Suspensions naproxen

Naprosyn (naproxen) suspension for oral administration contains 125 mg/5 mL of naproxen in a vehicle containing sucrose, magnesium aluminum silicate, sorbitol solution, and sodium chloride (30 mg/5 mL, 1.5 mEq), 

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In one such example, a study was performed to compare the pharmacokinetics of orally administered micronized naproxen suspension (Naprosyn ) with an intramuscular injection of nanoparticulate naproxen colloidal dispersion (average particle size ca. 300 mn, concentration 400 mg naproxen/mL). " In a crossover experiment, the patients ( = 3 per dose) were given oral and intramuscular naproxen at doses of 2.5 and 5.0mg/kg, corresponding to approximately 175 and 350 mg per injection, respectively. A summary of the pharmacokinetic data is presented in Table 4 later, and the pharmacokinetic profiles are shown in Fig. 10. For each dose, the overall bioavailabilities were comparable, but the absorption was somewhat slower for the intramuscular product in both cases. 

Naproxen is a naphthylpropionic acid derivative. It is the only NSAID presently marketed as a single enantiomer. Naproxen s free fraction is significantly higher in women than in men, but half-life is similar in both sexes (Table 36-1). Naproxen is effective for the usual rheumatologic indications and is available in a slow-release formulation, as an oral suspension, and over the counter. A topical preparation and an ophthalmic solution are also available. 

Furthermore, in human clinical trials, the time to onset of action of a nanoparticle oral suspension of naproxen reached signiLcant plasma lel Jar( less than 20 min, which was 12-fold fasterthan commercial formulations of larger particle size (Figure 17.11). 

FIGURE 17.11 ln uence of formulation on absorption of naproxen (500 mg) in humans (fed) mean plasma data from clinical trials = 23). Plasma levels of naproxen (mg/mL) are plotted as a function of time (h) where ( ) is Naproxen NanoCrys fedispersion, (0) is Naprox suspension, ancDO is Anapro tablet. 

The suspension and modified-release tablets produce the usual pattern of adverse effects (SEDA-15,101), although an enteric-coated formulation of naproxen in patients... 

In vivo studies proved the excellent performance of drug nanoparticles. For example, in humans the oral administration of the analgesic naproxene as drug nanoparticles led to an AUC (0-2 h) of 97.5 mg h 1 compared with just 44.7 mg h 1 for a commercial suspension and of 32.7 mg hP for the same drug as a tablet product. The corresponding tmax values were 1.96 h for the nanoparticles, 3.33 h and 3.20 h for the two commercial products. In a canine study, oral administration of the gonadotropin inhibitor danazol as a suspension of nanoparticles led to an absolute bioavailability of 82.3%, whereas with the conventional dispersion only 5.2% was achieved. 

Commercially available preparations of naproxen should be stored at room temperature, exposure of suspension to temperature exceeding 40Oc should be avoided (1). It should be kept in well-closed containers, protected from light (10). 

A naproxen oral suspension (Table 5.13) is an example for using tragacanth as a thickening agent. It is combined with sucrose and for taste improvement sodium chloride is added. 

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