The Effects of Some Physico-Chemical Factors and Pharmaceutical Excipients on the Bioavailability of Nitrofurantoin Oily and Aqueous Suspensions in Rats

ABSTRACT

The effects of some physico-chemical factors and various excipients, i.e., sucrose, aluminum stearate, hydrogenated castor oil, Cab-o-sil, and lecithin, either alone or in combination, from suspensions in fractionated coconut oil and distilled water have been investigated. In vitro drug release studies were performed according to the flask–stirrer method. In addition to adsorption and solubility studies, determination of partition coefficients and rheological measurements have been carried out. The experimental design was based on an 8×8 latin square using rats as the test animals. The results of the study showed that the rate and extent of absorption of nitrofurantoin are decreased significantly by the use of an oily rather than an aqueous vehicle. In vitro drug release data showed some correlation with in vivo parameters, and also with the apparent viscosity of the vehicles. However, no correlation was detectable between in vivo parameters and the apparent viscosity of the vehicles.

Key Words:

• Bioavailability
• Dosage forms
• Formulation
• Fractionated coconut oil (FCO)
• Gastric emptying rate (GER)
• Nitrofurantoin
• Oily vehicle