Development of modifiedin situgelling oral liquid sustained release formulation of dextromethorphan

Maghraby, Gamal M. El; Elzayat, Ehab M.; Alanazi, Fars K.

doi:10.3109/03639045.2011.634811

Cited by 34 publications

(17 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…During the dissolution study, temperature was maintained at 37±0.5°C, and fresh media was added after each withdrawal 24. The dissolution profiles were evaluated using dissolution efficiency,which was calculated from the area under the dissolution curve at time t (determined using the non-linear trapezoidal rule and expressed as a percentage of the area of the trapezoid described by 100% dissolution in the same time) 25…”

Section: Methodsmentioning

confidence: 99%

Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability

Alhasani¹,

Kazi²,

Ibrahim³

et al. 2019

IJN

View full text Add to dashboard Cite

Background: Ramipril (RMP) suffers from poor aqueous solubility along with sensitivity to mechanical stress, heat, and moisture. The aim of the current study is to improve RMP solubility and stability by designing solid self-nanoemulsifying drug delivery system (S-SNEDDS) as tablet. Methods: The drug was initially incorporated in different liquid formulations (L-SNEDDS) which were evaluated by equilibrium solubility, droplet size, and zeta potential studies. The optimized formulation was solidified into S-SNEDDS powder by the adsorbent Syloid ® and compressed into a self-nanoemulsifying tablet (T-SNEDDS). The optimized tablet was evaluated by drug content uniformity, hardness, friability, disintegration, and dissolution tests. Furthermore, pure RMP, optimized L-SNEDDS, and T-SNEDDS were enrolled in accelerated and long-term stability studies. Results: Among various liquid formulations, F5 L-SNEDDS [capmul MCM/transcutol/HCO-30 (25/25/50%w/w)] showed relatively high drug solubility, nano-scaled droplet size, and high negative zeta potential value. The optimized SNEDDS solidification with Syloid ® at ratio (1:1) resulted in a compressible powder with an excellent flowability. The optimized tablet (T-SNEDDS) showed accepted content uniformity, hardness, friability, and disintegration time (<15 minutes). The optimized L-SNEDDS, S-SNEDDS, and T-SNEDDS showed superior enhancement of RMP dissolution compared to the pure drug. Most importantly, T-SNEDDS showed significant ( P <0.05) improvement of RMP stability compared to the pure drug and L-SNEDDS in both accelerated and long-term stability studies. Conclusion: RMP-loaded T-SNEDDS offers a potential oral dosage form that provides combined improvement of RMP dissolution and chemical stability.

show abstract

Section: Methodsmentioning

confidence: 99%

Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability

Alhasani¹,

Kazi²,

Ibrahim³

et al. 2019

IJN

View full text Add to dashboard Cite

show abstract

“…A minimum of three replicates were considered for each sample. The dissolution profiles were characterized using dissolution efficiency (DE) which was calculated from the area under the dissolution curve at time t (determined using the non-linear trapezoidal rule) and expressed as a percentage of the area of the trapezoid described by 100% dissolution in the same time) [ 36 ].…”

Section: Methodsmentioning

confidence: 99%

Stabilization benefits of single and multi-layer self-nanoemulsifying pellets: A poorly-water soluble model drug with hydrolytic susceptibility

2018

View full text Add to dashboard Cite

Solidified self-nanoemulsifying drug delivery systems (SNEDDS) offer strong option to enhance both drug aqueous solubility and stability. The current study was designed to evaluate the potential stabilization benefits of solidifying cinnarizine (CN) liquid SNEDDS into single and multi-layer self-nanoemulsifying pellets (SL-SNEP and ML-SNEP, respectively). The selected formulations were enrolled into accelerated, intermediate and long-term stability studies. The chemical stability was assessed based on the % of intact CN remaining in formulation. The physical stability was assessed by monitoring the in-vitro dissolution and physical appearance of the formulations. The degradation pathway of CN within lipid-based formulation was proposed to involve a hydroxylation reaction of CN molecule. The chemical stability study revealed significant CN degradation in liquid SNEDDS, SL-SNEP and ML-SNEP (lacking moisture-sealing) within all the storage conditions. In contrast, the moisture sealed ML-SNEP showed significant enhancement of CN chemical stability within the formulation. In particular, ML-SNEP coated with Kollicoat Smartseal 30D showed superior CN stabilization and no significant decrease in dissolution efficiency, at all the storage conditions. The observed stability enhancement is owing to the complete isolation between CN and SNEDDS layer as well as the effective moisture protection provided by Kollicoat Smartseal 30D. Hence, the degradation problem could be eradicated completely. The incorporation of silicon dioxide had an important role in the inhibition of pellet agglomeration upon storage. Accordingly, ML-SNEP coated with Kollicoat Smartseal 30D and/or silicon dioxide could be an excellent dosage form that combine dual enhancement of CN solubilization and stabilization.

show abstract

“…In a previous study (16), solutions containing different concentrations (1-4 %, m/V) of alginate were evaluated for their rheological behavior and release profile. The most suitable concentration was found to be 2 % (m/V) (designated as A2), which was used as a standard vehicle for all formulations in this work.…”

Section: Preparation Of In Situ Gelling Systemsmentioning

confidence: 99%

Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100

2014

View full text Add to dashboard Cite

Alginate vehicles are capable of forming a gel matrix in situ when they come into contact with gastric medium in the presence of calcium ions. However, the gel structure is pH dependent and can break after gastric emptying, leading to dose dumping. The aim of this work was to develop modified in situ gelling alginate formulations capable of sustaining dextromethorphan release throughout the gastrointestinal tract. Alginate solution (2 %, m/m) was used as a vehicle for the tested formulations. Solid matrix of the drug and Eudragit S 100 was prepared by dissolving the drug and polymer in acetone. The organic solvent was then evaporated and the deposited solid matrix was micronized, sieved and dispersed in alginate solution to obtain candidate formulations. The release behavior of dextromethorphan was monitored and evaluated in a medium simulating the gastric and intestinal pH. Drug-polymer compatibility and possible solid-state interactions suggested physical interaction through hydrogen bonding between the drug and the polymer. A significant decrease in the rate and extent of dextromethorphan release was observed with increasing Eudragit S 100 concentration in the prepared particles. Most formulations showed sustained release profiles similar to that of a commercial sustained-release liquid based on ion exchange resin. The release pattern indicated strict control of drug release both under gastric and intestinal conditions, suggesting the potential advantage of using a solid dispersion of drug-Eudragit S 100 to overcome the problem of dose dumping after the rupture of the pH dependent alginate gels.

show abstract

Development of modifiedin situgelling oral liquid sustained release formulation of dextromethorphan

Abstract: Alginate-chitosan based in situ gelling system is promising for developing liquid oral sustained release.

Cited by 34 publications

References 18 publications

<p>Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability</p>

<p>Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability</p>

Stabilization benefits of single and multi-layer self-nanoemulsifying pellets: A poorly-water soluble model drug with hydrolytic susceptibility

Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100

Contact Info

Product

Resources

About