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http://dx.doi.org/10.4333/KPS.2005.35.1.001

The Effect of Solvents on Sold Dispersion of Ipriflavone with Polyvinylpyrrolidone In Vivo  

Jeong, Je-Kyo (Research Center, Samchundang Pharm. Co. Ltd.)
Ahn, Yong-San (Department of Polymer. Nano Science and Technology, Chonbuk National University)
Moon, Byung-Kwan (Department of Advanced Organic Materials Engineering, Chonbuk National University)
Choi, Myung-Kyu (Department of Polymer. Nano Science and Technology, Chonbuk National University)
Khang, Gil-Son (Department of Polymer. Nano Science and Technology, Chonbuk National University, Department of Advanced Organic Materials Enginnering, Chonbuk National University, Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
Rhee, John-M. (Department of Polymer. Nano Science and Technology, Chonbuk National University, Department of Advanced Organic Materials Enginnering, Chonbuk National University)
Lee, Hai-Bang (Department of Polymer. Nano Science and Technology, Chonbuk National University, Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
Publication Information
Journal of Pharmaceutical Investigation / v.35, no.1, 2005 , pp. 1-5 More about this Journal
Abstract
ABSTRACT -Ipriflavone is a synthetic flavonoid derivate that improves osteoblast cell activity inhibiting bone resorption. In order to improve the bioavailability, solid dispersions of ipriflavone with PVP (poly-N-vinylpyrrolidone, MW=40,000 g/mole) were prepared by a spray-drying method. During the manufacturing of solid dispersion, various solvents [ethanol (EtOH), acetonitrile, methylene chloride and cosolvent-EtOH:acetone=1:1] were used to dissolve the ipriflavone and PVP. Scanning electron microscopy (SEM) and differential scanning calorimetry (DSC) were used to evaluate the physicochemical interaction between ipriflavone and PVP. Particle size, crystallinity and the area of the endotherm $({\Delta}H)$ of solid dispersed ipriflavone using the acetonitrile as solvent were much smaller than those of the other preparation types. Bioavailability of ipriflavone in vivo was changed by solvents. When considering the result of in vivo test, solid dispersion of ipriflavone using the acetonitrile as solvent showed the best choice.
Keywords
Ipriflavone; Solid dispersion; Bioavailability; Various Solvents;
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1 Y.E. Nashed and A.K. Mitra, Synthesis and characterization of novel dipeptide ester prodrugs of acyclovir, Spectrochimica Acta Part A, Mol. Bio. Spectro., 59, 2033-2039 (2003)   DOI   ScienceOn
2 G., Khang, J.K. Jeong, J.S. Lee, J.M. Rhee and H.B. Lee, Recent development trends of the improving bioavailability by polymeric nanovehicles of poorly water soluble drugs, Polymer. Sci. Tech., 13, 342-359 (2002)
3 J.K. Jeong, J.H. Kim, G. Khang, J.M. Rhee and H.B. Lee, The preparation and characterization of solid dispersion of ipriflavone with PVP, J. Kor. Pharm. Sci., 32, 173-179 (2002)
4 G. Khang, J.K. Jeong, J.M. Rhee, H.C. Shin and H.B. Lee, Effect of hydrophilic polymers on solid dispersions of ipriflavone to improve bioavailability, Macromol. Chem. Symp., 14, 123-132 (2001)
5 K. Yamashita, T. Nakate, K. Okimoto, A Ohike, Y. Tokunaga, R. Ibuki, K. Higaki and T. Kimura, Establishment of new preparation method for solid dispersion formulation of tacrolimus, Int. J. Pharm., 267, 79-91 (2003)   DOI   ScienceOn
6 G. Khang, J.K. Jeong, J.M. Rhee, H.C. Shin and H.B. Lee, Solid dispersion in polymeric vehicles for bioavailability improvement of a poorly water-soluble drug: In Biomaterials and Drug Delivery toward New Millenium, K.D. Park, I.C. Kwon, N. Yui, S.Y. Jeong and K. Park (Eds.), Han Rim Won Publishing Co., Seoul, pp. 309-320 (2000)
7 K. Sekiguchi and N. Obi, Studies on absorption of eutectic mixture. A comparison of the behavior of eutectic mixture of sulfathiazole and that of ordinary sulfathiazole in man, Chem. Pharm. Bull., 9, 866-872 (1961)   DOI
8 C. McGuigan, M.J. Slater, N.R. Parry, A. Perry and S. Harris, Synthesis and antiviral activity of acyclovir-5'-(phenyl methoxy alaninyl) phosphate as a possible membrane-soluble nucleotide prodrug, Bio. Med. Chem. Let., 10, 645-647 (2000)   DOI   ScienceOn
