Solid dispersion: An alternative technique for bioavailability enhancement of poorly soluble drugs

Journal of Dispersion Science and Technology

Volumn 30, Issue 10, 2009, Pages 1458-1473

  Sinha, Shilpi ^a   Baboota, Sanjula ^a   Ali, Mushir ^a   Kumar, Anil ^a   Ali, Javed ^a  

^a HAMDARD UNIVERSITY   (India)

Author keywords

Amorphous state; Characterization; Dissolution enhancement; Poorly soluble drugs; Solid dispersion

Indexed keywords

AMORPHOUS STATE; CRYSTALLINE-TO-AMORPHOUS; DISSOLUTION RATES; GLASS TRANSITION TEMPERATURE; NEW DIMENSIONS; POORLY SOLUBLE DRUGS; SCALE-UP; SOLID DISPERSION;

BIOCHEMISTRY; CHARACTERIZATION; DISSOLUTION; DRUG INTERACTIONS; GLASS TRANSITION; MICROCRYSTALS;

DISPERSIONS;

EID: 70350666524     PISSN: 01932691     EISSN: 15322351     Source Type: Journal    
DOI: 10.1080/01932690903120136     Document Type: Article

References (131)

1. Lipinski, C.A., Lombardo, F., Dominyl, B.W., and Feeney, P.J. (1997) Adv. Drug. Del. Rev., 23: 3-25.
2. Bashiri, A. and Szabo-Revesz Eros, I.P. (2003) Pharm. Tech. Eur., 15: 27-32.
3. Dannenfelser, R., He, H., Joshi, Y., Bateman, S., and Serajuddin, A.T.M. (2004) J. Pharm. Sci., 93: 1165-1175.
4. Vasconcelos, T.F., Sarmento, B., and Costa, P. (2007) Drug Discovery Today, 12: 1068-1075.
5. Leuner, C. and Dressman, J. (2000) Eur. J. Pharm. Biopharm., 50: 47-60.
6. Gowariker, V.R., Viswanathan, N.V., and Sreedhar, J. (1986) Polymer Science; New Delhi, India: New Age Publishers.
7. Hancock, B.C. and Zografi, G. (1997) J. Pharm. Sci., 86: 1-12.
8. Sekiguchi, K. and Obi, N. (1961) Chem. Pharm. Bull., 9: 866-872.
9. Langer, M., Holtje, M., Urbanetz, N.A., Brandt, B., Holtje, H.D., and Lippold, B.C. (2003) Int. J. Pharm., 252: 167-179.
10. Kapsi, S.G. and Ayres, J.W. (2001) Int. J. Pharm., 229: 193-203.
11. Damian, F., Blaton, N., Naesens, L., Balzarini, J., Kinget, R., Augustijns, P., and Van den Mooter, G. (2000) Eur. J. Pharm. Sci., 10: 311-322.
12. Van Drooge, D.J., Hinrichs, W.L.J., Visser, M.R., and Frijlink, H.W. (2006) Int. J. Pharm., 310: 220-229.
13. Stefanescu, D.M. (1988) Solidification Processing of Eutectic Alloy; New York: TMS.
14. Pure and Applied Chemistry. (1994) Definitions of Terms Relating to Phase Transitions of the Solid State; IUPAC Recommendations 1994, vol. 66, p. 577.
15. Vippagunta, S.R., Wang, Z., Hornung, S., and Krill, S.L. (2007) J. Pharm. Sci., 96: 294-304.
16. Naima, Z., Siro, T., Juan-Manuel, G.D., Chantal, C., Rene, C.L., and Jerome, D. (2001) Eur. J. Pharm. Sci., 12: 395-404.
17. Law, D., Wang, W., Schimtt, E.A., Qiu, Y., Krill, S.L., and Fort, J.J. (2003) J. Pharm. Sci., 92: 505-515.
18. Lacoulonche, F., Chauvet, A., Masse, J., Egea, M.A., and Garcia, M.L. (1998) J. Pharm. Sci., 87: 543-551.
19. Gordon, M. and Taylor, J.S. (1952) J. Appl. Chem., 2: 493-500.
