Dissolution testing for sustained or controlled release oral dosage forms and correlation with in vivo data: Challenges and opportunities

International Journal of Pharmaceutics

Volumn 140, Issue 2, 1996, Pages 131-143

  Zahirul, M ^a   Khan, I ^a  

^a Res and Development Laboratories   (Australia)

Author keywords

Controlled release; Dissolution media; Dissolution review; Dissolution testing; Extended release; Food effect; In vitro in vivo correlation; Sustained release

Indexed keywords

BUFLOMEDIL; DICLOFENAC; DILTIAZEM; PHENYLPROPANOLAMINE; PROPRANOLOL; THEOPHYLLINE;

BIOAVAILABILITY; DISSOLUTION; DRUG DOSAGE FORM; DRUG FORMULATION; DRUG SOLUBILITY; FOOD DRUG INTERACTION; IONIC STRENGTH; PHARMACOKINETICS; PRIORITY JOURNAL; REVIEW; SUSTAINED RELEASE PREPARATION;

EID: 0030606871     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/0378-5173(96)04561-9     Document Type: Review

References (56)

1. AAPS FDA Workshop Committee, Scale-up of oral extended-release dosage forms. Pharm. Technol., 199(5) (1995) 46, 48, 50, 52, 54.
2. Abrahamsson, B., Johansson, D., Torstensson, A. and Wingstrand, K., Evaluation of solubilizers in the drug release testing of hydrophilic matrix extended-release tablets of felodipine. Pharm. Res., 11 (1994) 1093-1097.
3. Al-Angary, A.A., Khidr, S.H., Mahrous, G.M. and Gouda, M.W., In-vitro dissolution and in-vivo absorption of marketed sustained release theophylline preparations. Int. J. Pharm., 65 (1990) R5-R8.
4. Aoki, S., Uesugi, K., Tatsuishi, K., Ozawa, H. and Kayano, M., Evaluation of the correlation between in vivo and in vitro release of phenylpropanolamine HCl from controlled-release tablets. Int. J. Pharm., 85 (1992) 65-73.
5. Bailer, M., Sussan, S., Salach, O.A., Danenberg, H.D., Ben-David, J., Gibor, Y. and Laor, A., Criteria to assess in vivo performance of sustained release products: application to diltiazem formulations. J. Pharm. Sci., 84 (1995) 1160-1163.
6. Bodmeier, R., Guo, X., Sarabia, R.E. and Skultety, P.F., The influence of buffer species and strength on diltiazem HCl release from beads coated with aqueous cationic polymer dispersions. Eudragit RS, RL 30D. Pharm. Res., 13 (1996) 52-56.
7. Caramella, C., Gazzaniga, A., Iamartino, P. and Ravelli, V., Designing aspects in prolonged-release dosage forms. Pharm. Technol. Eur., 7(2) (1995) 18, 20-26.
8. Chetty, D.J., Ogundeji, M.O., Damani, L.A., Dawes, V.H. and Solomon, M.C., Susceptibility of diclofenac sodium tablet matrix formulations to dissolution test variables. Pharm. Technol. Eur., 6(10) (1994) 28, 32, 34-36, 38.
9. Cohen, J.L., Hubert, B.B., Leeson, L.J., Rhodes, C.T., Robinson, J.R., Roseman, T.J. and Shefter, E., The development of USP dissolution and drug release standards. Pharm. Res., 7 (1990) 983-987.
10. Dahl, T., Ling, T., Yee, J. and Bormeth, A., Effects of various granulating systems on the bioavailability of naproxen sodium from polymeric matrix tablets. J. Pharm. Sci., 79 (1990) 389-392.
11. Davis, S.S., Hardy, J.G., Taylor, M.J., Whalley, D.R. and Wilson, C.G., The effect of food on the gastrointestinal transit of pellets and an osmotic device (Osmet). Int. J. Pharm., 21 (1984) 331-340.
12. Davis, S.S., Khosla, R., Wilson, C.G. and Washington, N., Gastrointestinal transit of a controlled-release pellet formulation of tiaprofenic acid and the effect of food. Int. J. Pharm., 35 (1987) 253-258.
13. Davis, S.S., Khosla, R., Wilson, C.G., Washington, N., Leslie, S.T. and Malkowska, S., The gastrointestinal transit of a controlled release formulation of indomethacin. Int. J. Pharm., 60 (1990) 191-196.
14. Digenis, G.A., Sandefer, E.P., Parr, A.F., Beihn, R., McClain, C., Scheinthal, B.M., Ghebre-Sellassie, I., Iyer, U., Nesbitt, R.U. and Randinitis, E., Gastrointestinal behaviour of orally administered radiolabeled erythromycin pellets in man as determined by gamma scintigraphy. J. Clin. Pharmacol., 30 (1990) 621-631.
15. El-Arini, S.K., Shiu, G.K. and Skelly, J.P., An in vitro study of possible food-drug interactions of the controlled-release propranolol products. Int. J. Pharm., 55 (1989) 25-30.
16. El-Arini, S.K., Shiu, G.K. and Skelly, J.P., Theophylline-controlled release preparations and fatty food: an in vitro study using the rotating dialysis cell method. Pharm Res., 7 (1990) 1134-1140.
