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|Title:||Evaluation of the intestinal absorption of erythromycin in man: Absolute bioavailability and comparison with enteric coated erythromycin|
|Citation:||Pharmaceutical Research, 1995; 12(1):149-154|
|Publisher:||PLENUM PUBL CORP|
|Abstract:||To determine the role of acid hydrolysis on the gastrointestinal absorption of erythromycin, six healthy subjects received erythromycin as a 240 mg intravenous dose, a 250 mg oral solution administered via endoscope directly into the duodenum and bypassing the stomach, and an enteric-coated 250 mg capsule. Blood samples were collected for 6 hours and serum erythromycin quantified by a microbiological method. The time to achieve maximum serum concentrations for the solution was 0.25 +/- 0.08 (mean +/- SD) hours and for the capsule was 2.92 +/- 0.55 hours. The absolute bioavailability of erythromycin from the capsule was 32 +/- 7% and for the duodenal solution 43 +/- 14%. The ratio of the areas under the serum erythromycin concentration-time curve of capsule to solution was 80 +/- 28% (range 38 to 110%). There is substantial loss of erythromycin apart from gastric acid hydrolysis, which cannot be accounted for by hepatic first-pass metabolism. Attempts to further improve the oral bioavailability of erythromycin beyond 50% by manipulation of formulation are likely to be futile.|
|Keywords:||Duodenum; Humans; Erythromycin; Capsules; Solutions; Drug Administration Routes; Administration, Oral; Injections, Intravenous; Biological Availability; Intestinal Absorption; Chemistry, Pharmaceutical; Adult; Female; Male; Evaluation Studies as Topic|
|Appears in Collections:||Pharmacology publications|
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