20. Weuts, I., Kempen, D., Decorte, A., Verreck, G., Peeters, J., Brewster, M., and Van den Mooter, G. (2005) Eur. J. Pharm. Sci., 25: 313-320.
21. Fiebich, K. and Mutz, M. (1999) J. Them. Anal. Cal., 57: 75-85.
22. Van den Mooter, G., Wuyts, M., Blaton, N., Busson, R., Grobet, P., Augustijns, P., and Kinget, R. (2001) Eur. J. Pharm. Sci., 12: 261-269.
23. Heo, M.Y., Piao, Z.Z., Kim, T.W., Cao, Q.R., Kim, A., and Lee, B.J. (2005) Arch. Pharm. Res., 28: 604-611.
24. Damian, F., Blaton, N., Kinget, R., and Van den Mooter, G. (2002) Int. J. Pharm., 244: 87-98.
25. Gupta, P., Thilagavathi, R., Chakraborti, A.S., and Bansal, A.K. (2005) Mol. Pharm., 2: 84-391.
26. Drooge, D.J.V., Hinrichs, W.L.J., Visser, M.R., and Frijlink, H.W. (2006) Int. J. Pharm., 310: 220-229.
27. Weuts, I., Kempen, D., Verreck, G., Peeters, J., Brewster, M., Blaton, N., and Van den Mooter, G. (2005) Eur. J. Pharm. Sci., 25: 387-393.
28. Shibata, Y., Fuji, M., Kokudai, M., Noda, S., Okada, H.,Kondoh, M., and Watanabe, Y. (2007) J. Pharm. Sci., 96: 1537-1547.
29. Higuchi, W.I., Mir, N.A., and Desai, S.J. (1965) J. Pharm. Sci., 54: 1404-1410.
30. Craig, D.Q.M. (2001) Int. J. Pharm., 231: 131-144.
31. Serajuddin, A.T.M. (1999) J. Pharm. Sci., 88: 1058-1066.
32. Karavas, E., Georgarakis, E., Sigalas, M.P., Avgoustakis, K., and Bikiaris, D. (2007) Eur J. Pharm. Biopharm., 66: 334-347.
33. Muhrer, G., Meier, U., Fusaro, F., Albano, S., and Mazzotti, M. (2006) Int. J. Pharm., 308: 69-83.
34. Lofftsson, T. and Brewster, M.E. (1997) J. Pharm. Sci., 85: 1017-1025.
35. Henck, J.O., Griesser, U.J., and Burger, A. (1997) Pharm. Ind., 59: 165-169.
36. Smikalla, M.M. and Urbanetz, N.N. (2007) Eur J. Pharm. Sci., 66: 106-112.
37. Yoshioka, M. and Hancock, B.C. (1995) J. Pharm. Sci., 84: 983-986.
38. Ambike, A.A., Mahadik, K.R., and Paradkar, A. (2004) Int. J. Pharm., 282: 151-162.
39. Sertsou, G., Butler, J., Scott, A., Hempenstall, J., and Rades, T. (2002) Int. J. Pharm., 245: 99-108.
40. Gunawan, L., Johari, G.P., and Shanker, R.M. (2006) Pharm. Res., 23: 967-979.
41. Miyazaki, T., Yoshioka, S., Aso, Y., and Kojima, S. (2004) J. Pharm Sci., 93: 2710-2717.
42. Karel, S., Geert, V., Jef, Peeters., Brewster, M., and Van den Mooter, G. (2004) J Pharm Sci., 93: 124-131.
43. Dhumal, R.S., Shimpi, S.L., Paradkar, A.R. (2007) Acta Pharm., 57: 287-300.
44. School of Pharmacy, London. (2006). Solid dispersion of hydrophobic bioactive. Pat. No. WO=2006=085089.
45. Drooge, D.J.V., Hinrichs, W.L.J., and Frijlink, H.W. (2004) J. Pharm. Sci., 93: 713-725.
46. Ningyun, S., Xiuli, Wei., Baojian, W., Jian, C., Yi, L., and Wei, W. (2008) Powder Technol., 182: 72-80.
47. Newa, M., Bhandari, K.H., Li, D.X., Kwon, T., Kim, J.A., Yoo, B.K., Woo, J.S., Lyoo, W.S., Yong, C.S., and Choi, H.G. (2007) Int. J. Pharm., 343: 228237.
48. Yamashita, K., Nakate, T., Okimoto, K., Ohike, A., Tokunaga, Y., Ibuki, R., Higaki, K., and Kimura, T. (2003) Int J. Pharm., 267: 7991.
