Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs

Drug Discovery Today

Volumn 12, Issue 23-24, 2007, Pages 1068-1075

  Vasconcelos, Teófilo ^a,b   Sarmento, Bruno ^a   Costa, Paulo ^a  

^a UNIVERSITY OF PORTO   (Portugal)

^b DEPARTMENT OF RESEARCH AND DEVELOPMENT   (Portugal)

Author keywords

[No Author keywords available]

Indexed keywords

CHLORAMPHENICOL; SULFATHIAZOLE;

CRYSTALLIZATION; DISPERSION; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG MANUFACTURE; DRUG RESEARCH; DRUG SOLUBILITY; MELTING POINT; PARTICLE SIZE; PHYSICAL CHEMISTRY; REVIEW; WETTABILITY;

ADMINISTRATION, ORAL; BIOLOGICAL AVAILABILITY; DOSAGE FORMS; HUMANS; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; WATER;

EID: 36549042006     PISSN: 13596446     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.drudis.2007.09.005     Document Type: Review

References (88)

1. Youn Y.S., et al. Improved intestinal delivery of salmon calcitonin by Lys18-amine specific PEGylation: Stability, permeability, pharmacokinetic behavior and in vivo hypocalcemic efficacy. J. Contr. Release 114 (2006) 334-342
2. Sugawara M., et al. The use of an in vitro dissolution and absorption system to evaluate oral absorption of two weak bases in pH-independent controlled-release formulations. Eur. J. Pharm. Sci. 26 (2005) 1-8
3. Ikegami K., et al. Bioavailability and in vivo release behavior of controlled-release multiple-unit theophylline dosage forms in beagle dogs, cynomolgus monkeys, and göttingen minipigs. J. Pharm. Sci. 95 (2006) 1888-1895
4. Charman S.A., and Charman W.N. Oral modified-release delivery systems. In: Rathbone M.J., et al. (Ed). Modified-Release Drug Delivery Technology (2003), Marcel Dekker 1-10
5. van Drooge D.J., et al. Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale, using differential scanning calorimetry and gravimetric water vapour sorption techniques. Int. J. Pharm. 310 (2006) 220-229
6. Vippagunta S.R., et al. Factors affecting the formation of eutectic solid dispersions and their dissolution behavior. J. Pharm. Sci. 96 (2006) 294-304
7. Pouton C.W. Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system. Eur. J. Pharm. Sci. 29 (2006) 278-287
8. Bogdanova S., et al. Interactions of poly(vinylpyrrolidone) with ibuprofen and naproxen: experimental and modeling studies. Pharm. Res. 22 (2005) 806-815
9. Streubel A., et al. Drug delivery to the upper small intestine window using gastroretentive technologies. Curr. Opin. Pharmacol. 6 (2006) 501-508
10. Gardner D., et al. The intelisite capsule: a new easy to use approach for assessing regional drug absortion from gastrointestinal tract. Pharm. Tech. Eur. 9 (1997) 46-53
11. Desai J., et al. Characterization of polymeric dispersions of dimenhydrinate in ethyl cellulose for controlled release. Int J Pharm 308 (2006) 115-123
12. Tanaka N., et al. Development of novel sustained-release system, disintegration-controlled matrix tablet (DCMT) with solid dispersion granules of nilvadipine (II): In vivo evaluation. J. Contr. Release 112 (2006) 51-56
13. Ohara T., et al. Dissolution mechanism of poorly water-soluble drug from extended release solid dispersion system with ethylcellulose and hydroxypropylmethylcellulose. Int. J. Pharm. 302 (2005) 95-102
14. Leuner C., and Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm. 50 (2000) 47-60
15. Majerik V., et al. Bioavailability enhancement of an active substance by supercritical antisolvent precipitation. J. Supercrit. Fluids 40 (2007) 101-110
16. Prabhu S., et al. Novel lipid-based formulations enhancing the in vitro dissolution and permeability characteristics of a poorly water-soluble model drug, piroxicam. Int. J. Pharm. 301 (2005) 209-216
17. Sekiguchi K., and Obi N. Studies on Absorption of Eutectic Mixture. Ii. Absorption of Fused Conglomerates of Chloramphenicol and Urea in Rabbits. Chem. Pharm. Bull (Tokyo) 12 (1964) 134-144
