Oral Solid Controlled Release Dosage Forms: Role of GI-Mechanical Destructive Forces and Colonic Release in Drug Absorption Under Fasted and Fed Conditions in Humans
Rent the article at a discountRent now
* Final gross prices may vary according to local VAT.Get Access
Purpose. This study was undertaken to examine the effects of mechanical destructive forces on drug release from controlled release (CR) dosage forms in vitro and in vivo and their colonic release, using two CR tablets of acetaminophen A and B, showing slower and faster erosion rates, respectively.
Methods. In vitro release rates were determined by several official methods. Tablets were administered to healthy volunteers under fasting and fed conditions.
Results. Both tablets showed similar release rates under mild destructive conditions (e.g., paddle method at 10 rpm) but CR-B showed faster release under highly destructive conditions (e.g., rotating basket method at 150 rpm), where the tablet was eroded. The in vivo release from CR-B was faster than from CR-A, possibly because of enhanced erosion. The variable in vivo release from CR-B indicated large inter-subject differences in destructive GI forces. The fastest in vivo release from CR-B among individuals was approximated by the in vitro dissolution determined by destructive methods such as the rotating basket at 150 rpm. The slowest in vivo release from tablets A and B was lower than the dissolution by the paddle method at 10 rpm. The release from both tablets was markedly reduced at 3–4 hrs after dosing irrespective of feeding conditions which can be attributed to release inhibition in the colon.
Conclusions. Effects of GI destructive forces on the tablet erosion and the release inhibition in the colon must be considered in the development of CR dosage forms.
- Katori, N., Aoyagi, N., Terao, T. (1995) Estimation of agitation intensity in the GI tract in human and dog based on in vitro/in vivo correlation. Pharm. Res. 12: pp. 245-251
- Bain, J. C., Tan, S. B., Ganderton, D., Solomon, M. C. (1990) A discrepancy between pharmacopoeial dissolution tests and bioavailability. Pharm. Tech. Int. 2: pp. 36-40
- Aoki, S., Ando, H., Tatsuishi, K., Uesugi, K., Ozawa., H. (1993) Determination of the mechanical impact force in the in vitro dissolution test and evaluation of the correlation between in vivo and in vitro release. Int. J. Pharm. 95: pp. 67-75
- Wilson, C. G., Washington, N., Greaves, J. L., Kamali, F., Rees, J. A., Sempik, A. K., Lampard, J. F. (1989) Bimodal release of ibuprofen in a sustained-release formulation: A scintigraphic and pharmacokinetic open study in healthy volunteers under different condition of food intake. Int. J. Pharm. 50: pp. 155-161
- Wilson, C. G., Washington, N., Greaves, J. L., Washington, C., Wilding, I. R., Hoadley, T., Sims, E. E. (1991) Predictive modeling of the behavior of a controlled release buflomedil HCl formulation using scintigraphic and pharmacokinetic data. Int. J. Pharm. 72: pp. 79-86
- Abrahamsson, B., Alpsten, M., Hugosson, M., Jonsson, U. E., Sundgren, M., Svenheden, A., Tolli, J. (1993) Absorption, gastrointestinal transit and tablet erosion of felodipine extended-release tablets. Pharm. Res. 10: pp. 709-714
- Wingstrand, K., Abrahamsson, B., Edgar, B. (1990) Bioavailability from felodipine extended-release tablets with different dissolution properties. Int. J. Pharm. 60: pp. 151-156
- K. Sako, T. Mizumoto, T. Kajiyama, and T. Omura. In vitro and in vivo release behavior of erodable and non-erodable sustain release tablets of acetaminophen. Proceedings of the 6th Conference of the Academy of Pharmaceutical Society. and Technology, Japan. p. 25–27 (1990).
