Dissolution studies in vitro as a prognostic tool for oral absorption of modified release pharmaceutical dosage forms;A dissolução in vitro na previsão da absorção oral de fármacos em formas farmacêuticas de liberação modificada

Revista Brasileira de Ciencias Farmaceuticas/Brazilian Journal of Pharmaceutical Sciences

Volumn 38, Issue 4, 2002, Pages 375-399

  Manadas, Rui ^a   Pina, Maria Eugénia ^a   Veiga, Francisco ^a  

^a UNIVERSITY OF COIMBRA   (Portugal)

Author keywords

Absorption; Dissolution models; Hydrodynamics; In vitro dissolution; Modified release

Indexed keywords

DOSE RESPONSE; DRUG ABSORPTION; DRUG RELEASE; DRUG RESEARCH; DRUG SOLUBILITY; GASTROINTESTINAL ABSORPTION; HYDRODYNAMICS; INTESTINE; PHARMACEUTICS; REVIEW; VALIDATION PROCESS;

EID: 0036825614     PISSN: 15169332     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (90)

1. ADAMS, E., COOMANS, D., SMEYERS-VERBEKE, J., MASSART, D. L. Application of linear mixed effects models to the evaluation of dissolution profiles. Int. J. Pharm., Amsterdam, v. 226, n. 1-2, p. 107-125, 2001a.
2. ADAMS, E., DE MAESSCHALCK, R., DE SPIEGELEER, B., VANDER HEYDEN, Y., SMEYERS VERBEKE, J., MASSART, D. L. Evaluation of dissolution profiles using principal component analysis. Int. J. Pharm., Amsterdam, v. 212, n. 1, p. 41-53, 2001b.
3. AIACHE, J. M., AOYAGI, N., BLUME, H., DRESSMAN, J., FRIEDEL, H. D., GRADY, L. T., GRAY, V., HELBOE, P., HUBERT, B., KOPP-KUBEL, S., KRÄMER, J., KRISTENSEN, H., LANGENBUCHER, F., LEESON, L., LESKO, L., LIMBERG, J., MCGILVERAY, I., MÖLLER, H., QURESHI, S., SHAH, V. P., SIEWERT, M., SÜVERKRÜP, R., WALTERSSON, J. O., WHITEMAN, D., WIRBITZKI, E. FIP Guidelines for dissolution testing of solid oral products. Dissol. Technol., Liberty, v. 4, n. 4, p. 5-14, 1997.
4. AMIDON, G. L., LENNERNAS, H., SHAH, V. P., CRISON, J. R. Theoretical basis for a biopharmaceutic drug classification: correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res., New York, v. 12, n. 3, p. 413-420, 1995.
5. BAKER, R. W., LONSDALE, H. S. Controlled release: mechanisms and rates. In: TAQUARY, A. C., LACEY, R. E., eds. Controlled release of biologicaly active agents. New York: Plenum Press, 1974. p. 15-71.
6. BANAKAR, U. V. Pharmaceutical Dissolution Testing. DEKKER, M., ed., New York: Marcel Dekker, 1992. p.55-100.
7. BAYOMI, M. A., AL SUWAYEH, S. A., EL HELW, A. R. Excipient-excipient interaction in the design of sustainedrelease theophylline tablets: in vitro and in vivo evaluation. Drug Dev. Ind. Pharm., New York, v. 27, n. 6, p. 499-506, 2001.
8. BHANJA, R. S., PAL, T. K. In vitro release kinetics of salbutamol sulfate microcapsules coated with both Eudragit RS 100 and Eudragit RL 100. Drug Dev. Ind. Pharm., New York, v. 20, n. 3, p. 375-386, 1994.
9. BONNY, J. D., LEUENBERGER, H. Matrix type controlled release systems. Part 1. Effects of percolation on drug dissolution kinetics. Pharm. Acta Helv., Amsterdam, v. 66, n. 5 -6, p. 160-164, 1991.
10. BONNY, J. D., LEUENBERGER, H. Matrix type controlled release systems. Part 2. Percolation effects in nonswellable matrices. Pharm. Acta Helv., Amsterdam, v. 68, n. 1, p. 25-33, 1993.
11. BRAZEL, C. S., PEPPAS, N. A. Modeling of drug release from swellable polymers. Eur. J Pharm. Biopharm., Amsterdam, v. 49, n. 1, p. 47-58, 2000.
12. BRITISH PHARMACOPOEIA. London: HMSO, 1993. A160-162, A403, A514.
