Improved Dissolution of Naproxen Using a Self -Microemulsifying Delivery System and in vivo Evaluation of Efficacy in Rats
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Naproxen is a nonsteroidal anti-inflammatory drug (NSAID) administered to reduce pain, inflammation, and fever. The extended half-life of naproxen enables prolonged efficacy, leading to symptom relief and high patient satisfaction. However, naproxen has notably low solubility in water (15.9 mg/L). The present study aimed to enhance the solubility and dissolution rate of naproxen by using a self-microemulsifying delivery system (SMEDDS). Labrasol® was used as the primary oil and Labrafil® M1944 and Cremophor® RH-40 as the surfactants in the SMEDDS. The ratio of the selected oil to the surfactant was determined to identify the equilibrium range with good solubility. Subsequently, the efficacy was confirmed to be within the applicable range. The results indicated that the SMEDDS formulation showed higher dissolution rates than the salt-formulated purified naproxen product. Furthermore, the efficacy was compared with that of commercially available naproxen emulsion-filled soft gel capsules in an animal model of gastric ulcers, showing the excellent gastro-protective abilities of the naproxen SMEDDS. This study provides an appropriate oil and ratio for a naproxen SMEDDS, confirming it sefficacy, dissolution rate, and stability. These results will guide future directions in naproxen research and manufacturing.
Abstract
Naproxen is a nonsteroidal anti-inflammatory drug (NSAID) administered to reduce pain, inflammation, and fever. The extended half-life of naproxen enables prolonged efficacy, leading to symptom relief and high patient satisfaction. However, naproxen has notably low solubility in water (15.9 mg/L). The present study aimed to enhance the solubility and dissolution rate of naproxen by using a self-microemulsifying delivery system (SMEDDS). Labrasol® was used as the primary oil and Labrafil® M1944 and Cremophor® RH-40 as the surfactants in the SMEDDS. The ratio of the selected oil to the surfactant was determined to identify the equilibrium range with good solubility. Subsequently, the efficacy was confirmed to be within the applicable range. The results indicated that the SMEDDS formulation showed higher dissolution rates than the salt-formulated purified naproxen product. Furthermore, the efficacy was compared with that of commercially available naproxen emulsion-filled soft gel capsules in an animal model of gastric ulcers, showing the excellent gastro-protective abilities of the naproxen SMEDDS. This study provides an appropriate oil and ratio for a naproxen SMEDDS, confirming it sefficacy, dissolution rate, and stability. These results will guide future directions in naproxen research and manufacturing.
참고문헌 (13)
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