In vitro and in vivo evaluation of floating riboflavin pellets developed using the melt pelletization process.
Floating pellets were prepared using the melt pelletization process in a Mi-Pro high shear mixer (Pro-C-epT, Belgium). Formulations were based on a mixture of Compritol and Precirol as meltable binders and on the use of sodium bicarbonate and tartaric acid as gas-generating agents. Good floating abilities were obtained by using the gas-generating agents in both the inner matrix and the outer coating layer of the pellets. In vitro evaluation of floating capability was performed both by using the resultant weight apparatus and by counting floating pellets at the surface of beakers containing 0.1N HCl solution, in vivo evaluation of floating pellets capabilities was also performed. Riboflavin-containing floating pellets (FRF) were administered orally to nine healthy volunteers versus non-floating pellets (NFRF). Volunteers were divided in two groups, fasted group (n=4) 729 kcal and fed group (n=5) 1634 kcal as the total calorie intake on the testing day. An increase of urinary excretion of riboflavin was observed when the volunteers were dosed with the floating pellets, especially after feeding. As riboflavin has a narrow window of absorption in the upper part of small intestine, this phenomenon could be attributable to the gastric retention of floating pellets.
Hamdani
J
J
Laboratoire de Pharmacie Galénique et Biopharmacie, Université Libre de Bruxelles, Campus Plaine, CP 207, Boulevard du Triomphe, 1050 Brussels, Belgium.
Goole
J
J
Moës
A J
AJ
Amighi
K
K
D000328:Adult; D000465:Algorithms; D001682:Biological Availability; D003692:Delayed-Action Preparations / Q000737:chemistry; D004075:Diglycerides / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods*; D005215:Fasting / Q000652:urine; D005227:Fatty Acids / Q000737:chemistry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008297:Male; D008747:Methylcellulose / Q000737:chemistry; D008875:Middle Aged; D012256:Riboflavin / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine; D017693:Sodium Bicarbonate / Q000737:chemistry; D013644:Tartrates / Q000737:chemistry
D003692:Delayed-Action Preparations; D004075:Diglycerides; D005227:Fatty Acids; D013644:Tartrates; C086409:glyceryl behenate; D017693:Sodium Bicarbonate; D008747:Methylcellulose; C009032:precirol; D012256:Riboflavin; C029768:tartaric acid