Improvement of bioavailability of water insoluble drugs: Estimation of intrinsic bioavailability

Junhyoung Kim; Dong Hyun Jung; Hokyoung Rhee; Seung-Hoon Choi; Min Jae Sung; Woo Sik Choi

Korean Journal of Chemical Engineering, Vol.25, No.1, 171-175, January, 2008

DOI10.1007/s11814-008-0031-4 Export Citation

Improvement of bioavailability of water insoluble drugs: Estimation of intrinsic bioavailability

Junhyoung Kim¹, Dong Hyun Jung¹, Hokyoung Rhee¹, Seung-Hoon Choi¹, Min Jae Sung², and Woo Sik Choi^{2, 3, †}

¹Research Division, Insilicotech Co., Ltd., Seongnam 463-943, Korea
²Interdisciplinary Program in Powder Technology, Graduate School, Pusan National University, Busan 609-735, Korea
³Department of Pharmaceutical Manufacturing, Pusan National University, Busan 609-735, Korea

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A series of attempts to enhance the bioavailability of water insoluble drugs have been made by the fine grinding technique using a planetary ball mill in wet milling process. Here, the possibility of improving the dissolution properties of water insoluble drugs such as ursodeoxycholic acid (UDCA), diphenyl hydrantoin (phenytoin) and biphenyl dimethyl dicarboxylate (DDB) based on ultra-fine grinding process has been discussed with comparison to experimental data. Also examined was the intrinsic bioavailability estimated based on a molecular modeling approach and thermophysical data.

Keywords:Water Insoluble Drug;Bioavailability;Top-down Process;UDCA;DDB;Phenytoin

[References]

Chow WL, Riegelman S, J. Pharm. Sci., 60, 1281 (1971)
Chaumeil JC, Meth. Find. Clin. Pharmacol., 20, 211 (1998)
Yamamoto K, Nakano M, Arita T, Nakai Y, J. Pharmacokinet. Biopharm., 2, 487 (1974)
Morita M, Nakai Y, Fukuoka E, Nakajima S, Chem. Pharm. Bull., 32, 4076 (1984)
Pirttimaki J, Laine E, Ketolainen J, Paranen P, Int. J. Pharm., 95, 93 (1993)
Piyarom S, Yonemochi E, Oguchi T, Yamamoto K, J. Pharm. Pharmacol., 49, 384 (1997)
Yalkowsky SH, Banerjee S, in Aqueous Solubility, Methods’ of Estimation for Organic Compounds, Marcel Dekker, New York, NY (1992)
Christel ASB, Ulf N, Kristina L, Artursson P, Pharm. Res., 19, 182 (2002)
Chung HY, Yonemochi E, Saito T, Terada K, Tozuka Y, Oguchi T, Yamamoto K, Chung HY, Choi WS, Int. J. Pharm., 255, 49 (2003)
Kim HI, Kwak SS, Chung HY, Chung HY, Yamamoto K, Oguchi T, Tozuka Y, Yonemochi E, Terada K, Int. J. Miner. Process., 74, S165 (2004)
Choi WS, Kwak SS, Kim HI, Asian Journal of Pharmaceutical Sciences, 1, 27 (2006)
Choi WS, Chung HY, Yoon BR, Kim SS, Powder Technol., 115(3), 209 (2001)
Nystrom C, Mazur J, Darneff MI, Glazer M, J. Pharm. Pharmacol., 37, 217 (1985)
Egan WJ, Merz KM, Baldwin JJ, J. Med. Chem., 43, 3867 (2000)
Rogers D, Hopfinger AJ, J. Chem. Inf. Comput. Sci., 34, 854 (1994)
Mosier PD, Jurs PC, J. Chem. Inf. Comput. Sci., 42, 1460 (2002)
ADME modules of Cerius 2, Version 4.10, Accelrys Inc., San Diego CA
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Cheng A, Merz KM, J. Med. Chem., 46, 3572 (2003)
Arlt W, in Private communication on the prediction of thermophysical data, University of Erlangen, Germany (2005)

[Referenced By]

[1] Chow WL, Riegelman S, J. Pharm. Sci., 60, 1281 (1971)

[2] Chaumeil JC, Meth. Find. Clin. Pharmacol., 20, 211 (1998)

[3] Yamamoto K, Nakano M, Arita T, Nakai Y, J. Pharmacokinet. Biopharm., 2, 487 (1974)

[4] Morita M, Nakai Y, Fukuoka E, Nakajima S, Chem. Pharm. Bull., 32, 4076 (1984)

[5] Pirttimaki J, Laine E, Ketolainen J, Paranen P, Int. J. Pharm., 95, 93 (1993)

[6] Piyarom S, Yonemochi E, Oguchi T, Yamamoto K, J. Pharm. Pharmacol., 49, 384 (1997)

[7] Yalkowsky SH, Banerjee S, in Aqueous Solubility, Methods’ of Estimation for Organic Compounds, Marcel Dekker, New York, NY (1992)

[8] Christel ASB, Ulf N, Kristina L, Artursson P, Pharm. Res., 19, 182 (2002)

[9] Chung HY, Yonemochi E, Saito T, Terada K, Tozuka Y, Oguchi T, Yamamoto K, Chung HY, Choi WS, Int. J. Pharm., 255, 49 (2003)

[10] Kim HI, Kwak SS, Chung HY, Chung HY, Yamamoto K, Oguchi T, Tozuka Y, Yonemochi E, Terada K, Int. J. Miner. Process., 74, S165 (2004)

[11] Choi WS, Kwak SS, Kim HI, Asian Journal of Pharmaceutical Sciences, 1, 27 (2006)

[12] Choi WS, Chung HY, Yoon BR, Kim SS, Powder Technol., 115(3), 209 (2001)

[13] Nystrom C, Mazur J, Darneff MI, Glazer M, J. Pharm. Pharmacol., 37, 217 (1985)

[14] Egan WJ, Merz KM, Baldwin JJ, J. Med. Chem., 43, 3867 (2000)

[15] Rogers D, Hopfinger AJ, J. Chem. Inf. Comput. Sci., 34, 854 (1994)

[16] Mosier PD, Jurs PC, J. Chem. Inf. Comput. Sci., 42, 1460 (2002)

[17] ADME modules of Cerius 2, Version 4.10, Accelrys Inc., San Diego CA

[18] ChemIDplus Advanced, http://chem.sis.nlm.nih.gov/chemidplus

[19] Meylan WM, Howard PH, in PCGEMS & EPI (Sept 1994, Final Report), S.B. Robert, U.S. Environmental Protection Agency, Office of Pollution Prevention and Toxics, Washington, DC; prepared by Syracuse Research Corporation, Environmental Science Center, Syracuse, NY 13210 (1994)

[20] Cheng A, Merz KM, J. Med. Chem., 46, 3572 (2003)

[21] Arlt W, in Private communication on the prediction of thermophysical data, University of Erlangen, Germany (2005)