Current Issues of Pharmacy and Medical Sciences

Comparison of oral bioavailability of acetaminophen tablets, capsules and effervescent dosage forms in healthy volunteers

Curr Issues Pharm Med Sci., Vol. 31, No. 1, 5-9

Mona Fathi1, Sohrab Kazemi1,2, Farbod Zahedi3,
Mohamad Reza Shiran4, Ali Akbar Moghadamnia1,2*

1 Neuroscience Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
2 Cellular and Molecular biology research centre, health research institute, Babol University of Medical Sciences, Babol, Iran
3 Department of Pharmacology, Babol University of Medical Sciences, Babol, Iran
4 Department of Pharmacology, Mazandaran University of Medical Science, Sari, Iran

DOI: 10.1515/cipms-2018-0001

Abstract

A wide variety of acetaminophen dosage forms have been administered to relieve mild to moderate pain and fever, so far. The purpose of this study was to compare the oral bioavailability in healthy volunteers, of three of these dosage forms. We included healthy volunteers in our study and divided replace with placed them into three groups: tablet, capsule and effervescent. Each dosage form contained 500 mg of acetaminophen as active material. Blood samples were taken at 0.5, 1, 2, 4 and 8-hour intervals after receiving the dose. Acetaminophen blood levels were measured using HPLC method. Data were fit in a “one-compartment PK model”, using P-Pharm 1.5 software and analyzed under statistical tests. The maximum concentrations of acetaminophen in blood samples were measured at 1h after taking the drug (6.61±3.19 µg/ml, 11.29±3.94 µg/ml and 15.25±2.54 µg/ml in groups receiving capsule, tablet and effervescent, respectively). Pharmacokinetic (PK) data analysis & modeling from the three groups showed that the half-life of acetaminophen was 140.72 min in the tablet group, 140.29 min in capsule and 132.08 min in effervescent. The area under the blood levels curve were 47.04, 40.62 and 53.11 µgmin/ml, in tablet, capsule, and effervescent groups, respectively. Statistically significant differences in PK parameters were recorded as the study replace with we compared effervescent with tablets and capsule dosage forms (p < 0.05). According to the results, the effervescent form creates better PK parameters compared with tablet and capsule forms, therefore, it is suggested replace with we suggested that this form should be administer in cases of pain and fever to achieve quick drug efficacy.

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Keywords

pharmacokinetics, acetaminophen, HPLC, kinetic modeling, effervescent.

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