Formulation and evaluation of oral transmucosal ketamine as premedication in children

ABSTRACT

Fear of hospitals [operations, diagnosis and injections] where the children are separated from their parents, prior to anesthesia, is very common, where ketamine hydrochloride [KH] was widely used as a preanaesthetic medication by intravenous and intramuscular injection. So, this study is an attempt to produce another alternative method as preanesthesia. This study is designed to formulate and evaluate the efficacy and safety of oral transmucosal ketamine as premedication in children in a dose of 100 mg. Ketamine is chosen to be formulated in different traditional formulations for transmucosal administration including [lozenges, powders, chewable tablets and granules] in which KH concentration is 2% [100 mg / 5g of each dose]. The released studies from different oral transmucosal formulations were carried out in-vitro over a period of twenty one minutes at a thermostatically controlled water bath operating at 37°C +/- 0.5 and 50 r.p.m, by using dissolution tester. The results showed that chewable tablets > powder > granules > lozenges. Because lozenges are more preferable than other oral transmucosal dosage forms in children, different formulations of lozenges were prepared using different sugar bases, different binders and shapes of lozenges which gave the following results: Regarding the type of sugar bases; Glucose + sucrose combined base > glucose base > mannitol base > fructose base > maltose base > sucrose base. Regarding the type of binders; the release of ketamine from lozenges using gelatin as a binder was higher than using gum tragacanth as a binder. Regarding the shape of lozenges; the flat shape of ketamine lozenges gave more and rapid release than oval shape.