Abstract
This study aimed at comparing the release rate of artemether-lumefantrine tablets through artemether release in the presence of simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and food modified simulated gastric fluid (FMSGF) and intestinal fluid (FMSIF). Various quality control parameters including weight uniformity, tablet hardness, disintegration, friability and assay were assessed. SGF and SIF were employed as disintegration and dissolution media and compared with a food (1.3 ml full cream unsweetened evaporated milk, 2.67mg soluble starch) modified SIF and SGF (FMSIF and FMSGF) at 37 ± 0.5 o C. The product assessed complied with the official specification for uniformity of weight friability and assay. The titrimetric and spectrophotometric assays gave 97.45% and 103.25% of artemether content respectively (P<0.05). No significant differences were observed between the disintegration time for FMSGF and SGF (5.0min and 5.5min) for SIF and FMSIF (7.5min and 6.5min) respectively. There was significant difference in the percentage drug release in FMSGF compared to SGF (35% v 58%) but no significant difference in the release rate for media simulating dosing conditions in the intestine, FMSIF and SIF( 28% v 29%) respectively at P<0.05. Artemether-lumefantrine is well absorbed in the stomach and in the fasted state dosing condition.
Highlights
Malaria is by far the world’s most important tropical disease which has claimed many lives including pregnant women and newly born children
This study evaluates the in-vitro predictiveness of the in-vivo dissolution profile of artemetherlumefantrine fixed dose composition in the fed state especially with food composition typified by food consumed in tropical African setting
Food modified simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) (FMSGF and FMSIF): Food modified SGF and SIF were prepared by adding 100ml of peak milk and 25mg of soluble starch with 500ml of SGF and 300ml of SIF respectively rotating basket. 2.2 Method Tablet hardness: Ten tablets were randomly taken from the drug and placed on the edge of the tester and subjected to crushing strength of the tester
Summary
Malaria is by far the world’s most important tropical disease which has claimed many lives including pregnant women and newly born children. Solubilization and the release of drug are critical to drug absorption in vitro drug dissolution is predictive of in vivo performance[3,4,5]. Unpredictable food effects on the absorption of antimalarial drugs may be responsible for resistance development and treatment failure. As part of the drive to develop predictive in-vitro models to forecast the in-vivo performance of malaria drug products when taken with food or on empty stomach (lack of appetite), food modified simulated intestinal and gastric fluids are proposed 10-12. This study evaluates the in-vitro predictiveness of the in-vivo dissolution profile of artemetherlumefantrine fixed dose composition in the fed state especially with food composition typified by food consumed in tropical African setting
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