9 T. Hanabayashi, A. Imai and T. Tamaya, Effects of ipriflavone and estriol on postmenopausal osteoporotic changes, Int. J. Gyn. Obs., 51, 63-64 (1995)   DOI   ScienceOn
10 C.W. Pouton, Self-emulsifying drug delivery system: Assessment of the efficiency of emulsification, Int. J. Pharm., 27, 335-348 (1985)   DOI   ScienceOn
11 J.K. Jeong, G. Khang, J.M. Rhee, H.C. Shin and H.B. Lee, Comparative bioavailability of IP by pharmaceutical preparation types, J. Kor. Pharm. Sci., 30, 21-26 (2000)
12 T.P. Shakhtshneider, M.A. Vasiltchenko, A.A. Politov and V.V. Boldyrev, The mechanochemical preparation of solid disperse system of ibuprofen-polyethylene glycol, Int. J. Pharm., 130, 25-32 (1996)   DOI   ScienceOn
13 C. Leuner and J. Dressman, Improving drug solubility for oral delivery using solid dispersions, Eur. J. Pharm. Biopharm., 50, 47-60 (2000)   DOI   ScienceOn
14 J. Hyun and I.K. Chun, Dissolution characteristics of biphenyl dimethyl dicarboxylate from solid dispersions and permeation through rabbit deuodenal mucosa, J. Kor. Pharm. Sci., 24, 57-65 (1994)
15 E.J. Benjamin, B.A. Firestone, R. Bergstrim, M. Fass, I. Massey, I. Tsina and Y.T. Lin, Selection of a derivatives of the antiviral agent 9-[(1,3-dihydroxy-2-proxy)-methyllguanine with improved oral absorption, Pharm. Res., 4, 120-125 (1987)   DOI   ScienceOn
16 P. Jolimaitre, M. Malet-Martino and R. Martino, Fluorouracil prodrugs for the treatment of proliferative vitreoretinopathy : Formulation in silicone oil and in vitro release of fluorouracil, Int. J. Pharm., 259, 181-192 (2003)   DOI   ScienceOn
17 S.H. Kim and M.G. Lee, Pharmacokinetics of ipriflavone, an isoflavone derivative, after intravenous and oral administration to rats hepatic and intestinal first-pass effects, Life Sci., 70, 1299-1315 (2002)   DOI   ScienceOn
18 L.A. Hergert and G.M. Escandar, Spectrofluorimetric study of the $\beta$-cyclodextrin-ibuprofen complex and determination of ibuprofen in phamaceutical preparation and serum, Talanta, 60, 235-246 (2003)   DOI   ScienceOn
19 H. Schott, L.C. Kwan and S. Feldman, The role of surfactant in the release of very slightly soluble drugs from tablets, J. Pharm. Sci., 71, 1038-1045 (1982)   DOI
20 H.J. Kil, S.H. Cho, G. Khang, S.Y. Jeung, K.S. Seo, B.Y. Yoon, B.K. Kang and H.B. Lee, Preparation of solid dosage form containing SMEDDS of simvastatin by microencapsulation, J. Kor. Pharm. Sci., 33, 121-127 (2003)
21 R.H. Christopher, J.H. Porter, G.A. Edwards, A. Mullertz, H.G. Kristensen and W.N. Charman, Examination of oral absorption and lymphatic transport of halofantrine in a triplecannulated canine model after administration in selfmicroemulsifying drug delivery systems (SMEDDS) containing structured triglycerides, Eur. J. Pharm. Sci., 20, 91-97 (2003)   DOI   ScienceOn
22 Y.S. Ahn, H.Y. Lee, K.D. Hong. S.B. Jung, S.H. Cho, J.M. Rhee, H.B. Lee and G. Khang, Preparation and in vitro test of solid dispersion using acyclovir and water soluble polymer, J. Kor. Pharm. Sci., 34, 169-176 (2004)
23 Y.S. Ahn, J.H. Song, B.K. Kang, M.S. Kim, S.H. Cho, J.M. Rhee, H.B. Lee and G. Khang, Preparation and characterization of liquefied ibuprofen using self-microemulsion drug delivery system (SMEDDS), J. Kor. Pharm. Sci., 34, 35-42 (2004)
24 J.K. Jeong, G. Khang, J.M. Rhee, H.C. Shin and H.B. Lee, Effect of molecular weights and mixture ratios of polyvinylpyrrolidone on the bioavailability of ipriflavone solid dispersion, J. Kor. Pharm. Sci., 30, 235-239 (2000)
25 I.J. Oh, J.G. Park, Y.B. Lee and S.C. Shin, Inclusion complex of analgesic and anti-inflammatory agents with cyclodextrins (I): Enhancement of dissolution of ibuprofen by 2-hydroxypropyl-${\beta}$-cyclodextrin, J. Kor. Pharm. Sci., 23, 11-18 (1993)
26 H.S. Kim, S.K. Lee, S.U. Choi, H.S. Park, H.J. Jeon and Y.W. Choi, Improved dissolution characteristics of ibuprofen employing self-microemulsifying drug delivery system and their bioavailability in rats, J. Kor. Pharm. Sci., 32, 27-33 (2002)
27 D. Attwood, C. Mallon, and C.J. Taylor, Phase studies of oilin-water phospholipid microemulsions, Int. J. Pharm., 84, R5-R8 (1992)   DOI   ScienceOn