49. Nilüfer, Y., Aysegül, K., Yalç Ö., Ayhan, S., Sibel, A.Ö., and Tamer, B. (2003) Eur. J. Pharm. Biopharm., 56: 45345.
50. Sethia, S. and Squillante, E. (2004) J. Pharm. Sci., 93: 29852993.
51. Barker, S.A., Yap, S.P., Yuen, K.H., McCoy, C.P., Murphy, J.R., and Craig, D.Q.M. (2003) J. Control. Rel., 91: 477488.
52. Zerrouk, N., Chemtob, C., Arnaud, P., Toscani, S., and Dugue, J. (2001) Int. J. Pharm., 225: 4962.
53. Timko, R.J. and Lordi, N.G. (1979) J. Pharm. Sci., 68: 601605.
54. Lin, C.W. and Cham, T.M. (1996) Int. J. Pharm., 22: 909916.
55. Allen, L.V. and Yanchick, V.A. (1977) J. Pharm. Sci., 66: 494497.
56. Summers, M.P. and Enever, R.P. (1976) J. Pharm. Sci., 65: 16131618.
57. The role of plasticizers as functional excipients in pharmaceutical dosage forms prepared by hot-melt extrusion. (2004) Pharmaceutical Coatings Bulletin, 102: 6.
58. Van Laarhoven, J.A.H., Kruft, M.A.B., and Vromans, H. (2002) Int. J. Pharm., 232: 163173.
59. Nakamichi, K., Yasuura, H., Fukui., Oka, M., and Izumi, S. (2001) Int. J. Pharm., 218: 103112.
60. Munch, U., Mika, H.J., Eschermann, B., Schmidt, R., and Sczepanik, B. (1990) Orally administered solvent free pharmaceutical preparation with delayed active substance release and a method of preparing the preparation. Eur. Patent 0,552,227.
61. Grunhagen, H.H. (1996) Pharm. Tech. Eur., 8: 2228.
62. Ozkan, Y., Doganay, N., Dikmen, N., and Isimer, A. (2000) Il Farmaco, 55: 433438.
63. Huelsmanna, S., Backensfelda, T., Keitela, S., and Bodmeier, R. (2000) Eur. J. Pharm. Sci., 49: 237242.
64. Li, F. and Hu, J. (2004) Chem. Pharm. Bull., 52: 972973.
65. Zajc, N., Obreza, A., Bele, M., and Ca, S.S.C. (2005) Int. J. Pharm., 291: 5158.
66. Finia, A., Moyanob, J.R., Ginesb, J.M., Perez-Martinezb, J.I., and Rabasco, A.M. (2005) Eur. J. Pharm. Sci., 60: 99111.
67. Mooter, G.V.D., Weuts, I., Ridder, T.D., and Blaton, N. (2006) Int. J. Pharm., 316: 16.
68. Bulau, H.C., Ulrich, J. (1997) In Parameters Influencing the Properties of Drop-Formed Pastilles, edited by J. Ulrich; Aachen, Germany: Shaker Verlag.
69. Francois, D. and Jones, B.E. (1978) The hard capsule with the soft center. Paper presented at the European Capsule Technology Symposium, October 1113.
70. Serajuddin, A.T.M., Sheen, P.C., Mufson, D., Bernstein, D.F., and Augustine, M.A. (1988) J. Pharm. Sci., 77: 414418.
71. Joshi, H.N., Tejwani, R.W., Davidovich, M., Sahasrabudhe, V.P., and Mohammed Serajuddin, A.T.M. (2004) Int. J. Pharm., 269: 251258.
72. Law, S.L., Lo, W.Y., Lin, F.M., and Chaing, C.H. (1992) Int. J. Pharm., 84: 161166.
73. Wiley, G.J., Ullah, I., and Agharkar, S.N. (1995) Pharm. Tech., 19: 7276.
74. Habib, M.J. (2000) Pharmaceutical Solid Dispersion Technology; Washington, DC: CRC Press.
75. Law, D., Krill, S.L., Schmitt, E.A., Fort, J.J., Qiu, Y., Wang, W., and Porter, W.R. (2000) J. Pharm. Sci., 90: 10151025.