17. Pagan, P.G., Harrison, P.J. and Shankland, N., A correlation between cloud point and disintegration of hydroxyalkylcellulose controlled release matrices. J. Pharm. Pharmacol., 41 (1989) (Suppl.), 25P.
18. Fischer, W., Boertz, A., Davis, S.S., Khosla, R., Cawello, W., Sandrock, K. and Cordes, G., Investigation of the gastrointestinal transit and in vivo drug release of isosorbide-5-nitrate pellets. Pharm. Res., 4 (1987) 480-485.
19. Hamaguchi, T., Shinkuma, D., Yamanaka, Y., Miyake, M., Tamura, S. and Mizuno, N., Factors affecting dissolution rate of sulpiride from tablets coated with polyvinylacetal diethylaminoacetate, a gastric-fluid-soluble polymer. I. Effect of ionic strength of gastrointestinal fluids. Chem. Pharm. Bull., 43 (1995) 1204-1211.
20. Hattingberg, H.M.V., Moment analysis in vivo and in vitro. Methods Find. Exp. Clin. Pharmacol., 6 (1984) 589-595.
21. Hunter, E., Fell, J.T. and Sharma, H., The gastric emptying of pellets contained in hard gelatin capsules. Drug Dev. Ind. Pharm., 8 (1982) 751-757.
22. Jalil, R. and Ferdous, A.J., Effect of viscosity increasing agent and electrolyte concentration on the release rate of theophylline from HPMC based sustained release capsules. Drug Dev. Ind. Pharm., 19 (1993) 2637-2643.
23. Kabanda, L., Lefebvre, R.A., Bree, H.J.V. and Remon, J.P., In vitro and in vivo evaluation in dogs and pigs of a hydrophilic matrix containing propylthiouracil. Pharm. Res., 11 (1994) 1663-1668.
24. Kaniwa, N., Shameem, M., Katori, N., Aoyagi, N. and Kojima, S., The suitable temperature specification for the evaluation of controlled release products in vitro. Pharmazie, 50 (1995) 53-55.
25. Karim, A., Burns, T., Wearley, L., Streicher, J. and Palmer, M., Food-induced changes in theophylline absorption from controlled-release formulations. Part I. Substantial increased and decreased absorption with Uniphyl tablets and Theo-Dur sprinkle. Clin. Pharmacol. Ther., 38 (1985) 77-83.
26. Khan, M.Z.I., Recent trends and progress in sustained or controlled oral delivery of some water soluble drugs: morphine salts, diltiazem and captopril. Drug Dev. Ind. Pharm., 21 (1995) 1037-1070.
27. Khan, M.Z.I., Tucker, I.G. and Opdebeeck, J.P., Cholesterol and lecithin implants for sustained release of antigen: release and erosion in vitro, and antibody response in mice. Int. J. Pharm., 76 (1991) 161-170.
28. Khan, M.Z.I., Tucker, I.G. and Opdebeeck, J.P., Evaluation of cholesterol-lecithin implants for sustained delivery of antigen: release in vivo and single-step immunisation of mice. Int. J. Pharm., 90 (1993) 255-262.
29. Komuro, T., Yomota, C. and Kimura, T., In-vitro dissolution properties of indomethacin extended-release capsules. J. Pharm. Pharmacol., 43 (1991) 79-82.
30. Langenbucher, F., Numerical convolution deconvolution as a tool for correlating in vitro with in vivo drug availability. Pharm. Ind., 44 (1982) 1166-1172.
31. Liaw, J., Rubinstein, A. and Robinson, J.R., Bioavailability study of Theo-dur tablets in the fasted cannulated dog. Int. J. Pharm., 59 (1990) 105-114.
32. Liu, F.-Y, Sambol, N.C., Giannini, R.P. and Liu, C.Y., Pharmacokinetics of oral extended-release dosage forms. I. Release kinetics, concentration, and absorbed fraction. Pharm. Res., 12 (1995) 720-728.
33. Li Wan Po, A., Wong, L.P. and Gilligan, C.A., Characterisation of commercially available theophylline sustained-or controlled-release systems: in vitro drug release profiles. Int. J. Pharm., 66 (1990) 111-130.
34. Macheras, P., Koupparis, M. and Antimisiaris, S., An in vitro model for exploring CR theophylline-milk fat interactions. Int. J. Pharm., 54 (1989) 123-130.
35. Maturu, P.K., Prasad, V.K., Worsley, W.N., Shiu, G.K. and Skelly, J.P., Influence of a high fat breakfast on the bioavailability of theophylline controlled-release formulations: an in vitro demonstration of an in vivo observation. J. Pharm. Sci. 75 (1986) 1205-1206.
36. Marvola, M., Aito, H., Pohto, P., Kannikoski, A., Nykänen, S. and Kokkonen, P., Gastrointestinal transit and concomitant absorption of verapamil from a single-unit sustained-release tablet. Drug Dev. Ind. Pharm., 13 (1987) 1593-1609.
