Mefenamic acid solid dispersions: Impact of formulation composition on processing parameters, product properties and performance

Prasad, Elke; Robertson, John; Halbert, Gavin

doi:10.1016/j.ijpharm.2022.121505

Cited by 11 publications

(8 citation statements)

References 37 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…These results indicate the criticalness of drug loading in the formulation. Since the drug can be miscible in the liquid polymer to an extent, the higher quantities of the drug above the saturation level in the liquid polymer are essential for the preparation of CSD [64]. In an alternative approach to preparing CSDs, a hydrophilic solid crystalline carrier is utilized instead of a polymer.…”

Section: Crystalline Solid Dispersionsmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation—Where Are We Now?

Patil,

Vemula,

Narala

et al. 2024

AAPS PharmSciTech

View full text Add to dashboard Cite

Hot-melt extrusion (HME) is a globally recognized, robust, effective technology that enhances the bioavailability of poorly soluble active pharmaceutical ingredients and offers an efficient continuous manufacturing process. The twin-screw extruder (TSE) offers an extremely resourceful customizable mixer that is used for continuous compounding and granulation by using different combinations of conveying elements, kneading elements (forward and reverse configuration), and distributive mixing elements. TSE is thus efficiently utilized for dry, wet, or melt granulation not only to manufacture dosage forms such as tablets, capsules, or granule-filled sachets, but also for designing novel formulations such as dry powder inhalers, drying units for granules, nanoextrusion, 3D printing, complexation, and amorphous solid dispersions. Over the past decades, combined academic and pharmaceutical industry collaborations have driven novel innovations for HME technology, which has resulted in a substantial increase in published articles and patents. This article summarizes the challenges and models for executing HME scale-up. Additionally, it covers the benefits of continuous manufacturing, process analytical technology (PAT) considerations, and regulatory requirements. In summary, this well-designed review builds upon our earlier publication, probing deeper into the potential of twin-screw extruders (TSE) for various new applications. Graphical Abstract

show abstract

Section: Crystalline Solid Dispersionsmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation—Where Are We Now?

Patil,

Vemula,

Narala

et al. 2024

AAPS PharmSciTech

View full text Add to dashboard Cite

show abstract

“…Pure drug, physical mixture, or SD of drug equivalent to 100 mg of MA was used in each dissolution test. At different time intervals (5,15,25,35,45, 60 and 120 min), a 5 mL sample of dissolution medium was passed through a filter (0.45 µm), suitably diluted, and assayed for MA using a UV spectrophotometer (Jasco V-630, Japan) at 284 nm. In addition, 5 mL fresh medium was replaced after each withdrawal.…”

Section: Dissolution Studiesmentioning

confidence: 99%

“…Pharmaceutical efforts have recently focused on overcoming the solubility limitation of MA through several approaches such as complexation [7,8], self-emulsifying drug delivery system (SEDDS) [9], SMEDDS [10], Nanocrystals [11], freeze drying techniques [12], liposome encapsulation [13], and also solid dispersion (SD) [14,15]. SD technology is now firmly established as improving the solubility, dissolution rate, and oral absorption of poorly aqueous-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

“…SD generally provides the molecular dispersion of a drug within a polymer carrier and hence, provides a large drug surface area for dissolution [16]. Although SDs of MA have been previously formulated [14][15][16][17][18][19][20][21][22][23], there is an inherent lack of studies involving the combination of surfactants and super disintegrants in SDs of MA.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Development of Delayed-Release Matrix Tablets Comprising Solid Dispersion of Mefenamic Acid

