(M1130-12-68) Hydroalcoholic Media Effects on Ibuprofen Release from Low Acyl Gellan Gum

Purpose: Polysaccharides from renewable sources have come under increasing research focus in the design of oral controlled release dosage forms. As these polysaccharides can account for a major part of a tablets composition, it is important to evaluate their resilience in harsh conditions that can be experienced in the gastrointestinal (GI) tract. In 2005, Palladone®, an extended-release capsule, was withdrawn from the market after clinical testing showed subjects who took the product with alcohol had increased levels of the drug in their blood. The Food and Drug Agency (FDA) issued an alert to healthcare professionals regarding this as the ingestion of hydromorphone with alcohol potentially resulted in lethal peak plasma concentrations of drug. As a result, there has been a lot of interest in developing extended release matrices that are robust to alcoholic effects. In this study, ibuprofen was used as a model drug to investigate the effect of different alcohol concentration on low acyl gellan gum stifness. Drug release was then investigated in 0-5-40 % ethanol in pH 1.2 and phosphate buffer (pH 6.8)(1)

Methods: The low acyl fluid gel was prepared as previously mentioned by (Mahdi et al., 2015) (2). An automated USP dissolution apparatus II (basket method) was used to monitor the dissolution profiles of ibuprofen from the tablet matrices. The dissolution medium was 900 mL 0.1 N HCl (pH 1.2) and phosphate buffer (pH 6.8) equilibrated to 37 ± 0.5 °C with a basket stirring speed of 50 rpm. Samples were withdrawn at selected time intervals from 5 min up to 120 min using a peristaltic pump and the concentrations of ibuprofen in the samples determined by a UV spectrophotometer at 222 nm. For the effect of alcohol studies, drug release was monitored as above, however the media used for this testing comprised either of 0.1 M HCl or phosphate buffer (pH 6.8) with absolute ethanol ratios between 0-5-40% (v/v) ethanol.(2)

Results: The influence of aqueous and hydroalcoholic media on ibuprofen release from low acyl gellan were presented. It was interesting to note that there were hardly any differences between drug releases from pH 1.2 media and pH 1.2 media containing 40 % v/v absolute ethanol for all the individual matrices. Drug release profiles in pH 6.8 and the various hydroalcoholic media tested showed similarity for gellan gum fluid gel matrices also showed similarity up to 40 % v/v absolute ethanolic concentration but dissimilarity occurred at 40 % v/v absolute ethanoic concentration.

Conclusion: As in conclusion from this study, the release of ibuprofen will not affect by alcohol media in the stomach. However, alcohol with more than 40% will increase the release of drug from gellan gum

References: 1-Asare-Addo, K., Conway, B. R., Hajamohaideen, M. J., Kaialy, W., Nokhodchi, A., & Larhrib, H. (2013). Aqueous and hydro-alcoholic media effects on polyols. Colloids and Surfaces B: Biointerfaces, 111, 24-29
2-Mahdi, M.H., Conway, B.R. and Smith, A.M., 2014. Evaluation of gellan gum fluid gels as modified release oral liquids. International journal of pharmaceutics, 475(1-2), pp.335-343


Ibuprofen drug release at different hydro alcohol concentration pH 6.8


Ibuprofen drug release at different hydro alcohol concentration pH 1.2