76. Mooter, G.V.D., Augustijns, P., Blaton, N., and Kinget, R. (1998) Int. J. Pharm., 164: 6780.
77. Franco, M., Trapani, G., Latrofa, A., Tullio, C., Provenzano, M.R., Serra, M., Muggironi, M., Biggio, G., and Liso, G. (2001) Int. J Pharm., 225: 6373.
78. Prabhu, S., Brocks, D.R., and Betageri, G.V. (2001) Drug. Dev. Ind. Pharm., 27: 413418.
79. Babu, G.V.M., Prasad, D.S., and Murthy, K.V.R. (2002) Int. J. Pharm., 234: 117.
80. Pignatello, R., Ferro, M., Guidi, G.D., Salemi, G., Vandelli, M.A., Guccione, S., Geppi, M., Forte, C., and Puglisi, G. (2001) Int. J. Pharm., 218: 2742.
81. Abdul-Fattah, A.M. and Bhargava, H.N. (2002) Int. J. Pharm., 235: 1733.
82. Orientia, I., Biguccia, F., Luppia, B., Cerchiaraa, T., Zuccaria, G., and Giunchedib, P., and Zecchi, V. (2002) Eur. J. Pharm. Sci., 54: 229233.
83. Sang-Chul, S. and Kim, J. (2003) Int. J. Pharm., 251: 7984.
84. Watanabe, T., Hasegawa, S., Wakiyama, N., Kusai, A., and Senna, M. (2003) Int. J. Pharm., 250: 283286.
85. Yamashita, K., Nakate, T., Okimoto, K., Ohike, A., Tokunaga, Y., Ibuki, R., Higaki, K., and Kimura, T. (2003) Int. J. Pharm., 267: 7986.
86. Ruan, L., Yu, B., Fu, G., and Zhu, D. (2005) J. Phar. Bio. Anal., 38: 457464.
87. Nijlen, T.V., Brennan, K., Mooter, D.V.G., Blaton, N., Kinget, R., and Augustijns, P. (2003) Int. J. Pharm., 254: 173185.
88. Drooge, V.J.D., Hinrichs, W.L.J., Wegman, K.A.M., Visser, M.R.A., Eissens, C., and Frijlink, H.W. (2004) Eur. J. Pharm. Biopharm., 21: 511518.
89. Mooter, D.V.G., Weuts, I., Ridder, T.D., and Blaton, N. (2006) Int. J. Pharm., 316: 16.
90. Gong, K., Viboonkiat, R., Rehman, L.U., Buckton, G., and Darr, J.A. (2005) J. Pharm Sci., 94: 25832590.
91. Beten, D.B., Amighi, K., and Moes, A.J. (1995) Pharm. Res., 12: 12691272.
92. Ho, H.O., Shu, H.L., Tsai, T., and Sheu, M.T. T. (1996) Int. J. Pharm., 139: 223229.
93. Overhoff, K.A., Moreno, A., Miller, D.A., Johnston, K.P., and Williams, R.O. (2007) Int. J. Pharm., 336: 122132.
94. Satio, M., Ugajin, T., Nozawa, Y., Sadzuka, Y., Miyagishima, A., and Sonobe, T. (2002) Int. J. Pharm., 249: 7179.
95. Fujii, M., Okada, H., Shibata, Y., Teramachi, H., Kondoh, M., and Watanabe, Y. (2005) Int. J. Pharm., 293: 145153.
96. Reneker, D.H. and Chun, I. (1996) Nanotechnology, 7: 216223.
97. Deitzel, J.M., Kleinmeyer, J., Harris, D., and Beck, T.N.C. (2001) Polym., 42: 261272.
98. Dennis, A.B., Farr, S.J., Kellaway, I.W., Taylor, G., and Davidson, R. (1990) Int. J. Pharm., 65: 85100.
99. Remunan, C., Bretal, M., Nunez, A., and Vila, J.L. (1992) Int. J. Pharm., 80: 151157.
100. Vila, J.L.J., Remunan, C., and Martinez, R. (1990) S.T.P. Pharm., 6: 8892.
101. Sharma, P.K., Chaudhari, P.D., Badagale, M.M., Dave, K.D., Kulkarni, P.A., and Barhate, N.S. (2006) Current trends in solid dispersions techniques. Pharmainfo. Net, 17 May.
102. Gattefosse Technical Brochure. (1999) Pharmaceutical Excipient for Oral Semisolids Formulations, pp. 1215.