Sermkeaw

Plyduang

2023

Trends Sci

View full text Add to dashboard Cite

Mefenamic acid (MA), a member of nonselective nonsteroidal anti-inflammatory drugs (NSAIDs), has been widely use to relief pain and inflammation. Its medical uses are limited by poor aqueous solubility resulting in low bioavailability and gastric irritation. The aim of this study was to develop a mefenamic acid delayed-release matrix tablet formulation using solid dispersion (SD). Delayed-release drug delivery systems were designed to retard drug release in upper gastrointestinal tract avoiding gastrointestinal (GI) adverse reactions. SDs of MA were successfully prepared by solvent evaporation method employing methanol as a solvent. SDs incorporated surfactant and super disintegrant gave much higher rates of dissolution than SDs with combined carriers (PEG and surfactant), SD containing PEG and pure drug, respectively. The optimal SD containing MA:PEG4000:poloxamer188:crospovidone in the ratio 1:8:1:3 exhibited higher amount of drug release up to 8-fold compared with pure MA. FTIR and DSC were performed to identify the physicochemical interaction between drug and polymers. The resulting data justified that no change in the chemical structure of MA and the crystalline MA transformed into the amorphous state after preparation. The formulation F4 delayed-release tablet comprising SD of MA dissolved less than 4 % in artificial gastric fluid in the initial 2 h and released more than 95 % at 3 h in the artificial intestinal fluid. Accordingly, formulation F4 containing polyethylene oxide as a time-controlled matrix-forming polymer was a promising delayed-release solid dispersion system of MA. HIGHLIGHTS The present study demonstrated a mefenamic acid delayed-release matrix tablet formulation using solid dispersion (SD) The optimal SD of mefenamic acid exhibited higher amount of drug release (8-fold) compared with that of the pure drug The tablet formulation F4 containing polyethylene oxide is capable of releasing mefenamic acid in a typical delayed-release profile GRAPHICAL ABSTRACT

show abstract

“…Genistein solid dispersion has been successfully produced by the hot-melt extrusion method [ 16 ]. In SD systems, the solubility of insoluble drugs can be improved by reducing particle size and enhancing wettability and dispersibility by the formation of an amorphous state [ 19 , 20 ]. While the in vitro solubility of these was significantly improved, the SD absorption in vivo has not been studied.…”

Section: Introductionmentioning

confidence: 99%

Solid Dispersions of Genistein via Solvent Rotary Evaporation for Improving Solubility, Bioavailability, and Amelioration Effect in HFD-Induced Obesity Mice

Qiu,

Zhang,

Fan

et al. 2024

Pharmaceutics

View full text Add to dashboard Cite

Genistein (GEN) is an active pharmaceutical ingredient that presents the challenges of poor water solubility and low oral bioavailability. To tackle these challenges, a GEN solid dispersion was prepared by solvent rotary evaporation using polyvinylpyrrolidone K30 (PVP K30) as a carrier. The optimal formulation was determined by drug loading efficiency and in vitro release. The physical state of the solid dispersion was characterized by DSC, XRD, SEM and FT-IR. And the results of the in vitro release study indicate that the drug release of SD (1:7) increased 482-fold that of pure GEN at 60 min. Following oral administration to rats, the Cmax and AUC0–24 of SD (1:7) was increased 6.86- and 2.06-fold to that of pure GEN. The adipose fat index and body weight of the SD (1:7) group were significantly lower than those of the GEN group (p < 0.05). Meanwhile, the levels of TC and TG in the serum were significantly decreased in the SD (1:7) group compared with the GEN group (p < 0.05). All experiments revealed that solid dispersion could be a promising formulation approach to improve the dissolution rate, oral bioavailability, and effect on the reduction of lipid accumulation in high-fat diet-induced obesity mice.

show abstract

Mefenamic acid solid dispersions: Impact of formulation composition on processing parameters, product properties and performance

Cited by 11 publications

References 37 publications

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation—Where Are We Now?

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation—Where Are We Now?

Development of Delayed-Release Matrix Tablets Comprising Solid Dispersion of Mefenamic Acid

Solid Dispersions of Genistein via Solvent Rotary Evaporation for Improving Solubility, Bioavailability, and Amelioration Effect in HFD-Induced Obesity Mice

Contact Info

Product

Resources

About