13. CHANG, R. K., PRICE, J., WHITWORTH, C. W. Control of drug release rate by use of mixtures of polycaprolactone and cellulose acetate butyrate polymers. Drug Dev. Ind. Pharm., New York, v. 13, n. 6, p. 1119-1135, 1987.
14. COBBY, J., MAYERSOHN, M., WALKER, G. C. Influence of shape factors on kinetics of drug release from matrix tablets. I. Theoretical. J Pharm. Sci., New York, v. 63, n.5, p. 725-732, 1974a.
15. COBBY, J., MAYERSOHN, M., WALKER, G. C. Influence of shape factors on kinetics of drug release from matrix tablets. II. Experimental. J. Pharm. Sci., New York, v. 63, n. May, p. 732-737, 1974b.
16. COLOMBO, P., BETTINI, R., MASSIMO, G., CATELLANI, P. L., PEPPAS, N. A. Drug diffusion front movement is important in drug release control from swellable matrix tablets. J. Pharm. Sci., New York, v. 84, n. Aug, p. 991-997, 1995.
17. COSTA, P., LOBO, J. M. S. Formas farmacêuticas de liberação modificada. Rev. Port. Farm., Lisboa, v. 59, n. 4, p. 181-190, 1999.
18. COSTA, P., LOBO, J. M. S. Influence of dissolution medium agitation on release profiles of sustained-release tablets. DrugDev. Ind. Pharm., New York, v. 27, n. 8, p. 811-817, 2001a.
19. COSTA, P., LOBO, J. M. S. Modeling and comparison of dissolution profiles. Eur. J. Pharm. Sci., Amsterdam, v. 13, n. 2, p. 123-133, 2001b.
20. COX, D. C., DOUGLAS, C. C., FURMAN, W. B., KIRCHHOEFER, R. D., MYRICK, J. W. Guidelines for dissolution testing. Pharm. Technol., New York, v. 2, p. 41-53, 1978.
21. DE LA CRUZ PASTRANA, Y., BOZA RIVERA, A., ESPINO ENRIQUE, T., CARABALLO, I. Pharmacokinetic characterization of oral sustained release formulations: factors that influence pharmacokinetic profiles. Acta Farm. Bonaerense, La Plata, v. 19, p. 25-34, 2000.
22. DIGHE, S. V. Development of dissolution tests for immediate release and modified release oral dosage forms. Stuttgart: Medpharm Scientific Publishers, 1993. p.15-28.
23. DRESSMAN, J. B., AMIDON, G. L., REPPAS, C., SHAH, V. P. Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms. Pharm. Res., New York, v. 15, n. 1, p. 11-22, 1998.
24. DRESSMAN, J. B., FLEISHER, D. Mixing tank model for predicting dissolution rate control of oral absorption. J. Pharm. Sci., New York, v. 75, n. 2, p. 109-116, 1986.
25. EEC-DIRECTIVE-75/318. Quality of prolonged release oral solid dosage forms. London: 1992. p.2-8.
26. EL ARINI, S. K., LEUENBERGER, H. Modeling of drug release from polymer matrices: effect of drug loading. Int. J. Pharm., Amsterdam, v. 121, n.25, p. 141-148, 1995.
27. EL ARINI, S. K., LEUENBERGER, H. Dissolution properties of praziquantel-PVP systems. Pharm. Acta. Helv., Amsterdan, v. 73, n. 2, p. 89-94, 1998.
28. EUROPEAN PHARMACOPOEIA. London: EDQM, 1997. p. 194-198.
29. EUROPE, C. O. Standard Terms - Pharmaceutical dosage forms, routes of administration, containers. London: Pharmeuropa, 2000. p. 13-28.
30. FARINHA, A., BICA, A., TOSCANO, C., CAMPOS, R. C. Os ensaios de liberação in vitro na avaliação da qualidade biofarmacêutica de formas sólidas e semi-sólidas. LEF Boletim, Lisboa, v. 7, n. 26, p. 1-8, 2000.
31. FARINHA, A., PAIS, J. P., BICA, A. O ensaio de dissolução in vitro na avaliação da qualidade biofarmacêutica. LEF - Boletim, Lisboa, v. 4, n. 15, p. 1-7, 1997.
32. FDA-CDER. Guidance for industry, immediate release solid oral dosage forms, scale-up and post-approval changes: chemistry, manufacturing and controls, in vitro dissolution testing, and in vivo bioequivalence documentation. Rockville: Food and Drug Administration, 1995. p. 2-25.