103. Sutananta, W., Craig, D.Q.M., and Newton, J.M. (1995) J. Pharm. Pharmacol., 47: 355359.
104. Jones, M.C. and Leroux, J.C. (1999) Eur. J. Pharm. Biopharm., 48: 101108.
105. Vippagunta, S.R., Maul, K.A., Tallavajhala, S., and Grant, D.J.W. (2002) Int. J. Pharm., 236: 111123.
106. Chen, Y., Zhang, G.G.Z., Neilly, J., Marsh, K., Mawhinney, D., and Sanzgiri, Y.D. (2004) Int. J. Pharm., 286: 6980.
107. Lasic, D.D. (1993) Liposomes: From Physics to Applications; Amsterdam, the Netherlands: Elsevier.
108. Zidan, A.S., Habib, M.J., and Khan, M.A. (2007) J. Pharm. Sci., 97: 33883399.
109. Biswas, M., Akogyeram, C.O., Scott, K.R., Potti, G.K., Gallelli, J.F., and Habib, M.J. (1993) J. Controlled Rel., 23: 239245.
110. Hamdani, J., Moes, A.J., and Amighi, K. (2003) Int. J. Pharm., 260: 4757.
111. Chauhan, B., Shimpi, S., and Paradkar, A. (2005) AAPS Pharm. Sci. Tech., 6.
112. Kerc, J. and Srcic, S. (1995) Thermochim. Acta 248: 8195.
113. Giron, D. (1990) Jugosl., 40: 95157.
114. Giron, D. (1995) Thermochim. Acta 248: 159.
115. Leng, Y. (2008) Materials Characterization: Introduction to Microscopic and Spectroscopic Methods. New York: John Wiley.
116. Schafer, R.J. (1994) Dynamic Properties of Rubber: The Glass Transition Temperature. Lippincott and Peto, New York, Rubber World (Magazine=Journal).
117. Plastics Differential Scanning Calorimetry (DSC) Part 2: Determination of Glass Transition Temperature (1999) ISO 11357-2:1999. Distributed through American National Standards Institute (ANSI).
118. Qi, S., Gryczke, A., Belton, P., and Craig, D.Q.M. (2008) Int. J. Pharm., 354: 158167.
119. Gupta, P. and Bansal, A.K. (2005) AAPS Pharm. Sci. Tech., 6: E223E230.
120. Chauhan, B., Shimpi, S., and Paradkar, A. (2005) Eur. J. Pharm. Sci., 26: 219230.
121. Fini, A., Cavallari, C., and Ospitali, F. (in press) Eur. J Pharm Biopharm., 70: 409420.
122. Dong, Z., Chatterji, A., Sandhu, H., Choi, D.S., Chokshi, H., and Shah, N. (2008) Int. J. Pharm., 355: 141149.
123. Wang, X., Armas, H.N., Blaton, N., Michoel, A., and Mooter, G.V. (2007) Int. J. Pharm., 345: 95100.
124. Vrentas, J.S. and Vrentas, C.M. (1991) Macromolecules, 24: 24042412.
125. Andronis, V., Yoshioka, M., and Zografi, G. (1997) J. Pharm. Sci., 86: 346351.
126. Galop, M. (2005) Pharm. Res., 22: 293302.
127. Hasegawa, S., Hamaura, T., Furuyama, N., Horikawa, S., Kusai, A., Yonemochi, E., and Terada, K. (2004) Int. J. Pharm., 280: 3946.
128. Parikh, D.M. (1997) Handbook of Pharmaceutical Granulation Technology; New York: Marcel Dekker.
129. Bikiaris, D., Papageorgiou, G.J., Stergiou, A., Pavlidou, E., Karavas, E., Kanaze, F., and Georgarakis, M. (2005) Therm. Acta 439: 5867.
130. Karavas, E., Ktistis, G., Xenakis, A., and Georgarakis, E. (2006) Eur J. Pharm. Biopharm., 63: 103114.
131. Schachter, D.M., Xiong, J., and Tirol, G.C. (2004) Int. J. Pharm., 281: 89101.