Enhancing the dissolution of phenylbutazone using Syloid® based mesoporous silicas for oral equine applications

Abstract

Three mesoporous silica excipients (Syloid® silicas AL-1 FP, XDP 3050 and XDP 3150) were formulated with a model drug known for its poor aqueous solubility, namely phenylbutazone, in an attempt to enhance the extent and rate of drug dissolution. Although other forms of mesoporous silica have been investigated in previous studies, the effect of inclusion with these specific Syloid® silica based excipients and more interestingly, with phenylbutazone, is unknown. This work reports a significant enhancement for both the extent and rate of drug release for all three forms of Syloid® silica at a 1:1 drug:silica ratio over a period of 30 min. An explanation for this increase was determined to be conversion to the amorphous form and an enhanced drug loading ability within the pores. Differences between the release profiles of the three silicas were concluded to be a consequence of the physicochemical differences between the three forms. Overall, this study confirms that Syloid® silica based excipients can be used to enhance dissolution, and potentially therefore bioavailability, for compounds with poor aqueous solubility such as phenylbutazone. In addition, it has been confirmed that drug release can be carefully tailored based on the choice of Syloid® silica and desired release profile.

Development of a Solid Formulation Containing a Microemulsion of a Novel Artemisia Extract with Nematocidal Activity for Oral Administration

“…There are two types of Syloid ® XDP commercially available, 3050 and 3150, both having a high pore volume (1.7 cm 3 /g) and a high surface area (320 m 2 /g).While Syloid ® XDP 3150 has higher average particle size (150 µm) than Syloid ® XDP 3050 (50 µm), both are able to retain a high amount of liquid [ 13 , 14 ]. Syloid ® XDP 3150 shows better flow properties, improving the content uniformity and the formulation of loaded silica in tablets [ 15 , 16 ].…”

<p>Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity</p>

“…These forms of silica provide a high mesoporous network, large surface area, high adsorption capacity, besides its desirable pore size and surface morphology. 28 Lactose was used as a diluent to provide minimal disintegration time, sodium starch glycolate was exploited as superdisintegrant, glycerol as a cryoprotectant, and microcrystalline cellulose (Avicel) was used as filler, pregelatinized starch was added to enhance the bulk of the dosage form. Hydroxypropyl methylcellulose (HPMC) was used as a binder to maintain the integrity of the preparation, and gelatin - water-soluble polymer - served as a matrix-forming binder to uphold mechanical strength during manufacturing and patient handling.…”

Silica-Supported Ionic Liquids for Heat-Powered Sorption Desalination

“…Syloid FP silica are silica gels with a particularly high density of surface silanol groups (≡Si-OH), commercially used as moisture controllers in pharmaceutical and personal care products. 32,34 Average Pore Diameter (Å) 26-30 33,34 100-150 [34][35][36] BET Surface Area (m 2 g -1 )…”

“…605-740 33,34 340-405 [34][35][36] The two silicas were impregnated with 1-ethyl-3-methylimidazolium methanesulfonate (Emim-Oms) and 1-Ethyl-3-methylimidazolium acetate (Emim-Ac) ionic liquids. These two ionic liquids were selected for their high affinity with water after the analysis of their vapor liquid equilibrium data.…”