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.
Similar content being viewed by others
References
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.
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.
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.
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.
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.
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.
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.
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.
Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci. 1971;60:1281–302.
Ford JL. The current status of solid dispersions. Pharm Acta Helv. 1986;61:69–88.
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.
Liu L, Wang X. Improved dissolution of oleanolic acid with ternary solid dispersions. AAPS PharmSci Tech. 2007;8(4):E1–5.
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.
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.
Abdul-Fattah AM, Bhargava HN. Preparation and in vitro evaluation of solid dispersions of halofantrine. Int J Pharm. 2002;235:17–33.
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.
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.
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.
Kwon GS. Polymeric micelles for delivery of poorly water-soluble compounds. Crit Rev Ther Drug Carrier Syst. 2003;20:357–403.
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.
Hamed E, Sakr A. Application of multiple response optimization technique to extended release formulations design. J Control Rel. 2001;73:329–38.
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.
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.
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.
USP. The United States Pharmacopeia (USP) XXIX. NF XXIV. Rockville: US Pharmacopeial Convention; 2006. p. 2673.
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
Corresponding author
Rights 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
Received:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1208/s12249-009-9246-x