- Adithan, A., Thangam, J. (1982) A comparative study of saliva and serum paracetamol levels using simple spectrophotometric method. Br. J. Clin. Pharmacol. 14: pp. 107-109
- Verotta, D. (1986) An Inequality-constrained least squares deconvolution method. J. Pharmacokinet. Biopharm. 17: pp. 269-289
- Yamaoka, K., Tanigawara, T., Nakagawa, T., Uno, T. (1981) A pharmacokinetic analysis program (MULTI) for microcomputer. J. Pharmacobio-Dyn. 4: pp. 879-885
- Ogata, H., Shibazaki, T., Inoue, T., Ejima, A. (1979) Dissolution system for chloramphenicol tablet bioavailability. J. Pharm. Sci. 68: pp. 712-715
- Ogata, H., Aoyagi, N., Kaniwa, N., Ejima, A. (1986) Effect of food on the bioavailability of metronidazole from sugar coated tablets having different dissolution rates in subjects with low gastric acidity. Int. J. Clin. Pharmacol. Ther. Toxicol. 24: pp. 279-282
- El-Arini, S. K., Shiu, G. K., Skelly, J. P. (1990) Theophylline controlled release preparations and fatty food: An in vitro study using rotating dialysis cell method. Pharm. Res. 7: pp. 1134-1140
- T. Mizumoto, K. Sako and M. Fukui. In vitro/in vivo correlation of single unit CR dosage forms. Abstract of 111th Conference of Pharmaceutical Society of Japan. No.4: p.105 (1991)
- Davis, S.S., Hardy, J.G., Fara, J.W. (1986) Transit of pharmaceutical dosage forms through the small intestine. Gut. 27: pp. 885-892
- Aoyagi, N., Kaniwa, N., Takeda, Y., Uchiyama, M. (1994) The purpose of dissolution test in Japanese Pharmacopoeia and its application principles. J P Forum 3: pp. 46
- Hussain, Z., Friedman, M. (1990) Release and absorption characteristics of novel theophylline sustained-release formulations-In vitro-in vivo correlation. Pharm. Res. 7: pp. 1167-1171
- Ogata, H., Aoyagi, N., Kaniwa, N., Shibazaki, T., Ejima, A., Takasugi, N., Mafune, E., Hayashi, T., Suwa, K. (1984) Bioavailability of nalidixic acid from uncoated tablets in humans. Part I: Correlation with the dissolution rates of the tablets. Int. J. Clin. Pharmacol.Ther.Toxicol. 22: pp. 175-183
- Dietrich, R., Brausse, R., Benedikt, G., Steinijans, V.W. (1988) Feasibility of in vitro/in vivo correlation in the case of a new sustained-release theophylline pellet formulation. Arzneim-Forsch. 38: pp. 1229-1237
- Kaniwa, N., Ogata, H., Aoyagi, N., Shibazaki, T., Ejima, A., Watanabe, Y., Motohashi, K., Sasahara, K., Nakajima, E., Morioka, T., Nitanai, T. (1983) The bioavailability of flufenamic acid and its dissolution from capsules. Int. J. Clin. Pharmacol. Ther. Toxicol. 21: pp. 56-63
- Kimura, T., Sudo, K., Kanezaki, Y., Miki, K., Takeichi, Y., Kurosaki and, Y., Nakayama, T. (1994) Drug absorption from large intestine: Physicochemical factors governing drug absorption. Biol. Pharm. Bull. 17: pp. 327-333
- H. Nakajima, K. Sako, T. Sawada, A. Okada and M. Fukui. Continuously absorbable oral delivery systems using acetaminophen. Abstract of 114th Conference of Pharmaceutical Society of Japan. No.4: p.37 (1994).
- Oral Solid Controlled Release Dosage Forms: Role of GI-Mechanical Destructive Forces and Colonic Release in Drug Absorption Under Fasted and Fed Conditions in Humans
Volume 12, Issue 7 , pp 1049-1054
- Cover Date
- Print ISSN
- Online ISSN
- Kluwer Academic Publishers-Plenum Publishers
- Additional Links
- controlled release
- colonic release
- drug absorption
- Industry Sectors