Oral Biopharmaceutics and In vitro Pharmacokinetics of Commercially Available Pharmaceutical Formulations of Paracetamol: Implications in Paediatric Medicine
Ikeh GO
Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Enugu State University of Science and Technology, Nigeria.
Nwafor MN
*
Department of Clinical Pharmacy and Biopharmaceutics, Faculty of Pharmaceutical Sciences, Enugu State University of Science and Technology, Nigeria.
Ndubuisi MN
Pharmaceutical Society of Nigeria, Enugu Chapter, Nigeria.
Okolo KO
Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, Enugu State University of Science and Technology, Nigeria.
*Author to whom correspondence should be addressed.
Abstract
Aim: This study aimed to compare the oral pharmacokinetics of different paediatric paracetamol dosage forms that are commercially available in Nigeria.
Study Design: Experimental.
Place and Duration of Study: Faculty of Pharmaceutical Sciences, Enugu State University of Science and Technology, between March and December 2023
Methodology: The study used the regular in vitro dialysis membrane method to predict the in vivo drug release of commercially available paracetamol syrups (n=5) and dispersible tablets (n=5) in the Nigerian market. The sink condition followed the Conventional USP dissolution method, using a dialysis membrane sac. The drug samples were studied in simulated salivary fluid of pH 7.4, simulated gastric fluid of pH 1.2, and simulated intestinal fluid of pH 6.5 over 8 hours to simulate their passage in the gastrointestinal tract. At predetermined time intervals, 5 ml of the dissolution medium was drawn out from the system, diluted appropriately and its absorbance measured against a suitable blank at λ = 250 nm using a UV/Vis Spectrophotometer, while a fresh volume of 5 ml of dissolution medium was introduced into the dissolution vessel after each withdrawal.
Results: Syrup dosage forms showed a faster drug release kinetics, based on their values. Kinetic parameters obtained from the linear regression analysis of the in vitro release resulted in a zero-order release kinetics, with for paracetamol paediatric syrups, and for tablets. Two-way ANOVA test of the AUC of dosage forms showed that the time required to elicit therapeutic response was extremely significant (F=44.37, DFn=3, DFd= 32 and P-value < 0.0001).
Conclusion: The comparative in vitro pharmacokinetic study of paracetamol dosage forms revealed that the paediatric syrup formula has a better release kinetics than the scaled down adult formula.
Keywords: Paracetamol, dosage forms, paediatric medicine, biopharmaceutics, in vitro pharmacokinetics