18. Sekiguchi K., and Obi N. Studies on absorption of eutectic mixtures. I. A comparison of the behavior of eutectic mixtures of sulphathiazole and that of ordinary sulphathiazole in man. Chem. Pharm. Bull. 9 (1961) 866-872
19. Levy G. Effect of particle size on dissolution and gastrointestinal absorption rates of pharmaceuticals. Am. J. Pharm. Sci. Support Public Health 135 (1963) 78-92
20. Kanig J.L. Properties of Fused Mannitol in Compressed Tablets. J. Pharm. Sci. 53 (1964) 188-192
21. Goldberg A.H., et al. Increasing dissolution rates and gastrointestinal absorption of drugs via solid solutions and eutectic mixtures. IV. Chloramphenicol--urea system. J. Pharm. Sci. 55 (1966) 581-583
22. Simonelli A.P., et al. Dissolution rates of high energy polyvinylpyrrolidone (PVP)-sulfathiazole coprecipitates. J. Pharm. Sci. 58 (1969) 538-549
23. Chiou W.L., and Riegelman S. Preparation and dissolution characteristics of several fast-release solid dispersions of griseofulvin. J. Pharm. Sci. 58 (1969) 1505-1510
24. Urbanetz N.A. Stabilization of solid dispersions of nimodipine and polyethylene glycol 2000. Eur. J. Pharm. Sci. 28 (2006) 67-76
25. Vilhelmsen T., et al. Effect of a melt agglomeration process on agglomerates containing solid dispersions. Int. J. Pharm. 303 (2005) 132-142
26. Karavas E., et al. Application of PVP/HPMC miscible blends with enhanced mucoadhesive properties for adjusting drug release in predictable pulsatile chronotherapeutics. Eur. J. Pharm. Biopharm. 64 (2006) 115-126
27. Drooge D.J.V., et al. Characterization of the Mode of Incorporation of Lipophilic Compounds in Solid Dispersions at the Nanoscale Using Fluorescence Resonance Energy Transfer (FRET). Macromol. Rapid Commun. 27 (2006) 1149-1155
28. g drug. Powder Technol. 167 (2006) 20-25
29. Hasegawa S., et al. Effects of water content in physical mixture and heating temperature on crystallinity of troglitazone-PVP K30 solid dispersions prepared by closed melting method. Int. J. Pharm. 302 (2005) 103-112
30. Lloyd G.R., et al. A calorimetric investigation into the interaction between paracetamol and polyethlene glycol 4000 in physical mixes and solid dispersions. Eur. J. Pharm. Biopharm. 48 (1999) 59-65
31. Yoshihashi Y., et al. Estimation of physical stability of amorphous solid dispersion using differential scanning calorimetry. J. Therm. Anal. Calorim. 85 (2006) 689-692
32. Guyot M., et al. Physicochemical characterization and dissolution of norfloxacin/cyclodextrin inclusion compounds and PEG solid dispersions. Int. J. Pharm. 123 (1995) 53-63
33. Yao W.-W., et al. Thermodynamic properties for the system of silybin and poly(ethylene glycol) 6000. Thermochim. Acta 437 (2005) 17-20
34. Chiou W.L., and Riegelman S. Oral absorption of griseofulvin in dogs: increased absorption via solid dispersion in polyethylene glycol 6000. J. Pharm. Sci. 59 (1970) 937-942
35. Ceballos A., et al. Influence of formulation and process variables on in vitro release of theophylline from directly-compressed Eudragit matrix tablets. Il Farmaco 60 (2005) 913-918
36. Huang J., et al. Nifedipine solid dispersion in microparticles of ammonio methacrylate copolymer and ethylcellulose binary blend for controlled drug delivery: Effect of drug loading on release kinetics. Int. J. Pharm. 319 (2006) 44-54
37. Won D.-H., et al. Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process. Int. J. Pharm. 301 (2005) 199-208
38. Konno H., and Taylor L.S. Influence of different polymers on the crystallization tendency of molecularly dispersed amorphous felodipine. J. Pharm. Sci. 95 (2006) 2692-2705
39. 2 as a temporary plasticizer. Int. J. Pharm. 327 (2006) 45-50
40. Tanaka N., et al. Development of novel sustained-release system, disintegration-controlled matrix tablet (DCMT) with solid dispersion granules of nilvadipine. J. Contr. Release 108 (2005) 386-395
41. Rodier E., et al. A three step supercritical process to improve the dissolution rate of Eflucimibe. Eur. J. Pharm. Sci. 26 (2005) 184-193