37. Marvola, M., Kannikoski, A., Aito, H. and Nykänen, S., The effect of food on gastrointestinal transit and drug absorption of a multiparticular sustained-release verapamil formulation. Int. J. Pharm., 53 (1989) 145-155.
38. Möller, H. and Wirbitzki, E., Regulatory aspects of modified release dosage forms: special cases of dissolution testing using the flow-through system. Boll. Chim. Farmaceutico, 132 (1993) 105-115.
39. Nazareno, L.A., Holazo, A.A., Limjuco, R., Passe, S., Twardy, S.K., Min, B. and Massarella, J.W., The effect of food on pharmacokinetics of Zalcitabine in HIV-positive patients. Pharm. Res., 12 (1995) 1462-1465.
40. Ogiso, T., Iwaki, M., Tanino, T., Kawafuchi, R. and Hata, S., Effect of food on propranolol oral clearance and a possible mechanism of this food effect. Biol. Pharm. Bull., 17 (1994) 112-116.
41. Oth, M., Franz, M., Timmermans, J. and Möes, A., The bilayer floating capsule: a stomach-directed drug delivery system for misoprostol. Pharm. Res., 9 (1992) 298-302.
42. Price, J.M., Davis, S.S. and Wilding, I.R., Effect of fiber on gastrointestinal transit times in vegetarians and omnivores. Int. J. Pharm., 76 (1991) 123-131.
43. Rajabi-Siahboomi, A.R., Davies, M.C. and Melia, C.D., Identification of active molecular structures in thermally dependent release behaviour of diclofenac sodium from HPMC matrices. Proc. Int. Symp. Control. Release Bioact. Mater., 21 (1994) 25-26.
44. Sagara, K., Nagamatsu, Y., Yamada, I., Kawata, M., Mizuta, H. and Ogawa, K., Bioavailability study of commercial sustained-release preparations of diclofenac sodium in gastro-intestinal physiology regulated-dogs. Chem. Pharm. Bull., 40 (1992) 3303-3306.
45. Sagara, K., Yamada, I., Kawazoe, Y., Mizuta, H. and Shibata, M., Gastrointestinal physiology-regulated dogs: utilization of a bioavailability study of a new thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]-diazepine, an antagonist of platelet-activating factor, and its preparations. Biol. Pharm. Bull., 17 (1994) 117-120.
46. Shah, V.P., Noory, A., Noory, C., McCullough, B., Clarke, S., Everett, R., Naviasky, H., Srinivasan, B.N., Fortman, D. and Skelly, J.P., In vitro dissolution of sparingly water-soluble drug dosage forms. Int. J. Pharm., 125 (1995) 99-106.
47. Skelley, J.P., Amidon, G.L., Barr, W.H., Benet, L.Z., Carter, J.E., Robinson, J.R., Shah, V.P. and Yacobi, A., Report of the workshop on in vitro and in vivo testing and correlation for oral controlled modified-release dosage forms. J. Pharm. Sci., 79 (1990) 849-854.
48. Thoma, K., Pharmaceutical availability as an essential criterion of quality. S.T.P. Pharma. 3 (1987) 39-50.
49. Tandt, L.A.G.L., Stubbs, C. and Kanfer, I., The use of dissolution rate data to account for differences in the absorption profiles of two controlled modified-release capsule dosage forms of indomethacin in human volunteers. Int. J. Pharm., 104 (1994) 11-17.
50. Vidgren, M., Paronen, P., Bergström, K., Vainio, P. and Pikkarainen, P., Deposition and gastrointestinal transit of conventional sucralfate tablets. Acta Pharm. Nord., 3 (1991) 83-86.
51. Wagner, J.G. and Nelson, E., Per cent absorbed time plots derived from blood level and/or urinary excretion data. J. Pharm. Sci., 52 (1963) 610-611.
52. Wiegand, R.G. and Taylor, J.D., Kinetics of plasma drug levels after sustained release dosage. Biochem. Pharmacol., 3 (1960) 256-263.
53. Wilding, I.R., Davis, S.S., Sparrow, R.A., Bloor, J.R., Hayes, G. and Ward, G.T., The effect of food on the in vivo behaviour of a novel sustained release formulation of tiaprofenic acid. Int. J. Pharm., 83 (1992) 155-161.
54. Wilson, C.G., Washington, N., Greaves, J.L., Washington, C., Wilding, I.R., Hoadley, T. and Sims, E.E., Predictive modelling of the behaviour of a controlled release buflomedil HCl formulation using scintigraphic and pharmacokinetic data. Int. J. Pharm., 72 (1991) 79-86.
55. Wingstrand, K., Abrahamsson, B. and Edgar, B., Bioavailability from felodipine extended-release tablets with different dissolution properties. Int. J. Pharm., 60 (1990) 151-156.
56. Yamakita, H., Maejima, T. and Osawa, T., Preparation of controlled release tablets of TA-5707F with wax matrix type and their in vivo evaluation in beagle dogs. Biol. Pharm. Bull., 18 (1995) 984-989.