Effect of food on bioavailability of metronidazole from sugar-coated tablets having different dissolution rates in subjects with low gastric acidity
- PMID: 3733276
Effect of food on bioavailability of metronidazole from sugar-coated tablets having different dissolution rates in subjects with low gastric acidity
Abstract
The effect of food on the bioavailability of metronidazole from three commercial sugar-coated tablets varying markedly in drug dissolution behavior relative to pH was determined after oral administration in healthy male subjects with low gastric acidity. Four subjects, whose gastric acidities were evaluated as low (hypo- or anacidity) by using a non-intubation method (Gastrotest tablets administration method), received, in a cross-over fashion, a single 250 mg dose in sugar-coated tablet during periods of fasting and non-fasting. The tablet having the fastest and most pH-independent dissolution rate gave significantly higher Cmax and AUC0-32 than the other tablets having extremely slow dissolution at pH 5 or 7.2, when the drug was administered in the fasting state. However, there were no statistically significant differences in the above parameters among the tablets tested when they were administered postprandially. The improvement of the bioavailability of the tablets exhibiting poorer dissolution in the pH range of 5 to 7.2 is ascribed to suggestible vigorous agitation in the digestive tract stimulated by food intake.
Similar articles
-
Effects of food intake on the bioavailability of sulpiride from AEA film-coated tablet having a pH-dependent dissolution characteristic in normal or drug-induced achlorhydric subjects.Int J Clin Pharmacol Ther Toxicol. 1991 Aug;29(8):303-9. Int J Clin Pharmacol Ther Toxicol. 1991. PMID: 1743804
-
The bioavailability of diazepam from uncoated tablets in humans--Part II: effect of gastric fluid acidity.Int J Clin Pharmacol Ther Toxicol. 1982 Apr;20(4):166-70. Int J Clin Pharmacol Ther Toxicol. 1982. PMID: 7076346
-
Effect of food on bioavailability of nalidixic acid from uncoated tablets having different dissolution rates.J Pharmacobiodyn. 1984 Oct;7(10):760-7. doi: 10.1248/bpb1978.7.760. J Pharmacobiodyn. 1984. PMID: 6520698
-
The bioavailability of diazepam from uncoated tablets in humans--Part I: correlation with the dissolution rates of the tablets.Int J Clin Pharmacol Ther Toxicol. 1982 Apr;20(4):159-65. Int J Clin Pharmacol Ther Toxicol. 1982. PMID: 7076345
-
Gastric emptying of non-disintegrating solid drug delivery systems in fasted state: relevance to drug dissolution.Expert Opin Drug Deliv. 2010 Aug;7(8):967-76. doi: 10.1517/17425247.2010.495982. Expert Opin Drug Deliv. 2010. PMID: 20586705 Review.
Cited by
-
Justification of disintegration testing beyond current FDA criteria using in vitro and in silico models.Drug Des Devel Ther. 2017 Apr 11;11:1163-1174. doi: 10.2147/DDDT.S131213. eCollection 2017. Drug Des Devel Ther. 2017. PMID: 28442890 Free PMC article.
-
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.Pharm Res. 1995 Jul;12(7):1049-54. doi: 10.1023/a:1016270701021. Pharm Res. 1995. PMID: 7494801 Clinical Trial.
-
Gastric pH and gastric residence time in fasted and fed conscious cynomolgus monkeys using the Bravo pH system.Pharm Res. 2008 Jan;25(1):123-34. doi: 10.1007/s11095-007-9358-5. Epub 2007 Jul 6. Pharm Res. 2008. PMID: 17612796
-
Estimation of agitation intensity in the GI tract in humans and dogs based on in vitro/in vivo correlation.Pharm Res. 1995 Feb;12(2):237-43. doi: 10.1023/a:1016231010301. Pharm Res. 1995. PMID: 7784339 Clinical Trial.