42. Garcia-Zubiri I.X., et al. Thermal stability of solid dispersions of naphthalene derivatives with [beta]-cyclodextrin and [beta]-cyclodextrin polymers. Thermochim. Acta 444 (2006) 57-64
43. Van den Mooter G., et al. Evaluation of Inutec SP1 as a new carrier in the formulation of solid dispersions for poorly soluble drugs. Int. J. Pharm. 316 (2006) 1-6
44. Chiou W.L., and Riegelman S. Pharmaceutical applications of solid dispersion systems. J. Pharm. Sci. 60 (1971) 1281-1302
45. Karata A., et al. Improved solubility and dissolution rate of piroxicam using gelucire 44/14 and labrasol. Il Farmaco 60 (2005) 777-782
46. Damian F., 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. 10 (2000) 311-322
47. Li F.-Q., et al. In vitro controlled release of sodium ferulate from Compritol 888 ATO-based matrix tablets. Int. J. Pharm. 324 (2006) 152-157
48. Chauhan B., et al. Preparation and evaluation of glibenclamide-polyglycolized glycerides solid dispersions with silicon dioxide by spray drying technique. Eur. J. Pharm. Sci. 26 (2005) 219-230
49. Yuksel N., et al. Enhanced bioavailability of piroxicam using Gelucire 44/14 and Labrasol: in vitro and in vivo evaluation. Eur. J. Pharm. Biopharm. 56 (2003) 453-459
50. Dannenfelser R.M., et al. Development of clinical dosage forms for a poorly water soluble drug I: Application of polyethylene glycol-polysorbate 80 solid dispersion carrier system. J. Pharm. Sci. 93 (2004) 1165-1175
51. Cutler L., et al. Development of a P-glycoprotein knockout model in rodents to define species differences in its functional effect at the blood-brain barrier. J. Pharm. Sci. 95 (2006) 1944-1953
52. Serajuddin A.T. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs. J. Pharm. Sci. 88 (1999) 1058-1066
53. Karavas E., et al. Effect of hydrogen bonding interactions on the release mechanism of felodipine from nanodispersions with polyvinylpyrrolidone. Eur. J. Pharm. Biopharm. 63 (2006) 103-114
54. Craig D.Q.M. The mechanisms of drug release from solid dispersions in water-soluble polymers. Int. J. Pharm. 231 (2002) 131-144
55. Muhrer G., et al. Use of compressed gas precipitation to enhance the dissolution behavior of a poorly water-soluble drug: Generation of drug microparticles and drug-polymer solid dispersions. Int. J. Pharm. 308 (2006) 69-83
56. Rasenack N., and Muller B.W. Micron-size drug particles: common and novel micronization techniques. Pharm. Dev. Technol. 9 (2004) 1-13
57. Vasanthavada M., et al. Phase behavior of amorphous molecular dispersions I: Determination of the degree and mechanism of solid solubility. Pharm. Res. 21 (2004) 1598-1606
58. Johari G.P., et al. Dielectric studies of molecular motions in amorphous solid and ultraviscous acetaminophen. J. Pharm. Sci. 94 (2005) 2207-2223
59. Wang X., et al. Solid state characteristics of ternary solid dispersions composed of PVP VA64, Myrj 52 and itraconazole. Int. J. Pharm. 303 (2005) 54-61
60. Ghaderi R., et al. Preparation of biodegradable microparticles using solution-enhanced dispersion by supercritical fluids (SEDS). Pharm. Res. 16 (1999) 676-681
61. Bikiaris D., et al. Physicochemical studies on solid dispersions of poorly water-soluble drugs: Evaluation of capabilities and limitations of thermal analysis techniques. Thermochim. Acta 439 (2005) 58-67
62. Kang B.K., et al. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int. J. Pharm. 274 (2004) 65-73
63. Ghebremeskel A.N., et al. Use of surfactants as plasticizers in preparing solid dispersions of poorly soluble API: Selection of polymer-surfactant combinations using solubility parameters and testing the processability. Int. J. Pharm. 328 (2007) 119-129
64. Vasconcelos, T. and Costa, P. (2007) Development of a rapid dissolving ibuprofen solid dispersion. In PSWC - Pharmaceutical Sciences Wolrd Conference
65. Taylor L.S., and Zografi G. Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions. Pharm. Res. 14 (1997) 1691-1698
66. Zhou D., et al. A calorimetric investigation of thermodynamic and molecular mobility contributions to the physical stability of two pharmaceutical glasses. J. Pharm. Sci. 96 (2007) 71-83
