Pharmacokinetic properties of low-dose SoluMatrix meloxicam in healthy adults

Abstract

SoluMatrix® meloxicam has been developed using SoluMatrix Fine Particle Technology™ to produce a meloxicam drug product with enhanced absorption properties to enable treatment at lower doses than available oral meloxicam drug products. This follows recognition of serious dose-dependent adverse events (AEs) associated with nonsteroidal anti-inflammatory drugs, including meloxicam. This study investigated the pharmacokinetic (PK) properties of SoluMatrix meloxicam 5-mg (fasting conditions) and 10-mg capsules (fasting and fed conditions) and compared SoluMatrix meloxicam 10-mg capsules with meloxicam 15-mg tablets under fasting conditions. This four-period crossover study randomized 28 healthy adult participants to receive single doses of SoluMatrix meloxicam 5-mg capsules (fasting) and 10-mg capsules (fasting or fed) and meloxicam tablets 15 mg (fasting). Meloxicam plasma concentrations were assessed through 96 h postdose. Safety was assessed. Twenty-five participants (89.3 %) completed the study. Under fasting conditions, SoluMatrix meloxicam 10 mg [1252.8 (254.22) ng/mL] produced similar meloxicam mean (standard deviation (SD)) maximum plasma concentrations vs meloxicam 15-mg tablets [1288.8 (424.40) ng/mL]. The overall mean (SD) systemic meloxicam exposure was 33 % lower for SoluMatrix meloxicam 10 mg [29,173.01 (11,042.09) ng*h/mL] vs meloxicam 15-mg tablets [40,875.6 (11,733.47) ng*h/mL]. The median time to maximum plasma meloxicam levels occurred earlier following SoluMatrix meloxicam 5 mg (2.0 h) and 10 mg (2.0 h) administration vs meloxicam 15-mg tablets (4.0 h). Few study-medication-related AEs were reported. SoluMatrix meloxicam 10 mg was more rapidly absorbed and associated with a lower overall exposure compared with meloxicam 15-mg tablets in this study in healthy adults under fasting conditions.

Comparison of a Novel Formulation of Abiraterone Acetate vs. the Originator Formulation in Healthy Male Subjects: Two Randomized, Open-Label, Crossover Studies

“…The manufacturing process, which does not alter the active therapeutic ingredient, was previously shown to promote rapid absorption of new formulations of diclofenac and meloxicam [11, 12]. The present study in healthy subjects indicates that the use of SoluMatrix Fine Particle Technology™ enhances the bioavailability of abiraterone acetate.…”

“…Reduced particle size leads to an enhanced surface area, and this in turn leads to an enhanced rate of dissolution and absorption [11, 12]. The absorption of OAA is reported to be nearly saturated at a dose of 1000 mg [7, 8].…”

Benefits of Applying Nanotechnologies to Hydrogels in Efficacy Tests in Osteoarthritis Models—A Systematic Review of Preclinical Studies

“…In the clinical setting, nanotechnologies for OA are still under development, with very few clinical experiments. A search in the PubMed database and the Clinicaltrials register highlighted that NPs are generally tested as nano-based emulsions or formulations to deliver analgesic NSAIDs or anti-inflammatory gold nanoparticles by topical and oral applications, and these clinical studies, mostly of phases one and two, demonstrated safety and efficacy with significantly improved pain, stiffness, and physical function in patients affected by OA [ 67 , 68 , 69 , 70 , 71 , 72 , 73 , 74 , 75 ] (NCT00484120, NCT05347602).…”

Effect of Selected Surfactants on Kinetics of Meloxicam Release from Rectal Suppositories

“…Meloxicam is an oxicam, which has a low COX-2/ COX-1 ratio, with the inhibitory effect more focused on the inflammatory proteins (COX-2) with relatively little effect on the homoeostatic proteins (COX-1). Meloxicam is a frequently prescribed nonsteroidal antiinflammatory drug (NSAID) in the USA and is prescribed for the treatment of osteoarthritis (OA), rheumatoid arthritis (RA) and juvenile RA [3,4] . It is also one of the few NSAIDs approved for use in animals [4] .…”

“…In the dissolution process of sparingly soluble substances, an important role among auxiliary substances is played by surfactants [8,9] . The presence of surfactants in suppositories for rectal administration can cause some changes in the properties of the suppository base [3,10] . In particular, adding a surfactant to suppositories can facilitate the spread of the suppository bases in the rectum.…”