Oral Gels as an Alternative to Liquid Pediatric Suspensions Compounded from Commercial Tablets

Abstract

The aim of the study was to propose pharmacy-compounded oral gels as a new and alternative dosage form that is attractive to children as having a better masking taste than syrups and reducing the risk of spilling. The application and physical properties of the gels prepared with cellulose derivatives (hydroxyethylcellulose and carmellose sodium) or carbomers were evaluated. The results of the study showed the most suitable consistency, viscosity, and organoleptic properties for gels prepared with carbomer and cellulose derivatives at concentrations of 0.75% and 2.0%, respectively. The microbial stability of the gels was guaranteed by the use of methylparaben and potassium sorbate. VAL (valsartan) and CC (candesartan cilexetil) tablets, often used off-label in children, were pulverized and suspended in the hydrogel bases, resulting in final drug concentrations of 4 mg/g and 1 mg/g, respectively. There was no significant change in viscosity and consistency parameters when the pulverized tablets were added, and only small changes in viscosity and consistency were observed during 35 days of storage, especially in the gels with sodium carmellose and candesartan. On the basis of the drug assay, an expiry date of 25 °C was recommended: 35 days for valsartan and 14 days for candesartan preparations.

Keywords: candesartan cilexetil; carbomer; cellulose polymers; pediatric oral gels; stability; valsartan.

Figure 1

The curve and mechanical parameters of hydrogels were tested in a texture analyzer with a downstream and upstream movement of the probe.

Figure 2

Hydrogels are prepared from valsartan (VAL) and candesartan cilexetil (CC) tablets using hydrogel carriers with hydroxyethylcellulose (HEC), carmellose sodium (CMC), and carbomer (CAR).

Figure 3

The mechanical properties of hydrogels prepared with VAL and CC tablets using hydrogel media (HEC, CMC, and CAR) and stored at 25 °C for 35 days. The mechanical parameters at t0 for the placebo hydrogels are also presented. * Statistical significance was demonstrated after the addition of the tablet mass (p < 0.05). ^ Statistical significance was demonstrated in relation to time t0, (p < 0.05).

Figure 4

The representative hysteresis loops for HEC, CMC, and CAR gels were recorded for placebo gels at t0 (A) and gels with candesartan cilexetil (B) and valsartan (C) tablets after preparation (t0) and 35 days of storage at 25 °C.

Figure 5

Chromatograms of VAL (a) and CC (b) in CMC gels: after preparation (t0) and after 14 and 35 days of storage at 25 °C.

Figure 6

Stability (% of the initial content) of VAL and CC in oral hydrogels prepared with HEC, CMC, and CAR, stored at 25 °C and 4 °C for 35 days.