67. Yoshioka M., et al. Crystallization of indomethacin from the amorphous state below and above its glass transition temperature. J. Pharm. Sci. 83 (1994) 1700-1705
68. Gunawan L., et al. Structural relaxation of acetaminophen glass. Pharm. Res. 23 (2006) 967-979
69. Zhou D., et al. Physical stability of amorphous pharmaceuticals: Importance of configurational thermodynamic quantities and molecular mobility. J. Pharm. Sci. 91 (2002) 1863-1872
70. Shmeis R.A., et al. A mechanistic investigation of an amorphous pharmaceutical and its solid dispersions, part I: a comparative analysis by thermally stimulated depolarization current and differential scanning calorimetry. Pharm. Res. 21 (2004) 2025-2030
71. Bhugra C., et al. Prediction of the onset of crystallization of amorphous sucrose below the calorimetric glass transition temperature from correlations with mobility. J. Pharm. Sci. 96 (2007) 1258-1269
72. Vasanthavada M., et al. Phase behavior of amorphous molecular dispersions II: Role of hydrogen bonding in solid solubility and phase separation kinetics. Pharm. Res. 22 (2005) 440-448
73. Schachter D.M., et al. Solid state NMR perspective of drug-polymer solid solutions: a model system based on poly(ethylene oxide). Int. J. Pharm. 281 (2004) 89-101
74. Teberekidis V.I., and Sigalas M.P. Theoretical study of hydrogen bond interactions of felodipine with polyvinylpyrrolidone and polyethyleneglycol. THEOCHEM 803 (2006) 29-38
75. Van den Mooter G., et al. Physical stabilisation of amorphous ketoconazole in solid dispersions with polyvinylpyrrolidone K25. Eur. J. Pharm. Sci. 12 (2001) 261-269
76. Weuts I., et al. Salt formation in solid dispersions consisting of polyacrylic acid as a carrier and three basic model compounds resulting in very high glass transition temperatures and constant dissolution properties upon storage. Eur. J. Pharm. Sci. 25 (2005) 387-393
77. Owusu-Ababio G., et al. Comparative dissolution studies for mefenamic acid-polyethylene glycol solid dispersion systems and tablets. Pharm. Dev. Technol. 3 (1998) 405-412
78. Timko R.J., and Lordi N.G. Thermal characterization of citric acid solid dispersions with benzoic acid and phenobarbital. J. Pharm. Sci. 68 (1979) 601-605
79. Lin C.-W., and Cham T.-M. Effect of particle size on the available surface area of nifedipine from nifedipine-polyethylene glycol 6000 solid dispersions. Int. J. Pharm. 127 (1996) 261-272
80. Verreck G., et al. The effect of pressurized carbon dioxide as a temporary plasticizer and foaming agent on the hot stage extrusion process and extrudate properties of solid dispersions of itraconazole with PVP-VA 64. Eur. J. Pharm. Sci. 26 (2005) 349-358
81. Breitenbach J., and Lewis J. Two concepts, one technology: controlled release and solid dispersion with meltrex. In: Rathbone M.J., et al. (Ed). Modified-Release Drug Delivery Technology (2003), Marcel Dekker 125-134
82. Gupta M.K., et al. Hydrogen bonding with adsorbent during storage governs drug dissolution from solid-dispersion granules. Pharm. Res. 19 (2002) 1663-1672
83. Seo A., et al. The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer. Int. J. Pharm. 259 (2003) 161-171
84. Verreck G., et al. The effect of supercritical CO2 as a reversible plasticizer and foaming agent on the hot stage extrusion of itraconazole with EC 20 cps. J. Supercrit. Fluids 40 (2007) 153-162
85. Passerini N., et al. Preparation and characterisation of ibuprofen-poloxamer 188 granules obtained by melt granulation. Eur. J. Pharm. Sci. 15 (2002) 71-78
86. Ahuja N., et al. Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers. Eur. J. Pharm. Biopharm. 65 (2007) 26-38
87. Mizuno M., et al. Inhibition of a solid phase reaction among excipients that accelerates drug release from a solid dispersion with aging. Int. J. Pharm. 305 (2005) 37-51
88. Sethia S., and Squillante E. Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method. J. Pharm. Sci. 91 (2002) 1948-1957