Stability and compatibility of tegaserod from crushed tablets mixed in beverages and foods.
OBJECTIVE
The stability and compatibility of tegaserod from crushed tablets in selected beverages and foods were studied.


METHODS
Suspensions of tegaserod maleate tablets containing 6 mg of the drug base were prepared by crushing the tablets and mixing the powder with tap water, apple juice, orange juice, milk, applesauce, yogurt, and chocolate-hazelnut spread. Drug stability, drug comparability, suspension homogeneity, and completeness of a dose were measured by high-performance liquid chromatography at intervals up to three days at 20-25 degrees C and 5 degrees C. In vitro dissolution profiles were determined for crushed tegaserod tablets in water, apple juice, orange juice, and applesauce.


RESULTS
Tegaserod from crushed tablets was stable in and compatible with water, apple juice, orange juice, and applesauce, and the suspensions were homogeneous. The complete dose was delivered with these media. The dissolution profiles of crushed tegaserod tablets in water and in apple juice were comparable to those of intact tablets; the dissolution profiles in orange juice and applesauce were not comparable with those of intact tablets. The results with milk, yogurt, and chocolate-hazelnut spread as vehicles were inconclusive. The suspension in milk was not homogeneous, and the dose was incomplete.


CONCLUSIONS
Tegaserod from crushed tablets was stable in and compatible with water, apple juice, orange juice, and applesauce, but the dissolution profile in orange juice or applesauce was not acceptable. Apple juice may be the preferred vehicle because it masks the drug's taste.
Carrier
Marie-Noëlle
MN
Department of Bioanalytics and Pharmacokinetics, Novartis Pharma SAS, Rueil-Malmaison, France.
Garinot
Olivier
O
Vitzling
Christian
C
D001628:Beverages; D002851:Chromatography, High Pressure Liquid; D004344:Drug Incompatibility; D004356:Drug Storage; D005502:Food; D005765:Gastrointestinal Agents / Q000737:chemistry*; D007211:Indoles / Q000737:chemistry*; D012034:Refrigeration; D012995:Solubility; D013535:Suspensions; D013607:Tablets
D005765:Gastrointestinal Agents; D007211:Indoles; D013535:Suspensions; D013607:Tablets; C105050:tegaserod