The preparation of Garcinia Glycosides solid dispersion and intestinal absorption by rat in situ single pass intestinal perfusion
Main Article Content
Abstract
Garcinia Glycosides is a candidate drug obtained by structural modification of Gambogic Acid (GA), which was acquired through High Throughput Screening(HTS). As Garcinia Glycosides is an effective but insoluble anti-tumor drug, the aim of this study was to obtain a solid dispersion form Garcinia Glycosides by using solvent-melt method so that improve the solubility and dissolution rate. The solid dispersion was characterized by High Performance Liquid Chromatography (HPLC), infrared spectroscopy and evaluated the intestinal absorption of the drug by rat in situ single pass intestinal perfusion. The results showed the increase of solubility, dissolution velocity and absorption compared to other forms. This indicated that solid dispersion could greatly improve the relative bioavailability of Garcinia Glycosides in vivo.
Article Details
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
References
- Wang Y, Zhang Q, Liu J, et al. Synthesis and antitumor activities of Gareinia glycosides. Chin J New Drugs, 2013, 22:2739-2744.
- Li WJ, Chen Y, Li TW, et al. Formulation optimization and the release mechanism of Gareinia glycosides sustainedrelease tablets. Chin J Modern Appl Pharm, 2013, 10:1081- 1085.
- Fu YP, Wang R, Li TW, et al. Pharmacokinetics and tissue distribution of TJXG nano emulsion in rats. Chin Medical Herald, 2013, 11:19-22.
- Liu C, Zhu S, Zhou Y, et al. In Situ Intestinal Absorption of Cyclosporine A Solid Dispersion in Rats. Drug Dev Ind Pharm, 2008, 34(6):627-631. https://dx.doi.org10.1080/03639040701833948
- Chaud MV, Tamascia P, Lima AC, et al. Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel. Braz J Pharm Sci, 2010, 46 (3): 473-481. https://dx.doi.org/10.1590/S1984-82502010000300010
- Liu C, Zhu SJ, Zhou Y, et al. Enhancement of dissolution of cyclosporine A using solid dispersions with polyoxyethylene (40) stearate. Pharmazie Die Pharmazie-An Int J Pharm Sci, 2006, 61(8):681-684.
- Chaud MV, Paula FC, Moraes LC, et al. Assessment of Solubility and Intestinal Absorption In Vitro of Praziquantel in Solid Dispersions of Polyethylene Glycol 6000. Lat Am J Pharm, 2011, 30 (10): 1910-1915.
- Yang M, He S, Fan Y, et al. Microenvironmental pHmodified solid dispersions to enhance the dissolution and bioavailability of poorly water-soluble weakly basic GT0918, a developing anti-prostate cancer drug: Preparation, characterization and evaluation in vivo. Int J Pharm Sci, 2014, 475 (1-2): 97-109. https://doi.org/10.1016/j.ijpharm.2014.08.047
- Surampalli G, Nanjwade B, Patil PA. Corroboration of naringin effects on the intestinal absorption and pharmacokinetic behavior of candesartan cilexetil solid dispersions using in-situ rat models. Drug Dev Ind Pharm, 2015, 41 (7):1057-1065. https://dx.doi.org/10.3109/03639045.2014.925918
- Zhou, W, Di LQ, Bi XL, et al. Intestinal absorption of forsythoside A byrat circulation in situ. Acta Pharmaceutica Sinica, 2010, 45 (11):1373-1378.
- Dang YJ, Feng HZ, Zhang L, et al. In Situ Absorption in Rat Intestinal Tract of Solid Dispersion of Annonaceous Acetogenins. Gastroenterology Res Pract, 2012, 10:81-89.
- Shi CY, Tong Q, Fang J, et al. Preparation, characterization and in vivo studies of amorphous solid dispersion of berberine with hydrogenated phosphatidylcholine. Eur J Pharm Sci, 2015, 74:11-47. https://doi.org/10.1016/j.ejps.2015.04.001
- Streubel A, Siepmann J, Bodmeier R. Drug delivery to the upper small intestine window using gastroretentive technologies. Curr Opin Phar, 2006, 6 (5): 501-508. https://doi.org/10.1016/j.coph.2006.04.007
- Tanaka N, Imai K, Okimoto K, et al. Development of novel sustained-release system, disintegration-controlled matrix tablet (DCMT) with solid dispersion granules of nilvadipine (II): in vivo evaluation. J Controlled Release, 2006, 112(1):52-56. https://doi.org/10.1016/j.jconrel.2006.01.020
- Szts A, L´ang P, Ambrus R, et al. Applicability of sucrose laurate as surfactant in solid dispersions prepared by melt technology. Int J Pharm Sci, 2011, 410(1-2):107-110. https://doi.org/10.1016/j.ijpharm.2011.03.033