Technologies, Optimization and Analytical Parameters in Gastroretentive Drug Delivery Systems

Chordiya, Mayur; Gangurde, Hemant H; Borkar, V.G.

doi:10.18520/cs/v112/i05/946-953

Cited by 11 publications

(1 citation statement)

References 64 publications

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“…The height of the funnel was adjusted at 2 cm in such a way that the funnel tip just touched the top of the poured granules. The diameter made by pouring the particles through the cone was measured and the angle of repose (Ɵ) was calculated using the following equation: [25].…”

Section: Angle Of Reposementioning

confidence: 99%

Modulating the Drug Solubility of Aceclofenac by Design as Solid Lipid Particles: In Vitro/in Vivo Correlation

ABDOUN,

ALSUBAIYEL,

GABER

et al. 2023

Int J App Pharm

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Objective: The main objective of the study was to enhance the dissolution and hence the oral bioavailability of Aceclofenac (ACF). Methods: ACF was formulated as solid lipid particles (SLPs), which compressed into a tablet form for immediate release purpose and certain formulations were then coated by Eudragit RS100 polymer for sustained release action. SLPs of ACF were prepared by melt fusion method under the optimum conditions, using Compritol ATO 888 (Cr), Precirol ATO 5 (Pr), glyceryl monstearate, polyethylene glycols 4000, and Poloxamer 188 at different ratios SLP formulations were characterized for particle size, flow characteristics. The compressed tablets were identified in term of hardness, friability, content, moisture uptake, and in vitro release. Oral pharmacokinetics of the optimum tablet formulation and marketed tablet as reference were studied in rabbits. Results: SLP of acecloenac (ACF) showed accepted flowing properties, and the dissolution rate of the ACF from tablets was significantly enhanced compared to unprocessed drug. The results showed that about 45.5±2.5% of AC was released within 30 min from F1 while 12.7±4.5% was released from commercial AC tablets. The in vivo studies verified that the Cmax was 1.98±0.29, 2.10±0.33, and 4.83±86 µg/µl for the optimized immediate, sustained formula and commercial tablet, respectively. While the area under the curve from zero time to 24 h for the immediate and sustained release formula was 1.79, and 2.41 fold greater than the marketed formulation. Conclusion: The results showed that solid lipid particles under optimized conditions might be an efficient method for improving the solubility and hence the bioavailability of poorly soluble drugs likes ACF. The proper coating of the formula helps to achieve a convenient release of the drug.

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Section: Angle Of Reposementioning

confidence: 99%