Abstract
Pharmacomagnetography involves the simultaneous assessment of solid dosage forms (SDFs) in the human gastrointestinal (GI) tract and the drug plasmatic concentration, using a biomagnetic technique and pharmacokinetics analysis. This multi-instrumental approach helps the evaluation, as GI variables can interfere with the drug delivery processes. This study aimed to employ pharmacomagnetography to evaluate the influence of omeprazole on the drug release and absorption of metronidazole administered orally in magnetic-coated tablets. Magnetic-coated tablets, coated with Eudragit® E-100 (E100) and containing 100 mg of metronidazole, were produced. For the in vivo experiments, 12 volunteers participated in the two phases of the study (placebo and omeprazole) on different days to assess the bioavailability of metronidazole. The results indicated a shift as the pH of the solution increased and a delay in the dissolution of metronidazole, showing that the pH increase interferes with the release processes of tablets coated with E100. Our study reinforced the advantages of pharmacomagnetography as a tool to perform a multi-instrumental correlation analysis of the disintegration process and the bioavailability of drugs.
Highlights
The oral route is the simplest, most convenient, patient compliant, and safest drug administration mode [1,2]
UV-spectrophotometer and ourand metronidazole quantification by. This validation was based on assessing a series reference used, we found a Limit of detection (LOD) of 0.070453 μg/μL and a Limit of quantification (LOQ) of 0.234843 μg/μL
The tablet quality control assays recommended by U.S Pharmacopeia (USP) allowed the evaluation of the physical characteristics regarding the uniformity and properties of mechanical resistance, besides the average weight of non-coated tablets
Summary
The oral route is the simplest, most convenient, patient compliant, and safest drug administration mode [1,2]. A drug administered orally is in a solid dosage form (SDF), such as gastric soluble tablets. SDFs have the primary objective of providing immediate drug release or promoting release in specific locations to be absorbed in the gastrointestinal (GI) tract [3]. Several factors can modify the gastric environment’s pH, especially those related to drug co-administration, such as proton pump inhibitors (PPIs) [7,8,9]. PPIs increase the intragastric pH > 4, and they can directly interfere with the absorption of drugs taken simultaneously with this type of medication.
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