Solubility Enhancement of Etoricoxib by Cosolvency Approach

Abstract

The purpose of the present study was to examine and compare the cosolvency using three different cosolvents, namely PEG 400, PG, and glycerin on the aqueous solubility enhancement of a poorly aqueous soluble drug, etoricoxib, since solubilization of nonpolar drugs constitutes one of the important tasks in the formulation design of liquid dosage forms. The aqueous solubility of etoricoxib was 0.0767 ± 0.0018 mg/mL, which was significantly improved by the addition of PEG 400, PG, and glycerin as cosolvents. It was scrutinized that the less-polar solvents were found to increase the aqueous solubility by greater extent, thus accentuating hydrophobic interaction mechanism. Among various solvent-cosolvent blends investigated, water-PEG 400 showed highest solubilization potential. Thus, the study generated an important array of data to compare the effect of these cosolvents on the aqueous solubility of etoricoxib.

IUPAC-NIST Solubility Data Series. 102. Solubility of Nonsteroidal Anti-inflammatory Drugs (NSAIDs) in Neat Organic Solvents and Organic Solvent Mixtures

“…There has been only one publication reporting the solubility of etoricoxib in organic solvents. Nayak and Panigrahi 85 examined the solubility enhancement of etoricoxib using the cosolvency method. The very low aqueous solubility of etoricoxib can cause problems in preparing drug formulations, and can limit the drug's effectiveness by delaying the rate of absorption and onset of therapeutic action.…”

Attempts and outcomes of liquisolid technology: An updated chronological compilation of innovative ideas and adjuvants in the field

“…DSC and XRD simultaneously suggested the loss of drug crystallinity of upon liquisolid formulation which was further confirmed and validated by SEM that ensured the superiority of the technique. Bioavailability study indicated that the prepared optimal liquisolid formula did not differ significantly from the marketed famotidine tablets concerning C max , t max , and AUC (0)(1)(2)(3)(4)(5)(6)(7)(8) Figure 2). The role of nonvolatile solvents in enhancement of dissolution behavior can be easily observed by analyzing the obtained dissolution data, but the burden of further increment in these pharmaceutical parameters, falls on nature and type of carrier material used.…”

Untitled

“…As mentioned before solubility enhancement ratio was compared with midazolam water solubility. This different range can be explained by P.G and PEG400 dielectric constant which is 32 and 12.4, respectively 16 . The dielectric constant of phosphate buffer solution with the same ionic strength has been assumed78.5 in previous reports 34 .…”

“…They can reduce the interfacial tension between the aqueous solutions and disrupt waters selfassociation and reduce hydrophobic solute squeeze out. The most frequently used low toxic and due to their cilio-friendlyco-solvents for nasal use are propylene glycol, glycerin, polyethylene glycol (PEG), etc 16,32,33 .…”

“…Solubility enhancement techniques: Solubilization techniques which have used to improve solubility and further bioavailability of poor water soluble midazolam included buffer solutions, inclusion complexation, polymeric micellization and co-solvency 7,16 .…”