33. FDA-CDER. Guidance for industry. Extended release oral dosage forms: development, evaluation, and application of in vitro/in vivo correlations. Rockville: Food and Drug Administration, 1997a. p. 1-24.
34. FDA-CDER. Guidance for Industry. Dissolution testing of immediate release solid oral dosage forms. Rockville: Food and Drug Administration, 1997b. p. 17.
35. FINHOLT, P., SOLVANG, S. Dissolution kinetics of drugs in human gastric juice - the role of surface tension. J. Pharm. Sci., New York, v. 57, n. 8, p. 1322-1326, 1968.
36. FORD, J. L., MITCHELL, K., ROWE, P., ARMSTRONG, D. J., ELLIOTT, P. N. C., ROSTRON, C., HOGAN, J. E. Mathematical modeling of drug release from hydroxypropylmethylcellulose matrices: effect of temperature. Int. J. Pharm., Amsterdam, v. 71, p. 95-104, 1991.
37. GIBALDI, M., FELDMAN, S. Establishment of sink conditions in dissolution rate determinations - theoretical considerations and application to nondisintegrating dosage forms. J. Pharm. Sci., New York, v. 56, p. 1238-1242, 1967.
38. GINSKI, M. J., POLLI, J. E. Prediction of dissolution-absorption relationships from a dissolution/Caco-2 system. Int. J. Pharm., Amsterdam, v. 177, n. 1, p. 117-125, 1999.
39. HANSON, W. A. Handbook of Dissolution Testing. New York: Aster, 1991. p. 13-52.
40. HANSON-RESEARCH-CORPORATION. Dissolution: Past, Present & Future. 2. ed. Chatsworth: Hanson Research, 1996. p.2-12.
41. HARLAND, R. S., GAZZANIGA, A., SANGALLI, M. E., COLOMBO, P., PEPPAS, N. A. Drug/polymer matrix swelling and dissolution. Pharm. Res., New York, v. 5, n. Aug, p. 488-494, 1988.
42. HIGUCHI, T. Rate of release of medicaments from ointment bases containing drugs in suspension. J. Pharm. Sci., New York, v. 50, p. 874-875, 1961.
43. HIGUCHI, T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J. Pharm. Sci., New York, v. 52, p. 1145-1149, 1963.
44. HIGUCHI, T., DAYAL, S., PITMAN, I. H. Effects of solute-solvent complexation reactions on dissolution kinetics: testing of a model by using a concentration jump technique. J. Pharm. Sci., New York, v. 61, n. 5, p. 695-700, 1972.
45. HOPFENBERG, H. B. Controlled release polymeric formulations. Washignton: American Chemical Society, 1976. p. 7-23.
46. INFARMED. Farmacopeia Portuguesa VI, Lisboa, 1997. p. 116-121.
47. JUN, H. W., LAI, J. W. Preparation and in vitro dissolution tests of egg albumin microcapsules of nitrofurantoin. Int. J. Pharm., Amsterdam, v. 16, p. 65 -77, 1983.
48. KATORI, N., AOYAGI, N., TERAO, T. Estimation of agitation intensity in the GI tract in humans and dogs based on in vitro/in vivo correlation. Pharm. Res., New York, v. 12, p. 237-243, 1995.
49. KATZHENDLER, I., HOFFMAN, A., GOLDBERGER, A., FRIEDMAN, M. Modeling of drug release from erodible tablets. J. Pharm. Sci., New York, v. 86, n. 1, p. 110-115, 1997.
50. KHAN, K. A. Concept of dissolution efficiency. J. Pharm. Pharmacol., London, v. 27, p. 48-49, 1975.
51. KIM, H., FASSIHI, R. Application of a binary polymer system in drug release rate modulation. Part 1. Characterization of release mechanism. J. Pharm. Sci., New York, v. 86, p. 316-322, 1997a.
52. KIM, H., FASSIHI, R. Application of binary polymer system in drug release rate modulation. 2. Influence of formulation variables and hydrodynamic conditions on release kinetics. J. Pharm. Sci., New York, v. 86, n. 3, p. 323-328, 1997b.
