Modulation of the wettability of excipients by surfactant and its impacts on the disintegration and release of tablets

Yang, Baixue; Xu, Lu; Wang, Qiuxiao; Li, Sanming

doi:10.1080/03639045.2016.1185436

Cited by 16 publications

(6 citation statements)

References 37 publications

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“…The findings were consistent with a matrix tablet containing poly(maleic acid-alt-octadecene) potassium salts (PAM-18K), which was reported in the study to reduce the drug release rate when the hydrophobic polymer was added [ 21 ]. The wettability of surfactant excipients, as well as their effects on the disintegration and release of plain tablets, was investigated [ 38 ]. The results showed that the wetting ability by adding surfactants to the formulation affects the disintegration and release of the tablets.…”

Section: Resultsmentioning

confidence: 99%

Improvement in Solubility and Absorption of Nifedipine Using Solid Solution: Correlations between Surface Free Energy and Drug Dissolution

Tubtimsri

Weerapol

2021

Polymers

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Ternary solid solutions composed of nifedipine (NDP), amino methacrylate copolymer (AMCP), and polysorbate (PS) 20, 60, or 65 were prepared using a solvent evaporation method. The dissolution profiles of NDP were used to study the effect of the addition of polysorbate based on hydrophilic properties. A solid solution of NDP and AMCP was recently developed; however, the dissolution of NDP was <70%. In the present study, polysorbate was added to improve the dissolution of the drug by altering its hydrophilicity. The suitable formulation contained NDP and AMCP at a ratio of 1:4 and polysorbate at a concentration of 0.1%, 0.3%, or 0.6%. Differential scanning calorimetry and powder X-ray diffraction were used to examine the solid solutions. No peak representing crystalline NDP was observed in any solid solution samples, suggesting that the drug was molecularly dispersed in AMCP. The NDP dissolution from NDP powder and solid solution without PS were 16.82% and 58.19%, respectively. The highest dissolution of NDP of approximately 95.25% was noted at 120 min for the formulation containing 0.6% PS20. Linear correlations were observed between the surface free energy and percentages of dissolved NDP (R2 = 0.7115–0.9315). Cellular uptake across Caco-2 was selected to determine the drug permeability. The percentages of cellular uptake from the NDP powder, solid solution without and with PS20 were 0.25%, 3.60%, and 7.27%, respectively.

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Section: Resultsmentioning

confidence: 99%

Improvement in Solubility and Absorption of Nifedipine Using Solid Solution: Correlations between Surface Free Energy and Drug Dissolution

Tubtimsri

Weerapol

2021

Polymers

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“…Several research groups have developed new approaches to quantify the fundamental disintegration mechanisms using high-speed imaging (Berardi et al, 2018;Basaleh et al, 2020), terahertz pulsed imaging (Markl et al, 2018Al-Sharabi et al, 2020), magnetic resonance imaging (Quodbach et al, 2014a,b;Dvořák et al, 2020;Catellani et al, 1989), and water uptake and (swelling) force measurements (Caramella et al, 1986;Peppas and Colombo, 1989;Tomas et al, 2018). The liquid uptake and wettability of powder and pharmaceutical compacts were also investigated using the sessile drop method, where several groups observed a correlation between the wettability characteristics and the disintegration/dissolution performance of tablets for a range of different formulations (Yang et al, 2016(Yang et al, , 2018Liu et al, 2018;Yang et al, 2019).…”

Section: Introductionmentioning

confidence: 99%

Tablet disintegration performance: Effect of compression pressure and storage conditions on surface liquid absorption and swelling kinetics

Markl

Maclean

Mann

et al. 2021

International Journal of Pharmaceutics

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“…The PBS solution containing SDS (0.5 wt%) was used as the in vitro release medium. The addition of SDS was to increase the solubility of hydrophobic SIM, which was conducive to its release in the medium [ 33 ]. Two kinds of the SIM-loaded NFMs (NO.1 and NO.2) were cut into circular specimens with a diameter of 15 mm.…”

Section: Methodsmentioning

confidence: 99%

Preparation and Characterization of Simvastatin-Loaded PCL/PEG Nanofiber Membranes for Drug Sustained Release

Pan

Yang

2022

Molecules

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Simvastatin (SIM) particles are liposoluble drugs with large particle sizes, resulting in poor compatibility with electrospun polycaprolactone (PCL)/polyethylene glycol (PEG) nanofibers, so that part of them will be exposed to the electrospun nanofiber surface, which is easy to cause the burst release of drugs. Therefore, in this paper, stearic acid (SA) with good biocompatibility was innovatively added to increase the dispersion uniformity of SIM in the spinning solution, thus improving the performances of SIM-loaded PCL/PEG nanofiber membranes (NFMs). Accordingly, the effects of SA addition on the morphologies, mechanical properties, wettability, and drug release properties of the SIM-loaded NFMs were studied. The results showed that after SIM was dissolved in SA solution, the particle size of SIM was significantly reduced and could be evenly dispersed in the polymer spinning solution, thus obtaining the SIM-loaded composite NFMs with the best morphology and performance.

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Modulation of the wettability of excipients by surfactant and its impacts on the disintegration and release of tablets

Abstract: The modulation of the wetting of pharmaceutical excipients by surfactant had changed the disintegration time of tablets and drug release rate to a greater extent.

Cited by 16 publications

References 37 publications

Improvement in Solubility and Absorption of Nifedipine Using Solid Solution: Correlations between Surface Free Energy and Drug Dissolution

Improvement in Solubility and Absorption of Nifedipine Using Solid Solution: Correlations between Surface Free Energy and Drug Dissolution

Tablet disintegration performance: Effect of compression pressure and storage conditions on surface liquid absorption and swelling kinetics

Preparation and Characterization of Simvastatin-Loaded PCL/PEG Nanofiber Membranes for Drug Sustained Release

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