VF, Patel NM. Statistical evaluation of influence of viscosity and content of polymer on dipyridamole release from floating matrix tablets: a technical note. AAPS PharmSciTech. 2007;8(Sup 3):E1–5.

    Google Scholar 

  24. Huang YT, Tsai TR, Cheng CJ, et al. Formulation design of an HPMC-based sustained tablet for pyridostigmine bromide as a highly hygroscopic model drug and its in vivo/in vitro dissolution properties. Drug Dev Ind Pharm. 2007;33:1183–91.

    Article  PubMed  CAS  Google Scholar 

  25. USP. The United States Pharmacopeia (USP) XXIX. NF XXIV. Rockville: US Pharmacopeial Convention; 2006. p. 2673.

    Google Scholar 

Download references

Acknowledgment

This work was supported by the Shanghai City College Scientific Research Fund for Choosing and Cultivating Excellent Youth Teacher of China (szy-07034). The authors are grateful to Vice-professor Yue Su for her instruction on the statistics analysis, Ms. Fuyuan Ye for her FTIR and X-ray recording, and Mr. Jun Li for his DSC recording.

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Guowen Li.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Xie, Y., Li, G., Yuan, X. et al. Preparation and In Vitro Evaluation of Solid Dispersions of Total Flavones of Hippophae rhamnoides L.. AAPS PharmSciTech 10, 631–640 (2009). https://doi.org/10.1208/s12249-009-9246-x

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1208/s12249-009-9246-x

Key words

Navigation