53. KITAZAWA, S., JOHNO, I., MINOUCHI, T., OKADA, J. Interpretation of dissolution rate data from in vitro testing of compressed tablets. J. Pharm. Pharmacol., London, v. 29, n. 8, p. 453-459, 1977.
54. KOBAYASHI, M., SADA, N., SUGAWARA, M., ISEKI, K., MIYAZAKI, K. Development of a new system for prediction of drug absorption that takes into account drug dissolution and pH change in the gastro-intestinal tract. Int. J. Pharm., Amsterdam, v. 221, n. 1-2, p. 87-94, 2001.
55. KORSMEYER, R. W., GURNY, R., DOELKER, E., BURI, P., PEPPAS, N. A. Mechanisms of solute release from porous hydrophilic polymers. Int. J. Pharm. Amsterdam, v. 15, p. 25-35, 1983.
56. LANGENBUCHER, F. In vitro assessment of dissolution kinetics: description and evaluation of a column-type method. J. Pharm. Sci., New York, v. 58, n. 10, p. 1265-1272, 1969.
57. LANGENBUCHER, F. Linearization of dissolution rate curves by the Weibull distribution. J. Pharm. Pharmacol., London, v. 24, p. 979-981, 1972.
58. LIN, S. Y., YANG, J. C. In-vitro dissolution behavior of some sustained-release theophylline dosage forms. Pharm. Acta Helv., Amsterdam, v. 64, n. 8, p. 236-240, 1989.
59. MACHERAS, P., KOUPPARIS, M., APOSTOLELLI, E. Dissolution of 4 controlled release theophylline formulations in milk. Int. J. Pharm., Amsterdam, v. 36, n. 4, p. 73-79, 1987.
60. MACHERAS, P., REPPAS, C., DRESSMAN, J. B. Biopharmaceutics of orally administered dosage forms. Chiester: Taylor & Francis, 1995. p.75-91.
61. MITHANI, S. D., BAKATSELOU, V., TENHOOR, C. N., DRESSMAN, J. B. Estimation of the increase in solubility of drugs as a function of bile salt concentration. Pharm. Res., New York, v. 13, p. 163-167, 1996.
62. MOLLER, H., SIEWERT, M. FIP guidelines for dissolution testing of solid oral products. Pharm. Ind., Aulendorf, v. 57, n. 5, p. 362-369, 1995.
63. MOORE, J. W., FLANNER, H. H. Mathematical comparison of dissolution profiles. Pharm. Technol., New York, v. 20, p. 64-74, 1996.
64. MULYE, N. V., TURCO, S. J. A simple model based on first order kinetics to explain release of highly water soluble drugs from porous dicalcium phosphate dihydrate matrices. Drug Dev. Ind. Pharm., New York, v. 21, n. 8, p. 943-953, 1995.
65. OFOEFULE, S. I., OKOLI, S. E., CHUKWU, A. Mechanisms behind sustained release matrix tablets prepared with poly(acrylic) acid polymers. Acta Pharm., v. 50, n. 3, p. 229-238, 2000.
66. O'HARA, T., DUNNE, A., BUTLER, J., DEVANE, J. A review of methods used to compare dissolution profile data. Pharm. Sci. Technol. Today, New York, v. 1, p. 214-223, 1998.
67. PAGLIARA, A., REIST, M., GEINOZ, S., CARRUPT, P. A., TESTA, B. Evaluation and prediction of drug permeation. J. Pharm. Pharmacol., London, v. 51, n. 12, p. 1339-1357, 1999.
68. PEPPAS, N. A. Relation between the structure of polymers and the controlled release of active ingredients. Pharm. Acta Helv., Amsterdam, v. 58, p. 2-8, 1983.
69. PEPPAS, N. A. Analysis of fickian and non-fickian drug release from polymers. Pharm. Acta Helv., Amsterdam, v. 60, n. 110-1, p. 1985.
70. PILLAY, V., FASSIHI, R. In vitro release modulation from cross-linked pellets for site-specific drug delivery to the gastrointestinal tract. Part 1. Comparison of pH-responsive drug release and associated kinetics. J. Controlled Release, Amsterdam, v. 59, 20, p. 229-242, 1999.
71. POLLI, J. E., REKHI, G. S., AUGSBURGER, L. L., SHAH, V. P. Methods to compare dissolution profiles and a rationale for wide dissolution specifications for metoprolol tartrate tablets. J. Pharm. Sci., New York, v. 86, n. Jun, p. 690-700, 1997.
