Aceclofenac in Osteoarthritis - NSAID with Novel Mechanism of Action

Shah, Dilip D; Pal, Ananda K; Bedi, Gurinder; Grover, Anu; Singh, A; Purkait, Indranil; Jawdekar, Apurva; Pareek, Anil

doi:10.31080/asor.2020.03.0232

Cited by 2 publications

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“…ACF has a strong anti-inflammatory and analgesic action. Its stronger inhibition selectivity on COX 2 than COX 1 explains its safety in comparison to other NSAIDs and COX 2 selective inhibitors, as well as its improved stomach tolerance and fewer side effects (5) . ACF is weakly acidic drug with pka about 4.7 and belongs to BCS class II and it's practically insoluble in water (about 0.007 mg/mL) with high permeability and poor dissolution rate that leads to reduced oral bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Solubility and Dissolution Rate Enhancement of Aceclofenac by Solid Dispersion Employing Kneading and Solvent Evaporation Techniques

Alezzy

2024

Tikrit J. Pharm. Sci.

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Background: Aceclofenac (ACF) is a non-steroidal anti-inflammatory drug with potent anti-inflammatory and analgesic properties. ACF is belongs to BCS class II which has poor solubility in water (practically insoluble) and high permeability that leads to a low dissolution rate and reduced bioavailability. Objective: to enhance the solubility and dissolution rate of ACF using the solid dispersion method (SD) by two common techniques which were solvent evaporation (SE) and kneading (Kn) by using different carriers Mannitol, PVP k30, Soluplus®, and Urea in both techniques at 1:1 and 1:5 wight ratio. Methods: The effects of type of carrier and preparation method on solubility and dissolution rate of SD were studied. Solid dispersions were characterized for their, percentage yield, drug content, drug solubility and in-vitro dissolution rate in comparison with pure drug. Results: The best formula is obtained by the Kn formula (F16) which was formulated by the use of ACF: Soluplus®: with a weight ratio of 1:5 which gave a high percentage yield (99.5%), high drug content (99.8± 0.003%) and the best solubility enhancement which was 361 folds compared to pure ACF and faster dissolution rate which was 80% in 10 minutes compared to 20% for pure drug. Conclusion: the solubility and in-vitro dissolution rate of ACF was efficiently improved when prepared by SD techniques, utilizing both solvent evaporation and kneading methods. Furthermore, the kneading method was superior to solvent evaporation method due to the greater enhancement of solubility and dissolution rate obtained by all carriers and ratios with higher improvement by 1:5 ratio, and can be considered a successful and efficient strategy for solubility and in-vitro dissolution rate improvement of hydrophobic drugs.

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Section: Introductionmentioning

confidence: 99%

Solubility and Dissolution Rate Enhancement of Aceclofenac by Solid Dispersion Employing Kneading and Solvent Evaporation Techniques

Alezzy

2024

Tikrit J. Pharm. Sci.

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Preparation and Evaluation of Aceclofenac Solid Dispersion by Fusion Technique and Effervescent Assisted Fusion Technique: Comparative Study

A. E. Alezzy,

B. H. Al-Khedairy

2023

RJPT

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Solid dispersion (SD) is one of the most widely used methods to resolve issues accompanied by poorly soluble drugs. The present study was carried out to enhance the solubility and dissolution rate of Aceclofenac (ACE), a BCS class II drug with pH-dependent solubility, by the SD method. Effervescent assisted fusion technique (EFSD) using different hydrophilic carriers (mannitol, urea, Soluplus®, poloxamer 188, and poloxamer 407) in the presence of an effervescent base (sodium bicarbonate and citric acid) in different drug: carrier: effervescent base ratio and the conventional fusion technique (FSD) were used to prepare ACE SD. Solubility, dissolution rate, Fourier transformation infrared spectroscopy (FTIR), PowderX-ray diffraction study (PXRD), and Differential scanning calorimetry (DSC) were determined for the SD obtained from both techniques as a comparative study. The results showed that EFSD using ACE: Soluplus®: effervescent base in a ratio of 1:2:1 had higher solubility and dissolution rate than that obtained from FSD prepared by ACE: Soluplus® in a ratio of 1:2. However, the two techniques obtained the amorphous form according to XRD and DSC results. It can be concluded that EFSD is a promising method for the solubility and dissolution rate improvement of BCS class II drugs.

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Aceclofenac in Osteoarthritis - NSAID with Novel Mechanism of Action

Cited by 2 publications

References 0 publications

Solubility and Dissolution Rate Enhancement of Aceclofenac by Solid Dispersion Employing Kneading and Solvent Evaporation Techniques

Solubility and Dissolution Rate Enhancement of Aceclofenac by Solid Dispersion Employing Kneading and Solvent Evaporation Techniques

Preparation and Evaluation of Aceclofenac Solid Dispersion by Fusion Technique and Effervescent Assisted Fusion Technique: Comparative Study

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