72. POLLI, J. E., REKHI, G. S., SHAH, V. P. Methods to compare dissolution profiles. Drug Inf. J., East Hanover, v. 30, n. 4, p. 1113-1120, 1996.
73. PREECHAGOON, D., UDOMPRATEEP, A., MANWIWATTANAGUL, G. Improved dissolution rate of poorly soluble drug by incorporation of buffers. Drug Dev. Ind. Pharm., New York, v. 26, n. 8, p. 891-894, 2000.
74. PRISTA, L. N., ALVES, A. C., MORGADO, R. Tecnologia farmacêutica. Lisboa: Fundação Calouste Gulbenkian, 1996. p. 2171-2191.
75. QURESHI, S. A., MCGILVERAY, I. J. Typical variability in drug dissolution testing: study with USP and FDA calibrator tablets and a marketed drug (glibenclamide) product. Eur. J. Pharm. Sci., Amsterdam, v. 7, n. 3, p. 249-258, 1999.
76. QURESHI, S. A., SHABNAM, J. Cause of high variability in drug dissolution testing and its impact on setting tolerances. Eur. J. Pharm. Sci., Amsterdam, v. 12, n. 3, p. 271-276, 2001.
77. ROY, D., DUCHER, F., LAUMAIN, A., LEGENDRE, J. Y. Determination of the aqueous solubility of drugs using a convenient 96 well plate based assay. Drug Dev. Ind. Pharm., New York, v. 27, n. 1, p. 107-109, 2001.
78. SALOMON, J. L., DOELKER, E. Formulation of prolonged release tablets. Part 1. Inert matrices. Pharm. Acta Helv., Amsterdam, v. 55, n. 6, p. 174-182, 1980.
79. SANGALLI, M. E., GIUNCHEDI, P., MAGGI, L., CONTE, U., GAZZANIGA, A. Inert monolithic device with a central hole for constant drug release. Eur. J. Pharm. Biopharm., Amsterdam, v. 40, p. 370-373, 1994.
80. SHUKLA, A. J., PRICE, J. C. Effect of drug (core) particle size on the dissolution of theophylline from microspheres made from low molecular weight cellulose acetate propionate. Pharm. Res., New York, v. 6, n. 5, p. 418-421, 1989.
81. SIEVERT, B., SIEWERT, M. Dissolution tests for ER products. Dissol. Technol., Liberty, v. 5, n. 4, p. 5-11, 1998.
82. TONGWEN, X., BINGLIN, H. Mechanism of drug release into a perfect sink from a coated planar matrix with a super saturation loading in the core. Int. J. Pharm., Amsterdam, v. 197, n. p. 23-34, 2000.
83. UNITED STATES PHARMACOPEA. Rockville, Webcom Limited, 2002. p. 2011-2022.
84. VAN VOOREN, L., KRIKILION, G., ROSIER, J., DE SPIEGELEER, B. A novel bending point criterion for dissolution profile interpretation. Drug Dev. Ind. Pharm., New York, v. 27, n. 8, p. 885-892, 2001.
85. VARELAS, C. G., DIXON, D. G., STEINER, C. A. Zero-order release from biphasic polymer hydrogels. J. Controlled Release, Amsterdam, v. 34, p. 185-192, 1995.
86. VEIGA, F. Medicamentos orais de liberação controlada. Comprimidos matriciais hidrófilos. Bol. Fac. Farm. Coimbra, Coimbra, v. 12, n. 2, p. 17-87, 1988.
87. WAGNER, J. G. Interpretation of percent dissolved-time plots derived from In vitro testing of conventional tablets and capsules. J. Pharm. Sci., New York, v. 58, p. 1253-1257, 1969.
88. YUKSEL, N., KANIK, A. E., BAYKARA, T. Comparison of in vitro dissolution profiles by ANOVA-based, model-dependent and -independent methods. Int. J. Pharm., Amsterdam, v. 209, p. 57-67, 2000.
89. ZHANG, Y. E., SCHWARTZ, J. B. Effect of diluents on tablet integrity and controlled drug release. Drug Dev. Ind. Pharm., New York, v. 26, n. 7, p. 761-765, 2000.
90. ZULEGER, S., LIPPOLD, B. C. Polymer particle erosion controlling drug release. I. Factors influencing drug release and characterization of the release mechanism. Int. J Pharm., Amsterdam, v. 217, n. 1-2, p. 139-152, 2001.